Exploring the potential of porous silicas as a carrier system for dissolution rate enhancement of artemether.

Abstract

Malaria is a parasitic and vector determined blood-conceived infectious disease transmitted through infected mosquitoes. Anti-malarial drug resistance is a major health problem, which hinders the control of malaria. Drug-resistant malaria when surveyed, the results demonstrated safe proclivity to nearby all anti-malarial regimes accessible except from artemisinin and its derivatives. Artemether is a BCS class IV drug effective against acute and severe falciparum malaria hence; there is a strong need to improve its solubility. Silica is one of the most widely studied excipient.

Silica can be used in solubility enhancement by preparing its solid solution/dispersion with the drug. The objective of this research was to improve dissolution rate of Artemether using non-precipitated porous silica (Aeroperl® 300 Pharma) and precipitated silica like (EXP.9555, EXP.9560, and EXP. 9565). Specific surface area calculated from BET method of porous silicas viz. APL 300 (A), Exp. 9555 (B), Exp. 9560 (C), Exp. 9565 (D). was found to be 294.13 m2/g (A), 256.02 m2/g (B), 213.62 m2/g (C) and 207.22 m2/g respectively.The drug release from the developed formulation was found to be significantly higher as compared to neat ARM. This improved solubility and release kinetics of ARM may be attributed to high surface area, improved wettability and decreased crystallinity.

Solid-state characterization of the developed optimized formulation F3 was carried out with respect to FTIR chemical imaging, XRD, SEM, and DSC. All the porous silicas which we have explored in present context, showed a significant capability as a carrier for solubility enhancement of ARM.