Synthesis and Application of Cholic Acid Modified Polyamino Acid Block Copolymer

A technology of block copolymer and polyamino acid, which is applied in the directions of non-active ingredient medical preparations, emulsion delivery, pharmaceutical formulations, etc. Drug loading, overcoming the effect of early release
CN105524271BInactive Publication Date: 2018-07-03徐州康宇再生资源科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
徐州康宇再生资源科技有限公司
Publication Date
2018-07-03
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses the synthesis and application of a polyamino acid block copolymer modified by cholic acid. The hydrophilic chain of the block copolymer is polyethylene glycol, the hydrophobic chain is polyamino acid, and the end of the polyamino acid is modified by small molecule cholic acid. The side chain of the polyamino acid is lipoyl, and lipoic acid reacts with the amino group in the hydrophobic polyamino acid to form an amide bond; it can be cross-linked by self-assembling nanomicelles formed by the polyamino acid block copolymer modified by cholic acid to obtain The stable cross-linked reduction-sensitive polymer nanomicelles make the nanomicelles not easy to be destroyed outside the cell and in the blood, thus ensuring the stability of the drug encapsulated by the nanomicelles; once entering the tumor cells, the nanomicelles can quickly Dissociation by dissolving the cross-linking, the drug is released quickly, resulting in high-efficiency therapeutic effect; it overcomes the shortcomings of early drug release in vivo, low delivery efficiency, and slow intracellular release.
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Description

technical field

[0001] The invention relates to a cholic acid-modified polyamino acid block copolymer, in particular to a polyamino acid and an amphiphilic block polymer in which cholic acid is modified at the end of the polyamino acid and the side chain is modified with lipoic acid. Background technique

[0002] Polymer micelles are self-assembled in aqueous solution by amphiphilic polymers through intermolecular interactions (hydrogen bonds, hydrophilic / hydrophobic interactions, and van der Waals forces, etc.). It is an ordered molecular aggregate formed by self-assembly with hydrophobic groups as the inner core and hydrophilic groups as the outer shell. In addition to some common advantages of nano-drug carriers, polymer micelles also have superior physical and biochemical properties compared to other nano-carriers (such as liposomes and polymer nanoparticles): they have a clear core-shell structure , wherein the hydrophobic core part can be used to wrap hydrophobic drug...

Claims

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