Preparation and evaluation of lung targeting microspheres for protionamide in vitro and in vivo
- Author:
Zhen-Yong GUO
1
Author Information
1. Pharmaceutical Department of Peking University
- Publication Type:Journal Article
- Keywords:
Lung targeting;
Microspheres;
Poly(lactic-co-glycollic acid);
Protionamide
- From:
Chinese Pharmaceutical Journal
2012;47(22):1834-1838
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE: To testify the feasibility of targeted delivery of protionamide to lung through the iv administration of the biodegradable poly(lactic-co-glycollic acid) (PLGA) microspheres. METHODS: Based on the single-factor study, the preparation of protionamide-PLGA microspheres was optimized. The surface morphology of the microspheres was observed by scanning electron microscope (SEM). The mean diameter and the size distribution of microsphere, the drug loading, the incorporation efficiency, drug release in vitro, stability and tissue distribution after intravenous administration were also evaluated, respectively. RESULTS: Protionamide-PLGA microspheres were regular and spherical in shape. The average particle size was (9.86 ± 1.38) μm and over 81.53% of the microspheres was in the range of 7-15 μn. The drug loading and encapsulated ratio was (32.70 ± 0.37)% and (8.48 ± 0.24)%, respectively. The in vitro drug release could be well fitted by the Higuchi equation (Q=4.4303t1/2 ± 7.7241, r=0.9913). Compared with the aqueous formulation, the drug level in lung of BALB/C mice in microsphere group was much higher, and also kept for longer time. CONCLUSION: The protionamide-PLGA microspheres prepared in this study show significant sustained release and lung targeting effect.
