Method for preparing vesicle medicinal nanoparticles

Abstract

The invention relates to the technical field of medicines, and relates to design, preparation and application of vesicle nanoparticles of insoluble medicines. The invention comprises the following aspects: (1) a model medicine is dissolved in a good solvent to form a medicinal solution, and a functional stabilizer is dissolved in another solvent to form a poor medicinal solution; and (2) the medicinal solution is mixed with the poor solvent, and vesicle nanocrystal suspension of which the average effective particle size of less than 1 mu m is formed through self-assembly. A micromolecular material with high compatibility is selected, and a macromolecular polymer stabilizer is synthesized by a covalent binding technology; by microsedimentation, self-assembly and surface modification technologies, the medicine is stabilized in the poor solvent in a form of pure nanocrystals, and a problem that the insoluble medicines are hardly prepared into solution preparations and the problems of dumping and passivity of the traditional nanoparticles are solved; and compared with the traditional preparations, the vesicle nanoparticles have the advantages that the adverse reaction is reduced, toxic and side effects are reduced, the bioavailability is improved, and the vesicle nanoparticles have controlled-release and active targeting functions, and are convenient to use.

Description

technical field

[0001] The invention relates to the technical field of medicine, in particular to a vesicular drug nanoparticle

[0002] Preparation. Background technique

[0003] According to statistics, currently at least 40% of drugs are limited in use due to water solubility, and some drugs are even difficult to dissolve in organic solvents. For BCS class 2 and 4 poorly soluble drugs, when used for intravenous administration, an aqueous medium must be used. In order to improve the water solubility and drug loading of drugs, non-aqueous solvents, solubilizers, etc. are often used in the prescription, which makes the problems of biotoxicity and biocompatibility quite prominent. For example, paclitaxel injection uses polyoxyethylated castor oil , Docetaxel injection uses Tween-80 and ethanol. In 1995, Müller et al proposed a new drug delivery system - nanosuspensions (nanosuspensions). Nanosuspension is a submicron colloidal dispersion system formed by dispersing "pure...