Abstract:

The purpose of the study is to perform pre-formulation studies for alpha-mangostin (α-mangostin) and screening of additives (such as solid lipids, emulsifiers and cryoprotectants) and their combinations (ratio of lipids, ratio of drug: lipid, ratio of emulsifier: co-emulsifier and concentration of cryoprotectant) used in the formulation of solid lipid nanoparticles of α-mangostin. This screening is essential for the formulation of solid lipid nanoparticles (SLNP) that provide small particle size and PDI, high entrapment efficiency and zeta potential. This screening offers a rationale for selecting additives and their concentrations for formulating optimized SLNP. Preformulation studies showed melting point of 181.5°C, partition coefficient of 0.359 and drug solubility of 0.3072, 0.4576, 0.4892 and 0.5782 mg/mL in 1.2, 6.8, 7.0 and 7.5 pH buffers respectively. Ultimately, the DSC thermogram defines the sharp endotherm of α-mangostin at 195.98°C. Hot melt homogenization followed by ultrasonication technique is used to develop solid lipid nanoparticles. Process parameters such as homogenization speed (15,000 rpm) and ultra sonication (6 minutes) was optimized based on particle size and PDI. The optimized formulation of SLNP of α-mangostin contain 1:2:0.5:0.5:5 ratio of Drug: Solid lipid (0.8:1.2 ratio of Stearic acid: Precriol ATO5): Poloxamer 407: Sodium taurocholate: Mannitol.

Keywords: