5-aminolevulinic acid NANO particle as well as preparation method and device thereof

Abstract

The invention discloses a 5-aminolevulinic acid nano particle as well as a preparation method and a device thereof. The 5-aminolevulinic acid nano particle comprises therapeutically effective amount of 5-aminolevulinic acid, ion chelating agent and biodegradable polymer. The 5-aminolevulinic acid nano particle provided by the invention is stable in property, high in targeting selectivity, high in cell absorption rate, weakened in photo-bleaching phenomenon, and reinforced in photodynamic reaction, and is capable of enhancing tissue penetration depth combined with injection or micro-needle drug administration, so the 5-aminolevulinic acid nano particle has high application value.

Description

technical field [0001] The invention relates to a nanoparticle preparation of 5-aminolevulinic acid, a preparation method and a device thereof. technical background [0002] 5-Aminolevulinic acid, also known as 5-aminolevulinic acid, 5-aminofructonic acid, 5-aminolevulinic acid, is a water-soluble small molecule amino acid and is the precursor of protoporphyrin IX in the human body compound. When a large amount of exogenous 5-aminolevulinic acid enters the human body, it is preferentially absorbed by abnormal cells to synthesize excessive protoporphyrin IX. Protoporphyrin IX, as a photosensitive substance, generates oxygen active substances such as singlet oxygen and oxygen free radicals after partial illumination, and has a killing effect on abnormal cells. Based on this mechanism of action, DUSA successfully developed 5-aminolevulinic acid into a photosensitizer drug for photodynamic therapy Subsequently, Fudan Zhangjiang combined with national conditions also launched...

AI Technical Summary

Problems solved by technology

Due to the small molecular weight of 5-aminolevulinic acid, it is relatively easy to penetrate the stratum corneum, so it is currently the only photosensitizer that can be used for local external application; The output rate has become the most widely used photosensitizer at present, and it is irreplaceable

However, there are still some shortcomings in 5-aminolevulinic acid that limit the efficacy of photodynamic therapy with 5-aminolevulinic acid.

[0003] ① 5-aminolevulinic acid has poor stability and is easily hydrolyzed and enzymatically hydrolyzed after entering the body

[0004] ② The absorption rate of 5-aminolevulinic acid by diseased cells needs to be improved

Secondly, the targeting selectivity of 5-aminolevulinic acid to diseased cells needs to be further improved;

[0005] ③ "Photobleaching" affects the effect of 5-aminolevulinic acid photodynamic therapy

Clinically, due to the existence of "photobleaching", the photodynamic therapy effect of 5-aminolevulinic acid is weakened;

[0006] ④ The penetration depth of 5-aminolevulinic acid is limited

Water-soluble drugs prepared by this method For polymer nanoparticles, some drugs are located on the surface of the nanoparticles and cannot be wrapped inside the polymer nanoparticles to form a complete core-shell structure. The energy consumption is high, and the mechanical and thermal effects in the preparation process are easy to destroy the drugs. The encapsulation efficiency of the water-soluble drug polymer nanoparticles is low, the particle size of the nanoparticles is too large, and the size is not uniform enough; the volume of the external aqueous phase required for the volatilization of the organic solvent and the solidification of the nanoparticles makes the prepared nanoparticle colloid liquid The particle concentration is low. When the nanoparticle colloid is concentrated before freeze-drying, it is difficult to operate and easy to lose nanoparticles.

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