Atovaquone-loaded nanocapsules: influence of the nature of the polymer on their in vitro characteristics

被引:49
作者
Cauchetier, E
Deniau, M
Fessi, H
Astier, A
Paul, M
机构
[1] CHU Henri Mondor, Serv Pharm, Lab Pharmacotech, F-94010 Creteil, France
[2] CHU Henri Mondor, Parasitol Lab, F-94010 Creteil, France
[3] Univ H Poincare, Lab Pharm Clin, F-54000 Nancy, France
[4] Fac Pharm Claude Bernanrd, Lab Genie Pharmacotech & Biogalen, F-69000 Lyon, France
关键词
atovaquone; nanocapsules; PLA; PLAGA; PECL;
D O I
10.1016/S0378-5173(02)00556-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Nanocapsules with atovaquone concentration of 1000 mug/ml were prepared according to the interfacial deposition technique using different polymers: poly-E-caprolactone (PECL), poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLAGA). The following characteristics of nanoparticles were determined: percentage of encapsulation of atovaquone, percentage of encapsulation of benzyl benzoate (BB), nanoparticle size, nanoparticle wall thickness, suspension pH, and in vitro stability. The different formulations showed similar characteristics: maximal percentage of encapsulation (100%), particle size of approximately 230 nm, neutral pH and wall thickness of approximately 20 nm. The type of polymer used was the main factor influencing stability, in decreasing order: PECL > PLA > PLAGA. No release of atovaquone or benzylbenzoate was noted with PECL nanoparticles over 4 months. Release of atovaquone (25.9%) was found with PLA nanoparticles at 4 months. Release of both atovaquone (18.9%) and benzylbenzoate (54.2%) was noted with PLAGA nanoparticles from the third month, indicating a disruption of the nanoparticle membrane.
引用
收藏
页码:273 / 281
页数:9
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