Rakesh Kumar Marwaha

Box-Behnken Designed Fluconazole Loaded Chitosan Nanoparticles for Ocular Delivery

Box-Behnken Designed Fluconazole Loaded Chitosan Nanoparticles for Ocular Delivery The present study aimed to develop chitosan nanoparticles containing Fluconazole for ocular delivery using Box-Behnken design. The Fluconazole loaded chitosan nanoparticles were prepared by an ionic gelation method using Sodium tripolyphosphate (NaTPP) as cross linking agent. The effect of the factors - concentration of chitosan (x1), concentration of NaTPP (x2) and volume of NaTPP (x3) was studied on release of drug from nanoparticles. The results revealed that entrapment efficiency was highest at low level of chitosan concentration, high level of NaTPP concentration and low levels of NaTPP volume. The optimized batch (NP 3) showed encapsulation efficiency of 63.1%, particle size of 471 nm, ovoid shape surface morphology and in vitro cumulative percentage of drug release 39.19% in 7 h.

Permeability Evaluation Through Chitosan Membranes Using Taguchi Design

In the present study, chitosan membranes capable of imitating permeation characteristics of diclofenac diethylamine across animal skin were prepared using cast drying method. The effect of concentration of chitosan, concentration of cross-linking agent (NaTPP), crosslinking time was studied using Taguchi design. Taguchi design ranked concentration of chitosan as the most important factor influencing the permeation parameters of diclofenac diethylamine. The flux of the diclofenac diethylamine solution through optimized chitosan membrane (T9) was found to be comparable to that obtained across rat skin. The mathematical model developed using multilinear regression analysis can be used to formulate chitosan membranes that can mimic the desired permeation characteristics. The developed chitosan membranes can be utilized as a substitute to animal skin for in vitro permeation studies.

Development and Characterization of Gefitinib Loaded Polymeric Nanoparticles by Ionic Gelation Method

BACKGROUND There is a rapidly growing interest in the development of nanoparticle drug delivery mainly for anticancer drugs as it promises to solve several problems associated with anticancer drugs such as poor water solubility, low therapeutic index, nonspecific distribution and higher systemic toxicity, etc. OBJECTIVE The objective of the study was to investigate the effect of various critical variables like, concentration of chitosan, concentration of sodium tripolyphosphate (STPP) and volume of STPP on various characteristics of gefitinib loaded nanoparticles. METHODS Thirteen formulations of the polymeric nanoparticles were prepared using various concentrations of chitosan (0.1-1% w/v), STPP (0.2-1.5% w/v) and different volumes of STPP (8-20 ml) by ionic gelation method. Mannitol (5% w/v) was used as cryoprotectant. The prepared nanoparticle formulations were characterized for various parameters like particle size, zeta potential, process yield, encapsulation efficiency, drug content, and in vitro drug release. RESULTS The nanoparticle formulation NF-1 containing 0.1% w/v of chitosan and 10 ml volume of 0.2% w/v STPP showed best results in terms of particle size (123.8nm), polydispersity index (0.247), zeta potential (+30.4 mV), process yield (68.09%), drug content (74.32%), encapsulation efficiency (70.52%) and released (56.2 %) drug over a period of 24 h. The in vitro drug release analysis showed sustained release of gefitinib from nanoparticles and followed Korsmeyer-Peppas model. CONCLUSION The nanoparticle formulation with desired characteristics can be prepared at low concentration of chitosan and STPP along with low volume of STPP. The formulated nanoparticles may prove to be the best option for the treatment of cancer.

Synthesis, antimicrobial evaluation and QSAR studies of 2-chlorobenzoic acid derivatives.

In the present study, 2-chlorobenzoic acid derivatives were synthesized and evaluated for their antimicrobial activity against Gram-positive bacteria: Staphylococcus aureus, Bascillus subtilis, Gram-negative bacterium Escherichia coli, fungal strains: Candida albicans and Aspergillus niger by tube dilution method. Results of antimicrobial screening indicated that the synthesized compounds exhibited greater antibacterial potential against Gram-negative bacterium (Escherichia coli) than Gram-positive bacteria and the Schiffs bases of 2-chloro benzoic acid were more potent antimicrobial agents than its esters. Compound 6 (pMIC(am)=1.91 µM/ml, pMIC(ec)=2.27 µM/ml) emerged as most potent antimicrobial agent and was found comparable to standard drug norfloxacin (pMIC(ec)=2.61 µM/ml) against Escherichia coli. QSAR studies revealed that the antibacterial, antifungal and the overall antimicrobial activities of the 2-chlorobenzoic acid derivatives were governed by the topological parameters, second order and valence second order molecular connectivity indices ((2)χ and (2)χ(v)).