Design, Development and Characterization of Nanostructure Lipid Carriers (NLCs) by HPH Method Loaded with Anticancer Drug

Abstract

The Nanostructured Lipid Carriers (NLCs) was formulated with the aim to improve the aqueous solubility and thus ultimately oral bioavailability of Axitinib. Axitinib loaded NLCs were formulated using Compritol ATO 888 as solid-lipid, Oleic acid as liquid-lipid and Tween 80 as surfactant by the High-Pressure Homogenization technique. A full 23 factorial design was utilized to study the effect of the independent parameters, solid-lipid to the liquid-lipid ratio (6:4) and surfactant, on the dependent variables such as Mean Particle Size (MPS) and Entrapment Efficiency (%EE). Optimized formulation showed 202.2 nm MPS, -21.5 mV zeta-potential and 0.44 PDI, and 88% EE, which imparts good stability of developed NLCs. The physicochemical characterization of AXT loaded NLCs was done by examining the results of Differential Scanning Calorimetry, Fourier transform infrared spectroscopy study. The stability study of optimized formulation was found to be stable with no significant change in particle size, and drug content. In vitro release profiles of NLCs indicated a burst release for the first 2 hrs followed by a prolonged-release profile for AXT until about more than 10 hrs. The Axitinib NLCs may provide a better bioavailability, reduction in dose, dosing frequency, dose-related side effects and better control of the disease. A foresaid results showed the potential of NLCs for significant improvement in oral bioavailability of poorly soluble Axitinib in cancer treatment.
 Keywords: NLCs, full factorial design, high-pressure homogenization, in-vitro release