DEVELOPMENT OF HERBAL NANOPARTICULATE FORMULATION FOR THE TREATMENT OF SOLID TUMOR

Abstract

The purpose of this research was to prepare SLN formulation for incorporation of a herbal anticancer drug andrographolide (AD). The effectiveness of the drug is hampered by its low aqueous solubility (3.29 ± 0.73 and#956;g mL-1), and high lipophilicity having log P value = 2.632 ± 0.135, which result in poor bioavailability. newlineAD-SLNs were prepared by three different methods (Melting dispersion, solvent- emulsification evaporation and injection methods).The results demonstrated the successful preparation of AD-SLNs, using two lipids (cetyl alcohol and gelucire 50/13, seperately), tween 80 as an emulsifier and polyvinyl alcohol as a stabilizer. The solvent-injection method was optimized on the basis of smaller particle size and high entrapment efficiency. The formulation variables were optimized as 0.2% of concentration of stabilizer and surfactant in the ratios 1:10, v/v,aqueous: lipid phase as 25:1, v/v and drug: lipid ratio as 1:10 w/w.The AD-SLNs prepared by cetyl alcohol showed better Pharmacokinetic profile, as compared to AD-SLNs prepared by gelucire 50/13. In situ cell line studies exhibited the % cell inhibition at a newlineconcentration of 200 and#956;g mL-1 of AD and AD-SLNs at 72 h and the similar pattern of newlineinhibition was observed in all the cell lines, which include MCF-7, HT-29, Hep G2, SiHa, colo 320, A549 and Hela. Treatment with AD-SLNs decreased the tumor volume, tumor weight, and viable tumor cell and increased life span of the tumor-bearing mice. The SLNs prepared in our laboratory demonstrated characteristics that can be potentially utilized as an anticancer drug delivery system.