bluuebunny/crossref_metadata_2025 huggingface dataset:
Development and Evaluation of Enteric Coated Tablet Containing Diclofenac Sodium
Authors: Singh Chhater , Kumar Rajesh , Agarwal Kshitij , R.K. Nema
Published: August 2020

The influence of various polymers on the release rate of Diclofenac Sodium from enteric coated tablets was investigated in an attempt to formulate a delayed release solid dosage forms. Prepared the conventional diclofenac sodium tablets by wet granulation method (non-aqueous) using granulating fluid (isopropyl alcohol). Developed the aqueous coating formula using shacryl and non-aqueous coating formula using HPMCP and optimized the best aqueous coating formula. Coating was performed in a mini coating pan at 107 rpm using low-pressure air atomized liquid spray techniques. Comparative dissolution, disintegration and antiulcer studies were performed on the best products and marketed products. The Comparative antiulcer studies were performed on wister albino rats using conventional, dummy and enteric-coated tablets.
Formulation and In vitro Evaluation of Floating Microspheres of Misoprostol
Authors: Vanitha K , Varma M. Mohan , Alluri Ramesh
Published: August 2020

Misoprostol is a synthetic prostaglandin PGE1 analogue, which has proved to be an effective anti-secretory agent for oral use. The major indications of Misoprostol are in the prevention and treatment of NSAID-induced gastric and duodenal ulcers. Its half-life is 20-40 minutes. More than one third of patients with ulcers are resistant to H2 antagonists. So, these patients can be healed on Misoprostol. The objective of the present study was to formulate gastroretentive floating drug delivery system of an antiulcer drug Misoprostol. Floating microspheres of Misoprostol were prepared by an emulsification solvent evaporation technique using hydroxy propyl methyl-cellulose (HPMC K 100M) and ethyl cellulose. The percentage yield and drug entrapment efficiencies of these floating microspheres were within the range between: 70 ± 2.8 to 98 ± 2.9 % and 39.27 to 82.39 %, respectively. The determined mean particle size for all the microspheres were 250 ± 7.28 to 400 ± 2.32 µm. The flowability of these microspheres was found good. A high performance liquid chromatography (HPLC) method with ultra-violet (UV) detection was selected for the method of analysis.  The drug release was found to delay for 12 hours with the increasing drug to polymer ratio. The drug release kinetics followed Korsemeyer-Peppas and Higuchi model with anomalous (non-Fickian) diffusion mechanism for the drug release. The FTIR and DSC studies showed that there was an absence of chemical interaction between the drug and the excipients. The in vitro drug release from Misoprostol floating microspheres showed the drug release was dependent on the drug to polymer ratio. The drug release was found delayed with the increasing drug to polymer ratio.
Nanosuspensions: Recent Patents and Pharmaceutical Aspects as Drug Delivery Systems
Authors: Gharge Vikram S , Shinde Mukesh B , Pustake Bipin D , Kinage Krishna B , Kulkarni Anup A
Published: August 2020

Solubility is an essential factor for drug effectiveness, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Nanosuspension technology can be used to improve the stability as well as the bioavailability of poorly soluble drugs. Nanosuspensions are biphasic systems consisting of pure drug particles dispersed in an aqueous vehicle, stabilized by surfactants. These are simple to prepare and are more advantageous than other approaches. Techniques such as wet milling, high-pressure homogenization, emulsification–solvent evaporation and super critical fluid have been used in the preparation of nanosuspensions. It has the advantage of delivery by various routes, including oral, parenteral, pulmonary and ocular routes. The present article reviews the current methods used to prepare nanosuspensions and their application in drug delivery. More than 100 patents have been published on nanosuspensions in the recent days. This patent reviews covers different methods of pharmaceutical preparation and applications in drug delivery as well as the recent marketed published or granted patent surveys. This patent review is useful in enhanceing the knowledge of pharmaceutical application in drug delivery.
Fabrication of Triamcinolone Acetonide Cream and Ointment: Optimization, Evaluation and Pharmacodynamic Assessment
Authors: Chaurasia Sundeep , Mettu Mounika , Dommeti Srinivas , Hugar Jitendra C , Vure Prasad
Published: August 2020

The present investigation highlights, optimization and evaluation of topical Triamcinolone Acetonide (TA) cream and ointment along with their sensory test on healthy human volunteers. TA cream and ointment were prepared by fusion followed by high speed homogenization technique. The prepared creams and ointments were subjected to evaluated for physical parameters like pH, Fourier transform infrared spectroscopy, viscosity, assay, drug content, in vitro diffusion studies and accelerated stability study. Further, sensory test was performed with 30 healthy human volunteers. On the basis of physicochemical characterizations, we found that batch FC6 was the optimized batch for TA cream and batch F3 was the optimized batch for TA ointment formulations. Results of both the optimized formulations showed favorable viscosity as compared to reference listed drug (Fougera). In vitro diffusion study demonstrated increased drug release with optimized batch of both cream and ointment. The optimized TA cream and ointment showed good stability when stored at accelerated conditions for three months. Finally, sensory test results indicated ‘good feel’ when both optimized formulations applied on the human skin. In conclusion, TA cream and ointment offers great potential for topical drug delivery system in the treatment of anti-inflammatory disease which reduces the inflammation of skin.
In vitro and In vivo Evaluation of Propranolol Microspheres Loaded Buccal Gel
Authors: Deshmukh Gajanan J , Varma M. Mohan , D. V. R. N. Bhikshapathi
Published: August 2020

The selected propranolol microsphere formulation, S6 was employed for gel formulation with a variety of polymers like Carbopol 934, HPMC and Sodium CMC by mechanical stirring method in order to develop a sustained release propranolol microspheres containing bioadhesive gel. The prepared bioadhesive gels were evaluated for pH, viscosity, %drug content, in vitro drug release studies, bioadhesion, ex vivo permeation studies, accelerated stability and in vivo bioavailability studies. From all the above studies FG3 was found to be optimized formulation. In vitro experiments indicated a sustained release of 98.92% over 12 h and an acceptable bioadhesion quality for formulation FG3. Optimized formulation was characterized for FTIR, SEM and stability studies and found to be stable. Propranolol Optimized formulation exhibited significant increased bioavailability in vivo when compared with marketed tablet. The drug release from the optimized formulation follows zero order kinetics with anomalous Non-fickian diffusion. In vivo studies revealed that Propranolol Optimized formulation FG3 exhibited significant increased bioavailability when compared with marketed product, due to reduced first pass metabolism, when it is administered by the buccal route. Hence, it can be concluded that the formulation FG3 has potential to deliver Propranolol in a controlled and constant manner for prolong period over other formulations and can be adopted for a successful delivery of propranolol for buccal use.
Evaluation of Antiurolithiatic Activity of Lawsonia inermis Linn. in Rats
Authors: Patel Kruti M , K Shah Samir
Published: August 2020

This study was conducted to evaluate the potential antiurolithiatic effects of Lawsonia Inermis Linn. in rat models. Animals were divided into seven groups and urolithiasis was induced by ethylene glycol (0.75% v/v) in drinking water to all groups (Groups II-VII) except normal control (Group I) for 28 days. Methanolic extracts of Lawsonia inermis (MELI) bark (300 & 500 mg/kg, p.o.) were administered once daily, from 15th day to 28th day as curative regimen and from 1st day to 28th day as preventive regimen. Cystone (750 mg/kg, p.o.) was used as a standard drug for comparison. After 28 days, various biochemical parameters like urine volume, pH were measured. Calcium, phosphate and oxalate were measured in urine and kidney homogenate. Serum creatinine, uric acid and urea nitrogen were estimated. Histopathology of kidney was investigated. Treatment with the MELI extract significantly (p<0.05) restored all elevated parameters including calcium, phosphate and oxalate in urine and kidney homogenate; creatinine, uric acid and urea nitrogen in serum when compared to model control group. The histopathological study of the kidney also supported the above results. It was concluded that methanolic extract of bark of Lawsonia inermis Linn. has significant antiurolithiatic effect in experimental rats.
Functionalized Nano-graphene Oxide as Multi-modal Clinic for Effective Drug Delivery
Authors: Satapathi Soumitra , Mishra Rutusmita , Chatterjee Manisha , Roy Partha , Mohapatra Somesh
Published: August 2020

Nano-materials based drug delivery modalities to specific organs and tissues has become one of the critical endeavors in pharmaceutical research. Recently, two-dimensional graphene has elicited considerable research interest because of its potential application in drug delivery systems. Here we report, the drug delivery applications of PEGylated nano-graphene oxide (nGO-PEG), complexed with a multiphoton active and anti-cancerous diarylheptanoid drug curcumin. Specifically, graphene-derivatives were used as nanovectors for the delivery of the hydrophobic anticancer drug curcumin due to its high surface area and easy surface functionalization. nGO was synthesized by modified Hummer’s method and confirmed by XRD analysis. The formation of nGO, nGO-PEG and nGO-PEG-Curcumin complex were monitored through UV-vis, IR spectroscopy. MTT assay and AO/EB staining found that nGO-PEG-Curcumin complex afforded highly potent cancer cell killing in vitro with a human breast cancer cell line MCF7.
A Cohort Retrospective Study on the Necessity of a Faculty Development Program for Pharmacy Colleges in Khammam
Authors: Mathukumalli Sai Laxmi
Published: August 2020

The important asset of any educational institution, more so of those imparting professional knowledge and skill is its faculty members (Bligh, 2005). Pharmacy is one such professional course witnessing constant research and developments. Therefore, updating of knowledge is of paramount importance for faculty members to keep in pace with these fast developments (Cline 2003). The most effective way of training the faculty is by what is called as faculty development program (FDP). A cohort retrospective study with 2000 students and 88 faculty members from 9 colleges were evaluated on various aspects with the help of a score scale of 0-3. Pearsons coefficient of correlation (R) was applied to the data. Results indicate a significant correlation exists and between student score vs. institutional score for FDP(R=0.8237) and faculty performances vs. institutional score for FDP (R=0.9385) indicating that students and faculty from institutions having an FDP committee and conducting regular FDPs performed well, were more confident and competing well in their carriers. The need for FDP has already been felt in developed countries and necessary steps were taken to establish institutional FDP committees improve educational skills. Studies are very limited for the Indian scenario except an occasional paper (S. S. Agarwal, 2010). Therefore, the present study greatly substantiates other studies concluding that FDPs greatly enhanced teaching performance by instructors and improved learning outcomes for students, high satisfaction and change in the attitude of faculty towards teaching and development of educational skills and their efficient tackling of student diversity with varying cultural and academic background. This study concludes and recommends that educational bodies controlling pharmacy education in India should make FDP committee mandatory in every pharmacy college for better development of the profession.
Formulation Development of Diclofenac Sodium Emulgel Using Aloe vera Gel for Transdermal Drug Delivery System
Authors: H.R. Thanushree , G B Kiran Kumar , Acharya Ankit
Published: August 2020

Diclofenac sodium has many side effects like nausea, vomiting, GIT disorders. These side effects can be reduced by converting into emulgel formulations. The emulgel formulation of Diclofenac Sodium was prepared by incorporation method, using span 20 and tween 20 as non-ionic surfactants, clove oil and cinnamon oil as penetration enhancers, Aloe vera as a gel base and sesame oil as a solvent. The prepared emulgel formulations were evaluated for compatibility study, physical examination, viscosity, spreadability, in vitro diffusion studies, various release kinetic studies and stability studies. In vitro diffusion studies were carried out using cellophane membrane, results showed that emulgel formulations (F2-F7) showed higher cumulative percent drug release (49-65%) compared to normal gel (48%) and marketed gel (35%). Results of in vitro diffusion studies showed that formulation F3 and F6 exhibited 64% and 65% drug release respectively over a period of 6 hrs. In conclusion, a physiochemical stable diclofenac emulgel was formulated, which could deliver significant amount of drug across the skin in steady-state manner for the prolong period of time in the treatment of osteoarthritis.
Clinical Pharmacology of Modern Antiepileptic Drugs
Authors: Reddy D Samba
Published: August 2020

This article describes current antiepileptic drugs (AEDs) that are available for treatment of epilepsy. Epilepsy is characterized by repeated occurrence of seizures.  Epileptic seizures are classified into focal and generalized types. Around two-dozen AEDs are available for treating epilepsy. AEDs act on diverse molecular targets to selectively modify the abnormal excitability of neurons by reducing the focal seizure discharges or preventing spread of excitation. AEDs suppress seizures by blocking the voltage-gated sodium channels (phenytoin, carbama-zepine, valproate, lamotrigine, oxcarbazepine, topiramate), voltage-activated calcium channels (ethosuximide, gabapentin), potentiation of GABA inhibition (barbiturates, benzodiazepines, tiagabine), and reduction of glutamate excitation (felbamate, parampanel). Carbamazepine, phenytoin, and valproate are the first-line agents for partial seizures and generalized tonic-clonic seizures. Ethosuximide is the drug of choice for absence seizures. AEDs are orally-active and show unique pharmacokinetic features. Some AEDs cause enzyme induction and hence produce drug-drug interactions. Newer AEDs such as gabapentin, levetiracetam, tiagabine, and pregabalin do not cause enzyme induction. Despite many advances in epilepsy research, nearly 30% of people with epilepsy have drug-resistant or intractable seizures. Presently, there is no cure for epilepsy. Thus, newer and better AEDs that can better prevent refractory seizures and modify the disease are needed for curing epilepsy.
Green Synthesis and Characterization of Silver Nanoparticles using Glycine Max L. Seed Extract and their Antiepileptic Activity in Rats
Authors: Md Imad Uddin , D Kalyani , N Tejasri , A Mounika , A Sowndarya , J Anitha , Md Ashwaq Hussain
Published: August 2020

Glycine max is an edible oil seed and commonly known as Soybean. In this study, we report green, inexpensive method for synthesis of silver nanoparticles (SNPs) using of Glycine max seeds aqueous extract. Synthesized SNPs were characterized by UV-Visible spectroscopy (UV), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD) and Zeta Potential. Formation of Silver Nanoparticles from Glycine max Aqueous Extract (SNGMAE), indicated by appearance of dark brown color. UV depicted peak at 440nm, FTIR showed various functional groups present in plant extract capping in Silver Nanoparticles. Nanoparticle range of SNGMAE was identified by SEM and XRD, while stability was confirmed by Zeta Potential. Different constituents of aqueous extract viz., proteins, phytosterols, phospholipids, oils and carbohydrates are involved in the formation of SNPs. Synthesized SNGMAE was reconnoitered for antiepileptic activity in pentylenetetrazol (PTZ) and maximal electroshock induced epileptic (MESE) models, phenytoin (25mg/kg) was used as standard anti-epileptic drug. In negative control group of PTZ, all five stages of convulsions were observed, which were significantly reduced with phenytoin and with SNGMAE at 80 and 160mg/kg. MESE was characterized by appearance of flexion, extensor and clonus. In negative control group, these stages appeared for longer duration; these were decreased significantly in the treatment groups. In conclusion, these results show that SNGMAE may be a potent source of nanomedicine for the treatment of epilepsy.
Quercetin Loaded Nanostructured Lipid Carriers-based Gel for Rheumatoid Arthritis: Formulation, Characterization and in vivo Evaluation
Authors: Gokhale Jayanti P , Surana Sanjay S
Published: August 2020

Present research work describes the development of potential topical treatment containing nanostructured lipid carriers (NLCs) for rheumatoid arthritis (RA). Quercetin (QCT) is a renowned flavonol useful as model drug for carriers. QCT loaded NLCs were prepared and evaluated for particle size distribution, polydispersity index, zeta potential analysis, in vitro drug release study. Ex vivo study was carried out to evaluate the effect of NLCs on cell proliferation (HIG-82 cell line) and inflammation (TNF-α induction in RAW264.7 cells). The QCT-NLCs showed mean particle size of 155.6 ± 1.8 nm and polydispersity index (PDI) was 0.236 ± 0.4, entrapment efficiency of 95.63 ± 0.14 % and zeta potential of -27 ± 1.2 mV. For the ease of application, NLCs were incorporated into the gel base and final formulation was evaluated for rheological study, texture profile, drug release and antiarthritic activity. QCT-NLC gel showed pseudo plastic flow behavior with excellent texture profile parameters. In vitro drug release studies showed that, QCT-NLC gel has more prominent permeation profile as compared with QCT-loaded gel. In vivo activity was carried out using Complete Freund's adjuvant (CFA) induced arthritic model. Evaluation of the severity of rheumatoid arthritis was done by measurements of hind paw volume, arthritis score and haematological parameters such as rheumatoid factor (RF), C-reactive protein (CRP), red blood cells (RBCs), white blood cells (WBCs), erythrocyte sedimentation rate (ESR) and hemoglobin (Hb). Edema and erythema were not observed after administration of QCT-NLC- gel on the rat skin. In conclusion, the results of in vitro and ex vivo studies, QCT-NLC gel appears a viable formulation system for topical delivery of QCT in the treatment of RA.
Is Prenatal Valproate Exposure a Risk Factor for Autism
Authors: Reddy Doodipala Samba , Brewer Jonathan , Manchi Maunica
Published: August 2020

Sodium valproate (Depakene) and divalproex sodium (Depakote) are two commonly used drugs for epilepsy therapy. Sodium valproate, a first-generation antiepileptic drug, has commonly been used as a treatment for different forms of both epilepsy and psychiatric disorders ever since it was first clinically utilized in 1967. It is a simple 2-chain fatty acid that is believed to affect GABA metabolism, however, the mechanism is still unclear. It has been proven to have adverse side effects, such as neural tube defects if taken in utero during the first trimester of pregnancy and has therefore caused a reservation in the medical community for prescription of this drug in females. However, it is still one of the most commonly prescribed agents in young women of childbearing age with 23.4% of women actively receiving it for non-epileptic disorders, such as psychiatric disorders and 12% of women receiving it as an antiepileptic drug (AED). This may be cause for alarm due to the teratogenic effects that may result from usage of valproate. In this article, the potential of prenatal valproate to cause autism spectrum disorder will be outlined from a nonclinical and clinical perspective, as evident from this basic science report. Overall, valproate is clearly associated with teratogenic risks and hence should not be used in women with epilepsy during reproductive years.
Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach
Authors: Goudanavar Prakash , Acharya Ankit , C.H Vinay
Published: August 2020

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used.
Dissolution Behaviour of the Poorly Water-Soluble Drug Mefenamic Acid from Polymeric Micelles
Authors: Koshy Tibey Mary , Kulkarni Parthasarathi K
Published: August 2020

The aim of the work was to study the dissolution behaviour of the poorlywater-soluble drug mefenamic acid (MA), a NSAID, from polymeric micelles (PMs) of Pluronic F127 and DexbLG micelles.DexbLG Copolymer was synthesised by cross-linking reaction using Dextran and PLGA. Drug excipient compatibility study was carried out by Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). Pluronic F 127 and DexbLG Polymeric micelles formulation were prepared by co-solvent evaporation technique. Formulations were evaluated for particle size, Zeta potential, solubility studies, drug loading and encapsulation efficiency. Scanning electron microscopy (SEM) analysis was performed to study the size and surface morphology of the PMs. SEM image showed smooth surfaced spherical micelles. The drug loading efficiency was more inpluronic F 127 micelles. Polymeric micelles showed negative Zeta potential value indicating that they are stable and resist aggregation. Solubility of MA has increased to 6 - 13 folds from PMs of pluronic F127 and 4-11folds from DexbLG micelles. Particle size was less than 100 nm and polydispersity index was less than 0.5 indicating uniform size distribution. Percentage cumulative drug release from the Pluronic micelles was higher than DexbLG micelles. It can be concluded that MA PMs formulation has significantly increased the solubility and thereby increases the dissolution of the drug.These results suggest that polymeric micelles can be used to increase the solubility of poorly water-soluble drugs.
High-Performance Liquid Chromatographic Assay for Ziprasidone hydrochloride in Bulk and Polymeric-Microspheres based Matrix Tablet
Authors: Singh Kunwar Nagendra Krishna , Kar Mousumi
Published: August 2020

A significant percentage of psychiatric patients are treated with antipsychotic drug in the clinic. Thus, it is advantageous to use a rapid and reliable assay that is suitable for determination of antipsychotic drug in a single run. A simple and sensitive HPLC method was developed and validated for quantification of Ziprasidone hydrochloride (ZDH) and its polymeric microspheres-based matrix tablets. The chromatographic separation of ZDH was achieved on a C18 reverse-phase column (250 mm × 4.6 mm, 5µ, Enable) and a C18 guard column using acetonitrile-potassium dihydrogen phosphate buffer (pH 3.6 ± 0.1; 20.0 mM containing 0.2% v/v triethylamine) as a mobile phase in the ratio of 28:72%v/v at a flow rate of 1.0 mL/min which indicated a retention time within a short run time of 2 min. All the analytes were monitored using UV detection. The method was validated according to the International Conference on Harmonization guidelines Q2A and Q2B with respect to specificity, precision, linearity, accuracy, range, stability of analytical solution, robustness and system suitability. The LOQ was 20.0 ng/mL and correlation coefficient (R2) values for the linear range of 20.0-1000.0 ng/mL were 0.990 or greater for all the analytes. The satisfying recoveries (98.68-99.82%) and low relative standard deviation confirmed the suitability of the proposed method for the routine analysis of ZDH in bulk and its formulations.
Development and Evaluation of Ketoconazole Loaded Nano-sponges for Topical Drug Delivery
Authors: Pardeshi Harshal A. , Gambhire Makarand S , Gujar Kishore N. , Vaidhya Aniket A
Published: August 2020

Beta-cyclodextrin nanosponges (NS) based hydrogel had been studied as a topical delivery of ketoconazole (KTZ) for effective eradication of cutaneous fungal infection. The purpose of the present study was to develop KTZ loaded NS for topical drug delivery with skin targeting to minimizing the adverse side effects and providing a controlled release. The four types of NS were synthesized by varying the molar ratios of β-cyclodextrin (β-CD) to diphenylcarbonate (DPC) as a cross linker viz. 1:2, 1:4, 1:6, and 1:8. The KTZ loaded NS shows particle size 274.6-367 nm and high loading efficacy was obtained, FTIR, DSC, XRD studies confirmed the complexation of KTZ with NS. Hydrogel were evaluated comparatively with commercial product with respect to physicochemical properties, ex-vivo skin permeation and skin retention on human cadaver skin and antifungal activity. Ex-vivo study of KTZ-NS hydrogel exhibited controlled drug release up to 8 hrs whereas skin retention studies show avoidance of the systemic uptake and better accumulative uptake of the drug compared to marketed formulation. The zone of inhibition of KTZ-NS hydrogel was higher in comparison with commercial formulation against Candida albicans. These results indicate that the KTZ-NS is having controlled drug release, potential of skin targeting with enhanced antifungal activity.
Development and Optimization of Lovastatin-loaded Trans-dermal Proniosomal Gel using Box-Behnken Design
Authors: C Soujanya , P Ravi Prakash
Published: August 2020

In this study, a proniosome-based transdermal drug delivery system of lovastatin was developed by coacervation phase separation method. On the basis of the pilot trials, a 3-factor, 3-level Box–Behnken design was employed to characterize the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, entrapment efficiency, and drug release). TEM analysis of optimized formulation has demonstrated the presence of individual Proniosomes in spherical shape. Lovastatin optimized proniosomal formulation F1 shown better particle size and percentage entrapment efficiency and drug release of 99.49% within 24h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the systems predominantly released Lovastatin in a zero-order manner with a strong correlation coefficient (R2= 0.9990). The particle size and Zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged time may lead to improved efficacy and better patient compliance.
Clinical Overview of Innovative New Drug Approvals in 2017
Authors: Reddy D Samba
Published: August 2020

The FDA has approved 46 new drugs in 2017, another record approval in two decades on a similar pace to the gangbuster year of 2015. Many of these new medicines address significant and meaningful needs, or offer additional therapeutic choices for patients worldwide. These new drugs also cover a broad range of indications including immuno-oncology (Imfinzi and Bavencio), Parkinson’s disease (Xadago), eczema (Dupixent), psoriasis (Siliq and Tremfya), multiple sclerosis (Ocrevus), and different types of cancer (Idhifa, Aliqopa, Calquence, and Besponsa).  A few important orphan drugs were approved, including in mucopoly-saccharidosis type VII (Mepsevil) and Batten’s Disease (Brineuria). Many of these new drugs are for rare diseases and sub-types of cancer, which often target very small populations, although they can cost hundreds of thousands of dollars. Yet the pharma companies saw average returns on their research and development spending fall, reflecting more competitive pressures and the growing share of new products now coming from biotech companies. Recently, the US has introduced the Right-to-Try Act, wherein patients can access experimental treatments if they are unable to participate in any clinical trial of new drugs and if they have no other options. Such policies are expected to increase the database for new experimental drugs and help accelerate drug approvals.
Estimation of Glycopyrrolate by Analytical Quality by Design Supported Difference UV Spectrophotometric Method
Authors: Panda Sagar Suman , B V V Ravi Kumar , Panda Divyakalpa , V Raja Kumar
Published: August 2020

A novel difference UV spectrophotometric method was developed and validated for estimation of glycopyrrolate (GLP) in injection formulations using analytical quality by design approach. GLP shows two different absorbance maxima in 0.1M HCl and 0.1M NaOH. Principle of difference spectroscopy was utilized to avoid the variation in absorbance maximum and amplitude of analyte solutions were measured keeping analyte in 0.1M HCl in reference cell and analyte in 0.1M NaOH in sample cell. The amplitude was measured considering maxima at 219nm and minima at 233nm. Further, analytical quality by design approach proved worthy by ensuring method robustness prior to method development. Scanning speed and sampling interval were the two variables which were studied for the robustness purpose using an experimental design. The method validation studies were carried out to evaluate linearity, accuracy, precision, sensitivity etc. The method was applied successfully for estimation of GLP in bulk and present in injections.
Design, Development and Evaluation of Dexamethasone Sodium Phosphate Niosomal in-situ Gel for Visual Medication Conveyance
Authors: Patel Vipul P , Pande V. V , P. V. Khedkar
Published: August 2020

The main purpose of this study was to beat issues related with lachrymal seepage by eye drops, obscured vision with semi solid formulation, distinctive framework was joined together as niosomes and in-situ gel by fusing niosomes in-situ gel formulation, so it is anything but difficult to controlled and hold at the site for drag out timeframe. The Dexamethasone sodium phosphate, a glucocorticosteroid anti-inflammatory drug utilized as a part of treatment of eye hypersensitive condition, keratitis, after eye surgery, post cataract treatment. Niosomes containing Dexamethasone sodium phosphate definitions were prepared by solvent injection technique using cholesterol alongside different surfactants proportions. Prepared Niosomal preparations were fused in-situ gel formulation plan by scattering the Niosomes in solution of carbomer 974 P (0.2-0.6% w/v) and Hydroxypropyl-methylcellulose (HPMC) K4M (0.5-0.8% w/v). Prepared formulations were assessed for their vesicle measure, entanglement proficiency, in-vitro sedate discharge, thickness, in-vitro gelation study and so on. From the results it can be concluded that by utilizing cholesterol: Tween-80 (1:2) proportion, particle size of Niosomes was B4 was 368.7 nm with 93.15% drug entrapment efficiency. In-vitro drug release kinetics from Niosomal in-situ gel definition demonstrates that 98.42% drug release in 6 hrs with the utilization of 0.8% w/v of HPMC K4M and 0.6% w/v of Carbomer 974 P. In conclusion, the Niosomal in-situ gel is a practical contrasting option to routine eye drops due to excellence of its capacity to improve bioavailability through its more drawn out residence time and capacity to sustain the drug release.
Biosimilars Striving for US Uptake
Authors: George Bobby
Published: August 2020

Though biosimilars have to go through an abbreviated regulatory pathway for approval, it is quite challenging given the scientific and technical complexities associated with these products. As an increasing number of biologics face patent expiration, biosimilars offer an attractive opportunity. While companies would be desiring to have a footing in the developed markets like US and EU, considerable opportunities exist in developing/emerging markets. With more number of biosimilars making their commercial foray, starting to gain acceptance across formularies, the leading biologic players have started taking a hit on price, volume and market share of their blockbuster drugs. The pace of sales erosion due to biosimilars is expected to be gradual yet relentless. Since the enactment of Biologics Price Competition and Innovation (BPCI) Act, 12 biosimilars have been approved by the US Food and Drug Administration (FDA) till September 2018. However, only a small percentage have seen the light of the day in terms of commercial launches. These are primarily driven by legal challenges and hesitancy from insurers and healthcare providers. While originators have been trying all the means at their disposal to thwart competition by posing challenges, the biosimilar players are striving to take them head on with the anticipated revenues in mind. Stakeholders have made key recommendations to increase the uptake of biosimilars in US market. Regulatory agencies have to play a key role in promoting confidence in biosimilars among healthcare practitioners and patients. The FDAs much awaited Biosimilars Action Plan (BAP) is expected to revive the sedentary biosimilar market in the US. The medical community, payers, and the FDA should work together for ensuring the approved biosimilars are adopted and prescribed in a manner to bring down overall healthcare costs.
Development and Validation of Midostaurin Assay by RP-HPLC Method
Authors: Ahmed Abrar , Mahtab Tayyaba , Saleem Sumaiyya
Published: August 2020

Midostaurin is a multi-targeted protein kinase inhibitor that has been used for the treatment of acute myeloid leukemia.  Here, a rapid and precise reverse phase high-performance liquid chromatographic method has been developed for the validation of midostaurin, in its API form as well as in capsule dosage form. Chromatography was carried out on a X-Bridge C18 (4.6 x 250 mm, 5 µm) column using a mixture of methanol: water (75:25% v/v) as the mobile phase at a flow rate of 1.0 mL/min, the detection was carried out at 243nm and the retention time of the midostaurin was found to be 3.155. The method produce linear responses in the concentration range of 10-50 µg/mL of midostaurin. The method precision for the determination of assay was below 2.0 % RSD. The LOD and LOQ values obtained were 1.2 µg/mL and 3.8 µg/mL respectively. There were no significant changes observed upon changing chromatographic conditions indicating the method to be robust. Therefore this validated method can be useful in the quality control of bulk and pharmaceutical formulations of midostaurin.
A Comprehensive Review on Solid Lipid Nanoparticles as Delivery Vehicle for Enhanced Pharmacokinetic and Pharmacodynamic Activity of Poorly Soluble Drugs
Authors: Dudhipala Narendar
Published: August 2020

This article describes the current state and future perspectives of solid lipid nanoparticles for achieving high delivery of drugs with greater therapeutic outcomes.  The oral route is the most preferred route of administration for majority of drugs. Problems such as poor solubility or chemical stability in the environment of the gastrointestinal tract, poor permeability through the biological membranes or sensitivity to metabolism are well known to result in the rejection of potential drug candidates as oral delivery products. Hence, lipid-based drug delivery systems have been proposed as a means of bypassing the resistant chemical or physical barriers associated with poorly absorbed drugs. Solid lipid nanoparticles (SLNs) can be an attractive one option for oral drug delivery vehicles as they hold tremendous potential to improve the oral bioavailability of drugs, concomitant reduction of drug toxicity and stability of drug in both GIT and plasma. SLNs are in submicron size range and are made of biocompatible and biodegradable materials capable of incorporating both lipophilic and hydrophilic drugs. SLNs are considered as substitute to other colloidal drug systems and are being used as controlled and targeted delivery systems. The SNL technology has greatly revolutionized the delivery systems for poorly soluble drugs. This article describes the methodologies used for preparation and characterization of SNLs.  It outlined the development of stable solid lipid nanoparticles by different techniques. Further, it describes the current status of pharmacokinetic and pharmaco-dynamic studies reported on SLN systems. Finally, it provides a brief outlook on current marketed preparation and the future scope of SLN technology.
Development and Evaluation of Fast Disintegrating Tablets of Lornoxicam Solid Dispersions
Authors: Mohammadi Hafsa , V Hemanath Kumar , S Roshan , D. V. R. N. Bhikshapathi
Published: August 2020

Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.
Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle
Authors: P Ashok Kumar , S.P. Mancy , K Manjunath , Kulkarni Suresh V. , R Jagadeesh
Published: August 2020

Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.
Development and Validation of Stability Indicating RP-HPLC Method for Determination of Enzalutamide
Authors: Nerkar Pankaj Padmakar , Ansari Sameer , Chalikwar Shailesh
Published: August 2020

A simple, isocratic, and accurate reversed phase HPLC method was developed for the quantitative determination of enzalutamide. The chromatographic separation was achieved on an Qualisil BDS C18 (250 mm x 4.6mm, 5 μm) column using methanol: ammonium acetate buffer pH 4.2 adjusted with glacial acetic acid: (60:40, v/v) as a mobile phase, at a flow rate of 1 ml/min and detection at 236nm. The linear range for enzalutamide were 2.0 to        10 μg/mL was obtained with correlation coefficients ≥ 0.998. The retention time was found to be 6.30min. Enzalutamide was subjected to stress conditions hydrolysis (acid, base) oxidation, photolysis and thermal degradation and the stressed samples were analysed by the developed method. The method was validated for the precision, accuracy, linearity and robustness. The developed stability indicating method for enzalutamide was validated as per ICH guidelines.
Efficacy of Silver Nanoparticles Synthesized from Hymenocallis species (Spider Lilly) Leaf Extract as Antimicrobial Agents
Authors: Gupta K.K. , Kumari Neha , Sinha Neha , Gupta Akruti
Published: August 2020

Biogenic synthesis of silver nanoparticles synthesized from Hymenocallis species (Spider Lilly) leaf extract was subjected for investigation of its antimicrobial property against four bacterial species (E. coli, Salmonella sp., Streptococcus sp. & Staphylococcus sp.). The results revealed that synthesized nanoparticles solution very much justify the color change property from initial light yellow to final reddish brown during the synthesis producing a characteristics absorption peak in the range of 434-466 nm. As antimicrobial agents, their efficacy was evaluated by analysis of variance in between the species and among the different concentration of AgNPs solution, which clearly showed that there was significant variation in the antibiotic property between the four different concentrations of AgNPs solution and also among four different species of bacteria taken under studies. However, silver nanoparticles solution of 1: 9 and 1:4 were proved comparatively more efficient as antimicrobial agents against four species of bacteria.
Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System
Authors: Gande Suresh , Reddy S. Srikanth , D. V. R. N. Bhikshapathi
Published: August 2020

Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.
Improvement of Solubility and Dissolution Rate of Simvastatin by Solid Dispersion Technique
Authors: D.V. R. N. Bhikshapathi , M Vishwaja , R Suthakaran , B Usha Sri , Rao M. Ratan Seshagiri
Published: August 2020

The aim of present work is to enhance the solubility and bioavailability of Simvastatin by solid dispersion technique and characterize the same. Preliminary solubility studies were conducted to check the solubility in different polymers. Based on the results 20 formulations prepared by solvent evaporation method with varying ratios of Kleptose HPB, Soluplus, Kolliwax GMS II, Kolliphor P188 and PVPK-30. All the formulations were analyzed for solubility, percentage yield, drug content and in vitro drug release. The formulation SD20 with enhanced solubility of 20.05 ± 0.02μg/mL in Kolliwax GMS II, percentage yield of 99.13% and dissolution rate of 99.2 ± 2.3% within 90 min is chosen as optimized formulation. The formulation is further Characterized for Drug excipient interaction by FTIR, PXRD and SEM studies. The stability studies for 6 months indicated no significant changes in drug content or drug dissolution rate. Hence, improve dissolution characteristics of Simvastatin achieved by increasing its release and solubility through solid dispersion technique.