Characterization and in vitro assessment of paclitaxel loaded lipid nanoparticles formulated using modified solvent injection technique
D. Pandita 1, D. Pandita 2, A. Ahuja 1, T. Velpandian 3, V. Lather 4, T. Dutta 5, R. K. Khar 1
1 Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard University, New Delhi, India
2 Centro de Quimica da Madeira, Universidade da Madeira, Campus da Panteada, Funchal, 9000–390, Portugal, Email: deeptipandita@yahoo.co.uk
3 Department of Ocular Pharmacology, Dr. Rajender Prasad Centre of Ophthalmic Sciences and Research, All India Institute of Medical Sciences, New Delhi, India
4 Centro de Quimica da Madeira, Universidade da Madeira, Campus da Panteada, Funchal, Portugal
5 Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar, India
Abstract
This study investigates the design and characterization of solid lipid nanoparticles (SLNs) containing paclitaxel fabricated by a modified solvent injection technique using stearic acid as lipid and stabilized by a mixture of surfactants, for future evaluation of this colloidal carrier system for the oral delivery of paclitaxel, devoid of the side effects of Cremophor® EL. SLN formulations of paclitaxel stabilized by mixture of surfactants i.e. lecithin/poloxamer 188 were developed with smaller size and narrow size distribution. The paclitaxel-loaded SLNs exhibited spherical shape with smooth surface as analyzed by transmission electron microscopy (TEM). The average particle size obtained through this method was found to be ∼113 nm. The zeta potential was between –32 and –39 mV with poloxamer 188. Encapsulation efficiencies of about 72.18 ± 3.7 and 89.0 ± 2.4% were achieved using 0.05 and 0.25 mmol of paclitaxel, respectively. Paclitaxel showed a sustained in vitro release profile and was found to follow Higuchi kinetic equations. In vitro cytotoxicity assay confirmed that paclitxel entrapped in SLNs showed higher cytotoxicity against cultured hepatocelluler carcinoma cells than paclitaxel alone. The modified solvent injection technique used in this research proved to be a simple, easily available and effective method to produce SLNs and could be used for controlled delivery of different lipophilic drugs for cancer chemotherapy.