Amphiphilic polysaccharide derivative vector for specific medicine release in organism focusas well as preparation and application of pharmaceutical composition thereof

Abstract

The invention relates to an amphiphilic polysaccharide derivative vector for specific medicine release in an organism focus. In derivatives, a hydrophobic group is introduced to a polysaccharide skeleton through a disulfide-bond-containing connecting arm which can be degraded specifically to make polysaccharide provided with amphiphilic characteristics, nano micelles can be self-assembled in an aqueous medium, a medicine can be coated through action of the hydrophobic group and the medicine, the disulfide-bond-containing connecting arm can be specifically degraded by high-concentration glutathione serving as a reducing substance in focus cells after the medicine is loaded to reach at the focus by the nano micelles, the medicine is quickly released from micelle cores to be acted on an efficacy part due to dropping of the hydrophobic group, thereby the concentration, the curative effect and the bioavailability of the free medicine in the focus can be obviously improved. An auxiliary material can be used as a vector of an organic medicine, a water-insoluble medicine, an insoluble medicine or an amphiphilic medicine and can be used for medicine administration in blood vessels or by intramuscular injection and oral intake. A preparation method disclosed by the invention has the advantages of simplicity and mature process and is suitable for continuous production on a large scale.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an amphiphilic polysaccharide derivative that releases drugs specifically at the lesion site of a biological body as a drug carrier, and also relates to a preparation method and application of the carrier. Background technique [0002] Insoluble drugs have the disadvantages of poor oral absorption, low bioavailability, and difficulty in preparing suitable preparations. Therefore, improving the solubility and bioavailability of drugs is an urgent problem to be solved in medicine. At present, surfactants are often used or prepared into liposomes and clathrates to increase the solubility of drugs. However, due to the high critical micelle concentration (CMC) of some low molecular surfactants (10 -2 g / L), after being injected into the body, it is diluted by blood and has poor stability. At the same time, after a large amount of surfactant is injected into the body, it will p...

AI Technical Summary

Problems solved by technology

Some amphiphilic polysaccharide derivatives are now in the research stage, but these derivatives still have obvious disadvantages: the chemical bonds connecting polysaccharides and hydrophobic segments are mostly amide bonds or ester bonds, and the stability of these two chemical bonds in vivo is relatively low. High, so that the shedding of the hydrophobic segment is very slow, which leads to the elimination or metabolism of the drug that cannot be released in time after reaching the drug effect site, which is not conducive to the exertion of the curative effect

Specific release of drugs to the lesion site of organisms formed by introducing hydrophobic groups through linking arms containing disulfide bonds Amphiphilic polysaccharide derivatives have not yet been reported in any literature or patents

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