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Development of Adapalene Loaded Liposome Based Gel for Acne

Retinoids are considered the mainstay treatment for moderate to severe acne. Adapalene, a third-generation retinoid, has physiochemical properties which hinder the effective delivery of the drug to the skin. Therefore, the current study aimed to develop and evaluate adapalene liposomal loaded gel (A...

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Autores principales: Arooj, Asma, Rehman, Asim Ur, Iqbal, Muhammad, Naz, Iffat, Alhodaib, Aiyeshah, Ahmed, Naveed
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9956198/
https://www.ncbi.nlm.nih.gov/pubmed/36826305
http://dx.doi.org/10.3390/gels9020135
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author Arooj, Asma
Rehman, Asim Ur
Iqbal, Muhammad
Naz, Iffat
Alhodaib, Aiyeshah
Ahmed, Naveed
author_facet Arooj, Asma
Rehman, Asim Ur
Iqbal, Muhammad
Naz, Iffat
Alhodaib, Aiyeshah
Ahmed, Naveed
author_sort Arooj, Asma
collection PubMed
description Retinoids are considered the mainstay treatment for moderate to severe acne. Adapalene, a third-generation retinoid, has physiochemical properties which hinder the effective delivery of the drug to the skin. Therefore, the current study aimed to develop and evaluate adapalene liposomal loaded gel (ADA-LP gel) for the effective management of acne to improve tolerability and delivery to targeted sites as compared to the conventional dosage form of the drug. A novel spontaneous phase transition method (SPT) was used to formulate liposomes. Liposomal formulation (ADA-LP) was prepared and optimized based on particle size, zeta potential, and PDI. Optimized formulation was further characterized by different techniques and loaded into Carbopol gel. In vitro drug release, ex vivo permeation, and in vivo studies were performed using the prepared adapalene-loaded liposomal-based gel. The in vivo study was done employing the testosterone-induced acne model in mice. The optimized formulation had a size of 181 nm, PDI 0.145, and a zeta potential of −35 mV, indicating that the formulation was stable. Encapsulation efficiency was 89.69 ± 0.5%. ADA-LPs were loaded into the gel. Prepared ADA-LP showed a 79 ± 0.02% release of drug in a sustained manner, within 24 h. The ex vivo permeability study showed a total of 43 ± 0.06 µg/cm(2) of drug able to permeate through the skin within 24 h. Moreover, only 28.27 ± 0.04% was retained on the epidermis. The developed ADA-LP gel showed significant improvement in the acne lesions in mice with no visible scars and inflammation on the skin. Therefore, ADA-LP-based gel could be a promising carrier system for the safe and effective delivery of Adapalene.
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spelling pubmed-99561982023-02-25 Development of Adapalene Loaded Liposome Based Gel for Acne Arooj, Asma Rehman, Asim Ur Iqbal, Muhammad Naz, Iffat Alhodaib, Aiyeshah Ahmed, Naveed Gels Article Retinoids are considered the mainstay treatment for moderate to severe acne. Adapalene, a third-generation retinoid, has physiochemical properties which hinder the effective delivery of the drug to the skin. Therefore, the current study aimed to develop and evaluate adapalene liposomal loaded gel (ADA-LP gel) for the effective management of acne to improve tolerability and delivery to targeted sites as compared to the conventional dosage form of the drug. A novel spontaneous phase transition method (SPT) was used to formulate liposomes. Liposomal formulation (ADA-LP) was prepared and optimized based on particle size, zeta potential, and PDI. Optimized formulation was further characterized by different techniques and loaded into Carbopol gel. In vitro drug release, ex vivo permeation, and in vivo studies were performed using the prepared adapalene-loaded liposomal-based gel. The in vivo study was done employing the testosterone-induced acne model in mice. The optimized formulation had a size of 181 nm, PDI 0.145, and a zeta potential of −35 mV, indicating that the formulation was stable. Encapsulation efficiency was 89.69 ± 0.5%. ADA-LPs were loaded into the gel. Prepared ADA-LP showed a 79 ± 0.02% release of drug in a sustained manner, within 24 h. The ex vivo permeability study showed a total of 43 ± 0.06 µg/cm(2) of drug able to permeate through the skin within 24 h. Moreover, only 28.27 ± 0.04% was retained on the epidermis. The developed ADA-LP gel showed significant improvement in the acne lesions in mice with no visible scars and inflammation on the skin. Therefore, ADA-LP-based gel could be a promising carrier system for the safe and effective delivery of Adapalene. MDPI 2023-02-06 /pmc/articles/PMC9956198/ /pubmed/36826305 http://dx.doi.org/10.3390/gels9020135 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Arooj, Asma
Rehman, Asim Ur
Iqbal, Muhammad
Naz, Iffat
Alhodaib, Aiyeshah
Ahmed, Naveed
Development of Adapalene Loaded Liposome Based Gel for Acne
title Development of Adapalene Loaded Liposome Based Gel for Acne
title_full Development of Adapalene Loaded Liposome Based Gel for Acne
title_fullStr Development of Adapalene Loaded Liposome Based Gel for Acne
title_full_unstemmed Development of Adapalene Loaded Liposome Based Gel for Acne
title_short Development of Adapalene Loaded Liposome Based Gel for Acne
title_sort development of adapalene loaded liposome based gel for acne
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9956198/
https://www.ncbi.nlm.nih.gov/pubmed/36826305
http://dx.doi.org/10.3390/gels9020135
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