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Beclomethasone loaded liposomes enriched with mucin: A suitable approach for the control of skin disorders

Authors :
Ines Castangia
Matteo Aroffu
Mohamad Allaw
Matteo Perra
Biancamaria Baroli
Iris Usach
José Esteban Peris
Donatella Valenti
Octavio Diez-Sales
Amparo Ruiz Sauri
Amparo Nacher
Xavier Fernàndez-Busquets
Maria Manconi
Maria Letizia Manca
Source :
Biomedicine & Pharmacotherapy, Vol 177, Iss , Pp 116998- (2024)
Publication Year :
2024
Publisher :
Elsevier, 2024.

Abstract

Inflammatory skin disorders are the fourth leading cause of chronic non-fatal conditions, which have a serious impact on the patient quality of life. Due to their treatment with conventional corticosteroids, which often result in poor therapeutic efficacy, relapses and systemic side effects from prolonged therapy, these diseases represent a global burden that negatively impacts the global economy. To avoid these problems and optimize corticosteroid benefits, beclomethasone was loaded into liposome formulations specifically tailored for skin delivery. These formulations were enhanced with mucin (0.1 and 0.5 % w/v) to further ensure prolonged formulation permanence at the site of application. The addition of 0.5 % w/v mucin resulted in the formation of small unilamellar vesicles and multicompartment vesicles. Liposomes and 1mucin-liposomes were smaller (∼48 and ∼61 nm, respectively) and more monodispersed (PI ∼ 0.14 and ∼ 0.17, respectively) than 5mucin-liposomes, which were larger (∼137 nm), slightly polydispersed (PI ∼ 0.23), and less stable during storage (4 months in the dark at 25 °C). Liposomes were negatively charged (∼ −79 mV) irrespective of their composition, and capable of incorporating high amount of beclomethasone (∼ 80 %). In vitro studies on skin fibroblasts and keratinocytes confirmed the high biocompatibility of all formulations (viability ≥ 95 %). However, the use of mucin-liposomes resulted in higher efficacy against nitric oxide production and free radical damage. Finally, topical applications using 12-O-tetradecanoylphorbol-13-acetate-injured skin in vivo experiments showed that only the mucin-enriched formulations could restore healthy conditions within 4 days, underscoring promise as a treatment for skin disorders.

Details

Language :
English
ISSN :
07533322
Volume :
177
Issue :
116998-
Database :
Directory of Open Access Journals
Journal :
Biomedicine & Pharmacotherapy
Publication Type :
Academic Journal
Accession number :
edsdoj.62e448d8d9d4f83b0ea69e6a4502a2d
Document Type :
article
Full Text :
https://doi.org/10.1016/j.biopha.2024.116998