Nano drug carrier particles for improving bioavailability of rapamycin and preparation method thereof

Abstract

The invention discloses nano drug carrier particles for improving the bioavailability of rapamycin and a preparation method thereof, so as to carry out a drug effect optimization. The nano drug carrier particles are prepared in the following steps that according to the principle of an emulsion solvent evaporation method, a determined amount of PEG-PLGA and rapamycin are respectively dissolved in acetone; after being mixed uniformly, the PEG-PLGA, the rapamycin and the acetone are slowly added into water to be stirred by magnetic force; after a certain period of time, the obtained liquid is ultrasonically homogenated, and organic phase is removed in a vacuum dryer; the obtained water phase removes free medicine in a centrifugal tube; and then an ultrafiltration tube is used for concentration, and nano particles are obtained after freezing and drying. The method has the advantages of convenience in operation, simplicity and feasibility, good repeatability and the like. The prepared nano drug carrier particles can improve the utilization rate of the medicine by improving the absorptivity of the medicine and prolonging the cycling time in a human body. Meanwhile, the nano particles which are prepared through the method have good biocompatibility, and surface active groups can further modify ligands or targeted groups.

Description

technical field [0001] The invention relates to the field of biological materials and nanotechnology, in particular to a nanoscale drug carrier with suitable encapsulation efficiency and drug loading capacity, high biological safety, and capable of slowly releasing drug rapamycin and a preparation method thereof. Background technique [0002] Rapamycin is a potent immunosuppressive drug with low nephrotoxicity and is widely used in transplant surgery. At the same time, it can effectively inhibit the proliferation and migration of vascular smooth muscle cells after vascular injury, thereby reducing the occurrence of vascular restenosis, and it can also promote the proliferation of myocardial cells in myocardial defects, so it has great application prospects in the treatment of cardiovascular diseases. However, due to its own low solubility and the current mode of administration, its efficacy and application range are greatly limited. [0003] As an effective means to optimiz...

AI Technical Summary

Problems solved by technology

Cardiovascular disease, like cancer, is a serious threat to human health. However, due to the imperfect explanation of the pathological mechanism of some diseases and the lack of effective targeting groups, the research on drug delivery systems for the diagnosis and treatment of cardiovascular diseases lags far behind cancer. , and many drugs have not been well applied due to factors such as poor water solubility, low absorption rate, low bioavailability, and difficulty in oral administration. At present, the research on rapamycin nanocarriers at home and abroad is still in the initial stage. There is no effective sustained-release oral preparation of rapamycin on the market. In view of the good therapeutic effect of this drug in multiple disease fields, the development of a suitable nanocarrier for this drug meets the market demand and clinical needs

[0004] This patent uses the emulsified solvent volatilization method to prepare PEG-PLGA nanospheres loaded with rapamycin, and similar studies have not been reported