Synthesized nanostructured dendrimer as a solubility enhancer for poorly water-soluble Domperidone

ABSTRACTDomperidone (DOM), an antidopaminergic medication, is primarily used as an antiemetic to treat nausea and vomiting caused by a variety of etiologies. It is very insoluble in water and has a poor oral bioavailability of 13-17%. The objective of the current work is to increase domperidone aqueous solubility using nano-structured hydroxy-terminated dendrimers. Dendrimers are distinctive carriers for drug solubilization because of their many special characteristics in terms of size, shape, branching length, and surface functioning. Dendrimers have unique properties that make them potential carriers for many active medicinal compounds due to their structural adaptability. The potential of hydroxy-terminated dendrimers UG1.0, UG2.0, and UG3.0 as solubility enhancers for domperidone was investigated. The effect of concentration and generation of synthesized nano-structured dendritic macromolecules on the solubility of domperidone was studied. The formation of the complexes between domperidone drug molecules and dendrimers was characterized by the FT-IR spectra. The experimental results showed that the solubility of the domperidone was approximately proportional to dendrimer concentration and generation. The water solubility of domperidone has been increased as generation of the hydroxy-terminated dendrimer. Cytotoxicity assay using A-549 lung cancer cell lines and hemolysis results revealed that synthesized dendritic macromolecules are more biocompatible than commercially available polyamidoamine dendrimers (PAMAM). Keywords: Antiemetic, Cytotoxicity, Dendrimer, Domperidone, Hemolysis, Phase solubility.