Abstract
In vitro cytotoxicity of polymer-carriers, which in the side chains contain the cholinum ionic liquid units with chloride (Cl) or pharmaceutical anions dedicated for antituberculosis therapy, i.e., p-aminosalicylate (PAS) and clavulanate (CLV), was investigated. The carriers and drug conjugates were examined, in the concentration range of 3.125–100 μg/mL, against human bronchial epithelial cells (BEAS-2B) and adenocarcinomic human alveolar basal epithelial cells (A549) as an experimental model cancer cell line possibly coexisting in tuberculosis. The cytotoxicity was evaluated by MTT test and confluency index, as well as by the cytometric analyses, including Annexin-V FITC apoptosis assay. The polymer systems showed supporting activity towards the normal cells and no tumor progress, especially at the highest concentration (100 μg/mL). The analysis of cell death did not show meaningful changes in the case of the BEAS-2B, whereas in the A549 cell line, the cytostatic activity was observed, especially for the drug-free carriers, causing death in up to 80% of cells. This can be regulated by the polymer structure, including the content of cationic units, side-chain length and density, as well as the type and content of pharmaceutical anions. The results of MTT tests, confluency, as well as cytometric analyses, distinguished the polymer systems with Cl/PAS/CLV containing 26% of grafting degree and 43% of ionic units or 46% of grafting degree and 18% of ionic units as the optimal systems.
Highlights
In medicine, nano-sized materials can be applied as drug vehicles [1,2], where polymercarriers improve a drug’s effect on the body through controlled release [3,4]
Well-defined ionic graft copolymers, i.e., polymethacrylate backbones decorated by polymethacrylate grafts functionalized with ionic TMAMA moieties, were selected for biological studies, including both free carriers with chloride anions, as well as those carrying the pharmaceutical anions PAS and CLV as the cytostatic on cell lines and potentially antituberculosis drugs (Figure 1)
Previous physicochemical reports have indicated that these systems are promising for drug delivery, in which the content of the anionic drug can be regulated by the content of TMAMA and by the efficiency of anionic exchange of chloride to the drug [27]
Summary
Nano-sized materials can be applied as drug vehicles [1,2], where polymercarriers improve a drug’s effect on the body through controlled release [3,4]. In drug delivery systems (DDS), the bioactive substances can be loaded/encapsulated via physical interactions or chemically attached by a polymer matrix. The latter, known as the polymer-drug conjugates [5,6,7], are characterized by their stability, depending on the type of bonding, which requires the presence of specific sites in the polymer chain to ensure drug conjugation. Ionic strength seems to be advantageous for ionic drug attachment [8,9] In these cases, the carriers contain ionic groups, which are usually provided by ionic liquids (IL) as suitable (co)monomers introduced into the polymer chain [10,11,12]. In the case of the ionic polymer structure, drugs can be carried in ionic form as counterions, i.e., nicotinic, salicylic, ampicillin, naproxen, ibuprofenate anions [28,29,30], as well as in nonionic form as loaded guests [31], or both forms as the systems for combined therapy [32]
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