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螺内酯透明质酸富勒醇脂质体(HAECs)用于治疗多毛症的局部治疗:研究、统计优化和临床试验。

Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: studies, statistical optimization, and studies.

机构信息

Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.

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

出版信息

Drug Deliv. 2021 Dec;28(1):2289-2300. doi: 10.1080/10717544.2021.1989089.

Abstract

Spironolactone (SP) is a potassium sparing diuretic with antiandrogenic properties. This study aimed at formulating SP into hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism. HAECs were prepared by ethanol injection method, according to D-optimal design, after a proper study. HAECs were evaluated by measuring their entrapment efficiency (EE%), particle size (PS), and polydispersity index (PDI). Optimal hyaluronic acid enriched cerosomes (OHAECs) were subjected to further and and studies. The study concluded better interactions between SP and phosphatidyl choline in presence of hyaluronic acid (HA) and high stability of their binding in water. The prepared HAECs had acceptable EE%, PS, and PDI values. The statistical optimization process suggested OHAEC containing 10.5 mg ceramide III and 15 mg HA, utilizing Kolliphor RH40. OHAEC had EE% and PS of 89.3 ± 0.3% and 261.8 ± 7.0 nm, respectively. OHAEC was stable for up to 3 months. It also showed a mixed tubular and vesicular appearance under transmission electron microscope. The and studies concluded better skin deposition and accumulation of SP from OHAEC. The histopathological study demonstrated the safety of OHAEC for topical application. Therefore, OHAEC could be considered as effective system for topical application of SP to manage hirsutism, with prolonged action, coupled with minimized side effects.

摘要

螺内酯(SP)是一种具有抗雄激素作用的保钾利尿剂。本研究旨在将 SP 制成富含透明质酸的神经酰胺囊泡(HAECs),用于治疗多毛症的局部治疗。根据 D-最优设计,在适当研究后,通过乙醇注入法制备 HAECs。通过测量包封效率(EE%)、粒径(PS)和多分散指数(PDI)来评估 HAECs。对最佳透明质酸富集神经酰胺囊泡(OHAECs)进行了进一步的和研究。研究得出结论,在透明质酸(HA)存在的情况下,SP 与磷脂酰胆碱之间存在更好的相互作用,并且它们在水中的结合具有更高的稳定性。所制备的 HAECs 具有可接受的 EE%、PS 和 PDI 值。统计优化过程表明,含有 10.5mg 神经酰胺 III 和 15mgHA 的 OHAEC,利用 Kolliphor RH40。OHAEC 的 EE%和 PS 分别为 89.3±0.3%和 261.8±7.0nm。OHAEC 稳定 3 个月。在透射电子显微镜下,它还显示出混合管状和囊泡状外观。研究得出结论,OHAEC 可更好地促进 SP 的皮肤沉积和积累。组织病理学研究证明了 OHAEC 用于局部应用的安全性。因此,OHAEC 可被认为是用于管理多毛症的 SP 局部应用的有效系统,具有延长作用,同时减少副作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a7a/8567875/f8785ee5d730/IDRD_A_1989089_F0001_C.jpg

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