Amphiphilic chitosan derivative drug-loaded nano-micelle and preparation method

Abstract

The invention discloses an amphiphilic chitosan derivative drug-loaded nano-micelle and a preparation method and belongs to the field of pharmaceutical preparations. Amphiphilic chitosan derivatives form the micelle by means of self assembling, vitamin E succinate serves as a kernel, and thiolated chitosan serves as a shell; the hydrophobic kernel is used for entrapping a hydrophobic anti-HIV drug, the shell carrying positive charges is used for adsorbing cytomembrane, the loaded drug can be stably released in vivo, the hydrophilic shell is used for enhancing the solubility of the micelle and maintaining the stability of the micelle in a solution, and then the blood circulation time of the micelle after systematic administration is prolonged. The micelle can stably exist in all kinds of body fluid for more than 10 hours after particles are formed, the particle size is smaller than 200 nanometers, and it is beneficial for controlling the micelle particles to enter cells without being removed by macrophages. The delivery system can keep stability under the condition that serums exist, the drug is delivered into the cells, and good biocompatibility is achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an amphiphilic chitosan derivative (chitosan-vitamin E succinate-N-acetyl-L-cysteine) nano-micelle, a preparation method and an application thereof. Background technique [0002] With the deterioration of the global ecological environment and the increasing pace of people's life and work pressure, the morbidity and mortality of AIDS, a major disease that seriously threatens human life and health, are increasing year by year. China is the largest country in Asia, and its economy has developed rapidly in recent years, but at the same time, AIDS is also quietly attacking this country. Now China has become one of the fastest-growing countries in the world for AIDS. [0003] By the end of 2009, it was estimated that there were about 740,000 people living with HIV / AIDS in China, including 105,000 AIDS patients; it was estimated that there were 48,000 new HIV infections and 26,...

AI Technical Summary

Problems solved by technology

[0005] (1) Low solubility, most drugs are hydrophobic, poorly soluble in aqueous solution, easy to precipitate, need to add solubilizer, co-solvent or latent solvent to improve solubility;

[0006] (2) Toxic and side effects are large, and the distribution selectivity in the body after administration is poor

In addition, the addition of excipients is likely to cause serious side effects, such as allergic reactions after administration, toxic kidney damage, neurotoxicity, bone marrow suppression, etc., which seriously affect the therapeutic effect (Gao Zhixian. Li Xiaoqiang. Nano Biomedicine [M]. Beijing : Chemical Industry Press, 2007:1-30);

[0007] (3) The pharmacokinetic properties are poor, and it is rapidly eliminated by the liver and spleen after administration, requiring continuous infusion or higher doses; and if the drug is administered orally, not only because of its strong hydrophobicity, it is difficult to be absorbed Absorption, and also due to the physiological barriers existing in the body to prevent drug absorption;

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