Preparing method of triptolide stereoscopic stable liposome nano granule

Abstract

A preparation method of stereo stable triptolide liposome is characterised in comprising (1) dissolving triptolide and 1,2-propylene glycol in water, treating with ultrasound, adding ultrapure water to obtain solution A; (2) dissolving lecithin, cholesterol, and PEG 2000in methylene chloride to obtain solution B; (3) preparing PBS liquid of pH 6.8 with sodium hydrogen phosphate as basic liquid and sodium dihydrogen phosphate as acidic liquid; (4) treating solutions A and B to obtain W / O type emulsion; (5) rotation evaporating in aqueous thermostat under reduce pressure to obtain jello with high viscosity; and (6) adding PBS liquid, standing overnight, and treating with ultrasound to obatin stereo stable liposome. The product of the invention can maintain the original property and efftect of triptolide, reduce local excitation and toxic-adverse side effect of triptolide, thereby improving pharmic security.

Description

technical field [0001] The invention relates to a preparation method of triptolide sterically stabilized liposome nanoparticles, specifically, triptolide liposomes are surface-modified with PEG2000 through a reverse-phase rotary evaporation-ultrasonic emulsification method to prepare triptolide A method for sterically stabilizing liposomal nanoparticles. Background technique [0002] Triptolide is an epoxy diterpene lactone extracted from the root bark of Tripterygium genus Tripterygium in the family Euonymus. It is a cytotoxic anticancer drug, which has a strong inhibitory effect on the rejection of transplanted organs. However, the currently available triptolide preparations limit its use due to its severe side effects. Forming it into an inclusion compound can increase solubility, adjust drug release rate, improve drug bioavailability, and reduce drug irritation and side effects. [0003] Nanoparticles refer to solid colloidal particles with a particle size of 10-1000nm...

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Problems solved by technology

[0004] At present, there are two problems in the nanoparticle carrier delivery system: most of the currently used carrier materials are biodegradable synthetic polymers, which are prone to toxicity after continuous use; Increased distribution of the system and reduced circulation time in the body limit its application

According to references, although PEG4000 has good flexibility and strong resistance to cell uptake, it has a large molecular weight, is not easy to be firmly combined with the membrane, and is easy to form agglomerates, which affects the stability of liposomes; PEG1000 has a small molecular weight and poor hydrophilicity. Insufficient flexibility, easy to be swallowed by macrophages; PEG2000 has a moderate molecular weight, which can avoid the above defects and achieve better results

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