Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline

Abstract

The invention relates to nanocrystalline of a hydrophobic drug. The nanocrystalline of the hydrophobic drug is characterized by comprising the hydrophobic drug and amphipathic molecule of wrapping the outside of the hydrophobic drug, wherein the nanocrystalline is obtained by removing solvent molecules of an O / W type emulsion containing the hydrophobic drug. The nanocrystalline of the hydrophobic drug provided by the invention is uniform in particle size and good in dispersity in water and has universality; the effective components of the drug are kept well; the surface-wrapped amphipathic molecule can be doped with a targeting molecule; after the amphipathic molecule is doped with the targeting molecule, the targeting functionalization of a nanocrystalline preparation can be achieved; distribution of the drug in a tumor tissue is increased; and the toxic and side effects of chemotherapy drugs are reduced. The preparation method of the nanocrystalline of the hydrophobic drug provided by the invention is simple to operate and good in repeatability; the controllability of the particle size of the hydrophobic drug can be achieved; the product quality is easy to control; and the batch reproducibility of the drug is good.

Description

technical field [0001] The invention relates to a nanocrystal of a hydrophobic drug, a preparation method and a use method, in particular to a nanocrystal of an insoluble hydrophobic drug, a preparation method and a use method. Specifically, the present invention relates to an insoluble hydrophobic drug nanocrystal prepared by emulsion crystallization method, preparation and use method, the prepared hydrophobic drug nanocrystal can treat malignant tumors, such as breast cancer, ovarian cancer, leukemia, lymphoma And pancreatic cancer, etc., produce the ideal effect of treatment and prevention of tumor metastasis and recurrence. Background technique [0002] Administration of cytotoxic chemical drugs through the blood system is one of the important means of clinical tumor treatment. Compared with surgical treatment and radiotherapy, chemotherapy is a systemic treatment plan, which can exert a therapeutic effect on advanced tumors, metastatic and diffuse tumors, etc. Because...

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Problems solved by technology

Among them, the "top-down" technology requires mechanical grinding and high-pressure homogenization, the preparation conditions are severe, and the drug loss is serious during the process. Especially for heat-sensitive drugs, it will also lead to the decomposition and loss of active ingredients of the drug; secondly, the long-term contact between the grinding medium and the drug is still May cause drug contamination; in addition, most mechanical grinding is an intermittent batch process, the quality of each batch of drugs is not suitable for precise control, and it is difficult to meet the clinical approval requirements

Although the "bottom-up" technology does not have the above problems, because this technology does not change the surface properties of the drug particles like the "top-down" technology, the drug is still hydrophobic, and it is difficult to avoid this hydrophobicity. The particles are re-agglomerated in the aqueous solution, so the problem of hydrophobic and insoluble drugs cannot be fundamentally solved; in addition, the particle size obtained is generally large, and it is difficult to prepare nanoparticles with a particle size of less than 200nm, which cannot meet the requirements of clinical intravenous injection. requirements

Finally, the existing preparation technology also cannot guarantee the particle size uniformity of the drug particles, and the particle size deviation is extremely large, which is not conducive to achieving ideal product quality control and batch reproducibility of drug efficacy

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