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. 2020 Apr 29;12(5):406. doi: 10.3390/pharmaceutics12050406

Table 3.

Summary of polymer-drug conjugates, which are effective in vitro and in vivo against lung cancer.

Polymer-Drug Conjugates Carrier/Monomers Used Drugs Biological Outcomes Molecular Design Reference
Hyaluronic acid-dihydroartemisinin (HA-DHA) Hyaluronic acid Dihydroartemisinin The conjugates displayed high apoptosis when compared to the free drug The hydroxyl group of the drug was covalently linked to the carboxylic group of hyaluronic acid. [131]
Hyaluronic acid-Paclitaxel (HA-PLX) Hyaluronic acid Paclitaxel Significant cytotoxicity and apoptosis-inducing effect resulting from increased cellular uptake of the drug via HA-receptor mediated endocytosis. Paclitaxel was conjugated to the C-6 position of N-acetyl-D-glucosamine of the hyaluronic acid using hexanediamine as a linker. [132]
MPEG-b-norbornene functional PLA-b-P(α-BrCL) Polylactic acid, Polyethylene glycol Doxorubicin and paclitaxel The incorporation of both drugs into the carrier resulted in a synergistic effect in inhibiting the proliferation of A549 cancer cells. Both drugs were covalently incorporated into the polymer backbone [133]
Polylactide-Paclitaxel (PLA-PTX) Allyl-functionalized polylactide Paclitaxel Enhanced cytotoxic effect in vitro. A polymer-drug conjugate was also obtained by thiol-ene reaction of both thiol-functionalized SB and PTX with allyl-functionalized PLA. [134]
Polyethylene glycol-Paclitaxel (PEG-PTX) Polyethylene glycol Paclitaxel The conjugates exhibited sustained drug release with anti-tumor activity, which was less than the free drugs. The conjugates were prepared with either an azide linker or a succinic linker. The linear PEGs were modified with PTX at the hydroxyl. PTX was incorporated into the PEG molecule via an ester bond at the C-2′ position on the PTX side chain. [135]
N-(2-hydroxypropyl)methacrylamide-Doxorubicin N-(2-hydroxypropyl)methacrylamide Doxorubicin High cytotoxic activity against the lung cancer cells, which were 10-fold higher cytotoxic against B16-F10, 3LL, and HT29 cells when compared to peptide-doxorubicin. Doxorubicin was incorporated into N-(2-hydroxypropyl)methacrylamide. [136]
Poly-l-lysine-lipoic acid-Doxorubicin Poly-l-lysine-lipoic acid Doxorubicin The conjugates exhibited enhanced internalization and cytotoxicity effects in vitro. It also exhibited excellent good tumor-targeting capability. It was prepared by the modification of dimethylmaleic anhydride for enhanced cell internalization [137]