In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

You-Meei Lin1, Jui-Yu Wu2, Ying-Chen Chen3, Yu-Der Su3, Wen-Tin Ke3, Hsiu-O Ho31Department of Pharmacy, Shuang Ho Hospital, 2Department of Biochemistry, School of Medicine, 3School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROCObjectives: In situ formation of nanocr...

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Autores principales:	Lin YM, Wu JU, Chen YC, Su YD, Ke WT, Ho HO, Sheu MT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/9719d0abdf584daea68691c30136875e
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spelling	oai:doaj.org-article:9719d0abdf584daea68691c30136875e2021-12-02T00:40:26ZIn situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate1176-91141178-2013https://doaj.org/article/9719d0abdf584daea68691c30136875e2011-10-01T00:00:00Zhttp://www.dovepress.com/in-situ-formation-of-nanocrystals-from-a-self-microemulsifying-drug-de-a8495https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013You-Meei Lin1, Jui-Yu Wu2, Ying-Chen Chen3, Yu-Der Su3, Wen-Tin Ke3, Hsiu-O Ho31Department of Pharmacy, Shuang Ho Hospital, 2Department of Biochemistry, School of Medicine, 3School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROCObjectives: In situ formation of nanocrystals and dissolution profiles of fenofibrate (FFB) from a self-microemulsifying drug delivery system (SMEDDS) were characterized.Methods: SMEDDS formulated with Myritol&reg; and surfactant mixture (Smix) of D-&alpha;-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and either Tween&reg; 20 (A, C, E, G, M, S, N, T, O) or Tween&reg; 80 (B, D, F, H, P, U, Q, V, R) at various oil/Smix ratios (Group I: A and B of 0.42, C and D of 0.25, E and F of 0.11; Group II: G and H of 1.38, M and P of 1.11, S and U of 0.9, N and Q of 0.73, T and V of 0.58, and O and R of 0.46) and water contents (1: 9.5%, 2: 5.0%, 3: 0.0%, G-V: 4.5%). Their dissolutions were conducted at different rotation speeds. Two optimal SMEDDSs containing Tween 80(B2) or a higher oil/Smix ratio(Q) and B2(solution) were selected for pharmacokinetic study.Results: FFB particles formed within the nanosize range from Group I gradually increased with time but decreased with increasing stirring rates. However, the mean size of FFB formed by B series was as low as 200 nm, which was smaller than that of A series at three stirring rates. The release rate from both groups obviously increased with increasing stirring rate. However, incomplete release was observed for S and N in Tween 20 series, whereas a faster release rate and complete release were observed for Tween 80 series with an insignificant difference among them. Results of pharmacokinetic study demonstrated that the highest-ranked area under the curve and Cmax values were for Q(SMEDDS) and B2(solution), respectively. The relative bioavailability of Q(SMEDDS) with respect to Tricor&reg; was enhanced by about 1.14-1.22-fold.Conclusion: SMEDDS, consisting of Myritol 318 and TPGS combined with Tween 80 at 4:1, was able to enhance the oral bioavailability of FFB.Keywords: SMEDDS, fenofibrate, microemulsion, dissolution, TPGSLin YMWu JUChen YCSu YDKe WTHo HOSheu MTDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 2445-2457 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lin YM Wu JU Chen YC Su YD Ke WT Ho HO Sheu MT In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
description	You-Meei Lin1, Jui-Yu Wu2, Ying-Chen Chen3, Yu-Der Su3, Wen-Tin Ke3, Hsiu-O Ho31Department of Pharmacy, Shuang Ho Hospital, 2Department of Biochemistry, School of Medicine, 3School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROCObjectives: In situ formation of nanocrystals and dissolution profiles of fenofibrate (FFB) from a self-microemulsifying drug delivery system (SMEDDS) were characterized.Methods: SMEDDS formulated with Myritol&reg; and surfactant mixture (Smix) of D-&alpha;-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and either Tween&reg; 20 (A, C, E, G, M, S, N, T, O) or Tween&reg; 80 (B, D, F, H, P, U, Q, V, R) at various oil/Smix ratios (Group I: A and B of 0.42, C and D of 0.25, E and F of 0.11; Group II: G and H of 1.38, M and P of 1.11, S and U of 0.9, N and Q of 0.73, T and V of 0.58, and O and R of 0.46) and water contents (1: 9.5%, 2: 5.0%, 3: 0.0%, G-V: 4.5%). Their dissolutions were conducted at different rotation speeds. Two optimal SMEDDSs containing Tween 80(B2) or a higher oil/Smix ratio(Q) and B2(solution) were selected for pharmacokinetic study.Results: FFB particles formed within the nanosize range from Group I gradually increased with time but decreased with increasing stirring rates. However, the mean size of FFB formed by B series was as low as 200 nm, which was smaller than that of A series at three stirring rates. The release rate from both groups obviously increased with increasing stirring rate. However, incomplete release was observed for S and N in Tween 20 series, whereas a faster release rate and complete release were observed for Tween 80 series with an insignificant difference among them. Results of pharmacokinetic study demonstrated that the highest-ranked area under the curve and Cmax values were for Q(SMEDDS) and B2(solution), respectively. The relative bioavailability of Q(SMEDDS) with respect to Tricor&reg; was enhanced by about 1.14-1.22-fold.Conclusion: SMEDDS, consisting of Myritol 318 and TPGS combined with Tween 80 at 4:1, was able to enhance the oral bioavailability of FFB.Keywords: SMEDDS, fenofibrate, microemulsion, dissolution, TPGS
format	article
author	Lin YM Wu JU Chen YC Su YD Ke WT Ho HO Sheu MT
author_facet	Lin YM Wu JU Chen YC Su YD Ke WT Ho HO Sheu MT
author_sort	Lin YM
title	In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
title_short	In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
title_full	In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
title_fullStr	In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
title_full_unstemmed	In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
title_sort	in situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/9719d0abdf584daea68691c30136875e
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In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

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