Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

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 i...

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Autores principales:	Rofida Albash, Abdurrahman M. Fahmy, Mohammed I.A. Hamed, Khaled M. Darwish, Rania Moataz El-Dahmy
Formato:	article
Lenguaje:	EN
Publicado:	Taylor & Francis Group 2021
Materias:	in silico study spironolactone hirsutism dermatokinetic local accumulation efficiency index Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/ff17203c511e4590ace0a0fe6d3e6cf9
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spelling	oai:doaj.org-article:ff17203c511e4590ace0a0fe6d3e6cf92021-11-04T15:00:41ZSpironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies1071-75441521-046410.1080/10717544.2021.1989089https://doaj.org/article/ff17203c511e4590ace0a0fe6d3e6cf92021-01-01T00:00:00Zhttp://dx.doi.org/10.1080/10717544.2021.1989089https://doaj.org/toc/1071-7544https://doaj.org/toc/1521-0464Spironolactone (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 in silico 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 in vitro and ex-vivo and in-vivo studies. The in silico 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 ex vivo and in vivo 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.Rofida AlbashAbdurrahman M. FahmyMohammed I.A. HamedKhaled M. DarwishRania Moataz El-DahmyTaylor & Francis Grouparticlein silico studyspironolactonehirsutismdermatokineticlocal accumulation efficiency indexTherapeutics. PharmacologyRM1-950ENDrug Delivery, Vol 28, Iss 1, Pp 2289-2300 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	in silico study spironolactone hirsutism dermatokinetic local accumulation efficiency index Therapeutics. Pharmacology RM1-950
spellingShingle	in silico study spironolactone hirsutism dermatokinetic local accumulation efficiency index Therapeutics. Pharmacology RM1-950 Rofida Albash Abdurrahman M. Fahmy Mohammed I.A. Hamed Khaled M. Darwish Rania Moataz El-Dahmy Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
description	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 in silico 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 in vitro and ex-vivo and in-vivo studies. The in silico 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 ex vivo and in vivo 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.
format	article
author	Rofida Albash Abdurrahman M. Fahmy Mohammed I.A. Hamed Khaled M. Darwish Rania Moataz El-Dahmy
author_facet	Rofida Albash Abdurrahman M. Fahmy Mohammed I.A. Hamed Khaled M. Darwish Rania Moataz El-Dahmy
author_sort	Rofida Albash
title	Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
title_short	Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
title_full	Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
title_fullStr	Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
title_full_unstemmed	Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
title_sort	spironolactone hyaluronic acid enriched cerosomes (haecs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies
publisher	Taylor & Francis Group
publishDate	2021
url	https://doaj.org/article/ff17203c511e4590ace0a0fe6d3e6cf9
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Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

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