Linear copolymers based on cholinium functionalized with antibiotic anions for single– and dual–drug delivery systems

Author:

Keihankhadiv Shadi1,Neugebauer Dorota1

Affiliation:

1. Silesian University of Technology

Abstract

Abstract

The novel single and dual drug delivery systems (DDS) were designed by controlled polymerization of pharmaceutically functionalized choline-based monomers, i.e. [2-(methacryloyloxy)ethyl]trimethylammonium with counterions of cloxacillin (TMAMA/CLX), and ampicillin (TMAMA/AMP), providing the properties of antibiotics. This strategy was convenient to attain the well-defined linear copolymers with 38–93 mol. % of TMAMA contents, which were regulated by the initial ratio of TMAMA to methyl methacrylate comonomer. The compositions of polymers were controlled by the total monomer conversion (40–75%) resulting in a variable degree of polymerization (DPn = 160–300) and contents of pharmaceutical anions (CLX¯ 51–80% and AMP¯ 78–87%). In aqueous solution, particles of the polymer achieved nanoscale sizes, measuring between 274–380 nm for CLX¯ systems and 288–348 nm for CLX¯/AMP¯ systems. In vitro drug release, which was driven by the exchange reaction of the pharmaceutical to phosphate anions in PBS, imitating a physiological fluid, occurred in the range of 58–76% of CLX¯ (10.5–13.6 µg/mL) in the single systems, and 91–100% of CLX¯ (12.9–15.1 µg/mL) and 97–100% of AMP¯ (21.1–23.3 µg/mL) in the dual systems. In relation to the conventional systems delivering both antibiotics without polymer carrier, the studied choline-based polymer DDS, demonstrating effective content of drug(s) and their (co)release from the polymer carriers, seems to be a great alternative solution.

Publisher

Springer Science and Business Media LLC

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