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Molecules 2015, 20(6), 9496-9509; doi:10.3390/molecules20069496

Enhanced Supersaturation and Oral Absorption of Sirolimus Using an Amorphous Solid Dispersion Based on Eudragit® E

1
College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea
2
College of Pharmacy, Pusan National University, Busan 609-735, Korea
3
College of Pharmacy, Kyungsung University, Busan 608-736, Korea
4
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 406-840, Korea
*
Authors to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian Löbmann
Received: 10 April 2015 / Accepted: 20 May 2015 / Published: 25 May 2015
(This article belongs to the Collection Poorly Soluble Drugs)
View Full-Text   |   Download PDF [2647 KB, uploaded 25 May 2015]   |  

Abstract

The present study aimed to investigate the effect of Eudragit® E/HCl (E-SD) on the degradation of sirolimus in simulated gastric fluid (pH 1.2) and to develop a new oral formulation of sirolimus using E-SD solid dispersions to enhance oral bioavailability. Sirolimus-loaded solid dispersions were fabricated by a spray drying process. A kinetic solubility test demonstrated that the sirolimus/E-SD/TPGS (1/8/1) solid dispersion had a maximum solubility of 196.7 μg/mL within 0.5 h that gradually decreased to 173.4 μg/mL after 12 h. According to the dissolution study, the most suitable formulation was the sirolimus/E-SD/TPGS (1/8/1) solid dispersion in simulated gastric fluid (pH 1.2), owing to enhanced stability and degree of supersaturation of E-SD and TPGS. Furthermore, pharmacokinetic studies in rats indicated that compared to the physical mixture and sirolimus/HPMC/TPGS (1/8/1) solid dispersion, the sirolimus/E-SD/TPGS (1/8/1) solid dispersion significantly improved oral absorption of sirolimus. E-SD significantly inhibited the degradation of sirolimus in a dose-dependent manner. E-SD also significantly inhibited the precipitation of sirolimus compared to hydroxypropylmethyl cellulose (HPMC). Therefore, the results from the present study suggest that the sirolimus-loaded E-SD/TPGS solid dispersion has great potential in clinical applications. View Full-Text
Keywords: sirolimus; supersaturation; bioavailability; Eudragit® E; solid dispersion sirolimus; supersaturation; bioavailability; Eudragit® E; solid dispersion
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Cho, Y.; Ha, E.-S.; Baek, I.-H.; Kim, M.-S.; Cho, C.-W.; Hwang, S.-J. Enhanced Supersaturation and Oral Absorption of Sirolimus Using an Amorphous Solid Dispersion Based on Eudragit® E. Molecules 2015, 20, 9496-9509.

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