Administração transdérmica de cloridrato de raloxifeno encapsulado em nanopartículas lipídicas: estudos de pré-formulação para seleção dos lipídeos e tensoativos

• Ano de defesa: 2017
• Autor(a) principal: Alves, Guilherme Liberato
• Orientador(a): Taveira, Stephânia Fleury
• Banca de defesa: Taveira, Stephânia Fleury, Marreto, Ricardo Neves, Gelfuso, Guilherme Martins
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Federal de Goiás
• Programa de Pós-Graduação: Programa de Pós-graduação em Ciências Farmacêuticas (FF)
• Departamento: Faculdade de Farmácia - FF (RG)
• País: Brasil
• Palavras-chave em Português: Raloxifeno; Estudo de compatibilidade; Estudos de liberação e permeação cutânea; Carreadores lipídicos nanoestruturados
• Palavras-chave em Inglês: Compatibility studies; Release and permeation studies; Nanostructured lipidic carriers; Raloxifene
• Área do conhecimento CNPq: CIENCIAS DA SAUDE::FARMACIA
• Link de acesso: http://repositorio.bc.ufg.br/tede/handle/tede/11662

Introduction: Raloxifene hydrochloride (RLX) is a widely prescribed drug for the treatment of osteoporosis and breast cancer. However, RLX presents a low oral bioavailability (2%), being an excellent candidate for transdermal drug delivery. The aim of this work was to develop nanostructured lipid carriers (NLC) containing RLX for transdermal drug delivery. In order to choose proper excipients, a compatibility study was performed. Methodology: Compatibility study was performed with differential scanning calorimeter (DSC), thermogravimetric anaysis (TGA), derivative thermogravimetry (DTG), isothermal stress testing (IST) and solubility study. RLX quantification was performed by high performance liquid chromatography (HPLC). After choosing the excipients, CLN were obtained by the microemulsion technique. Characterization was performed for mean diameter, polidispersivity index (PdI), zeta potential, entrapment efficiency (EE%) and stability. In vitro release and permeation studies were performed in Franz diffusion cells. Results and discussion. Conclusions: Drug-excipient compatibility studies allowed the development of stable and monodisperse CLN, capable of controlling drug release and increase its permeation in the skin when compared to the non-encapsulated drug in the control formulation.