PEGylated Liposomes Incorporated with Nonionic Surfactants as an Apomorphine Delivery System Targeting the Brain: In Vitro Release and In Vivo Real-time Imaging

doi:10.2174/157341311794653686

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 藥學系(所) > 期刊論文 > Item 310902800/27072

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標題:	PEGylated Liposomes Incorporated with Nonionic Surfactants as an Apomorphine Delivery System Targeting the Brain: In Vitro Release and In Vivo Real-time Imaging
作者:	Hsu, Shu-Hui Saleh, A.Al-Suwayeh Chen, Chih-Chieh Chi, Chen-Hsien Fang, Jia-You
貢獻者:	藥學系
關鍵字:	Apomorphine PEGylated liposomes blood-brain barrier brain targeting drug delivery systems Nonionic Surfactants Real-time Imaging Parkinson's disease
日期:	2011-04
上傳時間:	2013-10-25 15:33:48 (UTC+8)
出版者:	Bentham Science Publ Ltd
摘要:	The clinical application of apomorphine, a dopamine receptor agonist for treating Parkinsons disease, is limited by its instability and the need for frequent injections. In the present work, apomorphine was encapsulated within liposomes to protect it from degradation and enhance the permeability across the blood-brain barrier (BBB). Stearylamine was used to produce a positive surface charge for the liposomes. The liposomal systems with different compositions were characterized by the mean size, zeta potential, drug encapsulation percentage, stability, and in vitro release characteristics. PEGylated liposomes and liposomes incorporating Brij 78 showed a size of 130~160 nm. When Tween 80 was added to the liposomes, the vesicle size increased to > 260 nm. Apomorphine was successfully entrapped by liposomes with an encapsulation percentage of > 70%, with the systems containing Brij 78 showing the highest level of 99%. The loading of apomorphine into liposomes resulted in slower release behavior compared to the drug in an aqueous solution. In comparison to free drug, apomorphine in PEGylated liposomes exhibited greater stability in plasma. The in vivo brain uptake of PEGylated liposomes after an intravenous bolus injection into rats was monitored by in vivo real-time bioluminescence imaging for 1 h. The results showed that the uptake of PEGylated liposomes into the brain was rapid and prolonged. PEGylated liposomes may offer a promising strategy for targeting apomorphine to the brain. This opens up new opportunities for treating Parkinsons disease.
關聯:	Current Nanoscience, 7(2), pp.191-199
显示于类别:	[藥學系(所)] 期刊論文

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