Targeted hydrophobic antitumor drug nano preparation and preparation method thereof

Abstract

The invention relates to a targeted hydrophobic antitumor drug nano preparation. The nano preparation comprises a hydrophobic antitumor drug and a carrier in a mass ratio being 1: (4-32.5), wherein the carrier comprises 37.5wt%-95.3wt% of albumin and 4.7wt%-62.5wt% of a hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared from albumin and hyaluronic acid in a mole ratio being 1: (1-20). The preparation method of the nano preparation comprises steps as follows: preparing the hyaluronic acid-albumin conjugate; preparing a carrier solution; preparing a drug solution; preparing the nano preparation. The nano preparation has more uniform particle size distribution and good dispersability, is stable and avoids agglomeration, the particle size is nearly unchanged after freeze-drying and redissolving, and the yield is high after the nano preparation is filtered by a millipore filter (0.22 mu m), and the pharmacological function is good.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a targeted hydrophobic antitumor drug nano-preparation and a preparation method thereof. Background technique [0002] In most tumors, blood vessels grow rapidly and irregularly, and the internal lymphatic system clears slowly. There are tumor penetration enhancing factors, which make macromolecules and nanoparticles easy to stay inside the tumor, which is called "enhanced permeability and retention effect" (Enhanced Permeability and Retention, EPR). Due to the EPR effect, nano drug delivery system can be passively targeted to tumors, and has received more and more attention in the application of tumor targeted therapy. Ordinary nano dosage forms, such as liposomes, nanoparticles, etc., will be recognized by the human reticuloendothelial system in the plasma, which will speed up the plasma clearance of nano preparations and reduce their therapeutic effect. Therefore, surface-...

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Problems solved by technology

[0007] However, the nano-preparation particles of CN201210142991 have a large particle size distribution coefficient and a wide particle size distribution, and after freeze-drying and reconstitution, due to the entanglement between the hyaluronic acid molecular chains of the modified human serum albumin, the particles are mutually aggregated, Adhesion, resulting in an increase in the particle size of the lyophilized product after reconstitution, so when the microporous filter (0.22 μm) is used for filtration, the filter membrane pores are prone to blockage, which reduces the particle concentration in the filtrate, resulting in a decrease in the drug content in the filtrate. Reduced, thus affecting the efficacy and reducing product yield

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