Conjugation of β-Adrenergic Antagonist Alprenolol to Implantable Polymer-Aescin Matrices for Local Delivery

Polymers

Ewa Oledzka²  Dagmara Pachowska²  Marcin Sobczak²  Agnieszka Lis-Cieplak²  Grzegorz Nalecz-Jawecki¹  Anna Zgadzaj¹  Waclaw Kolodziejski² 

[1] Department of Environmental Health Science, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Banacha 1,Warsaw 02-097, Poland; E-Mails:;Department of Inorganic and Analytical Chemistry, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Banacha 1, Warsaw 02-097, Poland; E-Mails:

关键词: biodegradable polymers;    sustained release/delivery;    macromolecular drug delivery systems;    aescin;    alprenolol;    conjugation;   

DOI  :  10.3390/polym7091484

来源: mdpi

【 摘 要 】

The sustained release of alprenolol, a β-adrenergic antagonist, could be beneficial for the treatment of various heart diseases while reducing the side effects resulting from its continuous use. The novel and branched copolymers uniquely composed of biodegradable components (lactide and glycolide) have been synthesized using natural and therapeutically-efficient β-aescin-initiator, and consequently characterized to determine their structures and physicochemical properties. The obtained matrices were not cyto- and genotoxic towards bacterial luminescence, protozoan, and Salmonella typhimurium TA1535. The copolymers release the drug in vitro in a sustained manner and without burst release. The value of the drug released was strongly dependent on the copolymer composition and highly correlated with the hydrolytic matrices’ degradation results.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.