Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles

Guilherme Carneiro,1 Elton Luiz Silva,1 Layssa Alves Pacheco,1 Elaine Maria de Souza-Fagundes,2 Nat&aacute;ssia Caroline Resende Corr&ecirc;a,3 Alfredo Miranda de Goes,3 M&ocirc;nica Cristina de Oliveira,1 Lucas Ant&ocirc;nio Miranda Ferreira11Department of Pharmaceut...

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Autores principales:	Carneiro G, Silva EL, Pacheco LA, Souza-Fagundes EM, Corr&ecirc;a NC, Goes AM, Oliveira MC, Ferreira LA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6595758cc98a42aaa7556a0d085c2040
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spelling	oai:doaj.org-article:6595758cc98a42aaa7556a0d085c20402021-12-02T07:15:35ZFormation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles1176-91141178-2013https://doaj.org/article/6595758cc98a42aaa7556a0d085c20402012-12-01T00:00:00Zhttp://www.dovepress.com/formation-of-ion-pairing-as-an-alternative-to-improve-encapsulation-an-a11734https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Guilherme Carneiro,1 Elton Luiz Silva,1 Layssa Alves Pacheco,1 Elaine Maria de Souza-Fagundes,2 Nat&aacute;ssia Caroline Resende Corr&ecirc;a,3 Alfredo Miranda de Goes,3 M&ocirc;nica Cristina de Oliveira,1 Lucas Ant&ocirc;nio Miranda Ferreira11Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, Brazil; 2Department of Physiology and Biophysics, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, Brazil; 3Department of Biochemistry and Immunology, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, BrazilAbstract: This work aims to develop solid lipid nanoparticles (SLNs) loaded with retinoic acid (RA) to evaluate the influence of two lipophilic amines, stearylamine (SA) and benethamine (BA), and one hydrophilic, triethylamine (TA), on drug-encapsulation efficiency (EE) and cytotoxicity in cancer cell lines. The SLNs were characterized for EE, size, and zeta potential. The mean particle size decreased from 155 &plusmn; 1 nm (SLNs without amine) to 104 &plusmn; 4, 95 &plusmn; 1, and 96 &plusmn; 1 nm for SLNs prepared with SA, BA, and TA, respectively. SA-RA-loaded SLNs resulted in positively charged particles, whereas those with TA and BA were negatively charged. The EEs were significantly improved with the addition of the amines, and they increased from 36% &plusmn; 6% (without amine) to 97% &plusmn; 2%, 90% &plusmn; 2%, and 100% &plusmn; 1% for SA, TA, and BA, respectively. However, stability studies showed higher EE for BA-RA-loaded SLNs than TA-RA-loaded SLNs after 30 days. The formulations containing SA loaded or unloaded (blank SLNs) with RA were cytotoxic in normal and cancer cell lines. In contrast, the blank SLNs containing TA or BA did not show cytotoxicity in human breast adenocarcinoma cells (MCF-7), while RA-loaded SLNs with the respective amines were significantly more cytotoxic than free RA. Furthermore, the cytotoxicity of BA-RA-loaded SLNs was significantly higher than TA-RA-loaded SLNs. These findings are in agreement with the data obtained in the evaluation of subdiploid DNA content and cell-cycle analysis, which showed better anticancer activity for BA-RA-loaded SLNs than TA-RA-loaded SLNs and free RA. Taken together, these findings suggest that the BA-RA-loaded SLN formulation is a promising alternative for the intravenous administration of RA in the treatment of cancer.Keywords: solid lipid nanoparticles, all-trans retinoic acid, cancer, treatment, antitumor activity, ion pairingCarneiro GSilva ELPacheco LASouza-Fagundes EMCorr&ecirc;a NCGoes AMOliveira MCFerreira LADove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 6011-6020 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Carneiro G Silva EL Pacheco LA Souza-Fagundes EM Corr&ecirc;a NC Goes AM Oliveira MC Ferreira LA Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
description	Guilherme Carneiro,1 Elton Luiz Silva,1 Layssa Alves Pacheco,1 Elaine Maria de Souza-Fagundes,2 Nat&aacute;ssia Caroline Resende Corr&ecirc;a,3 Alfredo Miranda de Goes,3 M&ocirc;nica Cristina de Oliveira,1 Lucas Ant&ocirc;nio Miranda Ferreira11Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, Brazil; 2Department of Physiology and Biophysics, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, Brazil; 3Department of Biochemistry and Immunology, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, BrazilAbstract: This work aims to develop solid lipid nanoparticles (SLNs) loaded with retinoic acid (RA) to evaluate the influence of two lipophilic amines, stearylamine (SA) and benethamine (BA), and one hydrophilic, triethylamine (TA), on drug-encapsulation efficiency (EE) and cytotoxicity in cancer cell lines. The SLNs were characterized for EE, size, and zeta potential. The mean particle size decreased from 155 &plusmn; 1 nm (SLNs without amine) to 104 &plusmn; 4, 95 &plusmn; 1, and 96 &plusmn; 1 nm for SLNs prepared with SA, BA, and TA, respectively. SA-RA-loaded SLNs resulted in positively charged particles, whereas those with TA and BA were negatively charged. The EEs were significantly improved with the addition of the amines, and they increased from 36% &plusmn; 6% (without amine) to 97% &plusmn; 2%, 90% &plusmn; 2%, and 100% &plusmn; 1% for SA, TA, and BA, respectively. However, stability studies showed higher EE for BA-RA-loaded SLNs than TA-RA-loaded SLNs after 30 days. The formulations containing SA loaded or unloaded (blank SLNs) with RA were cytotoxic in normal and cancer cell lines. In contrast, the blank SLNs containing TA or BA did not show cytotoxicity in human breast adenocarcinoma cells (MCF-7), while RA-loaded SLNs with the respective amines were significantly more cytotoxic than free RA. Furthermore, the cytotoxicity of BA-RA-loaded SLNs was significantly higher than TA-RA-loaded SLNs. These findings are in agreement with the data obtained in the evaluation of subdiploid DNA content and cell-cycle analysis, which showed better anticancer activity for BA-RA-loaded SLNs than TA-RA-loaded SLNs and free RA. Taken together, these findings suggest that the BA-RA-loaded SLN formulation is a promising alternative for the intravenous administration of RA in the treatment of cancer.Keywords: solid lipid nanoparticles, all-trans retinoic acid, cancer, treatment, antitumor activity, ion pairing
format	article
author	Carneiro G Silva EL Pacheco LA Souza-Fagundes EM Corr&ecirc;a NC Goes AM Oliveira MC Ferreira LA
author_facet	Carneiro G Silva EL Pacheco LA Souza-Fagundes EM Corr&ecirc;a NC Goes AM Oliveira MC Ferreira LA
author_sort	Carneiro G
title	Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
title_short	Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
title_full	Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
title_fullStr	Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
title_full_unstemmed	Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
title_sort	formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/6595758cc98a42aaa7556a0d085c2040
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Formation of ion pairing as an alternative to improve encapsulation and anticancer activity of all-trans retinoic acid loaded in solid lipid nanoparticles

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