Design and evaluation of liposomal delivery system for L-Asparaginese.
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Date
2012-08
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Abstract
Despite of its effective anti-tumour activity,L-Asparaginase has limited clinical
application due to the high rate of clinical hypersensitivity. In an attempt to develop a liposomal
drug delivery for L-Asparaginase, enzyme loaded liposomes were formulated using soy lecithin,
cholesterol and charge inducers by thin film hydration method. The effect of various
components of the liposomes including the concentration of lecithin and cholesterol with or
without the charge inducers on the entrapment efficiency and short term invitro cytotoxicity
study was systematically investigated. The average particle sizes of the vesicles were found to
be 43.2, 35.6 and 65.8 μm respectively for neutral, positive and negative liposomes. The
percentage of drug loading was found to be 1.95, 2.39 and 2.35 % respectively for neutral,
positive and negative liposomes.The invitro release study of L-Asparaginase was carried out
using normal saline as dissolution medium and the release was found to be 86.88, 78.29 and
82.04 % respectively for neutral, positive and negative liposomes. The release of LAsparaginase
from liposomes was followed first order kinetics obeying non-Fickian diffusion.
A short term cytotoxicity study was carried out using Ehrlich Ascites Carcinoma cells (EAC
cells) which revealed that the cytotoxicity concentration CTC50 for pure drug was found to be 64
mcg as compared to liposomal formulation of 50 mcg.
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Keywords
L-Asparaginase, liposomes, charge inducers, release kinetics, in vitro cytotoxicity studies
Citation
De Anindita, Venkatesh D Nagaswamy. Design and evaluation of liposomal delivery system for L-Asparaginese. Journal of Applied Pharmaceutical Science. 2012 Aug; 2(8): 112-117.