Development and characterization of a nanoemulsion containing propranolol for topical delivery

Tatiana Zanela da Silva Marques,1 Ralph Santos-Oliveira,2 Luciana Betzler de Oliveira de Siqueira,1 Verônica da Silva Cardoso,3 Zaida Maria Faria de Freitas,1 Rita de Cássia da Silva Ascenção Barros,1 Ana Lúcia Vazquez Villa,1 Mariana Sato de Sou...

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Autores principales:	Zanela da Silva Marques T, Santos-Oliveira R, Betzler de Oliveira de Siqueira L, Cardoso VS, Freitas ZMF, Barros RCSA, Villa ALV, Monteiro MSSB, Santos EP, Ricci-Junior E
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	infantile hemangiomas nanoemulsion propranolol ex-vivo permeation studies cytotoxicity Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/1ab7155a9db348069301afc127c4971e
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spelling	oai:doaj.org-article:1ab7155a9db348069301afc127c4971e2021-12-02T04:12:57ZDevelopment and characterization of a nanoemulsion containing propranolol for topical delivery1178-2013https://doaj.org/article/1ab7155a9db348069301afc127c4971e2018-05-01T00:00:00Zhttps://www.dovepress.com/development-and-characterization-of-a-nanoemulsion-containing-proprano-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Tatiana Zanela da Silva Marques,1 Ralph Santos-Oliveira,2 Luciana Betzler de Oliveira de Siqueira,1 Verônica da Silva Cardoso,3 Zaida Maria Faria de Freitas,1 Rita de Cássia da Silva Ascenção Barros,1 Ana Lúcia Vazquez Villa,1 Mariana Sato de Souza de Bustamante Monteiro,1 Elisabete Pereira dos Santos,1 Eduardo Ricci-Junior1 1Department of Drugs and Medicines, Faculty of Pharmacy, 2Institute of Nuclear Energy, 3Unit of Biocatalysis, Bioproducts and Bioenergy (Bioinivar), Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil Background: Propranolol (PPN) is a therapeutic option for the treatment of infantile hemangiomas. This study aimed at the development of nanoemulsion (NE) containing 1% PPN, characterization of the system, and safety studies based on ex vivo permeation, cytotoxicity, and biodistribution in vivo.Methods: The formulation was developed and characterized in relation to the droplet size, polydispersity index (PDI), pH, zeta potential, and electronic microscopy. Ex vivo permeation studies were used to evaluate the cutaneous retention of PPN in the epidermis and dermis. Cytotoxicity studies were performed in fibroblasts, macrophages, and keratinocytes. In vivo biodistribution assay of the formulations was performed by means of labeling with technetium-99m.Results: NE1 exhibited droplet size of 26 nm, PDI <0.4, pH compatible with the skin, and zeta potential of −20 mV, which possibly contributes to the stability. Electron microscopy showed that the NE presented droplets of nanometric size and spherical shape. NE1 provided excellent stability for PPN. In the ex vivo cutaneous permeation assay, the NE provided satisfactory PPN retention particularly in the dermis, which is the site of drug action. In addition, NE1 promoted cutaneous permeation of the PPN in small amount. In vivo biodistribution showed that the radiolabeled formulation remained in the skin and a small amount reached the bloodstream. NE1 presented low cytotoxicity to fibroblasts, macrophages, and keratinocytes in the concentrations evaluated in the cytotoxicity assay.Conclusion: We concluded that the formulation is safe for skin administration; however, cutaneous irritation studies should be performed to confirm the safety of the formulation before clinical studies in patients with infantile hemangiomas. Keywords: infantile hemangiomas, nanoemulsion, propranolol, ex vivo permeation studies, cytotoxicityZanela da Silva Marques TSantos-Oliveira RBetzler de Oliveira de Siqueira LCardoso VSFreitas ZMFBarros RCSAVilla ALVMonteiro MSSBSantos EPRicci-Junior EDove Medical Pressarticleinfantile hemangiomasnanoemulsionpropranololex-vivo permeation studiescytotoxicityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 2827-2837 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	infantile hemangiomas nanoemulsion propranolol ex-vivo permeation studies cytotoxicity Medicine (General) R5-920
spellingShingle	infantile hemangiomas nanoemulsion propranolol ex-vivo permeation studies cytotoxicity Medicine (General) R5-920 Zanela da Silva Marques T Santos-Oliveira R Betzler de Oliveira de Siqueira L Cardoso VS Freitas ZMF Barros RCSA Villa ALV Monteiro MSSB Santos EP Ricci-Junior E Development and characterization of a nanoemulsion containing propranolol for topical delivery
description	Tatiana Zanela da Silva Marques,1 Ralph Santos-Oliveira,2 Luciana Betzler de Oliveira de Siqueira,1 Verônica da Silva Cardoso,3 Zaida Maria Faria de Freitas,1 Rita de Cássia da Silva Ascenção Barros,1 Ana Lúcia Vazquez Villa,1 Mariana Sato de Souza de Bustamante Monteiro,1 Elisabete Pereira dos Santos,1 Eduardo Ricci-Junior1 1Department of Drugs and Medicines, Faculty of Pharmacy, 2Institute of Nuclear Energy, 3Unit of Biocatalysis, Bioproducts and Bioenergy (Bioinivar), Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil Background: Propranolol (PPN) is a therapeutic option for the treatment of infantile hemangiomas. This study aimed at the development of nanoemulsion (NE) containing 1% PPN, characterization of the system, and safety studies based on ex vivo permeation, cytotoxicity, and biodistribution in vivo.Methods: The formulation was developed and characterized in relation to the droplet size, polydispersity index (PDI), pH, zeta potential, and electronic microscopy. Ex vivo permeation studies were used to evaluate the cutaneous retention of PPN in the epidermis and dermis. Cytotoxicity studies were performed in fibroblasts, macrophages, and keratinocytes. In vivo biodistribution assay of the formulations was performed by means of labeling with technetium-99m.Results: NE1 exhibited droplet size of 26 nm, PDI <0.4, pH compatible with the skin, and zeta potential of −20 mV, which possibly contributes to the stability. Electron microscopy showed that the NE presented droplets of nanometric size and spherical shape. NE1 provided excellent stability for PPN. In the ex vivo cutaneous permeation assay, the NE provided satisfactory PPN retention particularly in the dermis, which is the site of drug action. In addition, NE1 promoted cutaneous permeation of the PPN in small amount. In vivo biodistribution showed that the radiolabeled formulation remained in the skin and a small amount reached the bloodstream. NE1 presented low cytotoxicity to fibroblasts, macrophages, and keratinocytes in the concentrations evaluated in the cytotoxicity assay.Conclusion: We concluded that the formulation is safe for skin administration; however, cutaneous irritation studies should be performed to confirm the safety of the formulation before clinical studies in patients with infantile hemangiomas. Keywords: infantile hemangiomas, nanoemulsion, propranolol, ex vivo permeation studies, cytotoxicity
format	article
author	Zanela da Silva Marques T Santos-Oliveira R Betzler de Oliveira de Siqueira L Cardoso VS Freitas ZMF Barros RCSA Villa ALV Monteiro MSSB Santos EP Ricci-Junior E
author_facet	Zanela da Silva Marques T Santos-Oliveira R Betzler de Oliveira de Siqueira L Cardoso VS Freitas ZMF Barros RCSA Villa ALV Monteiro MSSB Santos EP Ricci-Junior E
author_sort	Zanela da Silva Marques T
title	Development and characterization of a nanoemulsion containing propranolol for topical delivery
title_short	Development and characterization of a nanoemulsion containing propranolol for topical delivery
title_full	Development and characterization of a nanoemulsion containing propranolol for topical delivery
title_fullStr	Development and characterization of a nanoemulsion containing propranolol for topical delivery
title_full_unstemmed	Development and characterization of a nanoemulsion containing propranolol for topical delivery
title_sort	development and characterization of a nanoemulsion containing propranolol for topical delivery
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/1ab7155a9db348069301afc127c4971e
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Development and characterization of a nanoemulsion containing propranolol for topical delivery

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