Nishi Mody, Rajeev Sharma, Suresh P. Vyas*
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. Harisingh Gour Vishwavidyalaya, Sagar (M.P.) – 470003, India
*Address for Corresponding author
Prof. Suresh P. Vyas
Drug Delivery Research Laboratory
Department of Pharmaceutical Sciences
Dr. Harisingh Gour Vishwavidyalaya, Sagar-470003 M.P. (India)
Abstract
Objective: The objective of the present study was to formulate and investigate in vitro release kinetics profile of docetaxel loaded poly (lactic-co-glycolic acid) nanoparticulate drug delivery system in order to improvise the solubility of the drug as well as to attain a controlled release drug pattern in pursuit to reduce the toxicity and dosing frequency problems associated with the present marketed formulations. Materials and methods: Preformulation study of docetaxel such as physical properties (melting point, partition coefficient, and solubility), identification (UV and FTIR spectroscopy) and linearly regressed calibration curves for quantification were carried out prior to formulation development. Taking advantage of biodegradable and biocompatible, and FDA approved polymer “poly (lactic-co-glycolic acid)”, docetaxel loaded nanoparticles were developed. by emulsification - solvent evaporation technique. The morphology of the docetaxel loaded nanoprticles was observed via scanning electron microscopy (SEM). Synthesized docetaxel loaded nanoprticles were also characterized with regard to their particle diameters, zeta potential, drug loading capacities, and drug release kinetics. Results and conclusion: A nanoparticle formulation of PLGA encapsulating docetaxel was prepared via emulsification - solvent evaporation technique under optimized conditions. The developed formulation showed a favorable particle size below 200 nm for higher retention at tumor site owing to enhanced permeability and retention (EPR) effect. Entrapment efficiency was recorded to be 64.34±1.53%. In vitro studies showed that the docetaxel loaded nanoparticles exhibited a sustained drug release which suggested that nanoparticles are likely to reduce dose and dosing frequency. We also studied release behavior of docetaxel in terms of mechanism and pattern so that these aspects may be of great utility to formulation developers for cancer targeting and NPs development of similar drug. Developed NPs still warrant further investigation for assuring ex-vivo and in-vivo potential.
Keywords: PLGA; Docetaxel, nanoparticles, solid tumors, release kinetics
