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纳米制剂螺内酯和孕酮对大鼠实验性多毛症的炎症和激素水平的药物和药理学评价。

Pharmaceutical and Pharmacological Evaluation of the Effect of Nano-Formulated Spironolactone and Progesterone on Inflammation and Hormonal Levels for Managing Hirsutism Experimentally Induced in Rats.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt.

出版信息

AAPS PharmSciTech. 2021 Jul 13;22(5):204. doi: 10.1208/s12249-021-02003-z.

Abstract

Hirsutism is a dermatological condition that refers to the excessive growth of hair in androgen-sensitive areas in women. Recently, the enhancement of the visible signs of a hairy female has taken special concern that affected the quality of life. The present study was developed to compare the follicular targeting effect of topical spironolactone (SP) or progesterone (PG)-loaded nanostructured lipid carrier (NLC) on the management of hirsutism. Four NLC formulations were prepared using cold homogenization techniques and pharmaceutically evaluated. SP-NLC and PG-NLC topical hydrogels were prepared to explore their pharmacological effect on letrozole induced polycystic ovarian syndrome (PCOS) in rats. Inflammatory mediators, antioxidant, and hormonal parameters were assayed. Additionally, histopathological examination was carried out to confirm the successful induction of PCOS. Results confirmed that all NLC formulations have a spherical shape with particle size ranged from 225.92 ± 0.41 to 447.80 ± 0.66 nm, entrapment efficiency > 75%, and zeta potential (- 31.4 to - 36.5 mV). F1 and F3 NLCs were considered as selected formulations for SP and PG, respectively. Female Wistar rats treated with F1 formulation for 3 weeks displayed better outcomes as manifested by the measured parameters as compared to the other tested groups. A significant reduction in hair follicle diameter and density was observed after topical application of SP or PG nano-gels. Finally, the outcomes pose a strong argument that the development of topically administered SP-NLC can be explored as a promising carrier over PG-NLC for more effectual improvement in the visible sign of hirsutism.

摘要

多毛症是一种皮肤科疾病,指的是女性雄激素敏感部位的毛发过度生长。最近,女性多毛症的可见症状明显加重,影响了生活质量。本研究旨在比较局部螺内酯(SP)或孕激素(PG)负载的纳米结构脂质载体(NLC)对多毛症治疗的毛囊靶向作用。采用冷匀化技术制备了四种 NLC 制剂,并进行了药学评价。制备了 SP-NLC 和 PG-NLC 局部水凝胶,以探索其对来曲唑诱导的多囊卵巢综合征(PCOS)大鼠的药理作用。测定了炎症介质、抗氧化剂和激素参数。此外,还进行了组织病理学检查,以确认 PCOS 的成功诱导。结果证实,所有 NLC 制剂均呈球形,粒径为 225.92±0.41447.80±0.66nm,包封效率>75%,zeta 电位为(-31.4-36.5)mV。F1 和 F3 NLC 分别被认为是 SP 和 PG 的优选制剂。用 F1 制剂处理 3 周的雌性 Wistar 大鼠,与其他测试组相比,其测量参数表现出更好的结果。局部应用 SP 或 PG 纳米凝胶后,毛囊直径和密度显著减小。最后,结果有力地表明,局部给予 SP-NLC 的开发可以作为 PG-NLC 的一种有前途的载体进行探索,以更有效地改善多毛症的可见症状。

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