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. 2021 Jan 14;11(6):3226–3240. doi: 10.1039/d0ra09663f

HES conjugates with small molecules and biomolecules.

HES kind Drug Type of bond In vivo studies (models) Key findings Ref.
Small agents Not available Deferoxamine (DFO) Imine Murine model of acute iron toxicity Prevent the mortality 57
HES 130/0.4 Methotrexate (MTX) Ester P388 murine leukaemia, MV-4-11 human leukaemia Higher antitumor efficacy 58
HES 130/0.4 Doxorubicin (DOX) Imine B16F10 melanoma Acid-sensitive, enhanced antitumor activity and security 61
HES 130/0.4 Doxorubicin (DOX) Imine A375 human malignant melanoma Targeted acid-sensitive and improved antitumor efficacy 62
HES 130/0.4 Doxorubicin (DOX) Hydrazone No Acid responsiveness, better proliferation inhibition in HepG2 cells 63
HES 130/0.4 Doxorubicin (DOX) Imine RM-1-xenografted C57BL/6 mouse pH-responsive, improved distribution, anti-tumor and anti-metastasis 64
HES 200/0.5 Doxorubicin (DOX) Amide H22-tumor mice model Redox-sensitive, targeted drug delivery and better antitumor efficacy 65
HES 130/0.4 5-Fluorouracil (5-Fu) Ester SD rats Sustained-release of FUAC 66
HES 200/0.5 Curcumin (CUR) Ester No Improved solubility and stability of CUR, better anticancer activity 67
HES 200/0.5 cis-Platinum (Pt) Ester No Improved solubility of Pt, targeted delivery to HepG-2 cancer cells 28
HES 200/0.5, HES 130/0.4 10-Hydroxy camptothecin (10-HCPT) Amide Hep-3B solid tumor in nude mice Improved solubility and stability of 10-HCPT, higher cytotoxicity 70 and 71
HES 130/0.4 Paclitaxel (PTX) Disulfide bond 4T1-tumor mice model α-Amylase- and redox-responsive, increased in vivo half life time 73
Biomolecules HES 130/0.5 Erythropoietin (AGEM400) Thioether No Prolonged half-life, superior efficacy 77
HES 85 kDa Anakinra Imine Male Wistar rats Extended half-life 78