Abstract

Terpenes are structurally diverse natural compounds synthesized by plants, fungi, and marine organisms, exhibiting critical ecological functions and remarkable pharmacological potential. Their wide-ranging bioactivities include antimicrobial, anti-inflammatory, antioxidant, anticancer, and neuroprotective effects, making them promising leads for therapeutic development. However, their clinical utility is limited by low aqueous solubility, instability, and poor bioavailability. This review systematically integrates the structural subclasses of terpenes, monoterpenes, sesquiterpenes, diterpenes, triterpenes, tetraterpenes, and marine-derived analogues, with innovative formulation approaches that enhance pharmacokinetics and therapeutic performance. Emphasis is placed on nanotechnology-based delivery systems, such as nanoemulsions, liposomes, polymeric nanoparticles, and nanostructured lipid carriers, which have demonstrated substantial improvements in solubility, stability, and bioavailability. Clinical trial outcomes and pharmacokinetic data highlight significant gains, with several terpenes achieving enhanced oral bioavailability, reduced dosage requirements, and improved safety profiles. Structure–activity relationship analyses further elucidate how functional groups, stereochemistry, and conjugation length critically influence biological activity and therapeutic outcomes. Beyond pharmacology, this review underscores the ecological and industrial significance of terpenes, ranging from plant defense and pollination to their use in cosmetics, food, and biotechnology. Looking forward, interdisciplinary strategies such as synthetic biology, CRISPR-based genome editing, metabolic engineering, and AI-driven drug discovery are expected to revolutionize terpene research by enabling sustainable production, rational design of derivatives, and advanced targeted delivery. Collectively, these advances position terpenes as multifunctional biomolecules with the potential to bridge natural product chemistry, nanomedicine, and clinical therapeutics, thereby opening new avenues for drug discovery, biotechnology, and sustainable healthcare innovations.

Key words: Terpenes, biosynthesis, natural products, pharmacological applications, bioavailability, antimicrobial, anticancer, neuroprotection.