TY - JOUR
T1 - PLGA 50:50 nanoparticles of paclitaxel
T2 - Development, in vitro anti-tumor activity in BT-549 cells and in vivo evaluation
AU - Averineni, Ranjith K.
AU - Shavi, Gopal V.
AU - Gurram, Aravind K.
AU - Deshpande, Praful B.
AU - Arumugam, Karthik
AU - Maliyakkal, Naseer
AU - Meka, Sreenivasa R.
AU - Nayanabhirama, Udupa
PY - 2012/6/1
Y1 - 2012/6/1
N2 - Clinical administration of paclitaxel is hindered due to its poor solubility, which necessitates the formulation of novel drug delivery systems to deliver such extreme hydrophobic drug. To formulate nanoparticles which makes suitable to deliver hydrophobic drugs effectively (intravenous) with desired pharmacokinetic profile for breast cancer treatment; in this context in vitro cytotoxic activity was evaluated using BT-549 cell line. PLGA nanoparticles were prepared by emulsion solvent evaporation technique and evaluated for physicochemical parameters, in vitro anti-tumor activity and in vivo pharmacokinetic studies in rats. Particle size obtained in optimized formulation was <200 nm. Encapsulation efficiency was higher at polymer-to-drug ratio of 20:1. In vitro drug release exhibited biphasic pattern with initial burst release followed by slow and continuous release (15 days). In vitro anti-tumor activity of optimized formulation inhibited cell growth for a period of 168 h against BT-549 cells. AUC (0-∞) and t 1/2 were found to be higher for nanoparticles with low clearance rate.
AB - Clinical administration of paclitaxel is hindered due to its poor solubility, which necessitates the formulation of novel drug delivery systems to deliver such extreme hydrophobic drug. To formulate nanoparticles which makes suitable to deliver hydrophobic drugs effectively (intravenous) with desired pharmacokinetic profile for breast cancer treatment; in this context in vitro cytotoxic activity was evaluated using BT-549 cell line. PLGA nanoparticles were prepared by emulsion solvent evaporation technique and evaluated for physicochemical parameters, in vitro anti-tumor activity and in vivo pharmacokinetic studies in rats. Particle size obtained in optimized formulation was <200 nm. Encapsulation efficiency was higher at polymer-to-drug ratio of 20:1. In vitro drug release exhibited biphasic pattern with initial burst release followed by slow and continuous release (15 days). In vitro anti-tumor activity of optimized formulation inhibited cell growth for a period of 168 h against BT-549 cells. AUC (0-∞) and t 1/2 were found to be higher for nanoparticles with low clearance rate.
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U2 - 10.1007/s12034-012-0313-7
DO - 10.1007/s12034-012-0313-7
M3 - Article
AN - SCOPUS:84863495964
SN - 0250-4707
VL - 35
SP - 319
EP - 326
JO - Bulletin of Materials Science
JF - Bulletin of Materials Science
IS - 3
ER -
