DARU Journal of Pharmaceutical Sciences

, Volume 26, Issue 1, pp 65–75 | Cite as

Lipid-drug conjugates: a potential nanocarrier system for oral drug delivery applications

  • Subham BanerjeeEmail author
  • Amit Kundu
Review Article


Hydrophilic drugs are preferred candidates for most routes of drug administration, because of their enhanced solubility and dissolution under aqueous in vivo conditions. However, their hydrophilic nature also leads to decreased permeability across hydrophobic barriers. This is a severe limitation in situations where membrane permeability is the primary factor affecting bioavailability and efficacy of the drug. Highly impermeable cellular membranes or the tight endothelial junctions governing the blood-brain barrier are prime examples of this limitation. In other cases, decreased permeability across mucosal or epithelial membranes may require increased doses, which is an inefficient and potentially dangerous workaround. Covalent conjugation of hydrophilic drugs to hydrophobic moieties like short-chain lipids is a promising strategy for maintaining the critical balance between drug solubility and permeability. This article practically focuses on the production procedure of Lipid drug conjugates (LDCs), various formulation methodologies for preparing LDC nanoparticles with detailed about their in vitro physicochemical characterization at laboratory scale. Moreover, brief overviews on the role of LDCs in novel drug delivery applications as a substrate to various disease therapies are provided.

Graphical Abstract

Three dimensional (3-D) schematic representation of LDCs structures.


Lipid drug conjugates Oral administration Drug delivery Hydrophilic drug 



Lipid Nanoparticle Formulations


Lipid-drug Conjugates




Gastrointestinal Tract


Zeta Potential


Polydispersity Index




Biopharmaceutical Classification Systems



The authors are thankful to their respective institution and university for providing access to necessary literature resources and essential library facilities for writing this review article. Recognition also goes to all the authors of papers, books, patents, websites and all other published sources listed in the references that were used to prepare the contents of this review article.

Compliance with ethical standards

Consent for publication

Not applicable.

Declaration of interest

The authors declare that they have no competing interests.


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Copyright information

© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.Department of PharmaceuticsNational Institute of Pharmaceutical Education and Research (NIPER)-GuwahatiGuwahatiIndia
  2. 2.School of PharmacySungkyunkwan UniverfsitySeoulSouth Korea

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