A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting

Lin Zhang1*, Weiwei Zhu2*, Chunfen Yang1, Hongxia Guo1, Aihua Yu1, Jianbo Ji3, Yan Gao1, Min Sun1, Guangxi Zhai11Department of Pharmaceutical Engineering, College of Pharmacy, Shandong University, Jinan; 2Department of Pharmacy, Yantai Yuhuangding Hospital, Yantai; 3Department of Pharmacology, Colle...

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Autores principales:	Zhang L, Zhu WW, Yang CF, Guo HX, Yu AH, Ji JB, Gao Y, Sun M, Zhai GX
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d3cf50054f704097b8b34c7704461ec6
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spelling	oai:doaj.org-article:d3cf50054f704097b8b34c7704461ec62021-12-02T11:07:29ZA novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting1176-91141178-2013https://doaj.org/article/d3cf50054f704097b8b34c7704461ec62012-01-01T00:00:00Zhttp://www.dovepress.com/a-novel-folate-modified-self-microemulsifying-drug-delivery-system-of--a9020https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Lin Zhang1, Weiwei Zhu2, Chunfen Yang1, Hongxia Guo1, Aihua Yu1, Jianbo Ji3, Yan Gao1, Min Sun1, Guangxi Zhai11Department of Pharmaceutical Engineering, College of Pharmacy, Shandong University, Jinan; 2Department of Pharmacy, Yantai Yuhuangding Hospital, Yantai; 3Department of Pharmacology, College of Pharmacy, Shandong University, Jinan, China*These authors contributed equally to the workBackground: The objective of this study was to prepare, characterize, and evaluate a folate-modified self-microemulsifying drug delivery system (FSMEDDS) with the aim to improve the solubility of curcumin and its delivery to the colon, facilitating endocytosis of FSMEDDS mediated by folate receptors on colon cancer cells.Methods: Ternary phase diagrams were constructed in order to obtain the most efficient self-emulsification region, and the formulation of curcumin-loaded SMEDDS was optimized by a simplex lattice experiment design. Then, three lipophilic folate derivatives (folate-polyethylene glycol-distearoylphosphatidylethanolamine, folate-polyethylene glycol-cholesteryl hemisuccinate, and folate-polyethylene glycol-cholesterol) used as a surfactant were added to curcumin-loaded SMEDDS formulations. An in situ colon perfusion method in rats was used to optimize the formulation of FSMEDDS. Curcumin-loaded FSMEDDS was then filled into colon-targeted capsules and the in vitro release was investigated. Cytotoxicity studies and cellular uptake studies was used in this research.Results: The optimal formulation of FSMEDDS obtained with the established in situ colon perfusion method in rats was comprised of 57.5% Cremophor&reg; EL, 32.5% Transcutol&reg; HP, 10% Capryol&trade; 90, and a small amount of folate-polyethylene glycol-cholesteryl hemisuccinate (the weight ratio of folate materials to Cremophor EL was 1:100). The in vitro release results indicated that the obtained formulation of curcumin could reach the colon efficiently and release the drug immediately. Cellular uptake studies analyzed with fluorescence microscopy and flow cytometry indicated that the FSMEDDS formulation could efficiently bind with the folate receptors on the surface of positive folate receptors cell lines. In addition, FSMEDDS showed greater cytotoxicity than SMEDDS in the above two cells.Conclusion: FSMEDDS-filled colon-targeted capsules are a potential carrier for colon delivery of curcumin.Keywords: curcumin, SMEDDS, folate receptor, colon targetingZhang LZhu WWYang CFGuo HXYu AHJi JBGao YSun MZhai GXDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 151-162 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhang L Zhu WW Yang CF Guo HX Yu AH Ji JB Gao Y Sun M Zhai GX A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
description	Lin Zhang1, Weiwei Zhu2, Chunfen Yang1, Hongxia Guo1, Aihua Yu1, Jianbo Ji3, Yan Gao1, Min Sun1, Guangxi Zhai11Department of Pharmaceutical Engineering, College of Pharmacy, Shandong University, Jinan; 2Department of Pharmacy, Yantai Yuhuangding Hospital, Yantai; 3Department of Pharmacology, College of Pharmacy, Shandong University, Jinan, China*These authors contributed equally to the workBackground: The objective of this study was to prepare, characterize, and evaluate a folate-modified self-microemulsifying drug delivery system (FSMEDDS) with the aim to improve the solubility of curcumin and its delivery to the colon, facilitating endocytosis of FSMEDDS mediated by folate receptors on colon cancer cells.Methods: Ternary phase diagrams were constructed in order to obtain the most efficient self-emulsification region, and the formulation of curcumin-loaded SMEDDS was optimized by a simplex lattice experiment design. Then, three lipophilic folate derivatives (folate-polyethylene glycol-distearoylphosphatidylethanolamine, folate-polyethylene glycol-cholesteryl hemisuccinate, and folate-polyethylene glycol-cholesterol) used as a surfactant were added to curcumin-loaded SMEDDS formulations. An in situ colon perfusion method in rats was used to optimize the formulation of FSMEDDS. Curcumin-loaded FSMEDDS was then filled into colon-targeted capsules and the in vitro release was investigated. Cytotoxicity studies and cellular uptake studies was used in this research.Results: The optimal formulation of FSMEDDS obtained with the established in situ colon perfusion method in rats was comprised of 57.5% Cremophor&reg; EL, 32.5% Transcutol&reg; HP, 10% Capryol&trade; 90, and a small amount of folate-polyethylene glycol-cholesteryl hemisuccinate (the weight ratio of folate materials to Cremophor EL was 1:100). The in vitro release results indicated that the obtained formulation of curcumin could reach the colon efficiently and release the drug immediately. Cellular uptake studies analyzed with fluorescence microscopy and flow cytometry indicated that the FSMEDDS formulation could efficiently bind with the folate receptors on the surface of positive folate receptors cell lines. In addition, FSMEDDS showed greater cytotoxicity than SMEDDS in the above two cells.Conclusion: FSMEDDS-filled colon-targeted capsules are a potential carrier for colon delivery of curcumin.Keywords: curcumin, SMEDDS, folate receptor, colon targeting
format	article
author	Zhang L Zhu WW Yang CF Guo HX Yu AH Ji JB Gao Y Sun M Zhai GX
author_facet	Zhang L Zhu WW Yang CF Guo HX Yu AH Ji JB Gao Y Sun M Zhai GX
author_sort	Zhang L
title	A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
title_short	A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
title_full	A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
title_fullStr	A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
title_full_unstemmed	A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
title_sort	novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/d3cf50054f704097b8b34c7704461ec6
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A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting

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