Camila de Oliveira Pacheco1, Marcelo Gomes de Gomes1, Manoel Rodrigues da Silva Neto1, Alcides José Martins Parisotto1, Renata Bem Dos Santos1, Tamara Ramos Maciel2, Ana Cláudia Funguetto Ribeiro3, Renata Giacomeli3, Sandra Elisa Haas4,5,6. 1. Postgraduate Program in Pharmaceutical Sciences, Federal University of Pampa, Campus Uruguaiana, BR 472, Km 7, Uruguaiana, RS, 97500-970, Brazil. 2. Postgraduate Program in Pharmaceutical Sciences, Federal University of Santa Maria, Av. Roraima no. 1000, Santa Maria, RS, 97105-900, Brazil. 3. Postgraduate Program in Biochemistry, Federal University of Pampa, Campus Uruguaiana, BR 472, Km 7, Uruguaiana, RS, 97500-970, Brazil. 4. Postgraduate Program in Pharmaceutical Sciences, Federal University of Pampa, Campus Uruguaiana, BR 472, Km 7, Uruguaiana, RS, 97500-970, Brazil. sandrahaas@unipampa.edu.br. 5. Postgraduate Program in Pharmaceutical Sciences, Federal University of Santa Maria, Av. Roraima no. 1000, Santa Maria, RS, 97105-900, Brazil. sandrahaas@unipampa.edu.br. 6. Postgraduate Program in Biochemistry, Federal University of Pampa, Campus Uruguaiana, BR 472, Km 7, Uruguaiana, RS, 97500-970, Brazil. sandrahaas@unipampa.edu.br.
Abstract
BACKGROUND: Surface functionalization enhances the properties and characteristics of polymeric nanocapsules (NCs) mainly due to the surface charge, surfactants, and polymer coating type. Curcumin (CUR) is a bioactive compound with several proven pharmacological properties and low bioavailability. This study aimed to develop anionic (poly-ɛ-caprolactone; PCL) and cationic (Eudragit® RS100 (EUD)) NCs prepared with sorbitan monostearate (Span 60®) or sorbitan monooleate (Span 80®), coated with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and optimized using 23 factorial analysis. Subsequently, the biological activity was evaluated. METHODS: A two-level, three-factor design (polymer, Span type, and TPGS concentration) was used. The biological effects of CUR-loaded TPGS-coated cationic and anionic NCs were assessed in apomorphine-induced stereotyped behavior in rats. RESULTS: The type of polymer (anionic or cationic) and Span® had a factorial influence on the physical and chemical characteristics of NCs according to the changes in TPGS concentrations. Both cationic and anionic CUR-NCs could block apomorphine-induced behavioral changes. CONCLUSIONS: The CUR-loaded TPGS-coated NCs proved to be a promising brain delivery system.
BACKGROUND: Surface functionalization enhances the properties and characteristics of polymeric nanocapsules (NCs) mainly due to the surface charge, surfactants, and polymer coating type. Curcumin (CUR) is a bioactive compound with several proven pharmacological properties and low bioavailability. This study aimed to develop anionic (poly-ɛ-caprolactone; PCL) and cationic (Eudragit® RS100 (EUD)) NCs prepared with sorbitan monostearate (Span 60®) or sorbitan monooleate (Span 80®), coated with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and optimized using 23 factorial analysis. Subsequently, the biological activity was evaluated. METHODS: A two-level, three-factor design (polymer, Span type, and TPGS concentration) was used. The biological effects of CUR-loaded TPGS-coated cationic and anionic NCs were assessed in apomorphine-induced stereotyped behavior in rats. RESULTS: The type of polymer (anionic or cationic) and Span® had a factorial influence on the physical and chemical characteristics of NCs according to the changes in TPGS concentrations. Both cationic and anionic CUR-NCs could block apomorphine-induced behavioral changes. CONCLUSIONS: The CUR-loaded TPGS-coated NCs proved to be a promising brain delivery system.
Authors: Renata Bem Dos Santos; Kelly Ayumi Nakama; Camila Oliveira Pacheco; Marcelo Gomes de Gomes; Jaqueline Ferreira de Souza; Ana Claudia de Souza Pinto; Fernanda Alice de Oliveira; Amanda Luisa da Fonseca; Fernando Varotti; André Ricardo Fajardo; Sandra Elisa Haas Journal: Mater Sci Eng C Mater Biol Appl Date: 2020-08-11 Impact factor: 7.328
Authors: Simone M Vieira; Luana R Michels; Katiane Roversi; Vinícia G Metz; Barbra K S Moraes; Eduarda M Piegas; Rodrigo J Freddo; André Gundel; Teresa Dalla Costa; Marilise E Burger; Letícia M Colomé; Sandra E Haas Journal: Colloids Surf B Biointerfaces Date: 2016-05-25 Impact factor: 5.268