Medicine-phospholipid/albumin composite nanoparticles and preparation technology

Abstract

The invention provides medicine-phospholipid / albumin composite nanoparticles and a preparation technology. The preparation technology comprises the following steps: (1) preparing paclitaxel, phospholipid, cholesterol and a DSPE-PEG2000 (Distearoyl Phosphoethanolamine-Polyethylene Glycol 2000) stock solution; (2) preparing a paclitaxel liposome; (3) preparing albumin (BSA) stock solution; and (4) preparing the paclitaxel-phospholipid / albumin composite nanoparticles. The preparation method provided by the invention is simple and the problem that the solubility of a difficult-to-dissolve medicinein water is poor can be solved; and a preparation does not contain Cremophor EL and a toxic or side effect caused by a solubilizer in an injection process is avoided. Being different from common liposomes and albumin nanoparticles, the medicine-phospholipid / albumin composite nanoparticles prepared by the preparation technology have the characteristics that DSPE-PEG2000 is added into a prescription so that the stability of the nanoparticles is increased; and the encapsulation efficiency is high, the grain diameter is small and uniform, and the grain diameter of the nanoparticles is not obviously changed after the nanoparticles are stored at room temperature for two weeks.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and in particular relates to a drug-phospholipid / albumin composite nanoparticle and a preparation process. Background technique [0002] Paclitaxel (PTX), as one of the hottest new anticancer drugs after adriamycin, is of great significance in the field of tumor-related treatment. Paclitaxel is a kind of diterpenoid compound with excellent anticancer effect extracted from Taxus genus plants such as Pacific yew. The anti-cancer mechanism of paclitaxel is to promote extremely stable microtubule aggregation while blocking the normal physiological depolymerization of microtubules (in the G2 and M phases of the cell division cycle), thereby leading to cell death and hindering tumor growth. purpose of growth. Currently widely used in non-small cell tumors, ovarian cancer, breast cancer, prostate cancer and so on. However, the solubility of paclitaxel in water is extremely low (about 0.658...

AI Technical Summary

Problems solved by technology

[0004] Through investigation, it is found that the existing technology has the following deficiencies: the preparation process of albumin-bound paclitaxel nanoparticles (Abraxane) involves the use of organic solvents, and direct contact between albumin and organic solvents may lead to changes in protein structure and function

There is no report on the preparation method of nanoparticles that does not involve the use of organic solvents; at the same time, there is no study on the effect of pH value on the drug loading and particle size of nanoparticles

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