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Application of vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) in preparing porous drug carrier particles

A technology of vitamins and drugs, applied in the field of porous drug carrier particles, can solve problems such as multidrug resistance, reduce sensitivity to chemotherapy, and easily lead to hypersensitivity reactions

Inactive Publication Date: 2014-04-30
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The currently widely used drug carriers are prone to hypersensitivity reactions, and the subjects who administer the drug have little intake of the drug, and the drug has a greater impact on other body parts, which is likely to produce a large negative effect and easily lead to multidrug resistance (MDR) ) effect, thereby reducing the body's sensitivity to chemotherapy

Method used

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  • Application of vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) in preparing porous drug carrier particles
  • Application of vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) in preparing porous drug carrier particles
  • Application of vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) in preparing porous drug carrier particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Embodiment 1, preparation of PLGA microspheres loaded with docetaxel and PLGA / TPGS blended microspheres

[0071] Three kinds of microspheres loaded with docetaxel were prepared by solvent evaporation method. The preparation of MPT0 microspheres (PLGA microspheres) was as follows: 90 mg of PLGA / TPGS mixture and 10 mg of docetaxel were accurately weighed with a precision electronic balance, added to 8 mL of dichloromethane (DCM), and left at room temperature until fully dissolved. Measure 100mL of 0.03% TPGS solution with a graduated cylinder, put it into a 250mL beaker, and add the mixed solution of the first step into it for emulsification under the condition of stirring at a rotating speed of 400rpm. After stirring overnight, the organic solvent was removed and PLGA microspheres were formed. Centrifuge at 5000 rpm for 5 min and wash three times with deionized water to remove attached TPGS and docetaxel. The resulting precipitate was resuspended in 3 mL of deionized w...

Embodiment 2

[0074] Example 2, preparation and performance of PLGA nanoparticles loaded with docetaxel (or blank) and PLGA / TPGS blended nanoparticles

[0075] Nanoparticle preparation

[0076] According to the preparation conditions listed in Table 1, PLGA nanoparticles (NPT0) and PLGA / TPGS blended nanoparticles (NPT10 and NPT20) loaded with docetaxel were prepared with reference to the method of Example 1, and the solvent acetone was replaced by dichloro Methane, and the stirring speed was 800rpm for 2h, then reduced to 600rpm and stirred overnight, and the centrifugation condition used for harvesting nanoparticles was 20,000rpm, centrifuged at 4°C for 15min. In addition, blank PLGA nanoparticles and PLGA / TPGS blend nanoparticles were prepared by not adding docetaxel.

[0077] Characterization of Nanoparticles

[0078] Take the NPT0, NPT10 and NPT20 nanoparticle suspensions before freeze-drying, use dynamic light scattering to analyze the particle size and particle size distribution, an...

Embodiment 3

[0103] Example 3, preparation and characteristics of PLGA nanoparticles loaded with coumarin and PLGA / TPGS blended nanoparticles

[0104] Nanoparticle preparation

[0105] According to the preparation conditions listed in Table 1, with reference to the method of Example 2, the PLGA / TPGS blended nanoparticles loaded with coumarin-6 were prepared, except that docetaxel was replaced by coumarin-6, and the obtained nanoparticles Denote as NPT0C, NPT10C and NPT20C, wherein the percentage of TPGS in the PLGA / TPGS mixture when the numerical table is prepared.

[0106] Characterization analysis

[0107] Take the NPT0C, NPT10C and NPT20C nanoparticle suspensions before freeze-drying, use dynamic light scattering to analyze particle size and particle size distribution, and use laser Doppler velocimetry to measure the zeta potential of nanoparticles. Three replicate measurements were performed. Results are expressed as mean ± standard deviation (SD). The results are shown in Table 4....

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Abstract

The invention discloses application of vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) in preparing porous drug carrier particles, a method for preparing porous drug carrier particles, and the porous drug carrier particles. The method comprises the following steps: dissolving vitamin E TPGS, medicines and organic macromolecular polymer, such as PLGA (poly(lactic-co-glycolic acid)), in an organic solvent; emulsifying, removing the organic solvent in a volatizing manner to obtain the drug-loaded porous drug carrier particles with a porous structure on the surface. The porous drug carrier particles have the characteristics of small toxicity, high target, high encapsulation rate, porosity and drug in-vitro release acceleration, can be used for inhibiting P-gp induced drug transportation due to TPGS, so that the multi-drug resistance effect of an administrated object can be inhibited; furthermore, the porous drug carrier particles are utilized in administration, and the drug utilization is high, so that the dosage can be effectively reduced, and side effects can be further reduced.

Description

technical field [0001] The invention relates to the use of vitamin E TPGS in preparing porous drug carrier microparticles, a method for preparing porous drug carrier microparticles, and porous drug carrier microparticles. Background technique [0002] The currently widely used drug carriers are prone to hypersensitivity reactions, and the subjects who administer the drug have little intake of the drug, and the drug has a greater impact on other body parts, which is likely to produce a large negative effect and easily lead to multidrug resistance (MDR) ) effect, thereby reducing the body's sensitivity to chemotherapy. [0003] Therefore, at this stage, there is an urgent need to develop drug carriers that can efficiently deliver drugs to target locations and slowly release the delivered drugs, effectively improve drug utilization, reduce side effects and multidrug resistance, and have low toxicity. Contents of the invention [0004] The present invention aims to solve at l...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/16
Inventor 梅林朱慧君陈红波黄来强曾小伟
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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