The objective of this study was to develop an oral formulation that would improve the solubility and oral absorption of sirolimus using a TPGS micellar solution. The effect of TPGS on the solubility and stability of sirolimus was evaluated. The sirolimus-loaded TPGS micelles were prepared using the thin-film hydration method. The average size of the sirolimus-loaded TPGS micelles was 11 nm. The concentration of sirolimus in a 50 mg/mL TPGS micellar solution was 0.97 ± 0.12 mg/mL, which demonstrates an enhancement of approximately 400-fold from the solubility of sirolimus in water. Furthermore, pharmacokinetic studies in rats indicated that the TPGS micellar solution significantly improved the oral absorption of sirolimus. Therefore, the preliminary results from this study suggest that a TPGS micellar solution has great potential for clinical applications.
Bibliographical noteFunding Information:
This work was supported by the Priority Research Centers Program of the National Research Foundation of Korea (NRF), which is funded by the Ministry of Education, Science and Technology (2009-0093815), and by a grant from the Korea Healthcare Technology R&D Project of the Ministry for Health, Welfare and Family Affairs in the Republic of Korea (A080470).
All Science Journal Classification (ASJC) codes
- Medicine (miscellaneous)
- Biomedical Engineering
- Pharmaceutical Science