Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation

Khaled M Hosny1,2 1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of...

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Autor principal:	Hosny KM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	cubosomes central nervous system (cns) nose to brain delivery human immunodeficiency virus (hiv) intranasal saquinavir thermogelling Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/008d8787db144b1d9267d1ffa2e1b7c5
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spelling	oai:doaj.org-article:008d8787db144b1d9267d1ffa2e1b7c52021-12-02T10:51:19ZNanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation1178-2013https://doaj.org/article/008d8787db144b1d9267d1ffa2e1b7c52020-07-01T00:00:00Zhttps://www.dovepress.com/nanosized-cubosomal-thermogelling-dispersion-loaded-with-saquinavir-me-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Khaled M Hosny1,2 1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaTel +966561682377Email elswaify2000@yahoo.comBackground: Low bioavailability and poor permeability of the blood–brain barrier are problematic when delivering therapeutic agents and particularly anti–human immunodeficiency virus therapy to the central nervous system. The intranasal route offers an alternative for central nervous system delivery. Cubosomes have been reported as helpful vehicles for intranasal delivery of therapeutics to enable brain targeting.Objective: In this study, we aimed to develop the intranasal cubosomal thermogelling dispersion of saquinavir mesylate for central nervous system delivery.Methods: The Box–Behnken design was applied to study the effect of monoolein, Poloxamer 407, and polyvinyl alcohol as independent factors and the particle size, entrapment efficiency, gelation temperature, and stability index as responses. The optimized cubosomes were evaluated using transmission electron microscopy, ex vivo permeation, and in vivo pharmacokinetics.Results: The optimized formula consisting of monoolein (8.96%), Poloxamer 407 (17.45%), and polyvinyl alcohol (7.5%) was prepared and evaluated. Higher values for the steady-state flux, permeability coefficient, and enhancement factor were observed for the cubosomal thermogelling dispersion of saquinavir during ex vivo permeation in comparison with an aqueous suspension of saquinavir. From the pharmacokinetic profile, the relative bioavailability for the intranasal optimized formula was approximately 12-fold higher when compared with oral aqueous suspension and 2.5-fold greater when compared to the intranasal aqueous suspension of saquinavir.Conclusion: Overall, the saquinavir-loaded cubosomal thermogelling formulation is promising for central nervous system delivery by intranasal administration.Keywords: cubosomes, central nervous system, CNS, nose to brain delivery, human immunodeficiency virus, HIV, intranasal, saquinavir, thermogellingHosny KMDove Medical Pressarticlecubosomescentral nervous system (cns)nose to brain deliveryhuman immunodeficiency virus (hiv)intranasalsaquinavirthermogellingMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 5113-5129 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	cubosomes central nervous system (cns) nose to brain delivery human immunodeficiency virus (hiv) intranasal saquinavir thermogelling Medicine (General) R5-920
spellingShingle	cubosomes central nervous system (cns) nose to brain delivery human immunodeficiency virus (hiv) intranasal saquinavir thermogelling Medicine (General) R5-920 Hosny KM Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
description	Khaled M Hosny1,2 1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptCorrespondence: Khaled M HosnyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaTel +966561682377Email elswaify2000@yahoo.comBackground: Low bioavailability and poor permeability of the blood–brain barrier are problematic when delivering therapeutic agents and particularly anti–human immunodeficiency virus therapy to the central nervous system. The intranasal route offers an alternative for central nervous system delivery. Cubosomes have been reported as helpful vehicles for intranasal delivery of therapeutics to enable brain targeting.Objective: In this study, we aimed to develop the intranasal cubosomal thermogelling dispersion of saquinavir mesylate for central nervous system delivery.Methods: The Box–Behnken design was applied to study the effect of monoolein, Poloxamer 407, and polyvinyl alcohol as independent factors and the particle size, entrapment efficiency, gelation temperature, and stability index as responses. The optimized cubosomes were evaluated using transmission electron microscopy, ex vivo permeation, and in vivo pharmacokinetics.Results: The optimized formula consisting of monoolein (8.96%), Poloxamer 407 (17.45%), and polyvinyl alcohol (7.5%) was prepared and evaluated. Higher values for the steady-state flux, permeability coefficient, and enhancement factor were observed for the cubosomal thermogelling dispersion of saquinavir during ex vivo permeation in comparison with an aqueous suspension of saquinavir. From the pharmacokinetic profile, the relative bioavailability for the intranasal optimized formula was approximately 12-fold higher when compared with oral aqueous suspension and 2.5-fold greater when compared to the intranasal aqueous suspension of saquinavir.Conclusion: Overall, the saquinavir-loaded cubosomal thermogelling formulation is promising for central nervous system delivery by intranasal administration.Keywords: cubosomes, central nervous system, CNS, nose to brain delivery, human immunodeficiency virus, HIV, intranasal, saquinavir, thermogelling
format	article
author	Hosny KM
author_facet	Hosny KM
author_sort	Hosny KM
title	Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
title_short	Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
title_full	Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
title_fullStr	Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
title_full_unstemmed	Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
title_sort	nanosized cubosomal thermogelling dispersion loaded with saquinavir mesylate to improve its bioavailability: preparation, optimization, in vitro and in vivo evaluation
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/008d8787db144b1d9267d1ffa2e1b7c5
work_keys_str_mv	AT hosnykm nanosizedcubosomalthermogellingdispersionloadedwithsaquinavirmesylatetoimproveitsbioavailabilitypreparationoptimizationinvitroandinvivoevaluation
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Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation

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