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Ball-milled solid dispersions of BCS Class IV drugs: Impact on the dissolution rate and intestinal permeability of acyclovir.
Nart, Viviane; França, Maria Terezinha; Anzilaggo, Daiane; Riekes, Manoela Klüppel; Kratz, Jadel Müller; de Campos, Carlos Eduardo Maduro; Simões, Cláudia Maria Oliveira; Stulzer, Hellen Karine.
Afiliação
  • Nart V; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • França MT; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • Anzilaggo D; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • Riekes MK; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • Kratz JM; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • de Campos CE; Departamento de Física, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • Simões CM; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.
  • Stulzer HK; Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil. Electronic address: hellen.stulzer@gmail.com.
Mater Sci Eng C Mater Biol Appl ; 53: 229-38, 2015 Aug.
Article em En | MEDLINE | ID: mdl-26042711
Acyclovir, an analog of 2'-deoxyguanosine, is one of the most important drugs in the current approved antiviral treatment. However, it's biopharmaceutical properties, contribute to acyclovir's poor oral bioavailability, which restricts the clinical use of the drug. In this view, the aim of this work was to improve the dissolution rate and intestinal permeability of acyclovir through the development of ball milling solid dispersions with the hydrophilic carriers Pluronic F68®, hydroxypropylmethyl cellulose K100M® and chitosan. Solid dispersions were obtained and completely characterized through different solid state techniques. The solid state data demonstrated a decrease in the crystallinity (amorphous phase and defects) and the presence of hydrogen bonds for SD HPMC and SD CTS. The enhancement of dissolution rates was observed for all SDs developed. In addition, no detrimental effects over the in vitro antiviral activity were detected. The solid dispersions with Pluronic F68® significantly improved the intestinal permeability of acyclovir across Caco-2 cells. In summary, the SDs developed in this study could be considered as potential systems for solid dosage forms containing acyclovir with superior biopharmaceutical properties.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Aciclovir / Portadores de Fármacos / Modelos Biológicos Limite: Humans Idioma: En Revista: Mater Sci Eng C Mater Biol Appl Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Aciclovir / Portadores de Fármacos / Modelos Biológicos Limite: Humans Idioma: En Revista: Mater Sci Eng C Mater Biol Appl Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda