Skin permeation of buprenorphine and its ester prodrugs from lipid nanoparticles lipid emulsion, nanostructured lipid carriers and solid lipid nanoparticles

doi:10.3109/02652040902746679

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 藥學系(所) > 期刊論文 > Item 310902800/23305

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標題:	Skin permeation of buprenorphine and its ester prodrugs from lipid nanoparticles lipid emulsion, nanostructured lipid carriers and solid lipid nanoparticles
作者:	Jhi-Joung Wang Kuo-Sheng Liu K. C. Sung Chia-Yin Tsai Jia-You Fang
貢獻者:	藥物科技研究所
關鍵字:	Buprenorphine ester prodrug skin permeation lipid emulsion nanostructured lipid carriers solid lipid nanoparticles
日期:	2009-02
上傳時間:	2010-12-29 14:19:42 (UTC+8)
摘要:	The aim of this study was to develop and characterize lipid nanoparticle systems for the transdermal delivery of buprenorphine and its prodrugs. A panel of three buprenorphine prodrugs with ester chains of various lengths was synthesized and characterized by solubility, capacity factor (log K'), partitioning between lipids and water and the ability to penetrate nude mouse skin. Colloidal systems made of squalene (lipid emulsion, LE), squalene + Precirol (nanostructured lipid carriers, NLC) and Precirol (solid lipid nanoparticles, SLN) as the lipid core material were prepared. Differential scanning calorimetry showed that the SLN had a more-ordered crystalline lattice in the inner matrix compared to the NLC. The particle size ranged from 220-300 nm, with NLC showing the smallest size. All prodrugs were highly lipophilic and chemically stable, but enzymatically unstable in skin homogenate and plasma. The in vitro permeation results exhibited a lower skin delivery of drug/prodrug with an increase in the alkyl chain length. SLN produced the highest drug/prodrug permeation, followed by the NLC and LE. A small inter-subject variation was also observed with SLN carriers. SLN with soybean phosphatidylcholine (SLN-PC) as the lipophilic emulsifier showed a higher drug/prodrug delivery across the skin compared to SLN with Myverol, a palmitinic acid monoglyceride. The in vitro permeation of the prodrugs occurred in a sustained manner for SLN-PC. The skin permeation of buprenorphine could be adjusted within a wide range by combining a prodrug strategy and lipid nanoparticles.
關聯:	Journal of Microencapsulation 26(8)：p.734-747
显示于类别:	[藥學系(所)] 期刊論文

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