Galangin, a naturally available flavonoid, induces a variety of pharmacological activities and biological effects via several mechanisms. However, in vivo metabolism of galangin has not been fully explored, which means knowledge of its pharmacodynamics and application potential is limited. The objective of this study was to establish an ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry method for the rapid profiling and identification of galangin metabolites in vitro and in vivo using unique online information-dependent acquisition with multiple mass defect filtering combined with dynamic background subtraction in positive ion mode. A total of 27 metabolites were detected and characterized, among which eight metabolites in liver microsomes and four metabolites in intestinal microflora were characterized, and 27 metabolites from rat plasma, bile, urine, feces, and a number of different tissue samples were characterized. Thirteen major metabolic pathways including hydrogenation, hydroxylation, glycosylation, methylation, acetylation, glucuronidation, and sulfation were observed to be attributable to the biotransformation of the metabolites. This study provides evidence for the presence of in vitro and in vivo metabolites and the pharmacokinetic mechanism of galangin. Moreover, the study promotes the further development and utilization of galangin and the plant from which it is derived, Alpinia officinarum Hance.

Melanoma is an aggressive form of skin cancer arising from melanocytes, noted for its high metastatic potential and elevated mortality rate. Conventional treatment approaches are often limited by nonspecific systemic drug distribution, which can result in undesirable adverse effects and premature drug degradation. In this study, we report the development of a microneedle (MN)-mediated delivery platform, incorporating self-assembling polymeric micelles, combining a dissolvable MN patch with polymeric micelles designed to prevent ICG aggregation and co-encapsulate ZER and ICG, and enable combined chemotherapy and photothermal therapy against melanoma. These nanocarriers, referred to as ZER-ICG-polymer micelles, co-encapsulate Zerumbone (ZER)—a lipophilic sesquiterpenoid—and indocyanine green (ICG), a well-known photothermal agent. In vitro cytotoxicity assessments and intracellular distribution studies confirm a marked synergistic therapeutic effect under NIR light exposure, facilitating localized thermal ablation of melanoma cells. In vivo experiments using melanoma-bearing mice demonstrate that a single application of the ZER-ICG-loaded dissolvable microneedle patch, coupled with NIR irradiation, achieves potent photothermal performance and robust tumor growth inhibition, while inducing minimal systemic toxicity and negligible side effects. These findings highlight the promising potential of this transdermal delivery system for the treatment of superficial malignant tumors.