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制剂设计和冷冻干燥对非那雄胺纳米系统理化特性的影响。

Impact of formulation design and lyophilisation on the physicochemical characteristics of finasteride nanosystems.

机构信息

Gomal Centre of Pharmaceutical Sciences (GCPS), Faculty of Pharmacy, Gomal University, Dera Ismail Khan, Pakistan.

Faculty of Pharmacy, Universite de Strasbourg, Illkirch, Strasbourg, France.

出版信息

J Microencapsul. 2023 Mar;40(2):106-123. doi: 10.1080/02652048.2023.2178537. Epub 2023 Feb 24.

DOI:10.1080/02652048.2023.2178537
PMID:36749573
Abstract

The fundamental purpose of this study was to develop a stable lyophilised finasteride nanosystem (FNS-NS) for topical delivery. The FNS-NS was fabricated using an ultrasonication technique. The impact of two different cryoprotectants on the physicochemical characteristics of FNS-NS before and after lyophilisation was thoroughly investigated. The lyophilised FNS-NS had spherical shape with particle size lied between 188.6 nm ± 4.4 and 298.7 nm ± 4.7, low PDI values (0.26 ± 0.02 to 0.32 ± 0.02) and zeta potential ranging from -38.3 to +53.3 mV. The confocal laser microscopy depicted a comparatively higher cellular internalisation achieved for undecorated FNS-NS with respect to its chitosan-decorated counterpart. The lyophilised FNS-NS was stable for 90 days at proper storage conditions. The FNS-NS with 15% trehalose had appropriate physicochemical attributes that could be a promising carrier for topical delivery to treat androgenic alopecia.

摘要

本研究的根本目的是开发一种用于局部递药的稳定的冻干非那雄胺纳米系统(FNS-NS)。FNS-NS 是使用超声技术制备的。深入研究了两种不同的冷冻保护剂对冻干前后 FNS-NS 的物理化学特性的影响。冻干的 FNS-NS 呈球形,粒径在 188.6nm±4.4 到 298.7nm±4.7 之间,PDI 值较低(0.26±0.02 至 0.32±0.02),zeta 电位在-38.3 至+53.3mV 之间。共聚焦激光显微镜显示,未经修饰的 FNS-NS 的细胞内化程度相对较高,而壳聚糖修饰的 FNS-NS 则较低。在适当的储存条件下,冻干的 FNS-NS 可稳定 90 天。含有 15%海藻糖的 FNS-NS 具有适当的物理化学特性,可能是治疗雄激素性脱发的局部递药有前途的载体。

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