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Metabolisable ph sensitive polymersomes

A technology of polymers and vesicles, which is applied in nano-drugs, nanotechnology, liposome delivery, etc., and can solve problems such as non-specific distribution

Pending Publication Date: 2021-04-09
UCL BUSINESS PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, low pH and enzyme-rich endosomes and lysosomes can lead to drug degradation or nonspecific distribution

Method used

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  • Metabolisable ph sensitive polymersomes
  • Metabolisable ph sensitive polymersomes
  • Metabolisable ph sensitive polymersomes

Examples

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Embodiment

[0108]Synthetic vesicles are made of amphiphilic copolymers, the amphiphilic copolymer is poly [propylene 2 - ((2- (1H-imidazole-5-yl) acetamide group) -3- (T-butoxy) -3-oxopropyl) sulfurous) succinate] (a PPITS derivative; hereinafter referred to as "PPITS") as a hydrophobic block and poly (2- (methacryl) Oxygen) ethylphosphorcholiccholine) (PMPC) is made of hydrophilic block.

[0109]A new synthetic route has been developed to produce two-block PMPC-PPITS copolymers and studied their assembly into vesicles. The results show that the PMPC-PPITS copolymer is degraded by in situ hydrolysis and / or enzymatic degradation (for example, by lipase or esterase) into fumagate (due to the incomplete function of the polymented ester raw material) And propylene glycol (a metabolite, which is rapidly liver (half-life 2 hours) to form lactate, acetate, and pyruvate), or have a thiosuccarlate derivative having a tert-butyl group. And imidazole. It is therefore proved that PMPC-PPITS forms a polymer...

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PUM

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Abstract

The present application relates to pH-sensitive polymersomes. The polymersomes are capable of degradation at endosomes' mild acidic pH into resorbable materials, which also allows avoiding liposome premature degradation of the payload once internalised inside the cells. The polymersomes can thus be used in methods for the treatment or prevention of diseases.

Description

Technical field[0001]The present invention relates to an ambacial pH sensitive polymer vesicles. The polymer vesicle is made of FDA and MHRA as a metabolita material for Generally Recognize As Safe, GRAS. A derivative having an imidazole ring has been used as a hydrophobic portion of the amphiphilic block copolymer. A class of exemplary polymers, polypropylene (((1H-imidazole-5-yl) acetamide) -3-oxpropropyl) sulfonate (Polypropylene ((((1H-Imidazol-5) -yl) actamido) -3-oxopropyl) ThiO) Succinate, PPITS) and its derivative are pH sensitive, hydrophobic in neutral pH, hydrophilic, hydrophilic, hydrophilic, will be liver The components of metabolism or as the Krebscycle are re-absorbed. Therefore, the polymer vesicles can be used to treat or reduce the symptoms of diabetes, cancer, infectious and autoimmune diseases.Background technique[0002]It is important to use a pathway that will contribute to patient compliance to the target site using a pathway that will contribute to patient com...

Claims

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Application Information

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IPC IPC(8): A61K9/127
CPCA61K9/1273B82Y5/00B82Y40/00
Inventor 朱塞佩·巴塔利亚亚历山德罗·波马丹尼斯·赛钦
Owner UCL BUSINESS PLC
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