Effect of PEG2000 on drug delivery characterization from solid lipid nanoparticles.
Effect of PEG2000 on drug delivery characterization from solid lipid nanoparticles.
复制标题
PEG2000 对固体脂质纳米颗粒药物递送特性的影响。
DOI：
10.1002/jps.20550
复制
发表时间：
2006
期刊：
影响因子：
--
通讯作者：
H. Yuan
中科院分区：
文献类型：
--
作者：
Yun Hong;Fuqiang Hu;H. Yuan
本研究的目的是开发一种PEG 2000修饰的固体脂质纳米粒（SLN），并研究其特性。本文采用一种新型的溶剂扩散法在水溶液中制备了载药SLN。分别以单硬脂酸甘油酯和PEG 2000为载体材料和改性剂。以硫酸沙丁胺醇为模型药物，考察了包封率、粒径、Zeta电位（电荷）和释药特性。在pH7.2的磷酸盐缓冲液中，SLN混悬液的释药行为呈双相模式。对于基于单硬脂酸甘油酯的SLN，在前8小时的药物突释后，观察到在14天的监测期内明显延长的释放。在监测的延长释放期内，前5天存在延迟释放，每天释放近2.51%的药物，随后在最后9天出现略高的释放率（每天8.14%）。相比之下，PEG 2000修饰的SLN的药物释放速率更快。然而，需要进一步的工作，以优化各种包埋药物的释放行为。这些结果还表明，用PEG 2000修饰可以加速亲水性小分子药物从SLN中释放。
The purpose of this work is to develop a PEG2000-modified solid lipid nanoparticles (SLN) intended to encapsulate a drug within their matrix and to study their characteristics. In the present report, drug-loaded SLN were prepared by a novel solvent diffusion method in an aqueous system. Monostearin and PEG2000 were used as carrier material and modifying agent, respectively. The model drug salbutamol sulphate was incorporated to study the characterization of entrapment efficiency, size, zeta potential (charge) and drug delivery characterization. In the test solution of pH 7.2 phosphate buffer, drug-release behavior from SLN suspension exhibited a biphasic pattern. With the monoastearin-based SLN, a distinctly prolonged release over a monitored period of 14 days was observed after a burst drug release in the first 8 hours. Over the monitored period of prolonged release, there was delayed release in the first 5 days with nearly 2.51% of the drug released each day, following which a slightly higher release rate (8.14% per day) appeared in the last 9 days. In contrast, the drug release rate from PEG2000-modified SLN was faster. Nevertheless, further work is required in order to optimize the release behavior of various entrapped drugs. These results also demonstrate that modification with PEG2000 can accelerate release of hydrophilic small molecule drugs from SLN.