Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate

Gisela Bevilacqua Rolfsen Ferreira da Silva,1 Maria Virginia Scarpa,1 Iracilda Zepone Carlos,2 Marcela Bassi Quilles,2 Raphael Carlos Comeli Lia,3 Eryvaldo Socrates Tabosa do Egito,4 Anselmo Gomes de Oliveira1 1Departamento de Fármacos e Medicamentos, 2Departamento de Análise...

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Autores principales:	Silva GB, Scarpa MV, Carlos IZ, Quilles MB, Lia RC, Egito ES, Oliveira AG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7ba04ef0ed224b97ad75bb126b767c1d
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spelling	oai:doaj.org-article:7ba04ef0ed224b97ad75bb126b767c1d2021-12-02T02:31:41ZOil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate1178-2013https://doaj.org/article/7ba04ef0ed224b97ad75bb126b767c1d2015-01-01T00:00:00Zhttp://www.dovepress.com/oil-in-water-biocompatible-microemulsion-as-a-carrier-for-the-antitumo-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Gisela Bevilacqua Rolfsen Ferreira da Silva,1 Maria Virginia Scarpa,1 Iracilda Zepone Carlos,2 Marcela Bassi Quilles,2 Raphael Carlos Comeli Lia,3 Eryvaldo Socrates Tabosa do Egito,4 Anselmo Gomes de Oliveira1 1Departamento de Fármacos e Medicamentos, 2Departamento de Análises Clínicas, UNESP–Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, PPG em Nanotecnologia Farmacêutica, Rodovia Araraquara-Jaú Km 01, Araraquara, SP, Brazil; 3Instituto de Patologia Cirúrgica e Citopatologia (IPC), Araraquara, SP, Brazil; 4UFRN–Universidade Federal do Rio Grande do Norte, Programa de Pós-graduação em Ciências da Saúde, Natal, RN, Brazil Abstract: Methyl dihydrojasmonate (MJ) has been studied because of its application as an antitumor drug compound. However, as MJ is a poorly water-soluble compound, a suitable oil-in-water microemulsion (ME) has been studied in order to provide its solubilization in an aqueous media and to allow its administration by the parenteral route. The ME used in this work was characterized on the pseudo-ternary phase diagram by dynamic light scattering and rheological measurements. Regardless of the drug presence, the droplet size was directly dependent on the oil/surfactant (O/S) ratio. Furthermore, the drug incorporation into the ME significantly increased the ME diameter, mainly at low O/S ratios. The rheological evaluation of the systems showed that in the absence of drug a Newtonian behavior was observed. On the other hand, in the presence of MJ the ME systems revealed pseudoplastic behavior, independently of the O/S ratio. The in vivo studies demonstrated that not only was the effect on the tumor inhibition inversely dependent on the MJ-loaded ME administered dose, but also it was slightly higher than the doxorubicin alone, which was used as the positive control. Additionally, a small antiangiogenic effect for MJ-loaded ME was found at doses in which it possesses antitumor activity. MJ revealed to be nontoxic at doses higher than 350 mg/kg, which was higher than the dose that provides tumor-inhibition effect in this study. Because the MJ-loaded ME was shown to have anticancer activity comparable to doxorubicin, the ME described here may be considered a suitable vehicle for parenteral administration of MJ. Keywords: antitumor drug, nanocarrier, angiogenesis inhibition, antitumor activity, Ehrlich ascitic tumorSilva GBScarpa MVCarlos IZQuilles MBLia RCEgito ESOliveira AGDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 585-594 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Silva GB Scarpa MV Carlos IZ Quilles MB Lia RC Egito ES Oliveira AG Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
description	Gisela Bevilacqua Rolfsen Ferreira da Silva,1 Maria Virginia Scarpa,1 Iracilda Zepone Carlos,2 Marcela Bassi Quilles,2 Raphael Carlos Comeli Lia,3 Eryvaldo Socrates Tabosa do Egito,4 Anselmo Gomes de Oliveira1 1Departamento de Fármacos e Medicamentos, 2Departamento de Análises Clínicas, UNESP–Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, PPG em Nanotecnologia Farmacêutica, Rodovia Araraquara-Jaú Km 01, Araraquara, SP, Brazil; 3Instituto de Patologia Cirúrgica e Citopatologia (IPC), Araraquara, SP, Brazil; 4UFRN–Universidade Federal do Rio Grande do Norte, Programa de Pós-graduação em Ciências da Saúde, Natal, RN, Brazil Abstract: Methyl dihydrojasmonate (MJ) has been studied because of its application as an antitumor drug compound. However, as MJ is a poorly water-soluble compound, a suitable oil-in-water microemulsion (ME) has been studied in order to provide its solubilization in an aqueous media and to allow its administration by the parenteral route. The ME used in this work was characterized on the pseudo-ternary phase diagram by dynamic light scattering and rheological measurements. Regardless of the drug presence, the droplet size was directly dependent on the oil/surfactant (O/S) ratio. Furthermore, the drug incorporation into the ME significantly increased the ME diameter, mainly at low O/S ratios. The rheological evaluation of the systems showed that in the absence of drug a Newtonian behavior was observed. On the other hand, in the presence of MJ the ME systems revealed pseudoplastic behavior, independently of the O/S ratio. The in vivo studies demonstrated that not only was the effect on the tumor inhibition inversely dependent on the MJ-loaded ME administered dose, but also it was slightly higher than the doxorubicin alone, which was used as the positive control. Additionally, a small antiangiogenic effect for MJ-loaded ME was found at doses in which it possesses antitumor activity. MJ revealed to be nontoxic at doses higher than 350 mg/kg, which was higher than the dose that provides tumor-inhibition effect in this study. Because the MJ-loaded ME was shown to have anticancer activity comparable to doxorubicin, the ME described here may be considered a suitable vehicle for parenteral administration of MJ. Keywords: antitumor drug, nanocarrier, angiogenesis inhibition, antitumor activity, Ehrlich ascitic tumor
format	article
author	Silva GB Scarpa MV Carlos IZ Quilles MB Lia RC Egito ES Oliveira AG
author_facet	Silva GB Scarpa MV Carlos IZ Quilles MB Lia RC Egito ES Oliveira AG
author_sort	Silva GB
title	Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
title_short	Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
title_full	Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
title_fullStr	Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
title_full_unstemmed	Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
title_sort	oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/7ba04ef0ed224b97ad75bb126b767c1d
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Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate

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