Performance assessment of coumarin–quinoline hybrid-loaded PVA/sodium alginate composite hydrogel membranes with dual anticancer and antimicrobial drug delivery potential

Abstract

Cancer is one of the major issues faced by the modern health system. Therefore, the development of new, safer and more efficient chemotherapeutics is of prime importance. Traditional cancer therapies, including chemotherapy, are flawed, with off-target and on-target toxicity effects on normal cells; thus, newer strategies to improve cell selective targeting are required. In the present study, a polyvinyl alcohol/sodium alginate membrane as a coumarin–quinoline delivery system was prepared and characterized. It exhibited promising activity against cancer cells with enhanced bioavailability and selectivity. This delivery system is known for its ability to minimize side effects on healthy cells. The coumarin–quinoline hybrid was easily synthesized in high yields via facile reactions of preprepared N¹-(7-chloroquinolin-4-yl)propane-1,3-diamine (6) with coumarin-3-carbonyl chloride (3) in the presence of triethylamine at room temperature. The resultant coumarin–quinoline hybrid (CQ) was loaded onto hydrogel membranes made of poly(vinyl alcohol)/sodium alginate and encapsulated using a freeze–thaw method to form physically crosslinked chains. The results of cytotoxicity tests demonstrated that the prepared unloaded hydrogels exhibited cytotoxic effects against Vero cells, unlike control samples (100% cell viability recorded), with reduced cellular viabilities of 64–90%. The hydrogel formula (EA1-4) demonstrated the least cellular viability, while EA1-3 exhibited the highest cellular viability (Vero cells) among the unloaded hydrogels owing to the high SA contents in the membranes. The coumarin–quinoline hybrid-loaded membranes demonstrated a cellular viability of 62–84% owing to increasing coumarin–quinoline hybrid concentrations loaded in the hydrogels (EA2-1, EA2-2, EA2-3, and EA2-4), which decreased the viability of cells compared with CQ-free membranes. Specifically, cellular viability decreased upon increasing CQ concentration; thus, the EA2-4 formula (PVA/sodium alginate, 90 : 10%, 200 mg CQ) showed the highest activity. Statistical analysis of antimicrobial data showed that the EA2-4 formula offered the highest efficacy. After 42 hours of cultivation using the EA2-4 formula, the biofilm reduction percentages for Staphylococcus epidermidis (98.79 ± 2.67%), Staphylococcus aureus (94.96 ± 2.46%), and Bacillus cereus (97.96 ± 0.77%) significantly increased. The findings of this study suggest that the synthesized coumarin–quinoline hybrid-loaded members are good antimicrobial and anticancer biomaterials for versatile medical purposes.