V.K. Mourya - Academia.edu (original) (raw)

Papers by V.K. Mourya

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Nystatin and Terbinafine are antifungal drugs with well-known antifungal properties. In the prese... more Nystatin and Terbinafine are antifungal drugs with well-known antifungal properties. In the present study we investigated the potential of PAMAM and PPI dendrimers of different generations as tool for enhancement of antifungal activity of selected two antifungal drugs. Microbilogical study showed that PAMAM and PPI dendrimers could enhance the antifungal activities of Nystatin and Terbinafine against Candida albicans, Aspergillus niger and Sachromyces cerevasae. Results showed increase in the antifungal activity of Nystatin and Terbinafine in dendrimer solution compared to pure Nystatin and Terbinafine dissolved in DMSO (dimethylsulfoxide). The antifungal activity studies indicated that PAMAM and PPI dendrimers as potential tool for enhancement of antifungal activity of Nysatin and Terbinafine.

Indian journal of pharmaceutical sciences, 2011

The extended Hildebrand solubility parameter approach is used to estimate the solubility of satra... more The extended Hildebrand solubility parameter approach is used to estimate the solubility of satranidazole in binary solvent systems. The solubility of satranidazole in various dioxane-water mixtures was analyzed in terms of solute-solvent interactions using a modified version of Hildebrand-Scatchard treatment for regular solutions. The solubility of satranidazole in the binary solvent, dioxane-water shows a bell-shaped profile with a solubility maximum well above the ideal solubility of the drug. This is attributed to solvation of the drug with the dioxane-water mixture, and indicates that the solute-solvent interaction energy is larger than the geometric mean (δ(1)δ(2)) of regular solution theory. The new approach provides an accurate prediction of solubility once the interaction energy is obtained. In this case, the energy term is regressed against a polynomial in δ(1) of the binary mixture. A quartic expression of W in terms of solvent solubility parameter was found for predictin...

Indian Journal of Pharmaceutical Sciences, 2012

Rathi and Mourya: Solubility Prediction of Satranidazole by Extended Hildebrand Solubility The so... more Rathi and Mourya: Solubility Prediction of Satranidazole by Extended Hildebrand Solubility The solubility of satranidazole in several water-N,N-dimethylformamide mixtures was analysed in terms of solutesolvent interactions and data were treated on the basis of extended Hildebrand solubility approach. The solubility profile of satranidazole in water-N,N-dimethylformamide mixtures shows a curve with a solubility maxima well above the ideal solubility of drug. This is attributed to solvation of the drug with the water-N,N-dimethylformamide mixture, and indicates that the solute-solvent interaction energy (W) is larger than the geometric mean (d 1 d 2) of regular solution theory. The new approach provides an accurate prediction of solubility once the interaction energy (W) is obtained. In this case, the energy term is regressed against a polynomial in d 1 of the binary solvent mixture. A quartic expression of W in terms of solvent solubility parameter was found for predicting the mole fraction solubility of satranidazole in the studied mixtures. The method has potential usefulness in preformulation and formulation studies during which solubility prediction is important for drug design.

CRC Press eBooks, Dec 4, 2013

ABSTRACT The polymer properties of chitosan are spectacularly modified with their conversion to s... more ABSTRACT The polymer properties of chitosan are spectacularly modified with their conversion to sulfhydrylbearing derivatives. In the thiol-bearing derivatives, the mucoadhesive, cohesive properties and in situ gelling features are strongly improved. These properties further enrich the inherent permeation enhancement capabilities of native chitosan. The permeation-enhancing effect can be raised further by the combination of thiolated chitosans with the permeation mediator glutathione. Owing to these advantageous features, thiolated chitosans have been successfully employed for noninvasive peroral administration of peptide drugs, controlled and site-specific release of smaller drugs, coating of nanoparticles, and DNA delivery. Further applications, where thiolated chitosans might prove successful, include their use as scaffold material and coating material for stents in the field of tissue engineering. The elaboration of thiolated chitosan with derivativatized chitosan as backbone polymer is also gaining attention as with TMC. The graft copolymers of mercaptochitin and mercaptochitosan may serve as the candidates for applications in tissue engineering. The development of hydrogels of thiolated chitosans can also be foreseen.

Indian Journal of Pharmaceutical Sciences, 1998

The variation in the pKa values was observed in presence of different solvents used to improved s... more The variation in the pKa values was observed in presence of different solvents used to improved sample solubility. Quantitative expression has been developed to estimate pKa values of a specific compound. The information may be useful for the pKa estimation of other compounds.

The generation of supramolecular architectures with well-defined structures and functionalities i... more The generation of supramolecular architectures with well-defined structures and functionalities is recently garnering attraction. Self-assemblage of amphiphilic polymers leads to the formation of polymeric micelles that demonstrate unique set of characteristics such as excellent biocompatibility, low toxicity, enhanced blood circulation time, and solubilization of poorly water-soluble drugs. In this article, we provide an up-to-date review on important aspects of polymeric micelles. Critical factors for solubilization of hydrophobic drugs in the micellar core are discussed. Polymeric micelles can be used as ‘smart’ drug carriers for targeting certain areas of the body. Here, we have especially emphasized on the recent developments in the targetability of certain tissues such as cancerous tissues using polymeric micelles. Different stimuli exploited for creating stimuli-sensitive micelles are discussed comprehensively. Application of polymeric micelles in the photodynamic therapy is ...

European Chemical Bulletin, 2014

A simple and efficient method for the synthesis of chalcone derivatives using polyamine catalyst ... more A simple and efficient method for the synthesis of chalcone derivatives using polyamine catalyst has been described. The antibacterial activity of chalcones are also evaluated by using gram positive ( S. aureus, B. subtillus ) and gram negative bacteria ( Klebisila pneumonia, P. aerugenosa ) microorganisms.

The most preferred route for delivering therapeutic agents is oral drug delivery. However, this r... more The most preferred route for delivering therapeutic agents is oral drug delivery. However, this route is not feasible for delivery of hydrophilic macromolecules, such as therapeutic peptides, proteins, nucleotides, and efflux pump substrates, because of negligible oral bioavailability. This is because of the barriers confronted by these molecules along the oral route, such as diffusion barrier of mucus, enzymatic barrier of peptidases, and permeability barrier of membranes. The strategies to surmount these barriers are by utilization of permeation enhancers, enzyme inhibitors, and multi-functional polymers, ideally guaranteeing both permeation enhancement and enzyme inhibition. In case of multifunctional polymers, these effects can take place only if polymers offer strong muco-adhesive features for providing a tight contact with the mucosa during the whole period of peptide drug release and absorption. Among the group of multifunctional polymers exhibiting all of the aforementioned ...

Applications of Polymers in Drug Delivery, 2021

Abstract Polymers have been an important component in the development of drug delivery systems be... more Abstract Polymers have been an important component in the development of drug delivery systems because of their ability to release active ingredients for a longer period of time without fluctuations in plasma levels. The first polymeric based drug delivery system, a controlled release hydrogel, based on lactic acid was reported back in the 1960s, and today, the progress in technology of polymers has directed utilization of even polymers and recombinant products of those for delivery of gene and drug. For the past many years, biodegradable polymers have found widespread use in delivery of drugs and genes because of their biocompatible and biodegradable nature. Polymeric delivery systems for drug and gene with biodegradable nature for definite consignment and planned to apply individual biological functions is constantly a sizzling area of interest. A proper balance of physicochemical properties of polymers can be helpful to design several delivery technologies for various uses through different routes. Novel supramolecular structures, block copolymers as well as dendrimers have been exhaustively investigated for delivery of vectors, siRNA and genes as well as other macromolecules. Scheme and production of innovative amalgamations of polymers will grow the opportunity of novel and target-specific delivery of drug in coming future. In this chapter, we have highlighted essential polymeric systems to deliver drugs and their applications, the physiological barriers to drug delivery and latest developments in polymers to exemplify regions of research evolving the edges of drug delivery.

Industrial Applications of Marine Biopolymers, 2017

Advanced Materials Letters, 2012

Low molecular weight chitosan (LMWC) exhibits higher water solubility and produces nanoparticles ... more Low molecular weight chitosan (LMWC) exhibits higher water solubility and produces nanoparticles of fairly low particle size. However, poor drug loading and shorter circulation time in body limits its application in preparation of nanoparticles. Acylation of LMWC ensures extended circulation of nanoparticles in body and hence enhanced bioavailability of the drug. We therefore synthesized the acylated LMWC using palmitoyl chloride and confirmed its synthesis by FTIR and NMR spectroscopy. The nanoparticles of LMWC and low molecular weight palmitoyl chitosan (LMWPC) were prepared by miniemulsion and chemical crosslinking method using glutaraldehyde and 5-fluorouracil (5FU) as a model drug. The nanoparticles were evaluated for particle size, zeta potential, morphology, drug loading and drug release. TEM analysis revealed nanosize and spherical nature of the particles. The palmitoyl chain of LMWPC increased particle size from 83.2±2.5 nm to 93.4±3.2 nm whereas zeta potential of nanoparticles decreased from 12.5±2.2 mV to 4.2±1.1 mV due to diminished amino groups of LMWPC as a result of acylation. The drug loading in nanoparticles was increased from 13.8±0.95% to 30.2±1.9%. LMWC showed 80±2.08% as maximum drug released in 10 h while only 52.3±2.14% was released in 24 h for LMWPC. Hence, LMWPC nanoparticles ensure increased drug loading capacity and sustained drug release profile without significant change in particle size.

Indian Journal of Pharmaceutical Sciences, Jul 1, 1997

Soft Nanoscience Letters, 2016

The aim of present study was to use QbD approaches to evaluate the effect of independent product ... more The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride; for overcoming those limitations, lyophilization method is used. A 4 3 level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.

Amides and esters of sorbic, cinnam ic and ricinoleic acid have been synthesized and evaluated fo... more Amides and esters of sorbic, cinnam ic and ricinoleic acid have been synthesized and evaluated for their antibacterial activity against gram C+) ve S. aureus, B. subtilis and gram C-) ve E. coli. Most of the compounds have shown moderate to good activity against microorganisms under test. Linear regressio n ana lysis of descriptors related to li pophilicity, steric and electronic parameters against antibacterial activity have been performed. QSAR studies indicated the predominance of electronic and steric parameters over the lipophilicity parameters in contributing antibacterial act ivity.

Several natural biopolymers are polyelectrolyte in nature and used as drugs and drug delivery age... more Several natural biopolymers are polyelectrolyte in nature and used as drugs and drug delivery agents. Chitosan being a unique polyelectrolyte biopolymer with positive charge can interact with natural or artificial polyelectrolyte to form polyelectrolyte complexe (PEC). The properties of such complexes may be of interest to understand interaction mechanism in the formation of PECs, factors affecting PEC formation and physicochemical characteristics of PECs, utility as drug carrier or agent to cross biomembrane as well as their interactions with biomolecules or receptors. This chapter addresses concept of PEC, effect of properties of chitosan on PEC formation, polyanion complexes of importance available in literature with natural biopolymers like DNA, polysaccharide and synthetic polymers like acrylates etc and their utility in the area of life sciences.

Indian Journal of Pharmaceutical Sciences

Indian journal of biochemistry & biophysics, 2006

Diabetes mellitus is one of the most common non-communicable diseases, and is the fifth leading c... more Diabetes mellitus is one of the most common non-communicable diseases, and is the fifth leading cause of death in most of the developed countries. It can affect nearly every organ and system in the body and may result in blindness, end stage renal disease, lower extremity amputation and increase risk of stroke, ischaemic heart diseases and peripheral vascular disease. Hyperglycemia in diabetes causes non-enzymatic glycation of free amino groups of proteins (of lysine residues) and leads to their structural and functional changes, resulting in complications of the diabetes. Glycation of proteins starts with formation of Shiff's base, followed by intermolecular rearrangement and conversion into Amadori products. When large amounts of Amadori products are formed, they undergo cross linkage to form a heterogeneous group of protein-bound moieties, termed as advanced glycated end products (AGEs). Rate of these reactions are quite slow and only proteins with large amounts of lysine res...

Journal of Nanopharmaceutics and Drug Delivery, 2013

ABSTRACT A novel approach of using combination of low molecular weight (LMW) and high molecular w... more ABSTRACT A novel approach of using combination of low molecular weight (LMW) and high molecular weight (HMW) chitosan for preparation of nanoparticles is addressed here. The benefits of using LMW (2.5 kDa) and HMW (800 kDa) chitosans together for preparation of oral nanoparticulate drug delivery were evaluated. Keeping the degree of deacetylation constant (75%), nanoparticles were prepared with different ratios of LMW and HMW chitosans by W/O miniemulsion and chemical cross-linking. Transmission electron microscopy revealed their nanosize and spherical nature. With an increase in HMW chitosan proportion, particle size varied between 94.22 ± 9.31 nm and 243.2 ± 7.40 nm while zeta potential ranged from 9.05 ± 2.75 mV to 57.06 ± 6.94 mV. Simultaneously the loading of drug, 5-fluorouracil, increased from 13.8 ± 0.95% to 27.34 ± 0.48% and the highest entrapment efficiency obtained was 93.76 ± 0.86%. Particularly, nanoparticles prepared using LMW:HMW (1:1) chitosan provided desirable characteristics along with 58.93 ± 2.28% mucoadhesion and 73.37 ± 1.23% drug release in 24 h, demonstrating their promising potential as sustained drug delivery carriers. In vitro , cell line study proved the efficacy of prepared nanoparticles for anticancer therapy.