Vinca alkaloid derivatives, processes for their preparation and use

By designing vinblastine derivatives as a brain-targeted delivery system, the problem of nucleic acid drugs penetrating the blood-brain barrier was solved, achieving safe and efficient drug delivery with the effect of improving brain microcirculation and drug transport.

CN119119030BActive Publication Date: 2026-06-02SOUTHWEST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHWEST UNIV
Filing Date
2023-06-08
Publication Date
2026-06-02

AI Technical Summary

Technical Problem

Existing technologies struggle to safely and effectively deliver nucleic acid drugs to the central nervous system, particularly the brain, especially due to the blood-brain barrier, and traditional ionizable lipid nanoparticles present liver targeting and potential toxicity issues.

Method used

Using vinblastine derivatives as ionizable lipids, and by modifying their structure to increase their lipid solubility and charge adsorption, a brain-targeted delivery system was designed. The protonated amine structure of the vinblastine derivatives interacts with nucleic acid drugs electrostatically, achieving efficient penetration of the blood-brain barrier and improving intracellular transport.

Benefits of technology

Vincristine derivatives can improve drug penetration and brain targeting, reduce toxicity, enhance the charge adsorption capacity of drugs under acidic conditions, and improve cerebral microcirculation, making them suitable for long-term treatment of brain diseases.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present application relates to a long-changma class derivative and its preparation method and application, belong to long-changma class derivative preparation technical field. The long-changma class derivative disclosed by the present application has the following advantages: (i) the modification of the tail chain increases the fat solubility of the long-changma class compound, and does not affect the brain blood flow regulation of the long-changma class itself, helps to carry the drug to penetrate the blood-brain barrier, and plays a brain protection role, improves the brain microcirculation disorder; (ii) the tertiary amine group in the parent nucleus structure of the long-changma class derivative has the property of ionization under acidic conditions, can achieve efficient carrying and lysosome escape of nucleic acid drugs through charge adsorption, and improve intracellular transport; (iii) the long-changma class derivative inherits the inherent various pharmacological activities of long-changma, and has high safety. Therefore, the long-changma class derivative disclosed by the present application has good application prospect in brain-targeted delivery of drugs for treating brain diseases.
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