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A kind of external use triptolide lipid nanoparticle and preparation method

A nanotechnology of triptolide and solid lipid, which is applied in the field of medicine, can solve the problems of organic solvent residue and high equipment requirements, and achieve the effect of high encapsulation efficiency

Active Publication Date: 2020-07-31
FUDAN UNIV SHANGHAI CANCER CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method described is a rapid membrane emulsification method. This patent requires high equipment and is carried out under nitrogen conditions, and there is a possibility of residual organic solvents

Method used

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  • A kind of external use triptolide lipid nanoparticle and preparation method
  • A kind of external use triptolide lipid nanoparticle and preparation method
  • A kind of external use triptolide lipid nanoparticle and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Mix triptolide 7.5mg, stearic acid 75mg, TPGS 150mg, Transcutol HP 75mg at 80°C, -1 Stir for 10 minutes under the same conditions to form the oil phase;

[0093] Heat 20ml of deionized water to the same temperature as the oil phase, and add it dropwise to the oil phase to make the system appear uniform and transparent, and continue to stir for 10 minutes to obtain triptolide solid lipid nanoparticle colostrum;

[0094] Rapidly disperse the above colostrum into 20 times the volume of colostrum in ice water at a temperature of 0±2° C., stir and solidify for 10 minutes to obtain triptolide solid lipid nanoparticles.

Embodiment 2

[0096] Mix triptolide 7.5mg, glyceryl behenate 80mg, TPGS 150mg, Transcutol HP75mg at 80°C, -1 Stir for 10 minutes under the same conditions to form the oil phase;

[0097] Heat 25ml of deionized water to the same temperature as the oil phase, and add it dropwise to the oil phase to make the system appear uniform and transparent, and continue to stir for 10 minutes to obtain triptolide solid lipid nanoparticle colostrum;

[0098] The above-mentioned colostrum is rapidly dispersed into 15 times the volume of the colostrum in ice water at a temperature of 0±2° C., stirred and solidified for 10 minutes to obtain triptolide solid lipid nanoparticles.

Embodiment 3

[0100] Mix triptolide 6.3mg, glyceryl behenate 75mg, Tween 80 150mg, Transcutol HP 75mg at 90°C, -1 Stir for 10 minutes under the same conditions to form the oil phase;

[0101] Heat 15ml of deionized water to the same temperature as the oil phase, and add it dropwise to the oil phase to make the system appear uniform and transparent, and continue stirring for 10 minutes to obtain triptolide solid lipid nanoparticle colostrum;

[0102] Rapidly disperse the above colostrum into 20 times the volume of colostrum in ice water at a temperature of 0±2° C., stir and solidify for 10 minutes to obtain triptolide solid lipid nanoparticles.

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Abstract

The invention relates to the field of medicines, and in particular to triptolide lipid nanoparticles for external use as well as a preparation method and an application of the triptolide lipid nanoparticles, wherein the triptolide lipid nanoparticles include triptolide solid lipid nanoparticles and a triptolide nano-structural lipid carrier. The triptolide lipid nanoparticles mainly consist of thefollowing ingredients: triptolide which serves as a medicinal raw material, the lipid carrier, a surfactant, a cosurfactant and water. The nanoparticles prepared by the invention are relatively highin encapsulation efficiency and cumulated transdermal permeation amount in vitro; based upon in-vitro pharmacokinetic researches, it is indicated that the triptolide lipid nanoparticles are excellentin sustained release effect, and a 'peak-valley phenomenon' can be effectively avoided. Based upon in-vivo pharmacodynamic experiments, it is indicated that the triptolide lipid nanoparticles, while effectively developing a therapeutic effect, can greatly reduce toxic and side effects. A preparing process of the lipid nanoparticles is free from residue of organic solvents; the technological process is easy to control and capable of achieving large-scale production; and the method has a good application prospect in the field of transdermal drug delivery.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to triptolide lipid nanoparticles for external use and a preparation method thereof. Background technique [0002] Triptolide (TPL), also known as triptolide, is one of the main active ingredients of the traditional Chinese medicine Triptolide, and its molecular formula is C 20 h 24 o 6 , the structural formula is as follows: [0003] [0004] Triptolide has anti-inflammatory, analgesic, anti-tumor and immunomodulatory effects, and is often used in the treatment of rheumatoid arthritis, skin eczema, immunosuppression, nephrotic syndrome and malignant tumors, and has good effects. [0005] However, triptolide has a short half-life and high toxicity. After oral administration, the absorption and elimination rate is fast, and it is easy to cause adverse reactions in the digestive system and genitourinary system. 50 It is 0.8mg / Kg. Therefore, changing its administration route a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/585A61P17/00
CPCA61K9/0014A61K9/5031A61K31/585A61P17/00
Inventor 刘继勇顾永卫顾清杨盟唐晓萌王婷
Owner FUDAN UNIV SHANGHAI CANCER CENT
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