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Review
. 2016 Oct 28;1(3):277-296.
doi: 10.1002/btm2.10033. eCollection 2016 Sep.

Anticancer nanoparticulate polymer-drug conjugate

Quanyou Feng  1 , Rong Tong  1
Affiliations
Review

Anticancer nanoparticulate polymer-drug conjugate

Quanyou Feng et al. Bioeng Transl Med. .

Abstract

We review recent progress in polymer-drug conjugate for cancer nanomedicine. Polymer-drug conjugates, including the nanoparticle prepared from these conjugates, are designed to release drug in tumor tissues or cells in order to improve drugs' therapeutic efficacy. We summarize general design principles for the polymer-drug conjugate, including the synthetic strategies, the design of the chemical linkers between the drug and polymer in the conjugate, and the in vivo drug delivery barriers for polymer-drug conjugates. Several new strategies, such as the synthesis of polymer-drug conjugates and supramolecular-drug conjugates, the use of stimulus-responsive delivery, and triggering the change of the nanoparticle physiochemical properties to over delivery barriers, are also highlighted.

Keywords: drug delivery; nanomedicine; nanoparticle; polymer‐drug conjugate; stimuli‐responsive.

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Figures

Figure 1
Figure 1
(a) Two representative polymer‐drug conjugates (PDCs): hydrophilic polymer‐drug conjugates, and nanoparticles composed of amphiphilic polymer‐drug conjugates. Both the polymer's and nanoparticle's physicochemical properties have to be well characterized for the future translation of PDCs. (b) Scheme of the nanoparticle encapsulating drugs, which is compared to the conjugation strategy
Figure 2
Figure 2
Chemical structures of some polymer‐drug conjugates in the clinical trials. The drugs are highlighted in blue, the linkers in green
Figure 3
Figure 3
Three synthetic strategies of polymer‐drug conjugates
Figure 4
Figure 4
Schemes of various stimuli‐responsive linkers used in polymer‐drug conjugates, including pH‐sensitive linkers, redox‐sensitive linkers, photocaging groups, and photolysis linkers
Figure 5
Figure 5
The synthesis and drug release of a light‐triggerable polymer‐10‐hydroxylcamptothecin conjugate. The drugs are highlighted in blue, the linkers in green
Figure 6
Figure 6
The chemical structure of a conjugated polymer‐doxorubicin (blue) conjugate with redox‐sensitive thioacetal linker (green)
Figure 7
Figure 7
Two examples of polymer‐drug conjugates that can change the nanoparticle's (a) size or (b) charge to improve their tumor penetration. The drugs are highlighted in blue, the pH‐sensitive linkers in green
Figure 8
Figure 8
Four representative supramolecular drug conjugates that can assemble into nanoparticle for drug delivery
See this image and copyright information in PMC

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