Lipid nanoparticles with different oil/fatty ester ratios as carriers of buprenorphine and its prodrugs for injection

doi:10.1016/j.ejps.2009.06.008

CNU IR > Pharmacy and Science > Dept. of Pharmacy > Periodical Articles > Item 310902800/23304

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题名:	Lipid nanoparticles with different oil/fatty ester ratios as carriers of buprenorphine and its prodrugs for injection
作者:	Jhi-Joung Wang Kuo-Sheng Liu K.C. Sung Chia-Yin Tsai Jia-You Fang
贡献者:	藥物科技研究所
关键词:	Buprenorphine Prodrug Lipid nanoparticles Solid lipid nanoparticles Nanostructured lipid carriers Injection
日期:	2009-09
上传时间:	2010-12-29 14:19:41 (UTC+8)
出版者:	Elsevier
摘要:	Buprenorphine is a promising drug for the treatment of chronic pain and opioid dependence. The aim of the present work was to evaluate the feasibility of lipid nanoparticles with different oil/fatty ester ratios for injection of buprenorphine. To improve the release properties and analgesic duration of the drug, ester prodrugs were also incorporated into the nanoparticles for evaluation. Linseed oil and cetyl palmitate were respectively chosen as the liquid lipid and solid lipid in the inner phase of the nanoparticulate systems. Differential scanning calorimetry (DSC) was performed, and the particle size, zeta potential, molecular environment, and lipid/water partitioning were determined to characterize the state of the drug/prodrug and lipid modification. The in vitro release kinetics were measured by a Franz assembly. DSC showed that systems without oil (solid lipid nanoparticles, SLNs) had a more ordered crystalline lattice in the inner matrix compared to those with oil (nanostructured lipid carriers, NLCs and lipid emulsion, LE). The mean diameter of the nanoparticles ranged between 180 and 200 nm. The in vitro drug/prodrug release occurred in a delayed manner in decreasing order as follows: SLN > NLC > LE. It was found that the release rate was reduced following an increase in alkyl ester chains in the prodrugs. The in vivo antinociception was examined by a cold ethanol tail-flick test in rats. Compared to an aqueous solution, a prolonged analgesic duration was detected after an intravenous injection of buprenorphine-loaded SLNs and buprenorphine propionate (Bu-C3)-loaded NLCs (with 10% linseed oil in the lipid phase). The Bu-C3 in NLCs even showed a maximum antinociceptive activity for 10 h. In vitro erythrocyte hemolysis and lactate dehydrogenase (LDH) release from neutrophils demonstrated a negligible toxicity of these carriers. Our results indicate the feasibility of using lipid nanoparticles, especially SLNs and NLCs, as parenteral delivery systems for buprenorphine and its prodrugs.
關聯:	European Journal of Pharmaceutical Sciences 38(2)：p.138-146
显示于类别:	[Dept. of Pharmacy] Periodical Articles

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