Polymer-drug conjugates: Progress in polymeric prodrugs

Jayant Khandare, Tamara Minko

Research output: Contribution to journalReview articlepeer-review

560 Scopus citations


Polymers are used as carriers for the delivery of drugs, proteins, targeting moieties, and imaging agents. Several polymers, poly(ethylene glycol) (PEG), N-(2-hydroxypropyl)methacrylamide (HPMA), and poly(lactide-co-glycolide) (PLGA) copolymers have been successfully utilized in clinical research. Recently, interest in polymer conjugation with biologically active components has increased remarkably as such conjugates are preferably accumulated in solid tumors and can reduce systemic toxicity. Based on the site and the mode of action, polymer conjugates possess either 'tuned' degradable or non-degradable bonds. In order to obtain such bonds, most of the strategies involve incorporation of amino acids, peptides or small chains as spacer molecules through multiple steps to include protections and deprotections. There is a need to design efficient synthetic methods to obtain polymeric conjugates with drugs and other bioactive components. Designs should aim to decrease the steric hindrance exhibited by polymers and the biocomponents. In addition, the reactivity of polymer and drug must be enhanced. This is especially true for the use of high molecular weight linear polymers and bulkier unstable drugs such as steroids and chemotherapeutic agents. Further, it is essential to elucidate the structure activity relationship (SAR) of a drug when it is conjugated with a polymer using different conjugation sites, as this can vary the efficacy and mechanism of action when compared with its free form. This review will discuss the current synthetic advances in polymer-conjugation with different bioactive components of clinical importance. In addition, the review will describe the strategies for reduction of steric hindrance and increase in reactivity of the polymers, drugs and bioactive agents and highlight the requisite structure activity relationship in polymer-drug bioconjugates. Finally, we will focus on passive and active targeting of polymeric drug delivery systems to specific site of drug action.

Original languageEnglish (US)
Pages (from-to)359-397
Number of pages39
JournalProgress in Polymer Science (Oxford)
Issue number4
StatePublished - Apr 2006

All Science Journal Classification (ASJC) codes

  • Ceramics and Composites
  • Surfaces and Interfaces
  • Polymers and Plastics
  • Organic Chemistry
  • Materials Chemistry


  • Conjugation
  • Drug delivery
  • Enhanced permeability and retention
  • In vivo and in vitro
  • Polymer
  • Prodrug


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