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Enhancement of taxane bioavailablility cum anticancer potential using engineered lipohybrid system
3rd International Conference on Nanotek & Expo
December 02-04, 2013 Hampton Inn Tropicana, Las Vegas, NV, USA

Ankit Jain

Accepted Abstracts: J Nanomed Nanotechnol

Abstract:

Fabricated lipohybrid (FLH) systems have been developed with the purpose of improving bioavailability of paclitaxel combining concepts of thermoresponsive delivery and P-gp inhibition. FLH systems were composed of DPPC (thermosensitive lipid), Brij78 and pluronic F68 (PF68, P-gp inhibitor) for thermosensitive delivery of paclitaxel (PTX) with sizes below 150 nm. The use of 2% (v/v) Tween 80 (P-gp inhibitor) in the hydration media was able to increase the solubility of drug (leading to increase in entrapment efficiency from 81 to 92%). The transition temperature of the FLH systems were ~41?C leading to enhanced bioavailability upon hyperthermia. In vitro drug release at 40?1 o C was abrupt burst release (i.e., 100% within 5 min) whereas insignificant release at 37?0.5 o C. Cytotoxicity in PTX-resistant human lung cancer cell line (A549/T cells) brought favorable results that DPPC/Brij78/PF68 FLH system being hydrated with Tween 80 was highly toxic in MTT assay, and it showed 3.5 fold enhancement of cytotoxicity as compared to DPPC/Brij78 FLH system. This was accounted to enhanced bioavailability of paclitaxel due to both high entrapment and least efflux (P-gp inhibition) from cancer cells. Such FLH systems, possessing heralding features of thermo-sensitivity, high entrapment efficiency, that could not only enhance bioavailability but also anticancer potential, could serve as better alternative for the passive targeting of PTX-resistant human lung cancer