In vitro and in vivo evaluation of poly (acrylic acid) modified mesoporous silica nanoparticles as pH response carrier for β-elemene self-micro emulsifying.

Abstract

The strategy of formulating poorly soluble actives as liquid self-micro emulsifying drug delivery system (SMEDDS) has been explored in more than a thousand research papers. However, there have been a limited number of reports on pH sensitive solid SMEDDS. This study explored the feasibility of using poly (acrylic acid) modified mesoporous silica nanoparticles (MSNs-PAA) as a pH-mediated solid SMEDDS carrier for β-elemene. This SMEDDS was optimized using a central composite design-response surface methodology, pseudo ternary phase diagrams, and studies of the preliminary stability. MSNs-PAA was synthesized and used for loading β-elemene SMEDDS. Ele/MSNs-PAA was capable of pH-sensitive release of β-elemene. In addition to structural analyses, the morphological and stability of this SMEDDS was also investigated. In comparison of the β-elemene solution and the SMEDDS, the Ele/MSNs-PAA demonstrated improved Cmax, AUC and MRT after oral administration. These results suggested that the MSNs-PAA could be further developed as a promising approach for the pH sensitive release of β-elemene SMEDDS with enhanced oral bioavailability.