Title:Lipid-Drug Conjugates for Oral Bioavailability Enhancement
Volume: 5
Issue: 2
Author(s): Afzal Hussain, Mohd Usman Mohd Siddique, Sandeep Kumar Singh, Abdus Samad, Sarwar Beg and Mohammad Wais
Affiliation:
Keywords:
Conjugation, hydrophilic drugs, lipids, lipid-drug conjugate (LDC), oral bioavailability,
pharmaceutical application.
Abstract: Lipid-Drug Conjugate (LDC) is an emerging field of nanotechnology which has potential
applications in delivery of drugs and targeting them to specific site. Several molecules were supposed as
promising and good therapeutic candidates during in vitro studies but they failed during in vivo studies
showing the limited oral bioavailability as a major dilemma. LDC technological based approach played a vital
role in augmenting bioavailability of such drug candidates. In LDC system, lipids such as fatty acids,
diglycerieds, triglycerides and phophoglycerides covalently bind with drug molecule for improved lipophilic
character of drug. This could lead to better penetration and absorption through biological membrane which
ultimately enhances the bioavailability of the corresponding therapeutic agent. Drugs including phenytoin,
beta lactum antibiotics, noscapine, valproic acid, non-steroidal anti-inflammatory drugs (ibuprofen) were
successfully linked through covalent bond by different lipid carriers which improved their physicochemical
properties, intestinal absorption and target specificity. This chapter extensively reviewed the lipidic and
glycolipidic conjugates of various drugs which enhanced the bioavailability compared to free drug solution
exploring that such LCD technique can be used for the enhancement of bioavailability of poorly aqueous
soluble drugs. The chapter included several patents with informative results which would help for
pharmaceutical scientist working this area.
