HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: SAR and Lead Optimization Using CoMFA and CoMSIA Studies (1995-2016).

Background: Design of inhibitors for HIV-1 reverse transcriptase inhibition (HIV-1 RT) is one of the successful chemotherapies for the treatment of HIV infection. Among the inhibitors available for HIV-1 RT, non-nucleoside reverse transcriptase inhibitors (NNRTIs) have shown to be very promising and clinically approved drugs. However, the efficiency of many of these drugs has been reduced by the drug-resistant variants of HIV-1 RT.

Synthesis and Pharmacological Evaluation of Acrylate-Based Gastrosparing NSAID Prodrugs.

Dexibuprofen and aceclofenac are well-known NSAID molecules, their oral use leads to gastrointestinal (GI) toxicity. To circumvent that GI toxicity, the prodrug approach is a better alternative. Hence, this research was undertaken to synthesize prodrugs of dexibuprofen and aceclofenac using acrylic polymers with degradable ester bonds.

Carrot (Daucus carota L.): Nephroprotective against gentamicin-induced nephrotoxicity in rats.

Objectives: Daucus carota L.(DC) commonly known as carrot, folkorically used as ethnomedicine to treat nephrosis and other urinary disorders. Hence, the present study was aimed to investigate the nephroprotective effects of ethanolic root extract of DC against gentamicin-induced nephrotoxicity in Albino Wistar rats.

Liposomal Aloe vera trans-emulgel drug delivery of naproxen and nimesulide: A study.

Introduction: The present aim of this study was to formulate naproxen and nimesulide liposomal formulation for incorporation in Aloe vera transemulgel and to carry out in vitro and in vivo evaluation of the formulation.

Material And Methods: A. vera gel was prepared and used as a gel base for formulation.

Microemulsions based transdermal drug delivery systems.

Since the discovery of microemulsions by Jack H Schulman, there has been huge progress made in applying microemulsion systems in plethora of research and industrial process. Microemulsions are optically isotropic systems consisting of water, oil and amphiphile. These systems are beneficial due to their thermodynamic stability, optical clarity, ease of preparation, higher diffusion and absorption rates.

Role of various natural, synthetic and semi-synthetic polymers on drug release kinetics of losartan potassium oral controlled release tablets.

Objective: The objective of the present work was to formulate and to characterize controlled release matrix tablets of losartan potassium in order to improve bioavailability and to minimize the frequency of administration and increase the patient compliance.

Materials And Methods: Losartan potassium controlled release matrix tablets were prepared by direct compression technique by the use of different natural, synthetic and semisynthetic polymers such as gum copal, gum acacia, hydroxypropyl methyl cellulose K100 (HPMC K100), eudragit RL 100 and carboxy methyl ethyl cellulose (CMEC) individually and also in combination. Studies were carried out to study the influence of type of polymer on drug release rate.

Formulation, standardization and pharmacological studies of Saraswataristam: a polyhedral preparation.

Ayurvedic preparations achieved paramount importance in contemporary life owing to the safety and efficacy when compared with those of synthetic drugs. But due to lack of proper standardization at each stage from starting to culmination results in inferior quality and less demand. Saraswataristam, a fermented ayurvedic preparation, has been employed for treating central nervous system disorders and dermatological problems.

Formulation and pharmacodynamic evaluation of glibenclamide incorporated niosomal gel.

Objective: The research aims to formulate and develop the controlled release profile of glibenclamide by encapsulating glibenclamide into niosomes followed by incorporation into an aqueous gel base.

Materials And Methods: Glibenclamide incorporated niosomes were prepared by a modified ether injection technique using Span 20/Span 80 and cholesterol. The prepared niosomes were evaluated for chemical incompatibility by FT-IR, morphology, vesicle dimension, encapsulation efficiency, in-vitro diffusion and drug release kinetics.

An overview on in situ micronization technique - An emerging novel concept in advanced drug delivery.

The use of drug powders containing micronized drug particles has been increasing in several pharmaceutical dosage forms to overcome the dissolution and bioavailability problems. Most of the newly developed drugs are poorly water soluble which limits dissolution rate and bioavailability. The dissolution rate can be enhanced by micronization of the drug particles.

Solid self microemulsification of Atorvastatin using hydrophilic carriers: a design.

Context: Atorvastatin has a limited advantage to formulate oral dosage forms.

Objective: To enhance the solubility of Atorvastatin and to design the suitable solid self-microemulsifying drug delivery systems (S-SMEDDS) Materials and methods: The clear and transparent self-microemulsifying drug delivery system (SMEDDS) were formulated using coconut oil and isopropyl myristate as lipid phases; Tween 80 as surfactant; PEG 400 and glycerin as co-surfactant at 2:1, 3:1, 1:2 and 1:3 ratio. The pseudo ternary phase diagrams were constructed to identify the microemulsion region.

Formulation, characterization and comparative evaluation of Trivanga bhasma: a herbo-mineral Indian traditional medicine.

Bhasmas are unique Ayurvedic-metallic preparations with herbal juices/fruits, widely recommended to treat variety of chronic ailments. Trivanga bhasma, a calcinated preparation, is used to treat Diabetes mellitus and as Diuretic. In the present research an attempt has been made to carry out a comparative standardization of formulated Trivanga bhasma (TB1) prepared as per Ayurvedic formulary and marketed Trivanga bhasma (TB2) integrating conventional and modern analytical tools.

Cubosomes as targeted drug delivery systems - a biopharmaceutical approach.

Cubosomes are reversed bicontinuous cubic phases and possess unique physicochemical properties. These special systems are receiving much attention for the delivery of various hydrophilic, hydrophobic and amphiphilic drugs with enhanced bioavailability and high loading capacity. A wide variety of drugs are applicable for cubosome formulation for various routes of delivery.

Formulation, standardization and pharmacological studies of Saraswataristam: a polyhedral preparation.

Ayurvedic preparations achieved paramount importance in contemporary life owing to the safety and efficacy when compared with those of synthetic drugs. But due to lack of proper standardization at each stage from starting to culmination results in inferior quality and less demand. Saraswataristam, a fermented ayurvedic preparation, has been employed for treating central nervous system disorders and dermatological problems.

Selective cyclooxygenase inhibitors: current status.

For ages aspirin has established its value as an analgesic, anti-inflammatory drug, but in 1938, it was found to be a causative factor of gastric inflammation (ulcer). Later discovered non-steroidal anti-inflammatory drugs (NSAIDs) were found effective as aspirin but failed to overcome the goal of safer aspirin. As the method of prostaglandin inhibition through COX is a common mechanism to both the wanted and unwanted effects of aspirin and non-aspirin NSAIDs, the COX enzyme becomes a target for drug designers for the development of the "safe aspirin".

In-vitro assessment and pharmacodynamics of nimesulide incorporated Aloe vera transemulgel.

The aim of the investigation was to prepare nimesulide emulsion for incorporation in Aloe vera gel base to formulate 'nimesulide - Aloe vera transemulgel' (NAE) and to carryout in-vitro assessment and in-vivo anti-inflammatory studies of the product. Although the use of nimesulide is banned for oral administration, due to its potential for inducing hepatotoxicity and thrombocytopenia, the use of nimesulide for topical delivery is prominent in the treatment of many inflammatory conditions including rheumatoid arthritis. The drug loading capacity of transdermal gels is low for hydrophobic drugs such as nimesulide.

Transmucosal delivery of metformin- a comprehensive study.

Discovered in the 1920s, the biguanide metformin hydrochloride is still the first line drug in the management of Type 2 diabetes mellitus. Metformin hydrochloride is absorbed slowly and incompletely from the gastrointestinal tract. The present research work was undertaken with the aim of developing a fast dissolving film of metformin hydrochloride, suitable for oral trans mucosal administration.

Bioavailability and pharmacokinetic studies of rofecoxib solid dispersion.

The present investigation deals with the determination of bioavailability of Rofecoxib solid dispersion compared to pure rofecoxib (RFB). The study of a non-blinded, open-label, crossover design was conducted in six healthy volunteers. Blood samples were collected for 12 h at specified intervals of time after the administration of formulations and analysed by suitable HPLC method.

Modified pulsincap of ibuprofen--a novel approach for chronotherapy.

The aim of the present work was to develop colon specific drug delivery system for ibuprofen using natural polymers as carriers. We have investigated colon specific, pulsatile device to achieve time and site specific release of ibuprofen based on chronopharmaceutical considerations. The basic design consists of an insoluble hard gelatin capsule body, filled with ibuprofen surface solid dispersions and sealed with guar gum hydrogel plug.

Receptors and ligands role in colon physiology and pathology.

Colonic diseases are more prevalent during the past decade. Colorectal cancer, ulcerative colitis, Crohn's disease, diverticulitis, irritable bowel syndrome are the major reported colonic diseases. Innovative strategies are defensible in order to advance the efficacy of colonic disease treatment.

Formulation and evaluation of herbal anti-acne moisturizer.

The moisture content present in human skin makes it look young and the use of moisturizer results in fastening the moisture with a surface film of oil. Acne vulgaris is one of the most commonly seen diseases among the youth. The present study is focused on the use of herbs as moisturizer for acne treatment.

Anatomical, biochemical and physiological considerations of the colon in design and development of novel drug delivery systems.

The colon is composed of four distinct layers such as serosa, muscularis externa, sub mucosa and mucosa. There exists a difference in the anatomy, neural and blood supply and absorption characteristics as the length of the colon is traversed. At birth the mucosal surface of the colon is similar to that of the small intestine but rapid changes occur with the loss of the villi leaving flat mucosa with deep crypts.

Formulation and evaluation of chitosan solid lipid nanoparticles of carbamazepine.

The present work aims at preparing aqueous suspension of Solid lipid Nanoparticles containing Chitosan (CT) which is a biopolymer that exhibits a number of interesting properties which include controlled drug delivery. Carbamezapine (CBZ) is a lipophilic drug which shows it antiepileptic activity by inactivating sodium channels. The solid lipid Nanoparticles (SLN) of Chitosan-CBZ were prepared by using solvent injection method using ethanol as organic solvent.

Formulation and comparative evaluation of poly herbal anti-acne face wash gels.

Context: Rauvolfia serpentina (L). Benth. ex Kurz.

Synthesis, hydrolysis studies and phamacodynamic profiles of amide prodrugs of dexibuprofen with amino acids.

The present investigation deals with the synthesis of novel prodrugs of dexibuprofen with amino acids with an aim to achieve potent anti-inflammatory activity and less gastrointestinal toxicity. Structures of synthesized compounds were confirmed by spectral and elemental analyses. In vitro hydrolytic studies in simulated intestinal fluid, 80% plasma and rat faecal matter showed satisfactory release of dexibuprofen due to enzymatic cleavage.

Preparation and evaluation of famotidine polymorphs.

The main objective of this study was to compare the behaviour of drug release among the famotidine polymorphs prepared by using various additives and solvents, by solvent evaporation method. The famotidine polyvinyl pyrrolidone polymorphs with different concentrations (0.5, 1 and 1.