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Purpose: The present study was aimed at preparing and evaluating biodegradable nanoparticles of docetaxel (DTX). Method: Nanoparticles were prepared by emulsification solvent evaporation technique using polylactic-co-glycolide (PLGA) as biodegradable matrix. The formulations were then characterized with respect to size and its surface morphology, zeta potential, entrapment efficiency in vitro drug release profile, stability studies and in vivo tissue distribution study.
Results: The formulated DTX-PLGA nanoparticles were oval with diameter ranging from 200 nm to 400 nm. The entrapment efficiency was found to be in the range 51.07% to 62.16%. Highest cumulative percent drug release was observed F-1 (49.24 %) and lowest F-4 (36.25%) in 48 h. Based on the highest regression values (R), all four formulations followed Peppas Korsmeyer model. Formulation F-4 with optimal particle size, high entrapment efficiency and satisfactory in vitro release was selected for in vivo studies. The average targeting efficiency of drug loaded nanoparticles was found to be 11.23±0.126% of the injected dose in liver, 27.72±0.415% in lungs, 10.63±0.269% in kidney and 13.24±0.572% in spleen whereas accumulation of pure drug in liver was 7.93±.2.104%, in lungs it was 8.57±1.724%, in kidney it was 08.10±0.827% and spleen 11.35±0.503% of the injected dose.
Conclusion: The results revealed that, the drug loaded nanoparticles showed preferential drug targeting to lungs followed by liver, kidney and spleen. Stability studies indicated that 4? is the most suitable temperature for storage of PLGA nanoparticles. This drug delivery is endowed with several exclusive advantages and hence holds potential for further research and clinical application.
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Author(s): Deshmukh Narendra V Doijad Rajendra C Bhambere Deepak S Somapur C and Goje Arjun Patel Kareeshma S
Docetaxel, PLGA, nanoparticles, emulsification solvent evaporation