Novel Biodegradable Polyester Poly(Propylene Succinate): Synthesis and Application in the Preparation of Solid Dispersions and Nanoparticles of a Water-Soluble Drug

被引:42
作者
Bikiaris, Dimitrios N. [1 ]
Papageorgiou, George Z. [1 ]
Papadimitriou, Sofia A. [1 ]
Karavas, Evangelos [2 ]
Avgoustakis, Konstantinos [3 ]
机构
[1] Aristotle Univ Thessaloniki, Dept Chem, Lab Organ Chem Technol, Thessaloniki 54124, Greece
[2] Pharmaceut Ind, Pharmathen SA, Pallini Attikis 15351, Attica, Greece
[3] Univ Patras, Dept Pharm, Pharmaceut Technol Lab, Patras 26500, Greece
关键词
fluvastatin; melt mixing; nanoparticles; poly(propylene succinate); solid dispersions; ENZYMATIC DEGRADATION; RENEWABLE SOURCES; RELEASE; ACID; POLY(EPSILON-CAPROLACTONE); 1,3-PROPANEDIOL; FLUVASTATIN; EFFICACY; DELIVERY; POLYMERS;
D O I
10.1208/s12249-008-9184-z
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
Poly(propylene succinate) (PPSu) polymers of average molecular weights from 2,800 to 13,100 g/mol were synthesized and characterized with regard to crystallinity, thermal properties, and cytocompatibility. Higher molecular weight samples exhibited lower degree of crystallinity and melted at lower temperatures. Melting of the polymer appeared to begin at 38 degrees C. PPSu cytocompatibility was investigated based on human umbilical vein endothelial cells viability in the presence of increasing concentrations of polymer, and it was found that PPSu exhibited comparable cytocompatibility with poly (DL- lactide). The feasibility of applying PPSu as a drug carrier was shown for the first time, as solid dispersions and nanoparticles of sodium fluvastatin based in PPSu were prepared. Drug release rates decreased with increasing the molecular weight of PPSu in both solid dispersions and nanoparticles. For dispersions prepared from PPSu of the same molecular weight, drug release rates increased with drug loading. It appears that PPSu applicability as a drug carrier warrants further consideration.
引用
收藏
页码:138 / 146
页数:9
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