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载阿昔洛韦固体脂质纳米粒的处方工艺研究:设计、优化与评价。

Formulation of acyclovir-loaded solid lipid nanoparticles: design, optimization, and characterization.

机构信息

Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University , Tanta , Egypt.

出版信息

Pharm Dev Technol. 2019 Dec;24(10):1287-1298. doi: 10.1080/10837450.2019.1667385. Epub 2019 Sep 26.

Abstract

The goal of this study was to design, optimize, and characterize Acyclovir-loaded solid lipid nanoparticles (ACV-SLNs) concerning particle size, zeta potential, entrapment efficiency, and release profile. Full factorial design (2) was applied and the independent variables were surfactant type (Tween 80 and Pluronic F68), lipid type (Stearic acid and Compritol 888 ATO), and co-surfactant type (Lecithin and Sodium deoxycholate). The microemulsion technique was used followed by ultrasonication. The ACV-SLNs had a particle size range of about 172-542 nm. The polydispersity index (PDI) was found to be between 0.193 and 0.526. Zeta potential was in the range of -25.7 to -41.6 mV indicating good physical stability. Entrapment efficiency values were in the range of 56.3-80.7%. The drug release kinetics of the prepared formulations was best fitted to Higuchi diffusion model. After storing ACV-SLNs at refrigerated condition (5 ± 3 °C) and room temperature (25 ± 2 °C) for 4 weeks; we studied the change in the particle size, PDI, and zeta potential. The selected optimized formulation (F4) was containing Compritol, Pluronic F68, and Lecithin. These results indicated the successful application of this design to optimize the ACV-SLNs as a promising delivery system.

摘要

本研究旨在设计、优化并表征载阿昔洛韦固体脂质纳米粒(ACV-SLNs),考察其粒径、Zeta 电位、包封率和释放特性。采用全因子设计(2),考察表面活性剂种类(吐温 80 和泊洛沙姆 F68)、脂质种类(硬脂酸和 Compritol 888 ATO)和助表面活性剂种类(卵磷脂和脱氧胆酸钠)这 3 个自变量。采用微乳法,随后进行超声处理。ACV-SLNs 的粒径范围约为 172-542nm。多分散指数(PDI)在 0.193-0.526 之间。Zeta 电位在-25.7 到-41.6mV 之间,表明具有良好的物理稳定性。包封率在 56.3-80.7%之间。所制备的制剂的药物释放动力学最符合 Higuchi 扩散模型。在冷藏(5±3°C)和室温(25±2°C)条件下储存 ACV-SLNs 4 周后,研究了粒径、PDI 和 Zeta 电位的变化。选择优化后的配方(F4),其包含 Compritol、泊洛沙姆 F68 和卵磷脂。这些结果表明成功应用该设计优化了 ACV-SLNs,使其成为一种有前途的给药系统。

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