Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery

Dawei Gao, Shengnan Tang, Qi TongApplied Chemical Key Laboratory of Hebei Province, College of Environmental and Chemical Engineering, Yanshan University, Qinhuangdao, ChinaBackground: Oleanolic acid is a pentacyclic triterpene present in many fruits and vegetables, and has received much attention o...

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Autores principales:	Gao D, Tang S, Tong Q
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/122234888f5140aeb179288a285ce3d9
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spelling	oai:doaj.org-article:122234888f5140aeb179288a285ce3d92021-12-02T07:28:32ZOleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery1176-91141178-2013https://doaj.org/article/122234888f5140aeb179288a285ce3d92012-07-01T00:00:00Zhttp://www.dovepress.com/oleanolic-acid-liposomes-with-polyethylene-glycol-modification-promisi-a10326https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Dawei Gao, Shengnan Tang, Qi TongApplied Chemical Key Laboratory of Hebei Province, College of Environmental and Chemical Engineering, Yanshan University, Qinhuangdao, ChinaBackground: Oleanolic acid is a pentacyclic triterpene present in many fruits and vegetables, and has received much attention on account of its biological properties. However, its poor solubility and low bioavailability limit its use. The objective of this study was to encapsulate oleanolic acid into nanoliposomes using the modified ethanol injection method.Methods: The liposomes contain a hydrophobic oleanolic acid core, an amphiphilic soybean lecithin monolayer, and a protective hydrophilic polyethylene glycol (PEG) coating. During the preparation process, the formulations described were investigated by designing 34 orthogonal experiments as well as considering the effects of different physical characteristics. The four factors were the ratios of drug to soybean phosphatidylcholine (w/w), cholesterol (w/w), PEG-2000 (w/w), and temperature of phosphate-buffered saline at three different levels. We identified the optimized formulation which showed the most satisfactory lipid stability and particle formation. The morphology of the liposomes obtained was determined by transmission electron microscopy and atomic force microscopy. The existence of PEG in the liposome component was validated by Fourier transform infrared spectrum analysis.Results: The PEGylated liposomes dispersed individually and had diameters of around 110&ndash;200 nm. Encapsulation efficiency was more than 85%, as calculated by high-performance liquid chromatography and Sephadex&reg; gel filtration. Furthermore, when compared with native oleanolic acid, the liposomal formulations showed better stability in vitro. Finally, the cytotoxicity of the oleanolic acid liposomes was evaluated using a microtiter tetrazolium assay.Conclusion: These results suggest that PEGylated liposomes would serve as a potent delivery vehicle for oleanolic acid in future cancer therapy.Keywords: oleanolic acid, liposomes, ethanol injection, polyethylene glycolGao DTang STong QDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 3517-3526 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Gao D Tang S Tong Q Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
description	Dawei Gao, Shengnan Tang, Qi TongApplied Chemical Key Laboratory of Hebei Province, College of Environmental and Chemical Engineering, Yanshan University, Qinhuangdao, ChinaBackground: Oleanolic acid is a pentacyclic triterpene present in many fruits and vegetables, and has received much attention on account of its biological properties. However, its poor solubility and low bioavailability limit its use. The objective of this study was to encapsulate oleanolic acid into nanoliposomes using the modified ethanol injection method.Methods: The liposomes contain a hydrophobic oleanolic acid core, an amphiphilic soybean lecithin monolayer, and a protective hydrophilic polyethylene glycol (PEG) coating. During the preparation process, the formulations described were investigated by designing 34 orthogonal experiments as well as considering the effects of different physical characteristics. The four factors were the ratios of drug to soybean phosphatidylcholine (w/w), cholesterol (w/w), PEG-2000 (w/w), and temperature of phosphate-buffered saline at three different levels. We identified the optimized formulation which showed the most satisfactory lipid stability and particle formation. The morphology of the liposomes obtained was determined by transmission electron microscopy and atomic force microscopy. The existence of PEG in the liposome component was validated by Fourier transform infrared spectrum analysis.Results: The PEGylated liposomes dispersed individually and had diameters of around 110&ndash;200 nm. Encapsulation efficiency was more than 85%, as calculated by high-performance liquid chromatography and Sephadex&reg; gel filtration. Furthermore, when compared with native oleanolic acid, the liposomal formulations showed better stability in vitro. Finally, the cytotoxicity of the oleanolic acid liposomes was evaluated using a microtiter tetrazolium assay.Conclusion: These results suggest that PEGylated liposomes would serve as a potent delivery vehicle for oleanolic acid in future cancer therapy.Keywords: oleanolic acid, liposomes, ethanol injection, polyethylene glycol
format	article
author	Gao D Tang S Tong Q
author_facet	Gao D Tang S Tong Q
author_sort	Gao D
title	Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
title_short	Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
title_full	Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
title_fullStr	Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
title_full_unstemmed	Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
title_sort	oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/122234888f5140aeb179288a285ce3d9
work_keys_str_mv	AT gaod oleanolicacidliposomeswithpolyethyleneglycolmodificationpromisingantitumordrugdelivery AT tangs oleanolicacidliposomeswithpolyethyleneglycolmodificationpromisingantitumordrugdelivery AT tongq oleanolicacidliposomeswithpolyethyleneglycolmodificationpromisingantitumordrugdelivery
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Oleanolic acid liposomes with polyethylene glycol modification: promising antitumor drug delivery

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