β-Cyclodextrin complexation as an effective drug delivery system for meropenem

被引:41
|
作者
Paczkowska, Magdalena [1 ]
Mizera, Mikolaj [1 ]
Szymanowska-Powalowska, Daria [2 ]
Lewandowska, Kornelia [3 ]
Blaszczak, Wioletta [4 ]
Goscianska, Joanna [5 ]
Pietrzak, Robert [5 ]
Cielecka-Piontek, Judyta [1 ]
机构
[1] Poznan Univ Med Sci, Fac Pharm, Dept Pharmaceut Chem, Grunwaldzka 6, PL-60780 Poznan, Poland
[2] Poznan Univ Life Sci, Dept Biotechnol & Food Microbiol, Wojska Polskiego 48, Poznan, Poland
[3] Polish Acad Sci, Inst Mol Phys, Dept Mol Crystals, Smoluchowskiego 17, PL-60179 Poznan, Poland
[4] Polish Acad Sci, Inst Anim Reprod & Food Res, Tuwima 10, PL-10748 Olsztyn, Poland
[5] Adam Mickiewicz Univ, Fac Chem, Umultowska 89b, PL-61614 Poznan, Poland
关键词
Meropenem; beta-Cyclodextrin; Inclusion complex; Solubility; Stability; Microbiological activity; PHYSICOCHEMICAL CHARACTERIZATION; LACTAM ANTIBIOTICS; GAMMA-CYCLODEXTRIN; AQUEOUS-SOLUTION; SOLID-STATE; INCLUSION; STABILITY; CARBAPENEMS; DEGRADATION; TUBERCULOSIS;
D O I
10.1016/j.ejpb.2015.10.013
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Following the preparation of an inclusion complex of beta-cyclodextrin and meropenem, methods based on FT-IR, Raman and DSC were used for its characterization. An analysis of changes in the stability of meropenem after complexation showed that the complex may serve as a valuable delivery system significantly contributing to enhanced meropenem stability in aqueous solutions and in the solid phase. Due to a sustained transfer of meropenem from the cavity of the cyclodextrin it was possible to maintain a constant desired meropenem concentration over a period of 20 h, as confirmed by a release study. An evaluation of microbial activity not only demonstrated that the bactericidal action of meropenem was not stopped as a result of complexation but even pointed to greater growth inhibition in certain clinically important strains. The fact that investigations of meropenem stability and microbial activity proposed the carbonyl groups as those domains of a meropenem molecule that are instrumental in the formation of a complex with beta-cyclodextrin supports the findings of theoretical studies based on molecular modeling. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:24 / 34
页数:11
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