The search for pioneering phytotherapeutic approaches based on the use of new herbal compounds is gaining immense attention in modern therapy because of the lack of toxic adverse effects. Previous in vitro studies have demonstrated lemongrass essential oil as a valuable phytotherapeutic agent for a variety of purposes, covering the composition, medicinal properties, formulation development and toxicology. This book will give an overview of the historical and modern uses, ethnobotanical consideration, quality control, chemical composition and medicinal values, bioactivity reports and toxicity concerns of lemongrass essential oil. A microemulsion system has been formulated for skin delivery of lemongrass oil, making suitable for treating conditions like acnes and pimples. Drugs targeting acne vulgaris should have good inhibitory potential against P. acnes and also better performance to reduce pro-inflammatory lipids in sebum. Future research needs to include more comprehensive chemical characterisation of extracts, quality control and identification of bio-markers of clinical exposure with regards to composition and bioactivity.