Method for preparing nanometer particles of 5-ALA or 5-ALA derivatives

A 5-ALA, nanoparticle technology, applied in botanical equipment and methods, chemicals for biological control, food preparation, etc., can solve the problem of 5-ALA and its derivatives. Low utilization rate, loss of physiological activity and other problems, to achieve the effect of simple and fast method, high drug loading and uniform particle size distribution

Inactive Publication Date: 2013-11-13
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, 5-ALA and its derivatives can only be stored in acidic aqueous solution at a lower concentration for a short period of time; in neutral and alkaline aqueous solutions, 5-ALA and its derivatives quickly lose their physiological activity
In the traditional nano-p

Method used

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  • Method for preparing nanometer particles of 5-ALA or 5-ALA derivatives
  • Method for preparing nanometer particles of 5-ALA or 5-ALA derivatives

Examples

Experimental program
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Example Embodiment

[0031] Example 1

[0032] Preparation of PLA coated 5-ALA nanoparticles

[0033] 100 mg of PLA was added to 10 mL of anhydrous DCM, sealed and stirred overnight to completely dissolve the PLA.

[0034] Add 100 mg of 5-ALA to 10 mL of absolute ethanol, seal and stir overnight to completely dissolve 5-ALA.

[0035] Electrospray the prepared PLA / DCM solution and 5-ALA / absolute ethanol solution. The electrospray conditions are as follows: electrospray voltage 10KV, receiving distance 20cm, internal and external pushing speed ratio 2ml / h:4ml / h, after electrospray 1h Collect the obtained samples, vacuum dry for 24 hours, weigh and seal for storage.

Example Embodiment

[0036] Example 2

[0037] Preparation of PLA-PEG coated 5-ALA nanoparticles

[0038] 100 mg of PLA-PEG was added to 10 mL of anhydrous DCM, and sealed and stirred overnight to completely dissolve the PLA-PEG.

[0039] Add 100 mg of 5-ALA to 10 mL of absolute ethanol, seal and stir overnight to completely dissolve 5-ALA.

[0040] Electrospray the prepared PLA-PEG / DCM solution and 5-ALA / absolute ethanol solution. The electrospray conditions are as follows: electrospray voltage 10KV, receiving distance 20cm, internal and external pushing speed ratio 2ml / h:4ml / h, electrospray The samples were collected after 1 hour, dried in vacuum for 24 hours, weighed and sealed for storage.

Example Embodiment

[0041] Example 3

[0042] Preparation of PLA-coated 5-ALA methyl ester nanoparticles

[0043] 100 mg of PLA was added to 10 mL of anhydrous DCM, sealed and stirred overnight to completely dissolve the PLA.

[0044] Add 100 mg of 5-ALA methyl ester to 10 mL of absolute ethanol, and seal and stir overnight to completely dissolve 5-ALA methyl ester.

[0045] Electrospray the prepared PLA / DCM solution and 5-ALA methyl ester / absolute ethanol solution. The electrospray conditions are as follows: electrospray voltage 10KV, receiving distance 20cm, internal and external pushing speed ratio 2ml / h:4ml / h, electrospray Collect the obtained sample after 1h, vacuum dry for 24h, weigh and seal for storage.

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Abstract

The invention discloses a method for preparing nanometer particles of 5-ALA or 5-ALA derivatives by means of electrostatic spraying technology. The method uses polymer solution as shells and 5-ALA solution or 5-ALA derivative solution as cores, wraps the 5-ALA or the 5-ALA derivatives in polymer carrier in one step, and directly obtains nanometer particles with core-shell structures, so that various disadvantages of preparing carriers first and loading drugs next are avoided. Through regulation of preparation conditions such as the flow velocity, the concentration and the voltage, the nanometer particles are obtained, with even particle size distribution, high drug load and maintained biological activity of the 5-ALA or the 5-ALA derivatives. The nanometer particle prepared by the method has a drug load of 20 to 40% by weight. The method is simple, easy, and highly efficient.

Description

technical field [0001] The invention relates to the field of preparation of macromolecule nano-microsphere-loaded drugs, in particular to a method for preparing 5-ALA or its derivative nano-particles. Background technique [0002] 5-Aminolevulinic acid (5-ALA for short) is a non-protein amino acid that widely exists in biological organisms. Green agrochemicals, and 5-ALA and its derivatives also have great uses in medicine, as a second-generation photosensitizer, it has very important research in cancer treatment, tumor diagnosis and other clinical applications. [0003] Due to the important application prospects of 5-ALA and its derivatives, many researchers have done corresponding research on 5-ALA and its derivatives. Research on its physical and chemical properties, stability, physiological effects and its synthesis has been ongoing. However, Chinese scholars have done less research on 5-ALA and its derivatives, and there are only a handful of related documents. Foreig...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K41/00A61K8/41A61K8/02A23L1/29A01N37/44A61P35/00A01P13/00A01P3/00A01P21/00A01P7/04A23L33/00
Inventor 胡勇管艳萍张鲁中
Owner NANJING UNIV
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