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首页> 美国卫生研究院文献>International Journal of Nanomedicine >Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design
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Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

机译：使用Box-Behnken设计开发和优化用于眼氯霉素递送的固体脂质纳米颗粒制剂

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The purpose of the present study was to optimize a solid lipid nanoparticle (SLN) of chloramphenicol by investigating the relationship between design factors and experimental data using response surface methodology. A Box-Behnken design was constructed using solid lipid (X1), surfactant (X2), and drug/lipid ratio (X3) level as independent factors. SLN was successfully prepared by a modified method of melt-emulsion ultrasonication and low temperature-solidification technique using glyceryl monostearate as the solid lipid, and poloxamer 188 as the surfactant. The dependent variables were entrapment efficiency (EE), drug loading (DL), and turbidity. Properties of SLN such as the morphology, particle size, zeta potential, EE, DL, and drug release behavior were investigated, respectively. As a result, the nanoparticle designed showed nearly spherical particles with a mean particle size of 248 nm. The polydispersity index of particle size was 0.277 ± 0.058 and zeta potential was −8.74 mV. The EE (%) and DL (%) could reach up to 83.29% ± 1.23% and 10.11% ± 2.02%, respectively. In vitro release studies showed a burst release at the initial stage followed by a prolonged release of chloramphenicol from SLN up to 48 hours. The release kinetics of the optimized formulation best fitted the Peppas–Korsmeyer model. These results indicated that the chloramphenicol-loaded SLN could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.
机译：本研究的目的是通过使用响应面方法研究设计因素与实验数据之间的关系来优化氯霉素的固体脂质纳米颗粒（SLN）。使用固体脂质（X1），表面活性剂（X2）和药物/脂质比率（X3）水平作为独立因素构建Box-Behnken设计。用单硬脂酸甘油酯作为固体脂质，泊洛沙姆188作为表面活性剂，通过改进的熔融乳液超声和低温固化技术，成功制备了SLN。因变量是包封率（EE），载药量（DL）和浊度。分别研究了SLN的性质，如形态，粒径，ζ电位，EE，DL和药物释放行为。结果，所设计的纳米颗粒显示出近球形的颗粒，其平均粒径为248nm。粒度的多分散指数为0.277±0.058，ζ电势为-8.74mV。 EE（％）和DL（％）分别可达83.29％±1.23％和10.11％±2.02％。体外释放研究表明，在初始阶段突然释放，随后氯霉素从SLN延长释放长达48小时。优化配方的释放动力学最适合Peppas-Korsmeyer模型。这些结果表明，装载氯霉素的SLN可以潜在地用作具有改善的药物截留效率和受控的药物释放的递送系统。

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