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Introduction: In Ayurveda, Taila (medicated oils) and Ghrita (medicated clarified butter/ghee) are canonical lipid-based dosage forms used to deliver therapeutic agents systemically and locally. Classical pharmaceutics (Bhaishajya Kalpana) attribute to these vehicles abilities such as deep tissue penetration (sroto abhyantara), nourishment (dhatu poshana), and targeted action to lipid-rich tissues (neurological, reproductive, bone). Modern pharmacology recognizes lipid carriers (oils, liposomes, lipid emulsions) as efficient vehicles for enhancing solubility, lymphatic uptake, bioavailability, and tissue targeting. Methods: This narrative integrative review synthesizes classical Ayurvedic texts (Charaka, Sushruta, Ashtanga Hridaya, Rasashastra sources) and contemporary literature (pharmaceutics, pharmacokinetics, lipid-based drug delivery, and clinical reports). Databases searched included PubMed, Scopus, Web of Science, and Ayurvedic pharmacopeia resources (1950–2025). Eligible studies included formulation science, in vitro/in vivo pharmacokinetics, mechanistic reports, and clinical observations of medicated oils/ghritas. Results: Classical preparation processes (Sneha Paka for Taila and Sneha–Paka with dairy base for Ghrita) incorporate herbal kalka (paste) and aqueous decoctions to generate oil/ghee matrices enriched with both lipophilic and polar bioactives. Mechanistically, lipid matrices enhance extraction of lipophilic constituents, favor chylomicron formation and intestinal lymphatic transport (bypassing first-pass metabolism), improve CNS penetration for certain lipophiles, and provide sustained depot effects on topical application. Medicated ghrita shows advantages in delivery of lipophilic neuroactive molecules and systemic nourishment, whereas medicated oils excel for transdermal/arthritic and local administration. Preclinical and human pilot studies report improved tissue levels, enhanced therapeutic outcomes in neurodegeneration, wound healing, and musculoskeletal disorders, and acceptable safety when prepared under standardized protocols. Discussion: Taila and Ghrita combine centuries of pharmaceutic refinement with principles analogous to modern lipid-based delivery platforms (phytosomes, lipid nanoparticles, self-emulsifying systems). Key gaps include rigorous pharmacokinetic profiling in humans, standardized manufacturing (SOPs, marker assays), and mechanistic elucidation (lymphatic transport quantitation, BBB penetration studies). Conclusion: Taila and Ghrita are traditional lipid-based delivery systems with plausible and demonstrable modern pharmacological advantages. Integrative research that standardizes preparations and applies contemporary pharmaceutics will enable evidence-based deployment of these formulations in modern therapeutics.

KEYWORDS: Drug delivery, Ghrita, lipid carrier, Taila, lipid-based