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Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies

Background: Transfersomes can be used to enhance transdermal drug delivery due to their flexibility and ability to incorporate various molecules. For example, hydrocortisone (HC), a corticosteroid, is taken by different routes and serves as immunosuppressive, anticancer, and antiallergenic; however,...

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Autores principales: Abdelwahd, Asmae, Rasool, Bazigha K. Abdul
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10186384/
https://www.ncbi.nlm.nih.gov/pubmed/35676851
http://dx.doi.org/10.2174/2667387816666220608115605
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author Abdelwahd, Asmae
Rasool, Bazigha K. Abdul
author_facet Abdelwahd, Asmae
Rasool, Bazigha K. Abdul
author_sort Abdelwahd, Asmae
collection PubMed
description Background: Transfersomes can be used to enhance transdermal drug delivery due to their flexibility and ability to incorporate various molecules. For example, hydrocortisone (HC), a corticosteroid, is taken by different routes and serves as immunosuppressive, anticancer, and antiallergenic; however, it is poorly absorbed by the skin. Objective: Therefore, the current study suggested HC-loaded transfersomes as an alternative route of administration for reaching deeper skin layers or systemic circulation, to reduce the side effects of HC and improve its bioavailability. Methods: HC transfersomes were prepared by the thin-film hydration method and characterized for their vesicular size, zeta potential, drug entrapment efficiency, elasticity, FTIR spectroscopy, in vitro drug release, ex vivo permeation, and irritancy in rabbits. The optimized formulation, F15 (containing HC 20 mg, egg phosphatidylcholine (EPC) 400 mg, and 75 mg of Span 80), was chosen because it showed the highest (p< 0.05) EE% (60.4±0.80) and optimized sustained in vitro drug release (Q8 = 87.9±0.6%). Results: Extensive analysis of the drug release data from all formulas was performed using the DDSolver software which quantitatively confirmed the successful formulation. The Weibull equation was the best model to fit the release data compared to others, and the release mechanism was Fickian diffusion. Conclusion: The simulated pharmacokinetic parameters showed that F15 had the highest AUC, MDT, and DE. Furthermore, F15 significantly enhanced HC permeation by 12-folds compared to the control through the excised rat's skin. The skin irritancy test has proven F15 safety and skin compatibility.
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spelling pubmed-101863842023-05-17 Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies Abdelwahd, Asmae Rasool, Bazigha K. Abdul Recent Adv Drug Deliv Formul Drug Delivery Background: Transfersomes can be used to enhance transdermal drug delivery due to their flexibility and ability to incorporate various molecules. For example, hydrocortisone (HC), a corticosteroid, is taken by different routes and serves as immunosuppressive, anticancer, and antiallergenic; however, it is poorly absorbed by the skin. Objective: Therefore, the current study suggested HC-loaded transfersomes as an alternative route of administration for reaching deeper skin layers or systemic circulation, to reduce the side effects of HC and improve its bioavailability. Methods: HC transfersomes were prepared by the thin-film hydration method and characterized for their vesicular size, zeta potential, drug entrapment efficiency, elasticity, FTIR spectroscopy, in vitro drug release, ex vivo permeation, and irritancy in rabbits. The optimized formulation, F15 (containing HC 20 mg, egg phosphatidylcholine (EPC) 400 mg, and 75 mg of Span 80), was chosen because it showed the highest (p< 0.05) EE% (60.4±0.80) and optimized sustained in vitro drug release (Q8 = 87.9±0.6%). Results: Extensive analysis of the drug release data from all formulas was performed using the DDSolver software which quantitatively confirmed the successful formulation. The Weibull equation was the best model to fit the release data compared to others, and the release mechanism was Fickian diffusion. Conclusion: The simulated pharmacokinetic parameters showed that F15 had the highest AUC, MDT, and DE. Furthermore, F15 significantly enhanced HC permeation by 12-folds compared to the control through the excised rat's skin. The skin irritancy test has proven F15 safety and skin compatibility. Bentham Science Publishers 2022-10-19 2022-10-19 /pmc/articles/PMC10186384/ /pubmed/35676851 http://dx.doi.org/10.2174/2667387816666220608115605 Text en https://creativecommons.org/licenses/by/4.0/This is an Open Access article published under CC BY 4.0 https://creativecommons.org/licenses/by/4.0/legalcode
spellingShingle Drug Delivery
Abdelwahd, Asmae
Rasool, Bazigha K. Abdul
Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title_full Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title_fullStr Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title_full_unstemmed Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title_short Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
title_sort optimizing and evaluating the transdermal permeation of hydrocortisone transfersomes formulation based on digital analysis of the in vitro drug release and ex vivo studies
topic Drug Delivery
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10186384/
https://www.ncbi.nlm.nih.gov/pubmed/35676851
http://dx.doi.org/10.2174/2667387816666220608115605
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