Liposome-modified spermine derivative and liposome prepared by derivative

A technology of lipid modification and derivatives, which is applied in the preparation of carbamic acid derivatives, liposome delivery, carboxylic acid amide preparation, etc., can solve the problems of not reaching the therapeutic effect, and achieve long cycle performance and targeting, The effect of strengthening market competitiveness and improving accumulation capacity
CN104876831AActive Publication Date: 2015-09-02GUANGZHOU NANOTIDES PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGZHOU NANOTIDES PHARMA
Publication Date
2015-09-02

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Abstract

The invention provides a liposome-modified spermine derivative and a liposome prepared by the derivative. The spermine derivative is directly applied or is mixed with one or more selected from cholesterol, neutral lipids and polyethylene glycol (PEG)-modified lipids, which can be adopted as a carrier for entrapping or absorbing bioactive molecular drugs to be loaded into cells. In this way, the effect of regulation, intervention or treatment is realized. In a general formula (1), X1 represents -(CH2)- or carbonyl group, wherein n represents 1, 2 or 3; X2 represents -(CH2)-, ester group, amide group, oxygen, or sulfur; R1 and R2 independently represent C6-C18 alkyl group or lipophilic cholesterol molecules, respectively.
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Description

technical field

[0001] The present invention relates to the field of drug carriers, more particularly to a lipid-modified spermine derivative and a preparation method thereof, and a liposome using the derivative, which can introduce or deliver exogenous nucleotides to In cells (in vitro) or in animals / humans (in vivo) to play a specific role, the exogenous nucleotides include small interfering nucleotides (siRNA), DNA, messenger RNA (mRNA), microRNA (miRNA) or anti Antisense oligonucleotides, aptamers, etc. Background technique

[0002] Any DNA sequence in the genome, as well as every non-coding or coding RNA transcriptome molecule, can regulate its expression through specific exogenous nucleotides (including DNA and RNA), so as to achieve specific disease-specific treat. These treatments include gene therapy at the DNA level and nucleic acid interference (RNA interference, RNAi) therapy at the RNA level.

[0003] Gene therapy is to deliver specific sequences of nucleotid...

Claims

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