An oligonucleotide drug preparation for treating liver cancer and a preparation method and application thereof

The drug formulation composed of oligonucleotide drug PHN02ME, nucleoside phospholipids TPS or CPS, cationic lipid CLDA, and auxiliary lipid DSPE-PEG solves the problems of inaccurate targeted delivery and toxic side effects in the treatment of liver cancer, and achieves efficient, long-lasting anti-liver cancer efficacy and safety.

CN116421614BActive Publication Date: 2026-01-27PEKING UNIV +1
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Patent Information

Application Number
CN202310341239.4
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-03-31
Publication Date
2026-01-27
Estimated Expiration
2043-03-31

AI Technical Summary

Technical Problem

Current treatments for liver cancer suffer from problems such as inaccurate targeted delivery, short half-life, easy development of drug resistance, and toxic side effects. Existing nucleic acid drugs have not been effective in treating liver cancer.

Method used

A drug formulation composed of oligonucleotide drug PHN02ME, nucleoside phospholipids TPS or CPS, cationic lipid CLDA, and auxiliary lipid DSPE-PEG was developed to achieve a highly efficient and long-lasting anti-hepatocellular carcinoma effect through formulation ratio screening and solvent optimization.

Benefits of technology

It exhibits highly effective and long-lasting anti-hepatocellular carcinoma effects in an orthotopic hepatocellular carcinoma mouse model, restores liver damage caused by hepatocellular carcinoma, has high safety, significantly inhibits the proliferation of hepatocellular carcinoma cells, reduces tumor growth, and improves the quality of life of patients.

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Abstract

The application discloses an oligonucleotide drug preparation applied to liver cancer treatment and a preparation method and application thereof. The drug preparation is composed of an oligonucleotide drug, a carrier and a solvent, wherein the oligonucleotide drug is PHN02 ME , the oligonucleotide drug PHN02 ME adopts 5 cap modifications at two ends on the basis of a full thio sequence, and the carrier is composed of nucleotide phospholipid TPS or CPS, cationic lipid CLDA and auxiliary lipid DSPE-PEG. The application obtains a new liver cancer resistant drug preparation with great clinical application potential through preparation proportion adjustment and preparation solvent optimization. After low-dose and low-frequency intravenous administration of the preparation to mice, the growth of liver cancer in the mice is significantly inhibited, and the preparation shows ideal sustained release / long-acting anticancer effect, and the drug efficacy is better than that of a CT102 / DNCA / CLD / PEG preparation. The application lays a foundation for the wide clinical application of the liver cancer resistant antisense nucleic acid drug, and also has wide application prospects in the field of gene therapy.
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