Ampicillin-Ester Bonded Branched Polymers: Characterization, Cyto-, Genotoxicity and Controlled Drug-Release Behaviour

Molecules

Ewa Oledzka²  Marcin Sobczak²  Grzegorz Nalecz-Jawecki¹  Agata Skrzypczak¹ 

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

关键词: controlled release;    drug delivery system;    ampicillin;    cyto- and genotoxicity macromolecular conjugate;   

DOI  :  10.3390/molecules19067543

来源: mdpi

【 摘 要 】

The development and characterization of novel macromolecular conjugates of ampicillin using branched biodegradable polymers has been described in this study. The conjugates have been prepared coupling the β-lactam antibiotic with branched polymer matrices based on the natural oligopeptide core. The cyto- and genotoxicity of the synthesized polymers were evaluated with a bacterial luminescence test, two protozoan assays and Salmonella typhimurium TA1535. The presence of a newly formed covalent bond between the drug and the polymer matrices was confirmed by ¹H-NMR and FTIR studies. A drug content (15.6 and 10.2 mole %) in the macromolecular conjugates has been determined. The obtained macromolecular products have been subjected to further in vitro release studies. The total percentage of ampicillin released after 21 days of incubation was nearly 60% and 14% and this resulted from the different physicochemical properties of the polymeric matrices. This is the first report on the application of branched biodegradable polymeric matrices for the covalent conjugation of ampicillin. The obtained results showed that the synthesized macromolecular drug-conjugates might slowly release the active drug molecule and improve the pharmacokinetics of ampicillin.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.