Citation: Zibo Li, Qing Xu, Xuefeng Lin, Kunyi Yu, Ling Lin, Yangjia Liu, Zhiqiang Yu, Tiancai Liu, Dixian Luo. Integrating of lipophilic platinum(IV) prodrug into liposomes for cancer therapy on patient-derived xenograft model[J]. Chinese Chemical Letters, ;2022, 33(4): 1875-1879. doi: 10.1016/j.cclet.2021.10.077 shu

Integrating of lipophilic platinum(IV) prodrug into liposomes for cancer therapy on patient-derived xenograft model

Zibo Li ^{a, b, 1} ,
Qing Xu ^{b, 1} ,
Xuefeng Lin ^b ,
Kunyi Yu ^b ,
Ling Lin ^b ,
Yangjia Liu ^b ,
Zhiqiang Yu ^{b, *,} ,
Tiancai Liu ^{c, *,} ,
Dixian Luo ^{a, *,}

a.
Department of Laboratory Medicine, Huazhong University of Science and Technology Union Shenzhen Hospital (Nanshan Hospital), Shenzhen 518000, China
b.
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China
c.
School of Laboratory Medicine and Biotechnology, Institute of Antibody Engineering, Southern Medical University, Guangzhou 510515, China

yuzq@smu.edu.cn

liutc@smu.edu.cn

luodixian_2@smu.edu.cn

Received Date: 27 September 2021
Revised Date: 25 October 2021
Accepted Date: 26 October 2021
Available Online: 29 October 2021

Figures(6)

Platinum-based anticancer agents such as cisplatin and its analogues are widely used for treating multiple cancers. However, due to the inferior water-solubility, chemoresistance and consequent adverse side effects, their clinical applications are limited. Herein, cholesPt(IV), a lipophilic platinum(IV) prodrug was synthesized for manufacture of CholesPt(IV)-Liposomes aiming to resolve the predefined obstacles encountered by platinum drugs. Following systematic screening, CholesPt(IV)-Liposomes showed a small particle size (105.6 nm), the rapid release of platinum (Pt) ions, and notable apoptosis of cancer cells. In addition, according to the fluidity and safety results of animal experiments in mice, CholesPt(IV)-Liposomes also showed better therapeutic effect, which significantly inhibited the growth of patient-derived xenograft tumors of hepatocellular carcinoma with an inhibition ratio of 80.7%, and effectively alleviated the drug toxicity brought by traditional platinum drugs. Overall, this study provides a promising route to enhance the therapeutic efficiency of platinum drugs in cancer treatment.
- Lipophilic platinum(IV) prodrug,
- Liposome,
- Cancer therapy,
- Drug delivery,
- Patient-derived xenograft
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