Your browser doesn't support javascript.
loading
Thermo-reversible in situ forming implant with nanostructured lipid carriers (NLC) as a delivery system for the administration of estradiol valerate.
Pineda-Hernández, María Teresa; Pérez-Urizar, José Trinidad; Ganem-Rondero, Adriana.
Afiliação
  • Pineda-Hernández MT; División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, 54740, Cuautitlán Izcalli, Estado de México, Mexico.
  • Pérez-Urizar JT; Facultad de Ciencias Químicas, Universidad Autónoma de San Luis Potosí, San Luis Potosí, Mexico.
  • Ganem-Rondero A; División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, 54740, Cuautitlán Izcalli, Estado de México, Mexico. ganemq@hotmail.com.
Drug Deliv Transl Res ; 10(5): 1393-1402, 2020 10.
Article em En | MEDLINE | ID: mdl-31942699
A thermo-reversible in situ forming implant, based on the combination of Pluronic® F-127 and Pluronic® F-68 with nanostructured lipid carriers (NLC), was formulated with the aim of achieving the sustained release of estradiol valerate (EV). EV-loaded NLC, prepared by the hot high-pressure homogenization technique, presented an entrapment efficiency of 90 ± 2.9 %, a particle size (PS) of 122 ± 11.2 nm, a polydispersity index (PDI) of 0.344 ± 0.07, and a zeta potential (ZP) of - 10.5 ± 1.3 mV. Once obtained, NLC were then included in a thermo-reversible gel (EV-loaded NLC gel), which was characterized by its rheological behavior, gelation temperature, and injectability. The in vitro release tests showed that the EV-loaded NLC gel delayed the release significantly, in comparison with a solution of the drug and with the EV-loaded NLC. The EV-loaded NLC gel and a commercially available suspension containing estradiol were administered parenterally to rabbits. A 16.8-fold greater AUC and a 40-fold higher Cmax were obtained with the EV-loaded NLC gel, compared to the commercial suspension. A rapid initial release of EV in vivo, from the EV-loaded NLC gel, suggests that it is necessary to adjust the ratio of the copolymers or to include in the gel an additive that improves gelation time and gel strength, in order to achieve a sustained release. An interesting observation was that the in vitro profile, which has a three-phase behavior, coincides with what was observed in the in vivo study. Graphical abstract.
Assuntos
Palavras-chave
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: Portadores de Fármacos / Nanoestruturas / Estradiol / Lipídeos Limite: Animals Idioma: En Revista: Drug Deliv Transl Res Ano de publicação: 2020 Tipo de documento: Article País de afiliação: México País de publicação: Estados Unidos
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: Portadores de Fármacos / Nanoestruturas / Estradiol / Lipídeos Limite: Animals Idioma: En Revista: Drug Deliv Transl Res Ano de publicação: 2020 Tipo de documento: Article País de afiliação: México País de publicação: Estados Unidos