bluuebunny/crossref_metadata_2025 huggingface dataset:
CALCIUM CARBONATE ISOLATION FROM EGGSHELL TO MEET PHARMACOPOEIAL STANDARDS AND ITS EFFECTIVENESS AS AN ANTACIDS
Authors: SUPRIADI DADIH , MILANDA TIANA , C. ANIS YOHANA , MUCTARIDI  , ABDASSAH MARLINE
Published: September 2023

Objective: Calcium carbonate is widely used in the pharmaceutical field as excipients and therapeutic agents. Calcium carbonate can be obtained from limestone, chalk, marble and dolomite. Other alternative is from eggshell. Calcium carbonate source from eggshell has several advantages including higher calcium carbonate content, fewer contaminants metal limit, and more brittle. Therefore, in this study, calcium carbonate had been isolated from eggshells which was expected to meet the requirements of Indonesian Pharmacopoeia (sixth edition) and having activity as antacid.
Methods: Calcium carbonate were isolated from eggshells by mechanically and physically organic separation. The quality of calcium carbonate was examined according to the Indonesian Pharmacopoeia parameters including loss on drying; acid-insoluble substance, magnesium and alkali salt; limit of arsenic, lead, iron, mercury, heavy metal, and barium. Additional physicochemical characterization of calcium carbonate including particle size analyzer, FTIR and XRD were compared with those of commercial calcium carbonate.
Results: The results showed that the isolation produced 98.5±0.5 % of calcium carbonate. The calcium carbonate powder had an average size of 21±1.0 µm, while that of commercial was 8±1.3 µm. The resulted calcium carbonate revealed similar XRD patterns compared with that from commercial Calcium carbonate from the market. Based on database from FTIR instrument, the calcium carbonate sample had 99% similarity level compared with that from the reference. The sample of Calcium carbonate isolated from the eggshell (>mesh 100) had lower antacid activity (23.83 mEq) than that of commercial (24.56 mEq).
Conclusion: Calcium carbonate from eggshell fulfilled the requirements of Indonesian Pharmacopoeia.
IN VITRO MUCOLYTIC ACTIVITY DETERMINATION OF N-ACETYL CYSTEINE EFFERVESCENT TABLET USING SUSPENDED LEVEL VISCOMETER
Authors: SATISH NANGUDE , KAMBLE RAVINDRA , KAJAL VANHERE
Published: September 2023

Objective: The objective of the present study was to determine the in vitro mucolytic activity of N-Acetyl Cysteine (NAC) effervescent tablet using egg white solution and suspended level viscometer.
Methods: Egg white has similar physicochemical characteristics with airway mucus, thus in vitro mucolytic activity of NAC effervescent tablets was assessed using an egg white solution and a suspended level viscometer. This was also compared with API and marketed effervescent tablets. Outcomes were statistically analysed using a single-factor ANOVA and a paired t-test.
Results: The results show, in all three cases, i.e., API, Test tablet, and Commercial tablet, viscosity reduced linearly as the concentration was raised from 10 to 60 mg/10 ml having R2 values 0.9973, 0.9909, 0.9953 respectively. When compared to the negative control solution, viscosity rapidly decreased, which amounted to 71.10 %, 73.03 % and 84.63 % of API, Test tablet and Commercial tablet, respectively. The p values of single factor ANOVA and paired t-test were found to be very less than 0.05 in all cases.
Conclusion: NAC effervescent tablet's in vitro mucolytic activity was successfully assessed; results suggested that linearly decreases in viscosity as the concentration of NAC increases and statistical analysis shows significant differences in values.
MODULATING THE DRUG SOLUBILITY OF ACECLOFENAC BY DESIGN AS SOLID LIPID PARTICLES: IN VITRO/IN VIVO CORRELATION
Authors: ABDOUN SIHAM A. , ALSUBAIYEL AMAL M. , GABER DALIA A. , ALSAUDI BAYAN S. , ALRASHED HAIFA A. , ALJARBOOA NORAH F. , ALRADDADI RANEEM H. , ALHARBI RAZAN R. , MOHAMED HEBA A.
Published: September 2023

Objective: The main objective of the study was to enhance the dissolution and hence the oral bioavailability of Aceclofenac (ACF).
Methods: ACF was formulated as solid lipid particles (SLPs), which compressed into a tablet form for immediate release purpose and certain formulations were then coated by Eudragit RS100 polymer for sustained release action. SLPs of ACF were prepared by melt fusion method under the optimum conditions, using Compritol ATO 888 (Cr), Precirol ATO 5 (Pr), glyceryl monstearate, polyethylene glycols 4000, and Poloxamer 188 at different ratios SLP formulations were characterized for particle size, flow characteristics. The compressed tablets were identified in term of hardness, friability, content, moisture uptake, and in vitro release. Oral pharmacokinetics of the optimum tablet formulation and marketed tablet as reference were studied in rabbits.
Results: SLP of acecloenac (ACF) showed accepted flowing properties, and the dissolution rate of the ACF from tablets was significantly enhanced compared to unprocessed drug. The results showed that about 45.5±2.5% of AC was released within 30 min from F1 while 12.7±4.5% was released from commercial AC tablets. The in vivo studies verified that the Cmax was 1.98±0.29, 2.10±0.33, and 4.83±86 µg/µl for the optimized immediate, sustained formula and commercial tablet, respectively. While the area under the curve from zero time to 24 h for the immediate and sustained release formula was 1.79, and 2.41 fold greater than the marketed formulation.
Conclusion: The results showed that solid lipid particles under optimized conditions might be an efficient method for improving the solubility and hence the bioavailability of poorly soluble drugs likes ACF. The proper coating of the formula helps to achieve a convenient release of the drug.
IMPROVED MUCOADHESIVE PROPERTIES OF THIOLATED PECTIN FILM FOR BUCCAL DELIVERY OF DICLOFENAC
Authors: HARTRIANTI PIETRADEWI , LEONARD THEODORE EBENEZER , LORENZO SHERYL , CHRISCENSIA ERIKA , TRIAVIKA SAHAMASTUTI AGNES ANANIA
Published: September 2023

Objective: This study was aimed to study the effect of degree of esterification (DE) on the thiolation of pectin, the potential to be used as materials for buccal delivery of diclofenac as well as the effect of DE on the physicochemical and mucoadhesive properties of the buccal films.
Methods: Low-methoxyl pectin (LMP) and high-methoxyl pectin (HMP) were synthesized into low-methoxyl thiolated pectin (LMTP) and high-methoxyl thiolated pectin (HMTP) by esterification reaction using thioglycolic acid (TGA). The degree of thiolation was evaluated using Ellman’s reaction and FT-IR. Pectins were fabricated into buccal films with diclofenac as a drug model and glycerin as the plasticizer. The obtained films were then studied for swelling and erosion percentage, mucoadhesion time, and in vitro drug release.
Results: HMTP and LMTP showed no significant difference in the degree of thiolation regardless of DE (p>0.05). The fabricated LMTP and HMTP films showed significantly higher mucoadhesion time and swelling than HMP and LMP (p<0.05). Moreover, HMTP and LMTP also exhibited sustained release of diclofenac compared to LMP (p<0.05). HMTP showed the highest mucoadhesion time, swelling capacity, and retention of drug release among all groups (p<0.05).
Conclusion: Thiolated pectin showed prospective potential to be utilized as a biopolymer for buccal delivery of diclofenac with improved mucoadhesion and controlled drug delivery, regardless of their DE.
A STABILITY, ACCURACY, AND ROBUSTNESS REPRESENTING LIQUID CHROMATOGRAPHIC METHOD FOR THE QUANTIFICATION OF ZANUBRUTINIB AND ITS SPECIFIED IMPURITIES
Authors: KANTHETI SUBHASHINI , RAJU R. RAMESH
Published: September 2023

Objective: An innovative RP-HPLC isocratic method was established and then validated using Zanubrutinib and its specified impurities (Impurity-1, Impurity-2, Impurity-3, Impurity-4, and Impurity-5).
Methods: In this method, effective chromatographic separation was given an X-Bridge Phenyl column measuring 250 mm x 4.6 mm, packed column with 5μ as a particle size. Acetonitrile, 1% Ortho Phosphoric acid (pH: 2.7), and methanol in the volume ratios 40, 40, and 20 were utilized as a mobile phase at room temperature with an optimized 1.0 ml/min flow rate. Wavelength was detected at 225 nm by using a PDA detector.
Results: Retention times of zanubrutinib and its specified impurities were recorded at 13.284, 4.730, 6.816, 9.583, 10.726, and 12.287. Moreover, other parameters USP tailing is good, USP plate count above 4000, and USP resolution is greater than are equal to 2. The Obtained peaks are homogeneous, hence the purity angle is less than the purity threshold and No Purity Flag. According to ICH guidelines, this method was validated. Zanubrutinib (5-75 µg/ml), their quantified impurity-1, impurity-2, impurity-4, impurity-5 (0.1-1.5 µg/ml), and impurity-3 (0.1-1.5 µg/ml) are proved through linearity method in between LOQ to 75 quantified levels. The % recovery was present between 100.18-95.85, 103.15-93.80, which is a good and acceptance range (amongst 85% and 115%) for drug and specified impurities. The limit of quantitation (LOQ) and limit of detection (LOD) values were assessed for zanubrutinib and its specified impurities were tabulated. These values were calculated using slope (σ) and standard deviation (SD) methods. Method precision (M. P.) and Intermediate (I. P.) Intermediate (I. P.) precision was estimated by evaluating several (six) samples of a similar batch as per the planned technique on the day and the next day, using different columns and systems. Robustness information significantly affects the resolution between Zanubrutinib and specified impurities. The remaining parameters do not impact the parameter’s system suitability.
Conclusion: Hence this method was chosen for common analysis. Finally, the system-suitable parameters and validation parameters values are acceptable limits.
STRUCTURAL PREDICTION OF HUMAN ZIP 2 AND ZIP4 BASED ON HOMOLOGY MODELLING AND MOLECULAR SIMULATION
Authors: SYAHPUTRA GITA , GUSTINI NUNIK , LOUISA MELVA , PUTRA MASTERIA YUNOVILSA , FADILAH ADILAH
Published: September 2023

Objective: This study aimed to analyze the structural proteins of zinc transporters as the target for drug actions and their molecular interactions.
Methods: The present study is about the homology modelling and analysis of the zinc transporter function using the in silico molecular modelling method. Homology modelling predicts the 3D structure of a protein based on the sequence alignment with one or more template proteins of known structure. This study using in silico molecular modelling method, explains the 3D structure of human ZIP 2 and ZIP4 with Ramachandran Plot analysis, physical and chemical characteristics, transmembrane prediction with structural biology, and binding site prediction through molecular docking simulation.
Results: Based on the physicochemical properties of the 3D structure of the ZIP2 and ZIP4 proteins, each comprises 309 amino acids and 582 amino acids with pI values of 5.85 and 5.24. The amino acid composition analysis showed that both proteins contain many Leucine amino acids. The Ramachandran diagram concludes that both proteins are stable in the stereochemical conformation forming a secondary structure. The binding amino acids on ZIP2 include Glu281, His216, Ser284, and Arg46. The binding amino acids in ZIP4 include Gln148, Gln154, Thr155, His197, Ala138, and Lys157.
Conclusion: Establishment of the structure and function of human ZIP2 and ZIP4 as zinc transporters in cell membranes and prediction of ZIP2 and ZIP4 binding sites through molecular dcoking.
PREDICTION OF HIGH-RISK NSSNPS ASSOCIATED WITH WISP3 GENE EXPRESSION: AN IN SILICO STUDY
Authors: M. S. SAUNDARYA , DINESH SUSHA , SHARMA SAMEER
Published: September 2023

Objective: The primary aim of this investigation is to comprehensively examine the detrimental effects of non-synonymous single nucleotide polymorphisms (nsSNPs) on the WISP3 gene. This objective will be accomplished through intricate evaluations encompassing protein stability prediction, amino acid conservation analysis, investigation of protein-protein interactions (PPI), scrutiny of post-translational modifications (PTM), and the utilization of bioinformatics tools to forecast the potential association between nsSNPs and various diseases. By implementing these sophisticated methodologies, we aim to unveil the intricate mechanisms by which harmful nsSNPs influence the functionality and pathological implications of the WISP3 gene.
Methods: Retrieved rsIDs of SNPs from the dbSNP database and filtered using 5 in silico programs. Selected nsSNPs were subjected to further analysis i.e., protein stability and conservation analysis, solvent accessibility analysis, PPI and PTM analysis, prediction and evaluation of both native and mutant protein, and identification of cancer association and gene expression analysis.
Results: The study found that seven (C122Y, C145Y, C52Y, C78R, C75G, N233K, and R245I) of the nsSNPs are potentially vulnerable due to their higher conservancy and ability to reduce protein stability. Two (D271N and Q56H) of the nsSNPs from the initial screening were found to be associated with colon adenocarcinoma.
Conclusion: The study's findings could help researchers design experiments to validate the predictions and develop potential treatments for diseases associated with the WISP3 gene.
SOLID DISPERSION AS A POTENTIAL APPROACH TO IMPROVE DISSOLUTION AND BIOAVAILABILITY OF CURCUMIN FROM TURMERIC (CURCUMA LONGA L.)
Authors: AGUSTINA RENI , SETYANINGSIH DEWI
Published: September 2023

This review article attempts to outline techniques and solid dispersion carriers that have been applied to improve curcumin's solubility and bioavailability in turmeric extract. This paper also examines the variables that impact the efficacy of curcumin solid dispersion. Turmeric (Curcuma longa L.) contains curcuminoids as bioactive compounds consisting of curcumin, dimethoxy-curcumin, and bis-dimethoxy-curcumin. Curcumin, as the main component, is proven to have several pharmacological effects. However, it has limitations in modern drug development, such as poor stability, solubility, and bioavailability. Many studies have been conducted to overcome these limitations, including the application of solid dispersion. The preparation methods of curcumin solid dispersions are carried out by solvent evaporation, fusion/melting, and co-milling, using various types of carriers. However, the formation of a solid dispersion system only sometimes provides a considerable improvement in solubility, dissolution, and bioavailability. Differences in the selection of preparation methods, carriers, and solvents result in various arrangements of particles in the solid dispersion that may affect the performance of the system. In addition, the type of carrier also has a role in increasing curcumin permeability and bioavailability. Hydrophilic surfactant carriers have inhibitory activity against body transporters, such as P-gp and MRP, that can help to increase curcumin’s bioavailability. Natural Deep Eutectic Solvent (NADES) as a novel alternative solvent also has promising opportunities for the development of curcumin solid dispersion. Therefore, selecting appropriate preparation methods, carriers, and solvents should be considered to achieve optimum solubility, dissolution, and bioavailability of curcumin.
DEVELOPMENT VALIDATION OF QUERCETIN COMPOUNDS USING RP-HPLC AND IN VITRO ACTIVITY STUDIES ON MELASTOMA MALABATHRICUM LEAF NANOCREAM FOUNDATION PREPARATIONS
Authors: APRIDAMAYANTI PRATIWI , SARI RAFIKA , PRATIWI LIZA
Published: September 2023

Objective: A simple, accurate, precise, sensitive, and robust analytical method has been developed to analyze quercetin in the nano-cream foundation formula added to the ethyl acetate fraction of Melastoma malabathricum leaves.
Methods: The validation is consistent with ICH guidelines using a reversed-phase HPLC method with mobile-phase acetonitrile-phosphoric buffer conditions at pH 5.51 (40:60 v/v). The stationary phase has a C-18 column, a 0.5 ml/min flow rate, and an Ultraviolet detector at wavelength 370 nm. Furthermore, antioxidant activity testing used the FRAP method, and the SPF value was measured using a Elisa reader with wavelength 615nm and UV/Vis spectrophotometer in the wavelength range of 290-390 nm.
Results: The results showed that the retention time of quercetin was 11.462 min with a tailing factor of 1.045. Regression equation y=170220x-85497 had a concentration range of 3-18 µg/ml and a correlation value of 0.9998. The limit of Detection (LOD) and Limit of Quantification (LOQ) were 0.236 and 0.786 µg/ml, respectively. The accuracy method for the recovery value at concentration levels of 80%, 100%, and 120% was 95.233%-109.446%. The repeatability of intra-day and inter-day variations express the %RSD values of 1.258-1.378% and 1.012-1.258%. Meanwhile, the method's strength by changing the column temperature, maximum wavelength, mobile phase composition, and the flow rate was expressed by the %RSD value of 0.045-0.067%, 0.069-1.642%, 0.107-0.165%, and 0.141-0.318%, respectively. The analysis results of the quercetin content in the nano cream foundation formula were 0.021728±5.83x10-4 mg/g. Antioxidant activity with an IC50 value was 1444.157±15.538 µg/ml, and the SPF at a concentration of 8000 µg/ml was 11.370±1.083.
Conclusion: The development method of quercetin is simple, accurate, precise, sensitive, and robust. Quantitative analysis of quercetin biomarkers in nano cream preparations containing the ethyl acetate fraction of Melastoma malabathricum leaves using the RP-HPLC method.
TARGETING ANGIOGENESIS WITH FLUPHENAZINE-ZINC OXIDE NANOCONJUGATES: A POTENTIAL MECHANISM FOR IMPROVING ANTIPSYCHOTIC EFFICACY
Authors: DASARI NAGASEN , BALLA SUJIYA , KONDRAPU PYDIRAJU , GUMMADI RAMAKRISHNA , SURADA NOOKARAJU , KONDRU UMA MAHESWARI , PINDIPROLU SAI KIRAN S. S.
Published: September 2023

Objective: This study aimed to develop a more effective formulation of Fluphenazine (FLP) for the management of psychosis. Antipsychotics are widely used for the treatment of severe mental disorders such as schizophrenia and bipolar disorder. However, their clinical use is limited due to various side effects and low efficacy in a large number of patients. Nanoparticle-based drug delivery systems have shown great potential in improving the pharmacokinetics and pharmacodynamics of various drugs, including antipsychotics. Zinc oxide nanoparticles (ZnO NPs) have emerged as a promising carrier for drug delivery due to their unique physicochemical properties, biocompatibility, and low toxicity.
Methods: In this study, we reported the preparation and characterization of FLU-encapsulated ZnO NPs (FLU-ZnO-NPs) for the management of psychosis. The synthesized FLU-ZnO-NPs were characterized using various techniques, such as X-Ray Diffractometer, Energy Dispersive X-Ray analysis, Transmission Electron Microscopy, and Zetasizer (Malvern).
Results: The characterization results showed that the synthesized FLU-ZnO-NPs had improved solubility, enhanced bioavailability, targeted delivery, and reduced toxicity.
Conclusion: The development of FLU-ZnO-NPs could provide a more effective and safe treatment option for patients with mental disorders.
PHYSICAL AND CHEMICAL EVALUATIONS OF TOPICAL RADIANCE SERUM CONTAINING NANOEMULSION COMBINATION OF ASTAXANTHIN AND ZEAXANTHIN: DESIGNED AS ANTI-WRINKLE AND SKIN-BRIGHTENING SERUM
Authors: NURDIANTI LUSI , SETIAWAN FAJAR , RUSDIANA TAOFIK , GOZALI DOLIH , CAHYATI KENI IDA
Published: September 2023

Objective: The present study was conducted to formulate and evaluate the radiance serum containing the combination of astaxanthin and zeaxanthin nanoemulsion designed for anti-wrinkle and skin brightening serum by topical route of administration.
Methods: The nanoemulsion containing astaxanthin and zeaxanthin was prepared using the self-nano emulsifying method, followed by incorporation into the radiance serum by the conventional mixing method. The quantity and ratio of surfactant, co-surfactant, and oil phase have been optimized in the previous study, as well as the radiance serum formula. The evaluation of the nanoemulsion and radiance serum was carried out by physical and chemical characterization. At the end of the study, an antioxidant activity of the serum containing nanoemulsion of astaxanthin and zeaxanthin was performed by DPPH method and the antioxidant activity was compared to its pure forms. The evaluation of the ex vivo permeation study was carried out to evaluate its possibility as an anti-wrinkle and skin brightener.
Results: An astaxanthin and zeaxanthin nanoemulsion had a good physical properties with a globule size around of 20 nm (narrow particle size distribution), an entrapment efficiency range greater than 85%, and had a spherical morphology. The radiance serum had a good organoleptic and spreadability with the semifluid characteristic. Based on the result of antioxidant activity, the radiance serum had a highly active antioxidant activity. The radiance serum contained of astaxanthin and zeaxanthin nanoemulsion of 1% concentration, astaxanthin had a 2-6 times cumulative released compared than zeaxanthin (p<0.05) and all of the formulations exhibited a high skin permeation significantly.
Conclusion: A formulation of nanoemulsion-based serum containing astaxanthin and zeaxanthin for topical delivery has been successfully developed. Based on the results of physical evaluation and especially from the permeation study, it seems that radiance serum containing astaxanthin and zeaxanthin nanoemulsion was potential to be used as an anti-wrinkle and skin brightening, however this function must be proven in further research.
DEVELOPMENT AND EVALUATION OF GASTRIC FLOATING TABLETS OF RIBOFLAVIN USING BOX-BEHNKEN DESIGN
Authors: SVN PADMA , PAPPULA NAGARAJU , NAIK V. VASU , MURTHY KOLAPALLI VENKATA RAMANA
Published: September 2023

Objective: To develop and evaluate gastric floating tablets of riboflavin that was thermally fused using an experimental design method.
Methods: Gastric floating tablets were developed using the Box-Behnken design. The effect of sintering on various tablet properties is assessed. The prepared floating tablets were tested for characteristics like usual tablet quality control tests with special emphasis on buoyancy studies and in vitro drug release studies.
Results: The drug-excipient incompatibility studies indicated no interactions between riboflavin and carnauba wax. Sintering the powder at 1200, °C partially decreased its crystallinity and improved drug release for up to 16 h. The tablets demonstrated good flow properties, acceptable hardness, low friability, and uniformity in thickness and diameter. Statistical models successfully optimized the formulation to achieve desired characteristics and practical compressibility. The optimal amounts of the variables, according to Design Expert® 12 software, were 59.19 mg of carnauba wax, 14.63% w/w of sodium bicarbonate, a sintering temperature of 74.68 °C, and a sintering exposure time of 1.99 h.
Conclusion: In vitro dissolution studies were conducted on the optimized formulation to verify the model's predictions. The experimental results closely matched the predictions. The optimized formulations showed a floating lag time of 104 seconds and a floating duration of 12.3 h. The obtained T90 was found to be 11.3 h which followed zero order kinetics with a non-Fickian diffusion mechanism.
EVALUATION OF FABRICATED SOLID MICRONEEDLES AS SMART APPROACH FOR TRANSDERMAL DRUG DELIVERY SYSTEM OF ASTAXANTHIN
Authors: KAUR RAJWANT , ARORA SAAHIL , GOSWAMI MANISH
Published: September 2023

Objective: The lack of drugs to effectively cross the stratum corneum (SC), has recently been a significant barrier to transdermal administration. In order to increase the effectiveness of transdermal distribution, this issue has been solved through the development of micron-scale needles. The objective is to develop, formulate and evaluate biocompatible polymeric solid microneedles with a TDDS-loaded Astaxanthin patch involving the poke and patch method.
Methods: The solid microneedle arrays were fabricated using an SLA printer with high-resolution potential and was examined using scanning electron microscopy (25 microns at the z-axis and 140 microns at the x-axis, respectively). Fabricated Astaxanthin transdermal film was evaluated by many characterization parameters. The developed microneedle was examined for skin insertion and a drug permeation study was carried out across the porcine skin.
Results: Solid MN arrays of 1.85 µm tip-to-tip distance, 600 µm height, 300 µm width, and 30 µm tip diameter, were created using biocompatible Class I Dental SG resin. Microneedle crossed stratum corneum layer and penetrated porcine skin with 381.356 mm in depth, with no structural change. Transdermal patches loaded with astaxanthin drug was developed and using various polymer concentration consistent, good, and transparent films were created of thickness between 0.85±0.07 mm to 0.87±0.01 mm range, with average weights ranging from 168.02±1.05 to 172.22±1.25 10/cm2), Folding Endurance with 10-12 folds was reported for formulated transdermal films; also tensile strength was 0.414±0.002 kg/mm2 and drug content was 94.41±0.42% of the best formulation reported. According to studies on drug permeation, Astaxanthin transdermal patches did not significantly permeate porcine skin without being pierced by microneedles the medication exhibited good penetration characteristics.
Conclusion: Upon evaluation, formulated transdermal film was reported to be best for solid microneedle-TDDS of astaxanthin for improved patient compliance, bioavailability, and biomedical applications.
FORMULATION AND DEVELOPMENT OF MUCOADHESIVE NASAL DRUG DELIVERY OF ROPINIROL HCL FOR BRAIN TARGETING
Authors: SONAWANE AMRUTA , JAWALE GAYATRI , DEVHADRAO NITIN , BANSODE ASHWINI , LOKHANDE JYOTI , KHERADE DHANASHREE , SATHE PRATIKSHA , DESHMUKH NITIN , DAMA GANESH , TARE HARSHAL
Published: September 2023

Objective: The purpose of this research was to create polymeric nanoparticles of ropinirole HCl for nasal administration utilising the ionic gelation process.
Methods: The preparation method was optimized using box-behnken design employing chitosan concentration, guar gum concentration and surfactant concentration as independent variables were as Encapsulation efficiency and mucoadhesion of the formulation were selected as dependent variables. Differential scanning calorimetry and infrared spectroscopy analysis of the drug and polymers revealed that the drug and excipients are physicochemically compatible. Studies on entrapment efficiency, drug content, and In vitro release were conducted on the nanoparticles.
Results: Each formulation was determined to have a drug content of between 60% and 70% and an entrapment efficiency of between 65% and 84%. In vitro drug release tests demonstrated that ropinirole HCl will release between 65 and 81 percent after 5 h.
Conclusion: The results showed that the particle size, encapsulation effectiveness, and drug content were all significantly affected by the amounts of chitosan and guar gum.
IMPLICATION OF CENTRAL COMPOSITE DESIGN IN THE DEVELOPMENT OF SIMVASTATIN-LOADED NANOSPONGES
Authors: NOOTHI SADHANA , MALOTHU NARENDER , ARETI ANKARA , DESU PRASANNA KUMAR , KUMAR SARVAN
Published: September 2023

Objective: The present study’s objective was to apply a central composite design to develop the simvastatin-loaded nanosponge formulation to improve its oral bioavailability. Methods: With the help of a design expert (State-Ease version 13.0.1), a central composite design was selected for the formulation of simvastatin-loaded nanosponges by using a defined concentration of Eudragit L-100 (X1) and PVA (X2) as independent variables and particle size (Y1), percent (%) entrapment efficiency (EE) (Y2), in vitro drug release (Y3) as dependent variables. Fourteen (SF1-SF14) formulations were prepared using the emulsion solvent evaporation and evaluated for surface morphology, particle size, drug-excipient compatibility, %EE, and % drug release. The optimized model (SF14) obtained from a design expert was evaluated for in vivo pharmacokinetics in animal models. Results: SF14 was formulated and evaluated for morphology (shape and size) of the particle, % EE, in vitro % drug release, and its kinetics. The formulation showed particle size of 163±0.45 nm, 80.54 %±0.57 of EE, and 97.13%±0.38 of drug release at 8h. The release kinetics followed the zero-order and Higuchi mechanisms with non-fiction diffusion. In vivo results showed Cmax, Tmax, AUC0-t, AUC0-α, and MRT0-α for nanosponges were 0.175 µg/ml, 6 h, 1.561 µg/mlh, 1.755 µg/mlh, 11.77 h, respectively. Conclusion: The results indicated a significant increase in the bioavailability of the drug in nanosponges compared with standard drugs. The experimentally designed nanosponge formulations have been successfully developed, and evaluated parameters show that the nanosponge formulation of Simvastatin is a promising delivery through the oral route.
GLIBENCLAMIDE TRANSETHOSOME PATCH FOR TRANSDERMAL DELIVERY: FORMULATION AND EVALUATIONS
Authors: YUSUF NURUL ARFIYANTI , ABDASSAH MARLINE , MAULUDIN RACHMAT , CHAERUNISAA ANIS YOHANA
Published: September 2023

Objective: The glibenclamide transethosome patch is a patch containing glibenclamide encapsulated in nanoparticle-based vesicles that can improve the penetration of the compound into the skin. The research work aims to evaluate glibenclamide transethosome patches using HPMC and PVP as matrix polymers and glibenclamide as a drug model.
Methods: Glibenclamide transethosome patches were prepared using a solvent evaporation technique. Evaluations that have been carried out to assess the stability of the patch include weight variation, folding endurance, thickness, moisture absorption, moisture content, drug content, and drug release in vitro glibenclamide transethosome was carried out using Franz diffusion cell.
Results: The results of the evaluation of the glibenclamide transethosome patch showed a patch weight uniformity between 0.051-0.063 g and a CV (Coefficient of Variation) value of less than 5%. The resulting folding resistance of the patch can withstand without tearing over 200 folds. The thickness of the glibenclamide transethosome patch is between 0.14-0.24 cm. The moisture absorption capacity of the patch is between 2.1-23.5%. The moisture content of the patch is between 4.7-7.4%. The drug content of the patch is between 6.7–12.7 g/cm2. Drug release from the patch was between 45.9-82.1% after 480 min. Overall, in the moisture absorption test (F3; F4; F5), moisture content, drug content, and drug release (F1) gave significantly different results (p<0.05).
Conclusion: The glibenclamide transethosome patch showed evaluation results that met the requirements and were stable during the stability test. The polymer combinations also significantly influence drug release during stability tests.
THE DEVELOPMENT AND VALIDATION OF HPLC AND HPTLC-DENSITOMETRY METHODS FOR THE DETERMINATION OF 1, 4-NAPHTHOQUINONE CONTENT IN ELEUTHERINE BULBOSA EXTRACT
Authors: MUTIAH ROIHATUL , ROZIQIN AHMAD AINUR , UMAIRAH KARTIKA NIBRAS , TAUFIK IMAM , SURYADINATA ARIEF
Published: September 2023

Objective: The aim of this research was to develop and validate identification and Quantitation methods for 1,4-naphthoquinone in the extract of Eleutherine bulbosa.
Methods: High-performance liquid chromatography (HPLC) and high-performance thin-layer chromatography with densitometric detection (HPTLC-densitometry) were employed as analytical techniques. HPTLC-densitometry was performed at a wavelength of 249 nm, while UHPLC was conducted at a wavelength of 254 nm. Both methods were utilized to analyze 1,4-naphthoquinone in 96% ethanol extract of E. bulbosa as a Quantitation parameter in the standardization of the formulation. HPTLC separation was carried out on a 20 cm × 20 cm HPTLC glass plate coated with silica gel 60 F254 using a mobile phase of chloroform: methanol (8:2, v/v). For HPLC analysis, a C18 column with an isocratic method was employed using a mobile phase of 95% methanol in pump A and 0.5% chloroform in pump B. The calibration curve of peak area against concentration showed linearity within the range of 2500-15000 ppm/spot−1 and 3–21 μg/ml for HPTLC and HPLC, respectively. Both methods were validated for accuracy, precision, linearity, selectivity, LOD, and LOQ.
Results: The results showed that both methods exhibited linearity that met the standards, as they produced correlation coefficients (r) greater than 0.9900. Furthermore, both methods demonstrated good accuracy, with consecutive recovery values of 99.53% and 101.89%. On the other hand, the methods fulfilled the precision requirements, with respective values of 0.7159% and 2.884% (in compliance with the requirement of<5%). Additionally, to meet the LOD and LOQ requirements in HPTLC, the LOD value obtained was 163 ppm, and the LOQ value was 495 ppm. In HPLC, the retention time of the standard 1,4-naphthoquinone and the analyte compound in the extract of E. bulbosa were the same, at 3.507 min. The selectivity test on HPTLC indicated that the 1,4-naphthoquinone compound was at an RF value of 0.81, which was also detected in the extract of E. bulbosa at the same RF value.
Conclusion: In conclusion, our findings demonstrate that HPLC and HPTLC methods for the determination of 1,4-naphthoquinone content have met the standards for linearity, accuracy, precision, selectivity, LOD, and LOQ. Therefore, these methods can be recommended for the quality control of raw materials of E. bulbosa extract.
IN SILICO MOLECULAR SCREENING AND DOCKING APPROACHES ON ANTINEOPLASTIC AGENT-IRINOTECAN TOWARDS THE MARKER PROTEINS OF COLON CANCER
Authors: V. MAHALEKSHMI , N. BALAKRISHNAN , T. V. AJAY KUMAR , V. PARTHASARATHY
Published: September 2023

Objective: The present investigation explores the binding affinities of Irinotecan, which is a topoisomerase I inhibitor, against the targets such as AKT1, TNKS-2, MMP, EGFR, TNKS-1, and BRAF, which are the protein that was overexpressed by colorectal carcinogenesis.
Methods: In this study, the drug structure was drawn by chemdraw software and explored for its anti-cancer potential by Schrodinger software against selected targeted proteins such as epidermal growth factor receptor (EGFR), matrix metalloproteinase (MMPs), serine/threonine protein kinase Ba (AKT1), BRAF, tankyrases 1 (TNKS-1, and tankyrases 2 (TNKS-2).
Results: From the results of docking analysis, the targets with the maximum binding affinity towards the preselected drug Irinotecan were further subjected to ADME prediction by the QikProp module of Schrodinger Maestro version 2018.4. Molecular docking analysis revealed that surface protein targets AKT1, TNKS-2, MMP, and EGFR have the highest binding affinity towards the selected topoisomerase I inhibitor Irinotecan when compared to TNKS-1 and BRAF targets. The higher docking score of Irinotecan with extracellular colorectal cancer target proteins was discovered in this investigation.
Conclusion: Cancer is one of the most prevalent, lethal and risky malignant pathologies with an elevated prevalence and mortality rate worldwide. The current work will be more beneficial for rationalising the effective anticancer treatment according to the intensities of expression of the colon cancer target protein and for creating an optimum targeted drug delivery system of an anticancer agent to treat colon cancer.
PREPARATION AND EVALUATION OF PROPRANOLOL HCL AND CARBAMAZEPINE RELEASE PROFILES FROM POLY(Є-CAPROLACTONE) MICROPARTICLE BLENDS SYSTEM
Authors: MUHAIMIN MUHAIMIN , CHAERUNISAA ANIS YOHANA , HAZRINA AGHNIA
Published: September 2023

Objective: The goal of this research was to look into the physicochemical properties of poly(-caprolactone) microparticle blends that contained medicines of various solubilities (Propranolol HCl [Pro] and carbamazepine [CBZ]).
Methods: W/O/W emulsion for Pro and O/W emulsion for CBZ were used to create microparticle blends. With dispersion time intervals (DTI) of 0 and 60 min, the Pro emulsion (W/O) and CBZ oil phase (O) were dispersed in an external aqueous phase (W). Scanning electron microscopy was used to examine the morphology of microparticle blends (SEM). Focused beam reflectance measurements were utilized to monitor the particle size mean of emulsion droplets/hardened microparticles (FBRM). In phosphate buffer (pH 7.4), encapsulation efficiency (EE) and in vitro drug release were also examined.
Results: The final microparticle blends generated by solvent evaporation method were spherical and had two populations, according to the findings. The size of microparticle blends prepared with DTI 60 min and stirring duration 4 h was bigger than those prepared with DTI 0 min, according to FBRM data. In microparticle blends, encapsulation efficiency ranged from 62.05±3.74 percent to 66.38±4.16 percent for Pro and 70.56±4.62 percent to 73.85±4.11 percent for CBZ. After 28 d, drug release in phosphate buffer revealed that Pro release (33%) was shorter than CBZ release (60%) from microparticle blends with DTI 60 min. This was related to the interaction of the oil phase (CBZ) with hard particles from the primary emulsion (Pro), in which the oil phase occluded and covered surface structure of the harsh particles from the primary emulsion.
Conclusion: Novel microparticle blends comprising drugs/medicines with varying solubilities (e. g. propranolol HCl and carbamazepine) have a lot of promise as controlled-release drug delivery systems. The physical properties of microparticle blends were impacted by the type of dispersion time interval used.
REVIEW ON COMPREHENSIVE DESCRIPTION OF DEVELOPMENT AND ASSESSMENT OF CO-CRYSTAL DRUG DELIVERY SYSTEM
Authors: BIDHURI NAVEEN , PADHI SWARUPANJALI
Published: September 2023

Over the past few decades, co-crystal Drug Delivery System (DDS) has attracted interest due to their potential to increase the solubility, stability, and bioavailability of medications that aren't sufficiently soluble. In this study, we factualized to develop a co-crystal chemical delivery system utilizing an experimental model. We utilized caffeine and succinic acid as model chemicals and prepared co-crystals utilizing different methods, including solvent evaporation, grinding, and spray drying. The co-crystals have been characterized utilizing X-ray powder diffraction, Fourier-transform infrared spectroscopy, and differential scanning calorimetry. The solubility and dissolution rate of the co-crystals has been evaluated in simulated digestive and intestinal juices. The outcomes showed that when compared to co-crystals made utilizing the solvent evaporation and spray drying procedures, those organized utilizing the grinding approach exhibited the maximum solubility and dissolution rate. This study underlines the potential of co-crystals as a workable method for enhancing the administration of pharmaceuticals that are not adequately soluble and provides a helpful experimental paradigm for the development of co-crystal chemical delivery systems.
VIRTUAL BIOEQUIVALENCE IN PHARMACEUTICALS: CURRENT STATUS AND FUTURE PROSPECTS
Authors: C. SOWMYA , H. ABRAR AHMED , K. K. SURIYA PRAKAASH
Published: September 2023

Virtual bioequivalence studies (VBE) can assess the similarity and potential differences in pharmacokinetic and clinical performance between test and reference formulations based on the translational relationship between in vitro, in silico, and in vivo. The crucial data from clinical trials can be delivered with the help of virtual bioequivalence research, which will speed up the creation of novel and generic medications. Virtual bioequivalence study regulation, however, has not yet reached its complete development. The current status of VBE studies in the market is booming and many pharmaceutical industries have started adapting to its benefits in submitting bioequivalence results for approval from regulatory bodies. FDA had regulated the guidelines for virtual bioequivalence, which the various regulatory agencies accept for the approval of filing ANDA. The importance of implementing VBE has benefited at present in saving cost and time; low workforce and failures can be neglected. Determining the framework for virtual bioequivalence studies for all medications and discussing the potential uses of virtual bioequivalence in the future to support the waiver and optimization of in vivo clinical trials are the main objectives of this review article.
OPTIMIZATION AND CHARACTERIZATION OF ESSENTIAL OILS FORMULATION FOR ENHANCED STABILITY AND DRUG DELIVERY SYSTEM OF MEFLOQUINE
Authors: MOHAPATRA PRIYADARSHINI , CHANDRASEKARAN NATARAJAN
Published: September 2023

Objective: This work aims to choose suitable essential oil formulations to improve the bioavailability and long-term aqueous stability of mefloquine in drug delivery systems.
Methods: Oil phases of pomegranate oil, black cumin seed oil, and garlic oil. To choose the proper oil and surfactant for creating pseudo-ternary phase diagrams, cremophore EL, tween®20 and tween®80 (surfactants), and brij 35 (co-surfactants) were used in a variety of concentrations and combinations (Smix). Mefloquine was estimated to be soluble in a variety of oils, surfactants, and co-surfactants. Drug solubility, drug release research, thermodynamic stability, mean hydrodynamic size and zeta potential.
Results: Garlic with smix of cremophore EL and brij 35, Pomegranate with Tween 2.0, and Black cumin seed oil with Tween 80 showed the highest solubilization and emulsification capabilities and were further investigated using ternary phase diagrams. When combined with the co-surfactants under investigation, cremophore EL demonstrated a greater self-emulsification zone than tween® 80 and tween 20. Garlic oil, cremophore EL, and brij 35 nanoemulsion showed smaller size, greater zeta potential, less emulsification time, high transmittance, and better drug solubility than microemulsion formulations on especially those made with tween®20 and tween 80. Mefloquine loaded garlic oil nanoemulsion showed considerably low release in body fluid (32.48%) and a good release in intestinal fluid (82.78%) by 12 h in a drug release study.
Conclusion: Garlic oil as the oil phase and a mixture of cremophore EL and brij 35 as the surfactant phase are ideal surfactants and co-surfactant for mefloquine loaded garlic oil nanoemulsion with greater drug release in release kinetics investigation.
POTENTIAL HERB-DRUG INTERACTION OF DECALEPIS HAMILTONII VIA P-GP MEDIATED PHARMACOKINETIC INTERACTION WITH FEXOFENADINE IN RATS: AN IN SITU AND IN VIVO STUDY
Authors: SANDOPA DHANUNJAYA , VELLAPANDIAN CHITRA
Published: September 2023

Objective: The objective of this study was to investigate the influence of Decalepis hamiltonii (D. hamiltonii), a traditional plant used in herbal medicine, on the intestinal absorption and pharmacokinetics of fexofenadine, a substrate of P-glycoprotein (P-gp), in rats.
Methods: In situ intestinal perfusion tests were conducted to assess the intestinal permeability of fexofenadine. P-gp ATPase activity was also evaluated to understand the modulatory effects of D. hamiltonii on P-gp. An in vivo pharmacokinetic investigation was performed by administering oral fexofenadine to rats.
Results: The in situ study results revealed that the effective permeation (Peff) of fexofenadine was significantly diminished (p<0.001***) in aqueous extract of D. hamiltonii (AREDH, 200 mg/kg p. o.) pretreated group compared to normal control indicating modulation in absorption. Further, there was significant augmentation (p<0.01**) of P-gp ATPase activity in AREDH pretreated group (200 mg/kg p. o.) compared normal control indicating P-gp inductive potential of D. hamiltonii. Pharmacokinetic study results revealed that the peak plasma concentration (Cmax) and the area under the concentration-time curve (AUC) of fexofenadine was significantly downregulated (p<0.001***) in AREDH pretreated group (200 mg/kg p. o.) compared to the normal control group indicating the compromised absorption and bioavailability. However, no significant changes were observed in fexofenadine half-life (T1/2 k10), time to reach peak plasma concentration (Tmax), or elimination rate constant (k10).
Conclusion: In conclusion, D. hamiltonii significantly reduced the oral bioavailability of fexofenadine by promoting P-gp-mediated drug efflux during intestinal absorption. This suggests that the modulatory characteristics of D. hamiltonii may lead to herb-drug interactions when taken in combination with xenobiotics, emphasizing the importance of considering such interactions in clinical practice and further research.
PREPARATION AND OPTIMIZATION OF CILOSTAZOL NANOEMULSION ORAL LIQUID DOSAGE FORM
Authors: AL-SHAIBANI ABULFADHEL JABER NEAMAH , AL-GBURI KARRAR , ALBO HAMRAH KARRAR TALIB KHUDHAIR
Published: September 2023

Objective: Cilostazol has poor water solubility and low oral bioavailability. Therefore, the formulation of cilostazol as a nanoemulsion may enhance its solubility and improve oral bioavailability. Hence, the aim of this study was to formulate and characterize an oil-in-water (o/w) nanoemulsion of cilostazol as an oral liquid dosage form.
Methods: Pseudo-ternary phase diagrams were constructed using the aqueous titration method. Formulations of pseudo-ternary phase plots consisting of oil, various weight ratios of S mix (mixture of surfactant and co-surfactant), and deionized water were made. Different characterization studies, droplet size measurement, polydispersity index, drug content, zeta potential measurement, and in vitro release have been conducted to choose the optimized formula.
Results: The characterization studies have demonstrated that the optimized formula is (F-6), consisting of 20 % S mix (3:1), 10% ginger oil, and 70% deionized water. This formula had the following characteristics; droplet size (72.9-110 nm), polydispersity index (0.22), percentage of drug content (99.8%), and in vitro release of cilostazol nanoemulsion was significantly higher (P<0.05) in comparison with other formulations. A Scanning probe microscopy (SPM) study has revealed that the droplet size of F-6 was at the nano-scale.
Conclusion: In conclusion, the optimized cilostazol formula (F-6) is a promising formula which may have the capability of improving the oral bioavailability of cilostazol.
TAILORED BASELLA ALBA MUCILAGE-BASED BIPOLYMERIC HYDROGEL BEADS FOR CONTROLLED RELEASE OF DICLOFENAC SODIUM
Authors: CHOWDHURY MOUMITA , KUMAR DE PINTU
Published: September 2023

Objective: The present investigation aims to convert the underutilized Basella alba mucilage (BAM) into a smart carrier by formulating its bipolymeric hydrogel beads for the controlled release of Diclofenac sodium (DFS).
Methods: At first, mucilage from the stem and fruits of Basella alba was extracted, isolated, and evaluated. Basella alba mucilage was chemically modified to its carboxymethyl derivative to improve its physicochemical properties. Single and bipolymeric hydrogel beads of carboxymethylated Basella alba mucilage (CBAM) and Sodium carboxymethyl cellulose (SCMC) were formulated by the Ionotropic gelation method using aluminium chloride (AlCl3) as a cross-linking agent. A four-factor I-optimal response surface design was used to optimize the formulations. Drug and excipient compatibility was studied by Fourier transform infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) study. Scanning electron microscopy (SEM) was done to reveal the surface morphology. In vitro release of the drug in phosphate buffer (pH 6.8) and acidic buffer (pH 1.2) were compared for all the formulations. The effect of various formulation parameters on the release of the drug was studied, and the best-fitting model for release kinetics was determined.
Results: The degree of carboxymethylation was found to be 0.565±0.05. The bipolymeric beads were found to release 14% drug in 2 h in acidic media, minimize the release of the drug in the stomach to avoid the harsh effects of DFS and then provide controlled release in the intestine, releasing 80-90% of the drug in 10 h. The release kinetics followed the Hixon Crowell model, which suggests an erosion of the matrix to release the drug.
Conclusion: The bipolymeric hydrogel beads of tailored Basella alba mucilage were found to control the release of Diclofenac sodium.