Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation

Khaled M Hosny Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaTel +966561682377Email elswaify2000@yahoo.comBackground: Saqu...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autor principal:	Hosny KM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	saquinavir human immunodeficiency virus bioavailability factorial design self-nano emulsifying drug delivery system transdermal films. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6156ff2362464178b135745a1173d4f3
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:6156ff2362464178b135745a1173d4f3
record_format	dspace
spelling	oai:doaj.org-article:6156ff2362464178b135745a1173d4f32021-12-02T06:57:25ZDevelopment Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation1178-2013https://doaj.org/article/6156ff2362464178b135745a1173d4f32019-11-01T00:00:00Zhttps://www.dovepress.com/development-of-saquinavir-mesylate-nanoemulsion-loaded-transdermal-fil-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Khaled M Hosny Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaTel +966561682377Email elswaify2000@yahoo.comBackground: Saquinavir mesylate (SQR) tablets are widely used against human immunodeficiency virus. SQR has bioavailability issues owing to its poor aqueous solubility, extensive first-pass metabolism, and even low gastrointestinal tract permeability and absorption.Objective: An in-depth optimization process was carried out using factorial design to improve the permeation parameters and thereby the bioavailability of SQR by formulating self-nanoemulsifying drug delivery system (SNEDDS)-loaded polymeric transdermal films.Methods: The solubility of SQR in different nanoemulsion components was examined. Various combinations of selected components were prepared in an extreme vertices mixture design to identify the useful nanoemulsion zone and to develop SNEDDS with minimum globule size. The optimized SQR-SNEDDS was loaded in polyvinyl alcohol (PVA)-based transdermal films. The Box-Behnken design was used to optimize and evaluate SQR permeability. The prepared films were characterized for thickness, tensile strength, elongation, folding endurance, and accelerated stability studies. The optimized film was examined for ex vivo skin permeation and in vivo pharmacokinetic parameters.Results: The optimized SQR-SNEDDS was prepared in proportions of 0.1, 0.55, and 0.35 of clove oil, labrasol, and Transcutol, respectively. The implemented Box-Behnken design indicated the optimized film consisted of 1.0% PVA, 0.25% propylene glycol, and clove oil as the oil phase. The tensile strength, thickness, percent elongation, and folding endurance of the optimized SQR-SNEDDS film were 0.93 ± 0.013 kg/cm2, 0.22 ± 0.006 mm, 43.1 ± 0.022%, and >200 times, respectively. A higher Cmax and double the AUC were observed for SQR-SNEDDS–loaded film in comparison to pure SQR-loaded films.Conclusion: Implementation of a two-step design to optimize and control experimental factors in the preparation of SQR-SNEDDS and its loading onto PVA-based transdermal films was achieved. The films indicated improved ex vivo skin permeation, enhanced bioavailability, and overcame the limitations of the oral dosage form.Keywords: saquinavir, human immunodeficiency virus, bioavailability, factorial design, self-nano emulsifying drug delivery system, transdermal filmsHosny KMDove Medical Pressarticlesaquinavirhuman immunodeficiency virusbioavailabilityfactorial designself-nano emulsifying drug delivery systemtransdermal films.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 8589-8601 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	saquinavir human immunodeficiency virus bioavailability factorial design self-nano emulsifying drug delivery system transdermal films. Medicine (General) R5-920
spellingShingle	saquinavir human immunodeficiency virus bioavailability factorial design self-nano emulsifying drug delivery system transdermal films. Medicine (General) R5-920 Hosny KM Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
description	Khaled M Hosny Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaTel +966561682377Email elswaify2000@yahoo.comBackground: Saquinavir mesylate (SQR) tablets are widely used against human immunodeficiency virus. SQR has bioavailability issues owing to its poor aqueous solubility, extensive first-pass metabolism, and even low gastrointestinal tract permeability and absorption.Objective: An in-depth optimization process was carried out using factorial design to improve the permeation parameters and thereby the bioavailability of SQR by formulating self-nanoemulsifying drug delivery system (SNEDDS)-loaded polymeric transdermal films.Methods: The solubility of SQR in different nanoemulsion components was examined. Various combinations of selected components were prepared in an extreme vertices mixture design to identify the useful nanoemulsion zone and to develop SNEDDS with minimum globule size. The optimized SQR-SNEDDS was loaded in polyvinyl alcohol (PVA)-based transdermal films. The Box-Behnken design was used to optimize and evaluate SQR permeability. The prepared films were characterized for thickness, tensile strength, elongation, folding endurance, and accelerated stability studies. The optimized film was examined for ex vivo skin permeation and in vivo pharmacokinetic parameters.Results: The optimized SQR-SNEDDS was prepared in proportions of 0.1, 0.55, and 0.35 of clove oil, labrasol, and Transcutol, respectively. The implemented Box-Behnken design indicated the optimized film consisted of 1.0% PVA, 0.25% propylene glycol, and clove oil as the oil phase. The tensile strength, thickness, percent elongation, and folding endurance of the optimized SQR-SNEDDS film were 0.93 ± 0.013 kg/cm2, 0.22 ± 0.006 mm, 43.1 ± 0.022%, and >200 times, respectively. A higher Cmax and double the AUC were observed for SQR-SNEDDS–loaded film in comparison to pure SQR-loaded films.Conclusion: Implementation of a two-step design to optimize and control experimental factors in the preparation of SQR-SNEDDS and its loading onto PVA-based transdermal films was achieved. The films indicated improved ex vivo skin permeation, enhanced bioavailability, and overcame the limitations of the oral dosage form.Keywords: saquinavir, human immunodeficiency virus, bioavailability, factorial design, self-nano emulsifying drug delivery system, transdermal films
format	article
author	Hosny KM
author_facet	Hosny KM
author_sort	Hosny KM
title	Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
title_short	Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
title_full	Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
title_fullStr	Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
title_full_unstemmed	Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation
title_sort	development of saquinavir mesylate nanoemulsion-loaded transdermal films: two-step optimization of permeation parameters, characterization, and ex vivo and in vivo evaluation
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/6156ff2362464178b135745a1173d4f3
work_keys_str_mv	AT hosnykm developmentofsaquinavirmesylatenanoemulsionloadedtransdermalfilmstwostepoptimizationofpermeationparameterscharacterizationandexvivoandinvivoevaluation
_version_	1718399635064619008

Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation

Ejemplares similares