Bilosomes in Antidiabetic Therapy: A Comprehensive Review on Sitagliptin Formulation by Thin Film Hydration Method

V Karthik, S Rajarajan, Beny Baby, KM Ajay3, K Ramesh

Bilosomes have emerged as a novel vesicular drug delivery system designed to overcome the limitations of conventional carriers such as liposomes and niosomes. Their unique composition, incorporating bile salts into the lipid bilayer, enhances stability, protects drugs against enzymatic degradation, and improves gastrointestinal resistance. This structural innovation enables bilosomes to encapsulate both hydrophilic and lipophilic drugs, offering improved permeability, sustained release, and superior oral bioavailability. The review highlights the formulation processes, characterisation techniques, and comparative advantages of bilosomes, with a particular focus on Sitagliptin, a BCS Class III antidiabetic drug that suffers from poor intestinal permeability despite high solubility.
The article further discusses the methods of preparation, workflow optimisation, and evaluation strategies, while addressing challenges such as scale-up, GMP compliance, regulatory clarity, and long-term stability. Future perspectives emphasise the role of Quality by Design (QbD), probilosomes technology, and advanced manufacturing approaches in bridging laboratory success with clinical translation. Overall, bilosomes represent a promising and rational platform for oral delivery of Sitagliptin, offering enhanced therapeutic efficacy, patient compliance, and potential expansion into broader pharmaceutical applications.

Keywords – Bilosomes, Niosomes, Liposomes, Sitagliptin Phosphate, Thin film Hydration, Bile Salts, Oral Bioavailability, Nanocarriers.