Preparation and in-vitro Evaluation of Poly-ï¥-Caprolactone Nanoparticles Containing Atorvastation Calcium

Abstract

Preparation and evaluation of poly-e-caprolactone nanoparticles containing atorvastatin calcium (AC), a drug with poor solubility and poor bioavailability, is presented. The drug loaded nanoparticles were prepared by solvent displacement method using different experimental conditions.  The influence of different formulation variables, such as type and concentration of stabilizers in the aqueous phase, concentration of polymer and surfactant in the organic phase, addition of an anti-oxidant, pH of the aqueous phase and others, on particle size, drug entrapment efficiency, in-vitro drug release along with other physico-chemical properties of the nanoparticles was investigated using several full factorial designs. The optimized AC nanoparticles showed an average particle size of less than 200 nm, a drug loading capacity of more than 70% and released the drug in a controlled fashion over 24 hour. Transmission electron microscope (TEM) revealed that the prepared AC nanoparticles were nearly spherical. Short-term stability results of selected formulae were satisfactory.