Title:
POLYMERSOME DRUG LOADED WITH PLK1 INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/152298
Kind Code:
A1
Abstract:
Disclosed in the present invention are a polymersome drug loaded with a PLK1 inhibitor, a preparation method therefor and the use thereof. PEG-P(TMC-DTC)-based polymersome A3-Ps has a dense disulfide bond cross-linked membrane, resulting in excellent stability and rapid intracellular drug release. In addition, short-chain polyaspartic acid in an inner shell of the vesicle membrane can enhance the ability of a vesicle to load the molecular targeting drug volasertib (Vol), and the A3-Ps has a high drug-loading capacity and drug-loading rate and a small particle size. The Vol-loaded vesicle A3-Ps-Vol reduces the systemic toxicity of Vol while increasing the antineoplastic activity thereof. The A3-Ps-Vol has the best inhibitory activity against SKOV-3 cells compared with non-targeting Ps-Vol and free drug Vol, with the IC 50 being 49 nM, which is 3.5 times lower than that of free drug Vol. The double-targeting nano preparation is a highly efficient low-toxicity therapy for treating ovarian cancer.
Inventors:
ZHONG ZHIYUAN (CN)
WANG ZHE (CN)
XIA YIFENG (CN)
ZHAO SONGSONG (CN)
MENG FENGHUA (CN)
WANG ZHE (CN)
XIA YIFENG (CN)
ZHAO SONGSONG (CN)
MENG FENGHUA (CN)
Application Number:
PCT/CN2022/072328
Publication Date:
July 21, 2022
Filing Date:
January 17, 2022
Export Citation:
Assignee:
UNIV SOOCHOW (CN)
International Classes:
A61K9/127; A61K31/525; A61K47/34; A61K47/42; A61P35/00
Foreign References:
| CN113018263A | 2021-06-25 | |||
| CN112076159A | 2020-12-15 | |||
| CN110229323A | 2019-09-13 | |||
| CN111714457A | 2020-09-29 |
Other References:
WANG, ZHE ET AL.: "α3 Integrin-binding Peptide-Functionalized Polymersomes Loaded with Volasertib for Dually-Targeted Molecular Therapy for Ovarian Cancer", ACTA BIOMATERIALIA, vol. 124, 6 February 2021 (2021-02-06), XP086524356, DOI: 10.1016/j.actbio.2021.02.007
WANG ZHE, ZHAO SONGSONG, GU WENXING, DONG YANGYANG, MENG FENGHUA, YUAN JIANDONG, ZHONG ZHIYUAN: "Alpha 3 Integrin Binding Peptide-Functionalized Polymersomes Loading PLK1 Inhibitor Volasertib for Dually Targeted Molecular Therapy of Ovarian Cancer In vivo", SSRN ELECTRONIC JOURNAL, vol. 1, 12 November 2020 (2020-11-12), XP055952053, DOI: 10.2139/ssrn.3729648
ZHOU, CHENG ET AL.: "GE11 Peptide-installed Chimaeric Polymersomes Tailor-made for High-efficiency EGFR-targeted Protein Therapy of Orthotopic Hepatocellular Carcinoma", ACTA BIOMATERIALIA, vol. 113, 18 June 2020 (2020-06-18), XP086239091, DOI: 10.1016/j.actbio.2020.06.020
WANG ZHE, ZHAO SONGSONG, GU WENXING, DONG YANGYANG, MENG FENGHUA, YUAN JIANDONG, ZHONG ZHIYUAN: "Alpha 3 Integrin Binding Peptide-Functionalized Polymersomes Loading PLK1 Inhibitor Volasertib for Dually Targeted Molecular Therapy of Ovarian Cancer In vivo", SSRN ELECTRONIC JOURNAL, vol. 1, 12 November 2020 (2020-11-12), XP055952053, DOI: 10.2139/ssrn.3729648
ZHOU, CHENG ET AL.: "GE11 Peptide-installed Chimaeric Polymersomes Tailor-made for High-efficiency EGFR-targeted Protein Therapy of Orthotopic Hepatocellular Carcinoma", ACTA BIOMATERIALIA, vol. 113, 18 June 2020 (2020-06-18), XP086239091, DOI: 10.1016/j.actbio.2020.06.020
Attorney, Agent or Firm:
SUZHOU CREATOR PATENT AND TRADEMARK AGENCY, LTD (CN)
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