Preparation and Properties of Protamine/Pectin-Ag Biopolymer Microcapsules Containing a 2-Arylaminopyrimidine Derivative

被引：2

作者：

Gilevskaya, K. S. ^{[1
]}

Ignatovich, Zh. V. ^{[1
]}

Golubeva, M. B. ^{[2
]}

Koroleva, E. V. ^{[1
]}

Agabekov, V. E. ^{[1
]}

机构：

[1] Natl Acad Sci Belarus, Inst Chem New Mat, Minsk 220141, BELARUS

[2] Natl Acad Sci Belarus, Inst Bioorgan Chem, Minsk 220141, BELARUS

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2018年 / 51卷 / 10期

关键词：

microcapsules; pectin; Ag nanoparticles; imatinib analog; cytostatic activity; BCR-ABL; IMATINIB;

D O I：

10.1007/s11094-018-1717-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A synthetic 2-arylaminopyrimidine derivative (analog of imatinib mesylate) was incorporated into multilayer polyelectrolyte microcapsules prepared by alternating adsorption of protamine sulfate and pectin-Ag nanocomposite. The encapsulation effectiveness (EE) from an aqueous solution of the compound (4 mg/mL) was similar to 70% and reached 28 mass%. The release kinetics from the microcapsules depended significantly on the solution pH and ionic strength. Release of the imatinib analog was prolonged most in alkaline solutions. In vitro experiments on hemoblast suspension cultures showed that microencapsulation of the 2-arylaminopyrimidine derivative changed its antitumor activity and lowered the IC50 value by 1.4 - 2.2 times.

引用

页码：922 / 927

页数：6

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