Aim:: The aim of this in-depth review is to provide an overview of the pharmacologi-cal effects of Lobelia trigona and its bioactive components, highlighting its potential as a source of medicinal agents for various diseases Methods:: This review involved a comprehensive analysis of existing literature and research studies on the pharmacological effects of Lobelia trigona and its bioactive compounds. A bib-liography survey was carried out using various electronic databases like Google Scholar, Sci-enceDirect, Springer, Scopus, PubMed, Wiley, etc., and other offline as well as online aca-demic libraries were also used for the bibliography survey and compilation of data. Results:: Lobelia trigona was found to exhibit diverse pharmacological effects, primarily me-diated by bioactive alkaloids, such as lobeline, lobelanidine, and lobelanine. It demonstrated bronchodilator effects with potential applications in respiratory conditions, analgesic and anti-inflammatory properties for treating painful and inflammatory conditions, and cardiovascular effects, including vasodilation and hypotensive effects. The alkaloid lobeline was reported to have promising anti-addictive effects, particularly in smoking cessation. Nanocarrier-based formulations have the potential to address limitations, improve dosing schedules, and enhance the pharmacological effects of Lobelia trigona. Conclusion:: Lobelia trigona demonstrates diverse pharmacological effects, primarily attribut-ed to its bioactive alkaloids. It holds promise as a source of medicinal agents for a range of diseases. The potential synergy between the pharmacological effects of Lobelia trigona and nanocarrier technology highlights the significance of nanotechnology in improving Lobelia trigona-based therapeutics. However, further research is warranted to determine the clinical effectiveness, safety, biocompatibility, and long-term effects of nanocarrier-based Lobelia trigona formulations in different disease models.