Targeted delivery of low molecular drugs using chitosan and its derivatives

Jae Hyung Park, Gurusamy Saravanakumar, Kwangmeyung Kim, Ick Chan Kwon

Research output: Contribution to journalReview articlepeer-review

746 Citations (Scopus)


Chitosan has prompted the continuous impetus for the development of safe and effective drug delivery systems because of its unique physicochemical and biological characteristics. The primary hydroxyl and amine groups located on the backbone of chitosan allow for chemical modification to control its physical properties. When the hydrophobic moiety is conjugated to a chitosan molecule, the resulting amphiphile may form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site of action. Chemical attachment of the drug to the chitosan throughout the functional linker may produce useful prodrugs, exhibiting the appropriate biological activity at the target site. Mucoadhesive and absorption enhancement properties of chitosan increase the in vivo residence time of the dosage form in the gastrointestinal tract and improve the bioavailability of various drugs. The main objective of this review is to provide an insight into various target-specific carriers, based on chitosan and its derivatives, towards low molecular weight drug delivery. The first part of the review is concerned with the organ-specific delivery of low molecular drugs using chitosan and its derivatives. The subsequent section considers the recent developments of drug delivery carriers for cancer therapy with special focus on various targeting strategies.

Original languageEnglish
Pages (from-to)28-41
Number of pages14
JournalAdvanced Drug Delivery Reviews
Issue number1
Publication statusPublished - 2010 Jan 31

Bibliographical note

Funding Information:
This research was financially supported by the BioImaging Research Center at GIST, the Seoul R&DB program , the Real-Time Molecular Imaging Project , and Ministry of Health, Welfare and Family Affairs ( A062254 ).

Copyright 2010 Elsevier B.V., All rights reserved.


  • Chitosan
  • Low molecular drugs
  • Targeted delivery

ASJC Scopus subject areas

  • Pharmaceutical Science


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