Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system

Dae Ro Lee,1 Myoung Jin Ho,1 Hyuck Jun Jung,1 Ha Ra Cho,1 Jun Seo Park,1 Suk-Hyun Yoon,2 Yong Seok Choi,1 Young Wook Choi,3 Chung-Hun Oh,2,4,5 Myung Joo Kang1 1College of Pharmacy, 2Department of Medical Laser, Graduate School, Dankook University, Dongnam-gu, Choenan, Chungnam, 3College of Pharmacy...

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Autores principales:	Lee DR, Ho MJ, Jung HJ, Cho HR, Park JS, Yoon SH, Choi YS, Choi YW, Oh CH, Kang MJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	tacrolimus supersaturation microemulsion dissolution oral bioavailability Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/931046107ced4481ab57bf9e6157135a
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spelling	oai:doaj.org-article:931046107ced4481ab57bf9e6157135a2021-12-02T05:10:41ZEnhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system1178-2013https://doaj.org/article/931046107ced4481ab57bf9e6157135a2016-03-01T00:00:00Zhttps://www.dovepress.com/enhanced-dissolution-and-oral-absorption-of-tacrolimus-by-supersaturab-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Dae Ro Lee,1 Myoung Jin Ho,1 Hyuck Jun Jung,1 Ha Ra Cho,1 Jun Seo Park,1 Suk-Hyun Yoon,2 Yong Seok Choi,1 Young Wook Choi,3 Chung-Hun Oh,2,4,5 Myung Joo Kang1 1College of Pharmacy, 2Department of Medical Laser, Graduate School, Dankook University, Dongnam-gu, Choenan, Chungnam, 3College of Pharmacy, Chung-Ang University, Dongjak-gu, Seoul, 4Department of Oral Physiology, College of Dentistry, Dankook University, 5Abel Medi-Tech Inc., Dongnam-gu, Cheonan, Chungnam, Korea Abstract: A new Soluplus (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer)-based supersaturable self-emulsifying drug delivery system (S-SEDDS) was formulated to enhance oral absorption of tacrolimus (FK506) with minimal use of oil, surfactant, and cosurfactant. A high payload supersaturable system (S-SEDDS) was prepared by incorporating Soluplus, as a precipitation inhibitor, to SEDDS consisting of Capmul MCM, Cremophor EL, and Transcutol (FK506:vehicle:Soluplus =1:15:1). In vitro dissolution profile and in vitro pharmacokinetic aspect of S-SEDDS in rats were comparatively evaluated with those of conventional SEDDS formulas containing four times greater content of vehicle components (FK506:vehicle =1:60). Both formulations formed spherical drug-loaded microemulsion <70 nm in size when in contact with aqueous medium. In an in vitro dissolution test in a nonsink condition, the amphiphilic polymer noticeably retarded drug precipitation and maintained >80% of accumulated dissolution rate for 24 hours, analogous to that from conventional SEDDS. Moreover, pharmacokinetic parameters of the maximum blood concentration and area under the curve from S-SEDDS formula in rats were not statistically different (P>0.05) than those of conventional SEDDS. The results suggest that the Soluplus-based supersaturable system can be an alternative to achieve a comparable in vitro dissolution profile and in vivo oral absorption with conventional SEDDS, with minimal use of vehicle ingredients. Keywords: tacrolimus, supersaturation, precipitation inhibitor, Soluplus, microemulsion, oral bioavailabilityLee DRHo MJJung HJCho HRPark JSYoon SHChoi YSChoi YWOh CHKang MJDove Medical Pressarticletacrolimussupersaturationmicroemulsiondissolutionoral bioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 1109-1117 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	tacrolimus supersaturation microemulsion dissolution oral bioavailability Medicine (General) R5-920
spellingShingle	tacrolimus supersaturation microemulsion dissolution oral bioavailability Medicine (General) R5-920 Lee DR Ho MJ Jung HJ Cho HR Park JS Yoon SH Choi YS Choi YW Oh CH Kang MJ Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
description	Dae Ro Lee,1 Myoung Jin Ho,1 Hyuck Jun Jung,1 Ha Ra Cho,1 Jun Seo Park,1 Suk-Hyun Yoon,2 Yong Seok Choi,1 Young Wook Choi,3 Chung-Hun Oh,2,4,5 Myung Joo Kang1 1College of Pharmacy, 2Department of Medical Laser, Graduate School, Dankook University, Dongnam-gu, Choenan, Chungnam, 3College of Pharmacy, Chung-Ang University, Dongjak-gu, Seoul, 4Department of Oral Physiology, College of Dentistry, Dankook University, 5Abel Medi-Tech Inc., Dongnam-gu, Cheonan, Chungnam, Korea Abstract: A new Soluplus (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer)-based supersaturable self-emulsifying drug delivery system (S-SEDDS) was formulated to enhance oral absorption of tacrolimus (FK506) with minimal use of oil, surfactant, and cosurfactant. A high payload supersaturable system (S-SEDDS) was prepared by incorporating Soluplus, as a precipitation inhibitor, to SEDDS consisting of Capmul MCM, Cremophor EL, and Transcutol (FK506:vehicle:Soluplus =1:15:1). In vitro dissolution profile and in vitro pharmacokinetic aspect of S-SEDDS in rats were comparatively evaluated with those of conventional SEDDS formulas containing four times greater content of vehicle components (FK506:vehicle =1:60). Both formulations formed spherical drug-loaded microemulsion <70 nm in size when in contact with aqueous medium. In an in vitro dissolution test in a nonsink condition, the amphiphilic polymer noticeably retarded drug precipitation and maintained >80% of accumulated dissolution rate for 24 hours, analogous to that from conventional SEDDS. Moreover, pharmacokinetic parameters of the maximum blood concentration and area under the curve from S-SEDDS formula in rats were not statistically different (P>0.05) than those of conventional SEDDS. The results suggest that the Soluplus-based supersaturable system can be an alternative to achieve a comparable in vitro dissolution profile and in vivo oral absorption with conventional SEDDS, with minimal use of vehicle ingredients. Keywords: tacrolimus, supersaturation, precipitation inhibitor, Soluplus, microemulsion, oral bioavailability
format	article
author	Lee DR Ho MJ Jung HJ Cho HR Park JS Yoon SH Choi YS Choi YW Oh CH Kang MJ
author_facet	Lee DR Ho MJ Jung HJ Cho HR Park JS Yoon SH Choi YS Choi YW Oh CH Kang MJ
author_sort	Lee DR
title	Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
title_short	Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
title_full	Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
title_fullStr	Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
title_full_unstemmed	Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
title_sort	enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/931046107ced4481ab57bf9e6157135a
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Enhanced dissolution and oral absorption of tacrolimus by supersaturable self-emulsifying drug delivery system

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