Preparation and characterization of PLA microspheres as drug delivery system for controlled release of Cetirizine with carbon dots as drug carrier

Cetirizine, a metabolite of hydroxyzine and derivative of piperazine, belongs to a family of antihistamines, which is effective second-generation histamine H1-receptor antagonist with antiallergic properties, showing prominent substitute to other ‘non-sedating’ antihistamines, and helps in treatment of physical urticaria and allergic asthma. Fast disintegration of prescription ‘over-the-counter’ standard Cetirizine tablets might generate early “burst-released” kinetics, resulting in significant drug absorption and a higher serum concentration. So, it is enviable to design a drug delivery system for Cetirizine which delivers drug in body in controlled fashion. In this study, a single system was developed that included the benefits of both nanoparticles and microspheres for continual delivery of Cetirizine via a simple emulsification process. Initially, PEG C-Dot was formulated, and then Cetirizine drug was dissolved in PEG C-Dot, which was then encapsulated in PLA microspheres to form drug-conjugated C-Dot-encapsulated microspheres, which were characterized using UV–Vis spectroscopy, photoluminescence spectroscopy, Zeta potential, and FESEM techniques. In addition, FESEM images exhibited a uniform spherical morphology for the PLA microspheres. Cell viability of the nanocomposite was evaluated in normal HEK293 human embryonic cells by MTT assay. The aim of study was to optimize process parameters for uniformity on size, shape, and surface morphology of microspheres. Furthermore, optimized parameters were used to synthesize drug-conjugated C-Dot-encapsulated microspheres for controlled drug delivery. This study showed that engineered drug-conjugated C-Dot-encapsulated microspheres had excellent cell viability and imaging effects against HEK293 cell lines. These findings provide a novel platform for controlled drug delivery of Cetirizine and could pave the way for cancer therapy medications in future.