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

An aminolevulinic acid and nanoparticle technology, which is applied in the direction of making medicines into special physical or taking forms of devices, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the absorption rate of 5-aminolevulinic acid. It needs to be improved, the particle size of nanoparticles is too large, the molecular weight is too small, etc., to achieve the effect of reducing the phenomenon of photobleaching, increasing the depth of tissue penetration, and strengthening the photodynamic response

Inactive Publication Date: 2012-10-03
HUADONG HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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-aminolevu

Method used

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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Prescription 1:

[0056] 5-aminolevulinic acid: 4mg;

[0057] Sodium dioctyl sulfosuccinate: 4mg;

[0058] Glycolide-lactide copolymer 3992mg;

[0059] Glycolide-lactide copolymer, the molar ratio of monomers is 50:50, and the weight average molecular weight is 5,000 Daltons;

[0060] use figure 1 The device prepares described 5-aminolevulinic acid nanoparticles.

[0061] The process parameters are as follows:

[0062] Inside the airtight insulating protective shell 3, the pressure is 1333Pa;

[0063] A high-voltage electric field of 7 kV is formed between the top of the dual-channel nozzle 5 and the receiving cup 7, and the current is 20 mA;

[0064] The internal aqueous phase solution is a phosphate buffer solution containing 5-aminolevulinic acid and ion-complexing agent dioctyl sodium sulfosuccinate, with a pH of 5;

[0065] The weight content of 5-aminolevulinic acid is 1%;

[0066] The ion complexing agent is 1 time of the weight of 5-aminolevulinic acid; ...

Embodiment 2

[0074] Prescription 2:

[0075] 5-aminolevulinic acid: 1g; dextran sulfate: 10g; glycolide-lactide copolymer: 39g, the molar ratio of monomers is 25:75, and the weight average molecular weight is 180,000 Daltons;

[0076] use figure 1 The device prepares described 5-aminolevulinic acid nanoparticles.

[0077] The process parameters are as follows:

[0078] Inside the airtight insulating protective shell 3, the pressure is 0.133Pa;

[0079] A high-voltage electric field of 7 kV is formed between the top of the dual-channel nozzle 5 and the receiving cup 7, and the current is 0.1 mA;

[0080] The internal aqueous phase solution is a phosphate buffer containing 5-aminolevulinic acid and ion-complexing agent dextran sulfate, with a pH of 3;

[0081] The weight content of 5-aminolevulinic acid is 5%;

[0082] The ion complexing agent is 10 times of the weight of 5-aminolevulinic acid;

[0083] The ion complexing agent is sodium dextran sulfate;

[0084] The oil phase solutio...

Embodiment 3

[0091] Prescription 3:

[0092] 5-aminolevulinic acid: 1g; sodium dioctyl sulfosuccinate: 2g; polyethylene glycol-glycolide-lactide copolymer 47g, the molar ratio of glycolide-lactide monomer is 25:75, the weight average molecular weight is 65,000 Daltons;

[0093] use figure 1 The device prepares described 5-aminolevulinic acid nanoparticles.

[0094] The process parameters are as follows:

[0095] In the airtight insulating protective shell 3, the pressure is 13Pa;

[0096] A high-voltage electric field of 7 kV is formed between the top of the dual-channel nozzle 5 and the receiving cup 7, and the current is 10 mA;

[0097] The internal aqueous phase solution is a phosphate buffer containing 5-aminolevulinic acid and ion-complexing agent dioctyl sodium sulfosuccinate, with a pH of 4;

[0098] The weight content of 5-aminolevulinic acid is 2.5%;

[0099] The ion complexing agent is 2 times of the weight of 5-aminolevulinic acid;

[0100] The oil phase solution is an or...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K41/00A61K31/195A61K47/34A61P35/00A61P17/10A61P17/12A61P17/18A61P17/00A61P31/10A61P31/04A61J3/00
Inventor 王宏伟王秀丽石磊赵锋栾瀚森王浩杨莉
Owner HUADONG HOSPITAL
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