Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation

Mahmoud M Omar,1,2 Omiya Ali Hasan,1,2 Amani M El Sisi3 1Department of Pharmaceutics and Industrial Pharmacy, Deraya University, El-Minia, Egypt; 2Department of Pharmaceutics, Sohag University, Sohag, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, Egyp...

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Autores principales:	Omar MM, Hasan OA, El Sisi AM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Transfersome local anesthesia lidocaine permeation enhancement gelling agent. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/caab9ffe0cdb4e75894de89907803dbf
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spelling	oai:doaj.org-article:caab9ffe0cdb4e75894de89907803dbf2021-12-02T08:56:48ZPreparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation1178-2013https://doaj.org/article/caab9ffe0cdb4e75894de89907803dbf2019-02-01T00:00:00Zhttps://www.dovepress.com/preparation-and-optimization-of-lidocaine-transferosomal-gel-containin-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Mahmoud M Omar,1,2 Omiya Ali Hasan,1,2 Amani M El Sisi3 1Department of Pharmaceutics and Industrial Pharmacy, Deraya University, El-Minia, Egypt; 2Department of Pharmaceutics, Sohag University, Sohag, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, Egypt Aim: To develop the topical gel containing transferosomal lidocaine as alternative to painful local anesthetic injection. Materials and methods: The transfersomes were prepared by film hydration technique using soybean phosphatidylcholine and cholesterol. The prepared transfersomes were evaluated for the morphology, drug loading, %EE, particle size and in vitro release. The transferosomal gel of lidocaine was prepared using HPMC k15 as gelling agent and propylene glycol, dimethyl sulfoxide (DMSO), and polyamidoamine dendrimer third generation (PAMAM G3) solutions were used as permeation enhancer. The formulated gels were evaluated for pH, viscosity, drug content and ex-vivo permeation of the gel. The analgesic effect of the formulation was tested using tail flick test. Results: The transfersomes showed that transfersomes (F4) had the highest entrapment efficiency (%EE) approaching 79.87±2.35, low particle size 179.5 nm, and zeta potential of -43.5±4.74 mV. According to the rat tail flick test, the AUC0–90 minutes of the control formulation (lidocaine solution, A) was 352.32±5.87 seconds minutes. While the maximum AUC0–90 minutes value was found to be 570.5±6.81 seconds minutes for gel formulation (F) containing transfersomal lidocaine with PAMAM G3 dendrimer as permeation enhancer. In this case, the local anesthetic efficacy was increased by 1.62-folds as compared to control formulation. Conclusion: From the present study, it can be concluded that the topical gel loaded with transfersomal lidocaine shows enhanced skin permeation effect along with increase in local anesthetic action of lidocaine. Keywords: transfersome, local anesthesia, lidocaine, permeation enhancement, gelling agentOmar MMHasan OAEl Sisi AMDove Medical PressarticleTransfersomelocal anesthesialidocainepermeation enhancementgelling agent.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 1551-1562 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Transfersome local anesthesia lidocaine permeation enhancement gelling agent. Medicine (General) R5-920
spellingShingle	Transfersome local anesthesia lidocaine permeation enhancement gelling agent. Medicine (General) R5-920 Omar MM Hasan OA El Sisi AM Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
description	Mahmoud M Omar,1,2 Omiya Ali Hasan,1,2 Amani M El Sisi3 1Department of Pharmaceutics and Industrial Pharmacy, Deraya University, El-Minia, Egypt; 2Department of Pharmaceutics, Sohag University, Sohag, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, Egypt Aim: To develop the topical gel containing transferosomal lidocaine as alternative to painful local anesthetic injection. Materials and methods: The transfersomes were prepared by film hydration technique using soybean phosphatidylcholine and cholesterol. The prepared transfersomes were evaluated for the morphology, drug loading, %EE, particle size and in vitro release. The transferosomal gel of lidocaine was prepared using HPMC k15 as gelling agent and propylene glycol, dimethyl sulfoxide (DMSO), and polyamidoamine dendrimer third generation (PAMAM G3) solutions were used as permeation enhancer. The formulated gels were evaluated for pH, viscosity, drug content and ex-vivo permeation of the gel. The analgesic effect of the formulation was tested using tail flick test. Results: The transfersomes showed that transfersomes (F4) had the highest entrapment efficiency (%EE) approaching 79.87±2.35, low particle size 179.5 nm, and zeta potential of -43.5±4.74 mV. According to the rat tail flick test, the AUC0–90 minutes of the control formulation (lidocaine solution, A) was 352.32±5.87 seconds minutes. While the maximum AUC0–90 minutes value was found to be 570.5±6.81 seconds minutes for gel formulation (F) containing transfersomal lidocaine with PAMAM G3 dendrimer as permeation enhancer. In this case, the local anesthetic efficacy was increased by 1.62-folds as compared to control formulation. Conclusion: From the present study, it can be concluded that the topical gel loaded with transfersomal lidocaine shows enhanced skin permeation effect along with increase in local anesthetic action of lidocaine. Keywords: transfersome, local anesthesia, lidocaine, permeation enhancement, gelling agent
format	article
author	Omar MM Hasan OA El Sisi AM
author_facet	Omar MM Hasan OA El Sisi AM
author_sort	Omar MM
title	Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
title_short	Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
title_full	Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
title_fullStr	Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
title_full_unstemmed	Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
title_sort	preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/caab9ffe0cdb4e75894de89907803dbf
work_keys_str_mv	AT omarmm preparationandoptimizationoflidocainetransferosomalgelcontainingpermeationenhancersapromisingapproachforenhancementofskinpermeation AT hasanoa preparationandoptimizationoflidocainetransferosomalgelcontainingpermeationenhancersapromisingapproachforenhancementofskinpermeation AT elsisiam preparationandoptimizationoflidocainetransferosomalgelcontainingpermeationenhancersapromisingapproachforenhancementofskinpermeation
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Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation

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