Oral drug delivery route is one of the most convenient and extensively utilised routes for drug administration. But there exists class of drugs which exhibit poor bioavailability on oral drug administration. Designing of drug-lipid conjugates (DLCs) is one of the rationale strategy utilised in overcoming this challenge. This review extensively covers the various dimensions of drug modification using lipids to attain improved oral drug delivery. DLCs help in improving oral delivery by providing benefits like improved permeability, stability in gastric environment, higher drug loading in carriers, formation of self-assembled nanostructures, etc. The clinical effectiveness of DLCs is highlighted from available marketed drug products along with many DLCs in phase of clinical trials. Conclusively, this drug modification strategy can potentially help in augmenting oral drug delivery in future.
Keywords: bioavailability; lipid–drug conjugate; oral drug delivery; permeability.