Long-term controlled release of PLGA microparticles containing antidepressant mirtazapine

被引:9
作者
Vyslouzil, Jakub [1 ]
Dolezel, Petr [1 ]
Kejdusova, Martina [1 ]
Kostal, Vratislav [2 ]
Benes, Ludvik [3 ]
Dvorackova, Katerina [1 ]
机构
[1] Univ Vet & Pharmaceut Sci Brno, Fac Pharm, Dept Pharmaceut, Palackeho 1-3, Brno 61242, Czech Republic
[2] Tescan, Brno, Czech Republic
[3] Univ Pardubice, Fac Chem Technol, Joint Lab Solid State Chem, Pardubice, Czech Republic
关键词
Drug release; kinetics; PLGA; solvent evaporation method; BIODEGRADABLE POLYMERIC MICROSPHERES; DRUG-DELIVERY SYSTEMS; IN-VITRO; ACID) MICROSPHERES; SUSTAINED-RELEASE; PROTEIN; MICROENCAPSULATION; FORMULATION; MORPHOLOGY; PROFILES;
D O I
10.3109/10837450.2014.991874
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of the study was to prepare PLGA microparticles for prolonged release of mirtazapine by o/w solvent evaporation method and to evaluate effects of PVA concentration and organic solvent choice on microparticles characteristics (encapsulation efficiency, drug loading, burst effect, microparticle morphology). Also in vitro drug release tests were performed and the results were correlated with kinetic model equations to approximate drug release mechanism. It was found that dichloromethane provided microparticles with better qualities (encapsulation efficiency 64.2%, yield 79.7%). Interaction between organic solvent effect and effect of PVA concentration was revealed. The prepared samples released the drug for 5 days with kinetics very close to that of zero order (R-2=0.9549 - 0.9816). According to the correlations, the drug was probably released by a combination of diffusion and surface erosion, enhanced by polymer swelling and chain relaxation.
引用
收藏
页码:214 / 221
页数:8
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