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Self-assembling medicine carrying system of o-nitrophenyl propanoic acid taxol conjugates, and preparation method and application thereof

The technology of paclitaxel nitrophenylpropionate and nitrophenylpropionic acid is applied to the self-assembled drug loading system of o-nitrophenylpropionate-paclitaxel conjugate and the field of preparation thereof, which can solve the problem of low drug loading and affecting the use of paclitaxel and development, constraints and other issues

Active Publication Date: 2017-12-01
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the carrier delivery of paclitaxel is limited by the drug loading of the drug carrier and the stability of the drug carrier. Insufficient drug loading and drug leakage affect the use and development of paclitaxel
[0004] Carrier-free self-assembled nanosystems have the advantages of nano-drug delivery systems (such as passive targeting ability, prolonged circulation time in vivo, and improved pharmacokinetic behavior), while overcoming the low drug loading of traditional carrier nano-delivery systems. However, it is difficult to predict whether the drug can form a carrier-free self-assembled nanosystem and how to form a self-assembled nano-drug system.

Method used

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  • Self-assembling medicine carrying system of o-nitrophenyl propanoic acid taxol conjugates, and preparation method and application thereof
  • Self-assembling medicine carrying system of o-nitrophenyl propanoic acid taxol conjugates, and preparation method and application thereof
  • Self-assembling medicine carrying system of o-nitrophenyl propanoic acid taxol conjugates, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Preparation of o-nitrophenylpropionate paclitaxel conjugate self-assembled drug loading system

[0060] Dissolve the nitrophenylpropionate-paclitaxel conjugate in an appropriate amount of dimethyl sulfoxide to obtain a 4mg / ml o-nitrophenylpropionate-paclitaxel conjugate solution, pipette 200 μl dropwise into 4ml pure water, And keep stirring to get o-nitrophenylpropionate-paclitaxel conjugate self-assembled nano drug-loading system dispersion (NPPA-PTX NP), then transfer it into a dialysis bag, and use deionized water to dialyze for 24-48 hours to remove the two Methyl sulfoxide, that is, too.

Embodiment 2

[0061] Example 2: Preparation of o-nitrophenylpropionate paclitaxel conjugate self-assembled drug loading system

[0062] The 1 mg / ml o-nitrophenylpropionate-paclitaxel conjugate solution obtained by dissolving the o-nitrophenylpropionate-paclitaxel conjugate in an appropriate amount of ethanol was pipette 200 μl dropwise into 8ml 5% glucose solution, and Stir continuously to obtain the dispersion liquid of paclitaxel o-nitrophenylpropionate conjugate self-assembled nanometer drug-carrying system, then transfer it into a dialysis bag, and use deionized water to dialyze for 24-48 hours to remove ethanol.

Embodiment 3

[0063] Example 3: Preparation of o-nitrophenylpropionate paclitaxel conjugate self-assembled drug loading system

[0064] Dissolve the nitrophenylpropionate-paclitaxel conjugate in an appropriate amount of dimethyl sulfoxide and acetone mixed solution to obtain a 6mg / ml o-nitrophenylpropionate-paclitaxel conjugate solution, pipette 400μl dropwise into 10ml 5% alcohol-containing aqueous solution, and keep stirring to obtain the dispersion of o-nitrophenylpropionate-paclitaxel conjugate self-assembled nano drug-loading system, then transfer it to a dialysis bag, and use deionized water to dialyze for 24-48 hours to remove Dimethyl sulfoxide and acetone, too.

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Abstract

The invention relates to a self-assembling medicine carrying system of o-nitrophenyl propanoic acid taxol conjugates. The self-assembling medicine carrying system is characterized in that the medicine carrying system contains o-nitrophenyl propanoic acid taxol conjugates and a liquid solvent and optionally contains a surfactant or a solubilizing material. The self-assembling nanometer system with no carriers or few carriers has the advantages of a nanometer medication system, overcomes the defects of low medicine carrying quantity, medicine carrying instability and the like of a conventional carrier nanometer transferring system at the same time, and has good application prospects.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a self-assembled drug-loading system of paclitaxel o-nitrophenylpropionate conjugates, a preparation method and application thereof. Background technique [0002] Chemotherapy is one of the commonly used means of clinical anti-tumor treatment, and paclitaxel is a representative of chemotherapy drugs with outstanding efficacy. However, since the drug is insoluble in water and easy to crystallize, it is necessary to add a large amount of auxiliary materials such as solubilizers and co-solvents in the preparation to increase the solubility of the drug. However, the added excipients can cause obvious adverse reactions. For example, the polyoxyethylene castor oil added to the paclitaxel formulation Taxol can cause allergic reactions and neurotoxicity, and this formulation cannot specifically act on tumor tissue. , so it will also produce strong toxic and side effe...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/69A61K31/337A61K47/24A61P35/00A61P35/02
CPCA61K31/337A61K47/24
Inventor 张烜姚鑫
Owner PEKING UNIV
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