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Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers

OBJECTIVES: The objective of this study is to investigate the feasibility of transdermal drug delivery of Labetalol Hydrochloride (LHCl) and to study the effect of different penetration enhancers on the skin permeability of LHCl. METHODS: The permeability experiments were conducted using a horizonta...

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Autores principales: Zafar, Saqib, Ali, Asgar, Aqil, Mohammed, Ahad, Abdul
Formato: Texto
Lenguaje:English
Publicado: Medknow Publications 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2996075/
https://www.ncbi.nlm.nih.gov/pubmed/21180464
http://dx.doi.org/10.4103/0975-7406.72132
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author Zafar, Saqib
Ali, Asgar
Aqil, Mohammed
Ahad, Abdul
author_facet Zafar, Saqib
Ali, Asgar
Aqil, Mohammed
Ahad, Abdul
author_sort Zafar, Saqib
collection PubMed
description OBJECTIVES: The objective of this study is to investigate the feasibility of transdermal drug delivery of Labetalol Hydrochloride (LHCl) and to study the effect of different penetration enhancers on the skin permeability of LHCl. METHODS: The permeability experiments were conducted using a horizontal glass diffusion cell with a diffusional area of 2.37 cm-(2) on albino rat skin. The effect of various penetration enhancers namely turpentine oil, dimethyl formamide (DMF), menthol, dimethyl sulfoxide, pine oil, and 2-pyrollidone, and the effect of the concentration of drug and enhancer in the donor phase on the skin permeability of LHCl was studied. RESULTS: The apparent partition coefficient of the drug was found to be 6.95, suggesting it to be a lipophilic drug. The preliminary skin permeation studies revealed that the permeation of LHCL through albino rat skin was moderate (K(p) = 6.490 × 10(-2) cm hr(-1)) from isotonic phosphate buffer of pH 7.4. An appreciable increase in the LHCl permeability coefficient was observed on using a co-solvent (ethanol 95%) with the penetration enhancers in the donor phase. DMSO (10% v/v) was found to be the most effective enhancer for Labetalol hydrochloride (Enhancement Factor = 1.165). An increase in the concentration of drug and enhancer in the donor cell accentuated the permeability coefficient of LHCl. CONCLUSIONS: It was concluded that LHCl could be delivered via the dermal route with the use of 10% DMSO as the penetration enhancer.
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spelling pubmed-29960752010-12-21 Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers Zafar, Saqib Ali, Asgar Aqil, Mohammed Ahad, Abdul J Pharm Bioallied Sci Original Article OBJECTIVES: The objective of this study is to investigate the feasibility of transdermal drug delivery of Labetalol Hydrochloride (LHCl) and to study the effect of different penetration enhancers on the skin permeability of LHCl. METHODS: The permeability experiments were conducted using a horizontal glass diffusion cell with a diffusional area of 2.37 cm-(2) on albino rat skin. The effect of various penetration enhancers namely turpentine oil, dimethyl formamide (DMF), menthol, dimethyl sulfoxide, pine oil, and 2-pyrollidone, and the effect of the concentration of drug and enhancer in the donor phase on the skin permeability of LHCl was studied. RESULTS: The apparent partition coefficient of the drug was found to be 6.95, suggesting it to be a lipophilic drug. The preliminary skin permeation studies revealed that the permeation of LHCL through albino rat skin was moderate (K(p) = 6.490 × 10(-2) cm hr(-1)) from isotonic phosphate buffer of pH 7.4. An appreciable increase in the LHCl permeability coefficient was observed on using a co-solvent (ethanol 95%) with the penetration enhancers in the donor phase. DMSO (10% v/v) was found to be the most effective enhancer for Labetalol hydrochloride (Enhancement Factor = 1.165). An increase in the concentration of drug and enhancer in the donor cell accentuated the permeability coefficient of LHCl. CONCLUSIONS: It was concluded that LHCl could be delivered via the dermal route with the use of 10% DMSO as the penetration enhancer. Medknow Publications 2010 /pmc/articles/PMC2996075/ /pubmed/21180464 http://dx.doi.org/10.4103/0975-7406.72132 Text en © Journal of Pharmacy and Bioallied Sciences http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Zafar, Saqib
Ali, Asgar
Aqil, Mohammed
Ahad, Abdul
Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title_full Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title_fullStr Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title_full_unstemmed Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title_short Transdermal drug delivery of labetalol hydrochloride: Feasibility and effect of penetration enhancers
title_sort transdermal drug delivery of labetalol hydrochloride: feasibility and effect of penetration enhancers
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2996075/
https://www.ncbi.nlm.nih.gov/pubmed/21180464
http://dx.doi.org/10.4103/0975-7406.72132
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