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Polymer-Drug Conjugates/Prodrugs for Drug Delivery Application

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 August 2020) | Viewed by 9434

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Guest Editor
School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishop Hall Lane, Chelmsford CM1 1SQ, UK
Interests: dendrimer nanocarriers; biopolymers; clinical pharmaceutics; polymer nanoparticulates
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Special Issue Information

Dear Colleagues,

Polymer–drug conjugates/prodrugs are widely investigated for many drug delivery applications, such as enhanced water solubility, site-specific delivery (drug targeting), improved stability, etc. The covalent bond between the drug and polymer is normally selected according to the ultimate purpose of the drug delivery system. In other words, the release of drug from such a conjugate occurs via chemical or enzymatic cleavage of a labile bond. For example, for a polymer–drug conjugate designed for enhanced drug oral bioavailability, the covalent bond is selected to be stable in the gastrointestinal tract and during transit across epithelial cells, but labile once absorbed. However, the availability of suitable function groups of the drug and a polymer is crucial. In many studies, therefore, the drug is attached through a covalent bond via a linker/spacer to the functional groups of a polymer. Generally, the covalent linkage provides a stable system that is not dependent upon the physical or thermodynamic factors which apply to encapsulated systems. In addition, in some branched polymers, like dendrimers, there are great opportunities for tailoring/engineering the surface to facilitate drug conjugation and/or to attach the designed moieties that exhibit desired properties such as targeting, long circulation, etc. This Special issue of Molecules will provide a platform for presenting the latest design strategies for polymer–drug conjugation and their applications in drug delivery.

Dr. Mohammad Najlah
Guest Editor

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Keywords

  • Polymer macromolecules
  • Covalent bond drug delivery
  • Conjugation
  • Prodrug

Published Papers (2 papers)

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Research

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11 pages, 3057 KiB  
Article
A Nano Drug Delivery System Based on Angelica sinensis Polysaccharide for Combination of Chemotherapy and Immunotherapy
by Min-Zhe Wang, Xin He, Zhe Yu, Hong Wu and Tie-Hong Yang
Molecules 2020, 25(13), 3096; https://doi.org/10.3390/molecules25133096 - 07 Jul 2020
Cited by 22 | Viewed by 3514
Abstract
Combination of chemotherapy and immunotherapy has been a promising strategy in cancer treatment. Polysaccharides from Angelica sinensis (AP), a well-known Chinese herbal medicine, have been proved to have good immunomodulatory activity. In the present study, an enzyme-sensitive tumor-targeting nano drug delivery system (AP-PP-DOX [...] Read more.
Combination of chemotherapy and immunotherapy has been a promising strategy in cancer treatment. Polysaccharides from Angelica sinensis (AP), a well-known Chinese herbal medicine, have been proved to have good immunomodulatory activity. In the present study, an enzyme-sensitive tumor-targeting nano drug delivery system (AP-PP-DOX (doxorubicin), PP stood for peptide) was constructed. In this system, Angelica polysaccharides act as not only carriers to targeted delivery of drugs to tumor tissue but also effectors to improve tumor microenvironment and enhance immune function, resulting in synergistic antitumor effect with chemotherapy drugs. The structure of this conjugate was confirmed by FI-IR and 1H-NMR. The particle size and zeta potential of the nanoparticles were 129.00 ± 3.32 nm and −28.45 ± 0.22 mV, respectively. Doxorubicin (DOX) and AP could be quickly released from the AP-PP-DOX under the presence of matrix metalloproteinase 2 (MMP2). The released DOX showed good antitumor efficacy in vitro. The treatment of released AP moiety increased the expression of IL-2, while that of IL-10 was decreased, showing potential in restoring Th1/Th2 immune balance in tumor microenvironment. In a word, this drug delivery system, with specific tissue targeting and tumor microenvironment improvement, will open a new avenue for combination treatment of cancer. Full article
(This article belongs to the Special Issue Polymer-Drug Conjugates/Prodrugs for Drug Delivery Application)
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Review

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24 pages, 11117 KiB  
Review
Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
by Yayue Wang, Chang Zhang, Haoxing Wu and Ping Feng
Molecules 2020, 25(23), 5640; https://doi.org/10.3390/molecules25235640 - 30 Nov 2020
Cited by 15 | Viewed by 5481
Abstract
Prodrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated [...] Read more.
Prodrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated with the disease. In recent years, bioorthogonal chemistry has allowed the creation of prodrugs that can be chemically activated with spatio-temporal precision. In particular, tetrazine-responsive bioorthogonal reactions can rapidly activate prodrugs with excellent biocompatibility. This review summarized the recent development of tetrazine bioorthogonal cleavage reaction and great promise for prodrug systems. Full article
(This article belongs to the Special Issue Polymer-Drug Conjugates/Prodrugs for Drug Delivery Application)
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