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壳聚糖修饰的非那雄胺固体脂质纳米粒的理化性质及其经皮给药研究。

Physicochemical Characterization of Chitosan-Decorated Finasteride Solid Lipid Nanoparticles for Skin Drug Delivery.

机构信息

SRDDR, GCPS, Faculty of Pharmacy, Gomal University, D.I. Khan, Pakistan.

Faculty of Pharmacy, Gomal University, D.I. Khan, Pakistan.

出版信息

Biomed Res Int. 2022 Aug 6;2022:7792180. doi: 10.1155/2022/7792180. eCollection 2022.

Abstract

Finasteride is considered the drug of choice for androgenic alopecia and benign prostate hyperplasia. The aim of the study was to formulate nanodrug carriers of finasteride with enhanced retentive properties in the skin. The finasteride was formulated as solid lipid nanoparticles that were decorated with different concentrations of chitosan for improved retentive properties. Solid lipid nanoparticles (SLNs) were synthesized by "high-speed homogenization technique" using stearic acid as a solid lipid while PEG-6000 and Tween-80 were used as surfactants. The SLNs were evaluated for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, and drug release behavior. The mean particle size of SLNs was in the range of 10.10 nm to 144.2 nm. The PDI ranged from 0.244 to 0.412 while zeta potential was in the range of 8.9 mV to 62.6 mV. The drug entrapment efficiency in chitosan undecorated formulations was 48.3% while an increase in drug entrapment was observed in chitosan-decorated formulations (51.1% to 62%). The drug release studies of SLNs showed an extended drug release for 24 hours after 4 hours of initial burst release. The extended drug release was observed in chitosan-coated SLNs in comparison with uncoated nanoparticles. The permeation and retention study revealed higher retention of drug in the skin and low permeation with chitosan-decorated SLNs that ranged from 39.4 g/cm to 13.2 g/cm. TEM images depicted spherical shape of SLNs. The stability study confirmed stable formulations in temperature range of 5°C and 40°C for three months. It is concluded from this study that the SLNs of finasteride were successfully formulated and chitosan decoration enhanced the drug retention in the skin layers. Therefore, these formulations could be used in androgenic alopecia and benign prostate hyperplasia to avoid the side effects, drug degradation, and prolonged use of drug with conventional oral therapy.

摘要

非那雄胺被认为是治疗雄激素性脱发和良性前列腺增生的首选药物。本研究旨在制备具有增强皮肤滞留性能的非那雄胺纳米药物载体。将非那雄胺制成固体脂质纳米粒,并用不同浓度的壳聚糖进行修饰,以提高其滞留性能。固体脂质纳米粒(SLN)是通过“高速匀化技术”用硬脂酸作为固体脂质,聚乙二醇 6000 和吐温 80 作为表面活性剂合成的。对 SLN 的粒径、多分散指数(PDI)、Zeta 电位、药物包封效率和药物释放行为进行了评价。SLN 的平均粒径在 10.10nm 到 144.2nm 之间。PDI 范围为 0.244 至 0.412,Zeta 电位范围为 8.9mV 至 62.6mV。壳聚糖未修饰制剂的药物包封效率为 48.3%,而壳聚糖修饰制剂的药物包封效率则有所提高(51.1%至 62%)。SLN 的药物释放研究表明,在初始突释释放后 4 小时,药物可延长 24 小时释放。与未包被的纳米粒相比,壳聚糖包被的 SLN 显示出更长的药物释放。渗透和滞留研究表明,用壳聚糖修饰的 SLN 可使药物在皮肤中的滞留量增加,而渗透量减少,范围为 39.4μg/cm 至 13.2μg/cm。TEM 图像显示 SLN 呈球形。稳定性研究证实,在 5°C 和 40°C 的温度范围内,制剂在三个月内稳定。综上所述,成功制备了非那雄胺 SLN,壳聚糖修饰增强了药物在皮肤层的滞留。因此,这些制剂可用于治疗雄激素性脱发和良性前列腺增生,以避免常规口服治疗的副作用、药物降解和延长药物使用时间。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/980b/9375701/09953d7be9e9/BMRI2022-7792180.001.jpg

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