Abstract

NOVEL SALICIN PHYTOSOMAL COMPLEX: DEVELOPMENT AND OPTIMIZATION USING CENTRAL COMPOSITE DESIGN

Parul A. Ittadwar*, Shankar V. Bhojne and Prashant K. Puranik

Abstract

The present study encompasses the formulation of a novel Salicin phospholipid complex (Phytosome) using Central composite design as a tool for optimization and its characterization using various techniques. Salicin is an alcoholic β-glucoside with anti-inflammatory, analgesic and antipyretic activity obtained from various natural sources like willow bark, castoreum, populous species etc. But as a phytochemical it has been reported to show low aqueous solubility, low absorption, low bioavailability and hence lower activity. Phytosomes are complexes of phytochemical and phospholipid in a stoichiometric ratio in a non-polar solvent and are thus, supposed to enhance the overall properties of the phytochemical. These complexes have the bioactive phytoconstituent of herb extracts chemically bound by a lipid. Structurally Salicin possesses five hydroxyl polar groups which have the ability to bind with the polar group of phospholipid so as to form a phytosomal complex. Salicin phytosomes were formulated by solvent evaporation method and optimized using experimental design. The optimized batch showed 4.89 times enhanced solubility in water (135.73μg/ml) than the drug alone (27.73μg/ml) with complexation rate of 99.64%. The phytosomes were evaluated using FTIR, DSC, SEM and XRD. SEM showed the surface morphology of complex depicting the conversion of crystalline drug into amorphous complex. The in vitro permeation in the form of suspension was significantly higher for the complex (93.43%) than the drug (19.65%) after 7 hours. Hence, Salicin showed better solubility and permeation in the form of phytosomes which may eventually increase its absorption, bioavailability and pharmacological activity.

Keywords: Salicin, Phytosome, Central composite design, Partition coefficient, Solubility, Permeation.