PH-sensitive tumor targeted recombinant high-density lipoprotein as well as preparation method and application thereof

Abstract

The invention relates to a pH-sensitive tumor targeted recombinant high-density lipoprotein, which is prepared from the following ingredients in parts by weight: 1 to 5 parts of antitumor medicine, 15to 35 parts of phospholipid, 15 to 60 parts of albumin, 1 to 10 parts of cholesterol derivatives and 2 to 6 parts of linoleic acid. The pH-sensitive cholesterol derivatives in the ingredients effectively ensure the structure stability of rHDL in the blood circulation conveying process; the targeted conveying efficiency of the antitumor medicine to the tumor tissues is improved; after the rHDL istaken by tumor cells; acetal bonds in the pH-sensitive cholesterol derivatives are hydrolyzed into the original cholesterol; the catalysis condition of intracellular ACAT enzyme is met; the fast release of the antitumor medicine in the tumor cells is realized through the lipoprotein structure change; the tumor cells are effectively killed. The lipoprotein belongs to a tumor targeted carrier with huge development potential; the problems of low bioavailability and low tumor killing selectivity of the antitumor medicine in the prior art are solved.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a pH-sensitive tumor-targeting recombinant high-density lipoprotein and a preparation method. Background technique

[0002] At present, anti-tumor drugs, especially fat-soluble anti-tumor drugs, generally have problems such as low bioavailability and low tumor killing selectivity, for example, paclitaxel and doxorubicin, although they have good anti-tumor activity, their solubility in water is low (<0.03g / L), wide range of action, weak specificity, strong toxic and side effects, so its oral preparations and injections have encountered problems such as low bioavailability and low tumor killing selectivity in clinical application, so clinical treatment There is an urgent need for an effective method to improve the solubility of fat-soluble antineoplastic drugs, reduce the toxic and side effects of antineoplastic drugs, and increase the tumor killing effect of antine...

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