Journal
ARTIFICIAL CELLS NANOMEDICINE AND BIOTECHNOLOGY
Volume 41, Issue 2, Pages 85-91Publisher
INFORMA HEALTHCARE
DOI: 10.3109/21691401.2012.742100
Keywords
Bioavailability; micelle; sirolimus; stability; TPGS
Categories
Funding
- Priority Research Centers Program of the National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2009-0093815]
- Korea Healthcare Technology R&D Project of the Ministry for Health, Welfare and Family Affairs in the Republic of Korea [A080470]
- Korea Health Promotion Institute [A080470] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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.
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