In vitro/in vivo evaluation of microspheres containing Exendin-4 for treatment of type 2 diabetes mellitus / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 925-930, 2014.
Artículo
en Chino
| WPRIM
| ID: wpr-859698
ABSTRACT
OBJECTIVE:
To prepare poly(lactic-co-glycolic acid) (PLGA) microspheres of Exendin-4 and evaluate its characteristics.METHODS:
Exendin-4 microspheres were prepared by different preparation methods (W/O/W, S/O/O and S/O/W method) and characterized for encapsulation efficiency by high-performance liquid chromatography (HPLC), particle size by laser particle size analyzer, surface morphology by scanning electron microscopy (SEM), and Exendin-4 stability by circular dichroism (CD). Release rate in vitro was determined, and the microspheres were administered subcutaneously to type 2 diabetic rats to determine its pharmacokinetics and pharmacodynamics.RESULTS:
Exendin-4 was successfully encapsulated into PLGA microspheres by W/O/W method. The average size was 25-30 μm. Exendin-4 encapsulation efficiency was 82.2%. CD confirmed that the structural integrity of the peptide was intact. The burst release in 24 h was 15.2% and the cumulated release in 28 d was up to 90% in vitro. Animal study demonstrated the drug release from microspheres in vivo and in vitro had a good correlation(r=0.9623) and the blood glucose level was controlled for 4 weeks by Exendin-4 microspheres.CONCLUSION:
The PLGA microspheres can be used for the controlled delivery of Exendin-4.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Idioma:
Chino
Revista:
Chinese Pharmaceutical Journal
Año:
2014
Tipo del documento:
Artículo
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