bluuebunny/crossref_metadata_2025 huggingface dataset:
Anticancer Activity of Gymnema sylvestre R.Br.
Authors: A.V Srikanth , Maricar Sayeeda , M Lakshmi Narsu M , P Ravi Kumar , Baig Madhava Reddy
Published: August 2020

Anticancer Activity of Gymnema sylvestre R.Br.
In vitro Passive and Iontophoretically Assisted Transport of Salbutamol sulphate through Hairless Mice Skin
Authors: Abdul Faruk , Singh Gurpreet , Ishar Mohan Paul Singh
Published: August 2020

Investigations were carried out to ascertain the relative importance of the described mechanism in iontophoretic transport using an ionizable drug salbutamol sulphate, which has two pKa values 9.3 (for amino group) and 10.3 (for phenolic group). Ionization of salbutamol sulphate varies with pH, hence the rate and extent of transport across the skin can be enhanced, controlled and manipulated by the application of factors like anodal and cathodal current at varied pH of donor solution and current densities. To determine these parameters, experiments were performed and data was collected at 7.4, 9.3, 10.3 and 11 pH using 4mg/ml drug concentration and 0.3mA/cm2 current density for 6 hours. After establishing the pH for optimum transport of drug, effect of current density (0.1, 0.2, 0.3 and 0.4 mA/cm2) on the transport of drug (keeping drug concentration constant) were investigated. Passive diffusion of salbutamol sulphate was maximal at pH 10.3 and 9.3, when unionized form of drug was 50%. Anodal iontophoresis at pH 7.4 was most effective (significant result,                p < 0.05) in transport of drug across skin as compared to cathodal iontophoresis at pH 11. The effect of current density on steady state flux by salbutamol sulphate during anodal iontophoresis at 7.4 pH showed 2.26 and 28.05µg/cm2/h at 0.0 i.e., passive diffusion and 0.4 mA/cm2, respectively. Thus, flux was enhanced nearly 12 times during anodal iontophoresis.
Development of Topical Diclofenac Sodium Liposomal Gel for Better Antiinflammatory Activity
Authors: Jithan A V , M Swathi
Published: August 2020

The objective of this study was to develop a diclofenac liposomal gel intended for better anti-inflammatory activity compared to a normal gel after topical administration. Spherical multilamellar vesicular liposomes (MLVs) consisting of soya lecithin, cholesterol and diclofenac were prepared via thin film hydration methodology. Small unilamellar vesicles (SUVs) were then prepared out of MLVs. Entrapment efficiency, the drug associated with SUVs was subsequently determined. Liposomal gel formulations were then prepared by incorporation of SUVs into carbopol 934 gel previously prepared. The formulations were then characterized for in vitro drug release, ex vivo permeation studies, drug-lipid compatibility and rheological behaviour. Vesicle size/Zeta potential of the liposomes containing in one selected formulation were determined. Pharmacodynamics was also determined for selected diclofenac liposomal gel. Diclofenac liposomal gel formulation prepared showed more sustained and prolonged anti-inflammatory effect compared with diclofenac gel. Taken together, the results indicate that the diclofenac liposomal gel is better than the regular gel without liposomes. Drug-lipid compatibility studies indicated no interaction with drug and the polymer.
Formulation Study and Evaluation of Matrix and Three-Layer Matrix Tablets Oral Controlled Drug Delivery System Based on Xanthan Gum and Locust Bean Gum
Authors: Rao Y. Madhusudan , Ahmed S L , Narsu M L , Mohan S J
Published: August 2020

The present study was carried out to develop oral controlled release matrix tablets and three layer matrix tablets of highly water soluble diltiazem HCl using natural polymers Xanthan gum (XG), locust bean gum (LBG) and a mixture XG: LBG in 1:1 ratio as matrix forming agent, and anionic Sodium Carboxyl Methyl Cellulose as release retardant layer on the matrix core, Di calcium Phosphate (DCP) and Micro crystalline Cellulose (MCC) as fillers. Matrix core tablets were prepared with by granulation technique.The characterization of physical mixture of drug and excipeints was performed by infra red spectroscopy. The finding of the study indicated that the matrix tablets prolonged the release, but predominantly in a first order fashion, layering with SCMC granules on the matrix core, provided linear drug release with zero order kinetics. The influence of layers on matrix core and release rate was described by the peppas equation, model independent approach, Mean dissolution time (MDT) and dissolution efficiency (D.E 8%). The addition of SCMC layers on the matrix core could notably influence the dissolution behavior and mechanism of drug release. Increasing the quantity of layers caused decreased values of k and increased n value, in a linear relationship. MDT for matrix tablet (S6)  and three layer matrix tablets (S6L3) was found to be 5.16h and 11.97h, D.E 8% was 76.23% and 66.21% respectively.  These indicated that the release of drug is slower from the three layer matrix tablets. Type of fillers has a limited effect on the drug release mechanism from matrix tablets. Stability studies revealed that the formulation was stable at 45°±2°C and 75±5%RH. Hence natural polymer as matrix core and anionic polymer SCMC as retardant layer in the form of three layer matrix tablets provided the zero order release of highly water soluble Diltiazem HCl.
Development and Characterization of Aspirin-Phospholipid Complex for Improved Drug Delivery
Authors: Semalty A , Semalty M , Singh D , Rawat M S M
Published: August 2020

Aspirin (acetylsalicylic acid) is one of the most widely used analgesic.  Aspirin is poorly soluble in water and causes gastrointestinal (GI) irritation. To improve the solubility (and hence the bioavailability) and minimize the GI irritation, its complexes with soya-phospholipid-80 % (in  1: 1 molar ratio) were prepared in an organic solvent and evaluated for solubility, drug content, scanning electron microscopy (SEM), FT-IR spectra, X ray diffraction, differential scanning calorimetry (DSC) and in vitro dissolution study. Aspirin-phospholipid complex were found to be disc shaped with rough surface in SEM. Drug content in the complex was found to be 95.6 %. DSC thermograms, XRD and FTIR confirmed the formation of phospholipid complex. Solubility of the prepared complex was found to be improved. Aspirin complex and aspirin showed 90.93 % and 69.42 % of drug release at the end of 10 h in dissolution study in pH 1.2 acid buffer. It was concluded that the phospholipid complex of aspirin may be of potential use for improving the solubility of aspirin and hence its bioavailability. The complexes may also reduce GI toxicity of the drug.
Studies on the Preparation and Evaluation of Chitosan Nanoparticles containing Cytarabine
Authors: Debnath S , Datta D , Babu M N , Kumar R S , Senthil V
Published: August 2020

The activity of cytarabine was decreased by its rapid deamination to the biologically inactive metabolite uracil arabinoside. This rapid deamination is the reason for the ongoing research for effective formulation of cytarabine that can not be deaminated and exhibit better pharmacokinetic parameters. Protection of cytarabine from fast degradation and elimination was investigated by encapsulating the drug into chitosan nanoparticles. Cytarabine loaded nanoparticles prepared by ionotropic gelation were characterized by SEM and was found to in the range of 200 nm.The mechanism by which drug is being released is non-Fickian(anomalous) solute diffusion mechanism. It is evident from the result that initial burst release was retarded or delayed due to adsorption of coating material. The in vivo biodistribution study results showed that the nanoparticles were having better distribution of drug compared to free drug in different organs like spleen, lungs, kidney etc.
"Effect of Hydrophilic and Hydrophobic Polymers and in vitro Evaluation of Hydro – Dynamically Balanced System of Metoclopramide Hydrochloride"
Authors: V V Wamorkar , Varma M Mohan , B VijayKumar , V Malla Reddy
Published: August 2020

Objective of present studies was to develop Hydro-dynamically Balanced system (HBS) of Metoclopramide Hydrochloride by non-effervescent technique.  Different grades of polymers were used for prolonging release and flotation of the capsule. In order to study effect of concentration of release retardant, formulations of different combinations were studied. The floating capsules were evaluated for drug content, floating behavior, weight variation and in-vitro dissolution. After fitting the dissolution data into various models like zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer’s-Peppas, the selected formulation was found to follow Higuchi model with Fickian diffusion mechanism. Stability studies were carried out at 40°C/75% RH for 6 months and results showed no significant changes in physical appearance, floating behavior, and drug content. These experimental clearly indicated that metoclopramide HCl floating drug delivery systems may be formulated to match patient compliances.
Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles
Authors: Verma V K , A Ram
Published: August 2020

Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h.
Novel Approaches for Oral Delivery of Insulin and Current Status of Oral Insulin Products
Authors: V P Kinesh , D P Neelam , B Punit , S.B Bhavesh , K. S Pragna
Published: August 2020

Diabetes mellitus is a serious pathologic condition that is responsible for major healthcare problems worldwide and costing billions of dollars annually. Insulin replacement therapy has been used in the clinical management of diabetes mellitus for more than 84 years. The present mode of insulin administration is by the subcutaneous route through which insulin is presented to the body in a non-physiological manner having many challenges. Hence novel approaches for insulin delivery are being explored. Challenges to oral route of insulin administration are: rapid enzymatic degradation in the stomach, inactivation and digestion by proteolytic enzymes in the intestinal lumen and poor permeability across intestinal epithelium because of its high molecular weight and lack of lipophilicity. Liposomes, microemulsions, nanocubicles, and so forth have been prepared for the oral delivery of insulin. Chitosan-coated microparticles protected insulin from the gastric environment of the body and released intestinal pH. Limitations to the delivery of insulin have not resulted in fruitful results to date and there is still a need to prepare newer delivery systems, which can produce dose-dependent and reproducible effects, in addition to increased bioavailability.
Enhanced Dissolution Rate of Glipizide by a Liquisolid Technique
Authors: Mahajan Hitendra S , Dhamne Manoj R , Gattani, Surendra G. , Rasal Ashwini D , Shaikh Hannan T
Published: August 2020

This study aims to prepare immediate release glipizide liquisolid tablets using Avicel PH-102 and Aerosil 200 as the carrier and coating material respectively to increase dissolution rate of poorly soluble glipizide. This study also aims to evaluate treated Gellan gum as disintegrant in the preparation of liquisolid tablets. The solubility of glipizide was increased by use of liquisolid technique. The glipizide liquisolid tablets were evaluated for characteristics like drug content, friability, hardness, disintegration time, thermal analysis, X-ray diffraction (XRD) study and dissolution rates. The dissolution patterns of glipizide liquisolid tablets, carried out according to USP paddle method, and were compared with their commercial counterparts. The results obtained shows that all glipizide liquisolid tablets exhibits higher dissolution rates than those of marketed glipizide tablets. Dissolution rates increases with increasing concentration of liquid vehicles and maximum drug release achieved by formulations containing Polyethylene glycol 400 (PEG 400) as a liquid vehicle. The results of XRD and thermal analysis did not show any changes in crystallinity of drug and interaction between glipizide and excipients during the formulation process.
Pharmacognostical and Phytochemical Investigations of Cocculus pendulus (J.R. and G. Forst.) Diels Leaf
Authors: G Vidyasagar , H.A. Rabari , S S Pandya , Rao Shrinivas , B Gajra , Somani J U , Dedania R R
Published: August 2020

The leaves of Cocculus pendulus (J.R. & G. Forst.) Diels (Menispermaceae) is reported to have good medicinal values in the traditional system of medicines. The present study deals with pharmacognostical examination of morphological and microscopical characters and phytochemical investigations of Cocculus pendulus leaves including determination of loss on drying, ash values and extractive values. The preliminary phytochemical screening of powdered drug was also carried out. The qualitative chemical examinations revealed the presence of various phytoconstituents like alkaloids, carbohydrates, phytosterols, proteins and mucilages in the leaf extracts.
Formulation and Evaluation of Extended Release Trihexyphenidyl Hydrochloride Hard Gelatin Capsules
Authors: Y Madhusudan Rao , K Vinay Kumar , S Jagan Mohan , V Kiran Kumar
Published: August 2020

This work aims at investigating different types and levels of hydrophilic high molecular weight matrix agents, (including HPMC K15M, Metalose-60 SH, Metalose-65 SH and Metalose-90SH-SR), hydrophobic diluent (Talc) and formulation methods (Non-aqueous granulation and direct filling by simple mere mixture) in an attempt to formulate hard gelatin extended release matrix capsules containing Trihexyphenidyl HCl (Benzhexol). The drug release from all the extended release matrix capsules show polymer as well as talc concentration dependent retardation affect. The Metalose 90SH-SR concentration was optimized to approximately 27% w/w of total capsule net content weight. The hydrophobic diluent’s talc concentration was optimized and the useful concentration was approximately 17.45% w/w of the total net capsule content weight. The lactose concentration was also optimized and the effective concentration was found to be approximately 48.36% w/w. The prepared hard gelatin extended release capsules were evaluated for weight variation, Average net content, locked length, content uniformity, assay (drug content) and in-vitro drug release studies. From the in-vitro release studies of the prepared formulations, one formula was optimized from each method. All the formulations showed linear release profiles and extended the release of trihexyphenidyl HCl (Benzhexol) over 10 –12 h. The release profiles of extended release matrix capsules of trihexyphenidyl HCl (THP HCl) from the selected formulations were close to zero order and follow diffusion dependent release. The prepared extended release matrix capsules of trihexyphenidyl HCl (Benzhexol) produced from the optimized formulations ‘NAG-M90SH-SR-5 and DB M90SH-SR-4’ complied with the USP XXVII specifications. The difference factor (f1) and similarity factor (f2) was calculated for all these formulations and found to the below 15 and above 50. Irrespective of the formulation method type and its procedure, the prepared hydrophilic extended release matrix capsules showed non-Fickian anomalous transport (coupled diffusion in the hydrated matrix and polymer relaxation) as the values of release exponent (n) are in between 0.50 and 0.89. Finally it was clear that it is possible to design a formulation with any of the above two methods giving the desired drug release profile suggesting that nonaqueous granulation, Direct filling were good methods for preparing extended release matrix capsules of trihexyphenidyl HCl (Benzhexol).
Stimulants and Atomoxetine Use and Expenditures in Children and Adolescents in the United States
Authors: Aparasu Rajender R. , Bhatara V
Published: August 2020

This study examined national level prevalence and expenditure patterns of stimulants and atomoxetine in children and adolescents in the United States.  The 2003-2004 Medical Expenditure Panel Survey (MEPS) data were used to examine the utilization pattern of stimulants (amphetamine, dextroamphetamine, methylphenidate, and dexmethyl-phenidate) and atomoxetine in persons less than 20 years of age. Annual population, prescription, and expenditure estimates including 95% confidence intervals (CI) were derived after adjusting for the complex survey design of the MEPS.  Prescription expenditures in the MEPS represent the amount paid to pharmacies from all sources, including payments by insurance and patients. The expenditures were adjusted to 2004 US dollar using the Consumer Price Index.   In 2003-2004, an estimated 2.67 million (95% CI, 2.30 - 3.03 million) children and adolescents used stimulants or atomoxetine annually for an overall prevalence of 3.19% (95% CI, 2.78 - 3.60). Prevalence of stimulants alone was 2.78% (95% CI, 2.39-3.17%) with methylphenidates accounting for most of the usage. Children and adolescents using stimulants or atomoxetine were most often males (70%), whites (86%), and 10-14 years of age (52%). Nearly 90% of them reported an Attention Deficit Hyperactivity Disorder (ADHD) diagnosis. Annual expenditures for stimulants and atomoxetine were estimated at $1.69 billion (95% CI, $1.40 - 1.98 billion), with stimulants representing 79% of the expenditure. The average prescription cost was highest ($99.48) for atomoxetine and lowest ($75.70) for methylphenidates. Atomoxetine accounted for one-fourth of the prevalence and one-fifth of the expenditures in children.  In conclusion, although stimulants accounted for most of the usage and expenditures, atomoxetine has emerged as the leading stimulant alternative in children and adolescents. High prescription costs and utilization patterns for atomoxetine are likely to influence future prescription expenditure burdens in pediatric ADHD. More research is needed on the relative cost and effectiveness of various stimulant preparations and atomoxetine.
Analgesic and Anti-inflammatory Activity of Ficus glomerata in Experimental Animal Models
Authors: Menezes Cylma , G Kunal , N Reema , D Satyanarayana , K Jagadish
Published: August 2020

The anti-inflammatory and analgesic activity of various extracts of Ficus glomerata Roxb. were evaluated in experimental animals. We have determined the anti-inflammatory and analgesic activity of various extracts of the dried fruits of Ficus glomerata by oral administration at doses of 200 and 400 mg/kg of body weight to healthy animals. The extracts were studied for their anti-inflammatory activity in carageenan induced hind paw edema in rats and the paw volume was measured plethysmometrically after 3 hours of injection. The extracts were also evaluated for analgesic activity using Eddy’s hot plate method in Swiss albino mice. The extracts of Ficus glomerata significantly reduced carageenan induced hind paw edema in rats and analgesic activity evidenced by increase in the reaction time by Eddy’s hot plate method in Swiss albino mice. The extracts showed a similar anti-inflammatory and analgesic effect comparative to the standard drugs indomethacin and diclofenac sodium respectively. The present results indicated the ethanolic extract of Ficus glomerata exhibited more significant activity than other extracts in the treatment of pain and inflammation.
Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide
Authors: R Natarajan , Patel N , N N Rajendran , Rangapriya M
Published: August 2020

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.
Valsartan Loaded Solid Lipid Nanoparticles: Development, Characterization, and In vitro and Ex vivo Evaluation
Authors: Sawant Krutika K , Parmar B , Mandal S A , Petkar K C , Patel L D
Published: August 2020

Valsartan is an antihypertensive drug with poor oral bioavailability ranging from 10-35% because of poor solubility, dissolution and most importantly, extensive first pass hepatic metabolism. The present study deals with the development and characterization of Valsartan-loaded solid lipid nanoparticles (VSLNs) to enhance the solubility, bypass the first pass hepatic metabolism, and enhance the lymphatic absorption leading to improved bioavailability. VSLNs were developed using glyceryl behenate (Compritol 888 ATO®) as the lipid and Poloxamer 407 (Pluronic F 127) as the surfactant by the solvent injection method. VSLNs were characterized for mean particle Size (MPS), zeta potential, percentage drug entrapment (PDE), DSC Scans, XRD and TEM analysis. In vitro drug release studies were performed in 0.067 M phosphate buffer of pH 6.8 using dialysis diffusion bag method. Ex vivo drug release studies were also performed for both VSLNs and valsartan suspension in stomach and intestine. The optimized formulation of having the 80 mg lipid, 10 mg drug and 250 mg surfactant was found to have particle size distribution of 142.5 ± 1.859 nm, zeta potential of – 14.3 ± 0.384 mV, and 84.59 ± 0.328% drug entrapment. Based on these results, it is concluded that SLNs show promise for improving the oral bioavailability of valsartan.
Essentials of Pharmaceutical Product Development for Magnetically Modulated Drug Delivery Systems
Authors: K R Vinod , D Sridhar , S Sandhya , D Banji , T Rohit Reddy
Published: August 2020

There is a renewed focus on developing formulation strategies for the regional drug targeting. Magnetic drug targeting provides an innovative approach that may include two and three dimensional arrays of magnetic drug delivery systems. Applications of magnetic microsphere-based drug delivery include chemotherapy, arthritis, gene, and cell transplantation therapy. This article describes different formulation approaches, routes of administration, and mechanisms of magnetic-based drug targeting. Magnetic materials have to be synthesized before considering the formulation development. Although the preparation evaluation of magnetic drug delivery is comparable with conventional microspheres and nanoparticles, characterization of magnetic properties of the final formulation is very essential for success of this approach.  In vivo evaluation studies include tumor targeting in animals, histological evaluation using MRI and course of the magnetic drug delivery system by image mapping using suitable biological markers.
Antimicrobial Efficacy of Terminalia chebula Fruit Extract Treated Cotton Fabric for Healthcare Applications
Authors: R Rathinamoorthy , S Udayakumar , G Thilagavathi
Published: August 2020

The study was focused on treatment of water and methanol extracts of Terminalia chebula fruits and citric acid as a cross linking agent on cotton plain-woven fabric. The active antimicrobial compounds in extracts were analyzed by high performance liquid chromatography.  The fabric samples were tested for antibacterial activity against bacterial strains like Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, and Salmonella typhi under agar diffusion test and quantitative analysis.  The results indicated that the treated cotton fabric shows a clear microbial resistance with 27-38 mm zone of inhibition in the agar diffusion test against all the above mentioned strains. The treated samples showed 99% of reduction against Staphylococcus aureus and 86.25% reduction against Escherichia coli as per quantitative analysis. The Fourier Transform –Infra Red analysis confirmed the presence of active substances (saponin, ascorbic acid and gallic acid) in the treated samples. Process parameters were optimized using the response surface methodology adopted using Box-Behnken design and the correlation coefficient was found to be 0.932 in the case of Staphylococcus aureus and 0.66 in the case of Escherichia coli.
Spectrophotometric Determination of Alendronate Sodium by using Sodium-1,2-Naphthoquinone-4-Sulphonate
Authors: Panda Sagar Suman , B V V Ravi Kumar , Patanaik D
Published: August 2020

A simple, precise and accurate spectrophotometric method was developed for analysis of the osteoporesis drug alendronate sodium (ALS). The method is based on reaction of the drug with sodium-1,2-naphthoquinone-4-sulphonate (NQS) in presence of alkali to form a brown colored complex giving absorption maximum at 525 nm. The drug obeyed Beer’s law in the range of 5-70 µg/ml with a correlation coefficient of 0.999. The LOD and LOQ values are 1.7 µg/ml and 5.0 µg/ml, respectively. The average recoveries for recovery study were found to be in the range of 99.37%-100.46%. The R.S.D. values for intraday and inter-day precision were found to be 0.48 and 0.62, respectively. The optimized assay conditions were applied successfully for determination of ALS in pharmaceutical dosage forms. No interference was observed from the excipients present in the dosage form. The method is statistically validated as per the ICH requirements.
Formulation Development of Aceclofenac Loaded Nanosupension by Three Square (32) Factorial Design
Authors: Patak Atul A , P Jorwekar, , Chaudhari P D
Published: August 2020

In the present study, aceclofenac loaded polymeric nanosuspension were formulated and evaluated.  Aceclofenac is a potent analgesic under BCS Class II. Due to the need for its frequent dosing, aceclofenac is an ideal candidate for sustained or controlled drug delivery. For optimization of prepared formulation, the three square (32) factorial design was used.  Tween 80 (X1) and combination of Eudragit RL 100 and RS 100 (X2) were used as independent variables and particle size (Y1), entrapment efficiency (Y2), and Percent drug release (Y3) were taken as dependent variables. The formulations were evaluated for particle size, zeta potential and drug entrapment. The in vitro drug release profile supports nanosuspension form to be used as a sustained release vehicle for aceclofenac. The formulation was characterized by differential scanning calorimetric analysis, in vivo studies and stability testing.
Integrating Nanotechnology into the Life Sciences: Lessons Learned
Authors: Bunker Kristin L , Wolfe Julianne , Wu Linxian
Published: August 2020

As nanomaterials are more frequently incorporated into the life science industry, the need to thoroughly understand their functionality becomes paramount. This review article will provide insight and lessons learned from numerous nanomaterial characterization projects where sample properties were evaluated to better understand various attributes that contribute to functionality.  The lessons address a broad spectrum of topics ranging from sample preparation to the rapidly evolving regulatory landscape.  Many of the hurdles encountered in maturing a product involving nanotechnology stem from navigating this regulatory landscape.  There is a lack of standardization within the nanotechnology community including government agencies, industry, and academia.  As a result, there are a number of important issues to address, most notably the issue of nanotechnology safety.  There are other areas that also emerge as significant challenges in nanotechnology integration: appropriate quality control measures, sample preparation and analysis selection and using nanomaterial characterization in improving products and processes throughout the product lifecycle. Specific examples are used to illustrate these challenges and provide insight to their corresponding solutions. Through these shared experiences, a broader picture emerges of what is entailed in resolving the analytical challenges of nanotechnology and life science integration, the likes of which can be translated to numerous other situations both current and prospective.
A Comparative Study of Triple-Layered Aceclofenac Matrix Tablets Formulated using Xanthan Gum and Guar Gum
Authors: Semalty Mona , Bisht T , Semalty A
Published: August 2020

The aim of the present study was to develop sustained release, multilayered-matrix tablet of aceclofenac using natural polymers-guar gum (GG) and xanthan gum (XG) as carrier for core matrix and hydroxyl propylmethyl cellulose (HPMC K-15M), sodium carboxymethylcellulose (NaCMC) and ethyl cellulose (EC) and polyvinylpyrrolidone (PVP-K30) for preparing bottom and top layers. The formulated tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, swelling index and in vitro drug release. The physicochemical properties of tablets were found within the limits. The physiochemical investigation showed that aceclofenac matrix tablet prepared with xanthan gum showed better dissolution profile as compared to that of guar gum. Matrix tablets of xanthan gum with 6% W/V xanthan gum (MTX1) showed the highest percent drug release (88.98%), while matrix tablets of guar gum with 6% W/V guar gum (MTG1) showed the highest percent drug release (73.89%) at the end of 8 hours in pH 6.8 phosphate buffer. Among the matrix tablet of xanthan gum MTX4 (with 24% W/V of xanthan) showed the lowest percent drug release (49.6%) and while among the guar gum tablets MTG4  (with 24% W/V of guar gum) showed the lowest percent drug release (48.65%) at the end of 8 hours. It was concluded that increasing the concentration of gum from 6% W/V to 24% W/V in the formulation decreased the amount of drug release from the tablet. The xanthan gum based matrix tablets of aceclofenac were found to be superior to that of guar gum matrix tablets for potential therapeutic uses.
Preparation of BSA Nanoparticles by Desolvation Technique Using Acetone as Desolvating Agent
Authors: A Krishna Sailaja , P Amareshwar
Published: August 2020

In order to see the functionality and toxicity of nanoparticles in various food and drug applications, it is important to establish procedures to prepare nanoparticles of a controlled size. Desolvation is a thermodynamically driven self-assembly process for polymeric materials. In this study, we prepared BSA nanoparticles using the desolvation technique using acetone as desolvating agent. Acetone was added intermittently into 1% BSA solution at different pH under stirring at 700 rpm. Amount of acetone added, intermittent timeline of acetone addition, and pH of solution were considered as process parameters to be optimized. The effect of the process parameters on size of the nanoparticles was studied. The results indicated that the size control of BSA nanoparticles was achieved by adding acetone intermittently. The standard deviation of average size of BSA nanoparticles at each preparation condition was minimized by adding acetone intermittently. The intermittent addition in polymeric aqueous solution can be useful for size control for food or drug applications.
Development of Innovative Orally Fast Disintegrating Film Dosage Forms: A Review
Authors: Panda Bibhu Prasad , Dey N.S , Rao M.E.B.
Published: August 2020

Over the past few decades, there has been an increased interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. The discovery and development of new chemical entities is not only an expensive but also time consuming affair. Hence the pharmaceutical industries are focusing on the design and development of innovative drug delivery systems for existing drugs. One such delivery system is the fast disintegrating oral film, which has gained popularity among pediatric and geriatric patients. This fast disintegrating film with many potential benefits of a fast disintegrating tablet but devoid of friability and risk of choking is more acceptable to pediatric and geriatric patients. Formulation of fast disintegrating film can be achieved by various techniques, but common methods of preparation include spraying and casting. These film forming techniques use hydrophilic film former in combination with suitable excipients, which allow the film to disintegrate or dissolve quickly in the mouth within a few seconds without the administration of water. In view of the advantages of the fast disintegrating films over the fast disintegrating tablets and other dosage forms, it has the potential for commercial exploitation. The oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and innovative orally fast- disintegrating films and their future scenarios on a global market as a pharmaceutical dosage form.
Development of Promethazine Hydrochloride Mucoadhesive Patches for Buccal Delivery: In vitro, Ex vivo and In vivo Characterization
Authors: Rao Y. Madhusudan , K S C Chopparapu , Reddy P. Chinna , Doodipala Narender
Published: August 2020

Promethazine hydrochloride (PMZ HCl), an antiemetic, undergoes extensive first-pass metabolism (bioavailability 25%). The purpose of the present investigation was to develop mucoadhesive patches for transbuccal delivery of PMZ HCl using solvent casting technique with Hydroxy ethyl cellulose (Natrosol 250 E) and hydroxylpropyl methyl cellulose as mucoadhesive polymers and propylene glycol as the plasticizer and evaluate their physicochemical characteristics, in vitro drug release, moisture absorption, surface pH, mechanical properties, in vitro bioadhesion, in vivo residence time, and ex vivo drug permeation through porcine buccal membranes from optimized buccal patch and stability studies. The physicochemical interaction between PMZ HCl and polymers was investigated by Fourier Transform Infrared Spectroscopy. Ex vivo drug permeation through porcine buccal membrane was performed and 83.7% of the drug permeated in 6 hours with flux 0.19 mg h–1cm–2. The optimized formulation AA4 showed maximum drug release (98%) in 6 hours in the Higuchi model release profile. Moisture absorption, surface pH, tensile strength, elongation at break, peak detachment force and work of adhesion values of the optimized formulation were found to be 68.1%, pH 6.7, 12.3 kg/mm2, 69.2 % mm2, 7.5 N and 2.73 mJ respectively. Formulation AA4 showed 77.6% of the drug permeated through porcine buccal membrane in 6 hours and flux calculated to be 0.45 mg h–1cm–2. FTIR studies showed no evidence of interaction between the drug and polymers. In vivo mucoadhesive behaviour of the optimized formulation was studied in healthy human volunteers and subjective parameters were evaluated. The stability of the optimized formulation was studied and no significant changes were detected in drug content, in vitro release and ex vivo permeation after 6 months.
Formulation and Evaluation of Gliclazide Tablets Containing PVP-K30 and Hydroxypropyl-β-cyclodextrin Solid Dispersion
Authors: Varma Mohan M , P Satish Kumar
Published: August 2020

Gliclazide is an anti-diabetic drug. It is a BCS class-II (poorly water soluble) drug and its bioavailability is dissolution rate limited. The dissolution rate of the drug was enhanced by using the solid dispersion technique. Solid dispersions were prepared using PVP-K30 (polyvinylpyrrolidone) and hydroxypropyl-β-cyclodextrin (HP BCD) as the hydrophilic carriers. The solid dispersions were characterized by using DSC (Differential scanning calorimetry), XRD (X-ray diffractometry) and FTIR (Fourier transform infrared spectroscopy). Solid dispersions were formulated into tablets. The formulated tablets were evaluated for the quality control parameters and dissolution rates. The solid-dispersion tablets enhanced the dissolution rate of the poorly soluble drug. The optimized formulation showed a 3 fold faster drug release compared to the branded tablet. The XRD studies demonstrated the remarkable reduction in the crystallinity of the drug in the solid dispersion. The faster dissolution rate of the drug from the solid dispersion is attributed to the marked reduction in the crystallinity of the drug. The DSC and FTIR studies demonstrated the absence of the drug-polymer interaction.
Moxifloxacin Loaded Polymeric Nanoparticles for Sustained Ocular Drug Delivery
Authors: Gadad A P , P Sharath Chandra , P M Dandagi , Mastiholimath V S
Published: August 2020

Efficient drug delivery to the ocular region is a challenging goal. Only a very small amount (about l-3%) of the dosage actually penetrates through the cornea and reaches intraocular tissues. To overcome these problems of conventional dosage forms, novel drug delivery systems like nanoparticles were designed. Moxifloxacin-loaded poly (lactic-co-glycolic acid) nanosuspension was prepared with the aim of providing sustained effect for ocular delivery for 24 hours. Nanosuspensions were prepared by nanoprecipitation method using poly(lactic-co-glycolic acid) and evaluated for particle size, surface morphology, zeta potential, drug entrapment efficiency, in vitro release and ex vivo transcorneal permeability, and were compared with marketed products. Microbiological efficacy was tested against Staphylococcus aureus and Pseudomonas aeroginosa using cup plate method. Spherical uniform particles (202.5 nm) with a polydispersity index of 0.226 and negative zeta potential (– 25.45 mV) were obtained for MF4 (drug to polymer ratio 1:0.4). Drug entrapment efficiency for MF4 was found to be 83.1%. The cumulative percent drug release for formulation MF4 after 24 hours was 86.1%, showing a sustained effect in controlling the bacterial conjunctivitis thereby avoiding frequent administration of dosage. MFX-loaded PLGA nanoparticles (MF4) showed a significantly higher drug permeation capability compared to the commercial marketed eye drops in ex vivo transcorneal permeation studies and also showed better antimicrobial efficacy compared to the marketed formulation. The results indicate that Moxifloxacin-loaded PLGA nanosuspension could be utilized as a potential drug delivery system for sustained release in ophthalmic application.
Schiff Base: An Overview of its Medicinal Chemistry Potential for New Drug Molecules
Authors: Sahu Rakesh , Thakur D S , P Kashyap
Published: August 2020

Schiff base denotes a reaction product of a primary amine and a carbonyl compound. Schiff bases possess a wide variety of biological activity specially antibacterial and antifungal properties. Metal complexes of Schiff base have been studied for their biological activities. This review articles provide a summary of medicinal chemistry features of Schiff base and various reports published on biological activities of Schiff base and its metal complexes.
Regulatory Framework and Challenges in Developing Biosimilar Monoclonal Antibodies and Related Biological Products
Authors: George Bobby
Published: August 2020

Monoclonal antibodies (mAbs) were initially used as laboratory reagents, later they were adopted as clinical diagnostic reagents, and eventually as therapeutic agents. The develop-ment of therapeutic mAbs commenced in the early 1980s and by 1986 the first mAb for human use “Orthoclone OKT3®” was approved by the US Food and Drug Administration (FDA). The next wave of antibody products were mostly anticancer agents which were approved in the US and Europe in the 1990s. The technological evolution from murine-based therapeutic mAbs to chimeric (part murine part human protein), humanized, and fully human antibodies has led to a reduction in immune-mediated clearance and hypersensitivity, improved the safety and feasibility of repeated administration making them therapeuti-cally viable.Since the commercialization of the first therapeutic mAb, these products have become a dominant component of the biopharmaceutical marketgenerating revenues of several billion dollars.The area of biosimilar antibody development is positioned for substantial growth with regulatory agencies like the European Medicines Agency (EMA) coming up with new guidelines on similar biological medicinal products followed by Health Canada, the US FDA and others, addressing biosimilar product development. With few of the blockbuster mAbs going off-patent in the next decade, companies with expertise in manufacturing biosimilar mAbs with the right kind of business and regulatory strategy are likely to have good value proposition.
Current Approaches and Pharmaceutical Applications of Colloidosome Drug Delivery Systems
Authors: Kumar S. Pradeep , D Prathibha
Published: August 2020

Recently a number of lipid based systems like lipospheres, liposomes, niosomes, ethosomes, and transferosomes have been developed. The purpose of this review article on colloidosome drug delivery was to compile the focus on the types, properties, fabrication techniques, characterization and stability of colloidosomes. This system also solves the problem of insolubility, instability, rapid degradation and is widely used in specialized areas like protein delivery, gene delivery, targeting to the brain and tumor targeting. In a series of vascular systems, colloidosome represents an advanced tool in drug delivery. Colloidosomes are an emerging vesicular system in drug delivery. Vesicular drug delivery reduces the cost of therapy by improved bioavailability of medication, especially in the case of poorly soluble drugs. Colloidosomes have a great encapsulation efficacy with a wide control over size, permeability, mechanical strength and compatibility.
Formulation and Evaluation of Proniosome Based Drug Delivery System of the Antifungal Drug Clotrimazole
Authors: S Pankaj , T Rini , Dandagi P M
Published: August 2020

In the present study proniosomal gel of clotrimazole was formulated by using lecithin, cholesterol as encapsulating agents, nonionic surfactants Span and Tween with different grades. Evaluation of proniosomal gels for pH, vesicle size analysis, encapsulation efficiency, drug diffusion profiles, ex-vivo skin permeation and ex-vivo drug deposition studies on guinea pig skin, irritation test on rabbit and stability studies was performed. The preliminary compatibility studies revealed that there were no interactions between clotrimazole and excipients which was evident from FTIR and DSC studies. The physical characteristics of proniosomal gels were found to be within the acceptable limits. The vesicle size was found to be in the range 5.25-15.23μm. The proniosomes were spherical and homogenous in structure when observed under optical microscopy. The ex-vivo skin permeation and ex-vivo drug deposition studies showed the drug release from formulations F3, F4 and marketed formulation was 48.60%, 36.9% and 27.48 % respectively and the percent of clotrimazole deposited in skin after 24 h was found to be 35.7%, 43.6% and 15.17% for formulation F3, F4 and marketed formulation respectively. The release from the proniosomal gel was prolonged when compared to conventional formulation and showed a two fold increase in the drug deposition in the skin compared to conventional cream. No obvious erythema, edema or inflammation was observed on rabbits’ skin after one week of application of the selected formulation. Results of antifungal studies revealed that the developed proniosomal gel is more efficient when compared with the marketed formulation. The stability studies showed that proniosomal gels were stable at 5±3°C and 25±2°C. The above results indicated that the proniosomal gels of clotrimazole could be formulated for sustained release.
Formulation and Evaluation of Levetiracetam Extended Release Tablets
Authors: Singh Sudarshan , Bhavesh Shankar , Nayak Sanjaykumar , Bothara Sunil
Published: August 2020

Extended release formulation of levetiracetam is approved by the food and drug administration as an add-on to other antiepileptic drugs for adults with partial onset seizures. The main objective of present study was to developed and evaluate matrix tablet of levetiracetam by using various grade of hydroxypropylmethylcellulose (HPMC) polymer. Various trials were taken by using HPMC K4M, K15M, and K100M.  Different parameters like Physical properties, FTIR, DSC, in vitro drug release profile and swelling index were determined. In vitro drug release was performed in phosphate buffer pH 6.8. The in vitro release profile was compared with model independent method. Stability studies were performed as per ICH guidelines for 1 month at (40 °C ± 2 °C/75 % ± 5 % RH).Data analysis was performed for determination of drug mechanism and order of drug release. The in vitro drug release profile of optimized formulation was compared with marketed formulation LEVERAXR. The regression value for zero order, first order, Higuchi and Korsmeyer Peppas was found to be 0.9604, 0.9245, 0.9889 and 0.9729, respectively. Similarity factor (f2) and dissimilarity factor (f1) was found to be 88.61 and 1.82, respectively. The FTIR and DSC study shows that there is no chemical interaction between levetiracetam and excipients. From the data analysis, it was concluded that optimized formulation follow Higuchi model having diffusion mechanism. The order of drug release was considered zero  order release. Stability study shows that there was no remarkable change in drug release after 1 month. It is concluded that the formulation is stable at accelerated conditions.