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

Abstract

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 ~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.