Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations.
Nanomedicine (Lond)
; 14(7): 889-910, 2019 Apr.
Article
em En
| MEDLINE
| ID: mdl-30874464
ABSTRACT
AIM:
To prepare nanostructured lipid carriers (NLCs) loaded with asenapine maleate (ASPM) to increase its oral bioavailability by intestinal lymphatic uptake. MATERIALS &METHODS:
ASPM-NLCs were prepared by ultrasound dispersion technique, by adopting Design of Experiment approach, and characterized.RESULTS:
The optimized formulation exhibited good physicochemical parameters. Differential scanning calorimetry and x-ray diffraction studies indicated the amorphized nature of ASPM in lipid matrix. In vitro drug release study indicated the sustained release of drug from NLCs. ASPM-NLCs showed greater permeability across Caco2 cells and everted rat ileum. ASPM-NLCs showed greater cellular uptake, superior preclinical oral bioavailability and higher efficacy in reducing the L-DOPA-carbidopa-induced locomotor count compared with plain drug.CONCLUSION:
ASPM-NLCs were successfully developed that showed enhanced performance both in vitro and in vivo.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Portadores de Fármacos
/
Nanoestruturas
/
Compostos Heterocíclicos de 4 ou mais Anéis
/
Lipídeos
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Maleatos
Limite:
Animals
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Humans
/
Male
Idioma:
En
Revista:
Nanomedicine (Lond)
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Índia