Abstract

FORMULATION, OPTIMIZATION AND CHARACTERIZATION TUMOR TARGETING SOLID LIPID NANOPARTICLES OF PACLITAXEL

Shikha Singh*, Nishi Prakash Jain and S. K. Jain

Abstract

Tumors are characterized by poorly differentiated, highly chaotic arrangement of vessels which have unsealed endothelial cell–cell junctions and discontinuous basement membrane. These are characterized by interstitial hypertension, low extracellular pH, hypoxia, angiogenesis, tumor– stromal cell interaction, cancer stem cells, and abnormal lymphatics and key microenvironmental features of solid tumors greatly impact the extravasation of polymeric nanomedicines like solid lipid nanoparticles (SLNs). Solid Lipid Nanoparticles (SLNs) are rapidly developing field of nanotechnology is one of the approaches to improve bioavailability by targeting the antineoplastic drug Paclitaxel (PTX) to the tumor. The present research work is to formulate and optimize the Paclitaxel SLNs by simple solvent injection method. Solid Lipid Nanoparticles (SLNs) of Paclitaxel were formulated by taking Tristearin and Stearylamine as lipid matrix, Tween 80 as surfactant and soya lecithin as co emulsifier. Sonication and stirring were important process to optimize the size of Solid Lipid Nanoparticles. The optimization was carried out of various variables on the basis of particle size, shape, and polydispersity index and drug entrapment efficiency. Solid Lipid Nanoparticles (SLNs) of Paclitaxel optimized with Tristearin and Stearylamine ratio (1.5:1.0), drug lipid ratio(1:10) with 1% of Tween80, stirring at speed about 3000 for 60 minutes and 2 minutes of sonication for minimum size. The optimized Formulation of SLN showed a % cumulative drug release of 79.94±1.88% up to 48 hours in PBS (pH 7.4).

Keywords: Tumor, Solid Lipid Nanoparticles (SLNs), Paclitaxel (PTX), Tristearin, Stearylamine.