Paclitaxel polymer nanoparticle and preparation method

A nanoparticle and paclitaxel technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem that the release speed of polylactic acid cannot be adjusted, by-products and raw material residues, preparation The problem of complex process, etc., to avoid the residue of by-products and catalysts, low cost, and simple preparation process.

Inactive Publication Date: 2013-06-26
SHANGHAI NAT ENG RES CENT FORNANOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] a) A single-component polymer material can effectively control the release of paclitaxel, such as paclitaxel polylactic acid nanoparticles. A large number of studies have shown that the release process of paclitaxel-loaded lactic acid nanoparticles is faster than the theoretical release effect than the ideal state At the same time, since there is only one component of polylactic acid, although the ratio of paclitaxel in polylactic acid can be adjusted, the release rate of polylactic acid cannot be adjusted.
[0011] b) The synthesis cost of multi-component co-block polymer materials is extremely high, the preparation process is complicated, and there are residual problems of by-products and raw materials in chemical synthesis, such as paclitaxel polylactic acid-glycolic acid copolymer nanoparticles, polylactic acid- Glycolic acid copolymers may have residual lactic acid monomers during material synthesis

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  • Paclitaxel polymer nanoparticle and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Investigate the effect of polymer material type on paclitaxel / polylactic acid nanoparticles. Weigh 3 g of polylactic acid, poly(lactic acid-glycolic acid) (lactic acid: glycolic acid = 50: 50), polyhydroxybutyric acid, polyhydroxybutyric acid / polylactic acid (polyhydroxybutyric acid: polylactic acid = 50: 50 ) mixtures were respectively dissolved in 100ml of dichloromethane, magnetically stirred at room temperature to dissolve until completely dissolved, 0.3g of paclitaxel was added, and magnetically stirred for 10 minutes until uniformly dissolved to form an organic phase. Weigh 30g of polyvinyl alcohol and dissolve it in 1000ml of water, dissolve at high temperature for 1 hour until completely dissolved and cool to room temperature to form a water phase. Take out 2ml of the above-mentioned organic phase and 200ml of the aqueous phase and place them in a dry beaker, and perform ultrasonic treatment at 100W for 10 minutes (work for 3 seconds, rest for 3 seconds) to form...

Embodiment 2

[0043]Investigate the effect of organic solvent types on paclitaxel / polylactic acid nanoparticles. Weigh 1g of polyhydroxybutyric acid / polylactic acid (polyhydroxybutyric acid:polylactic acid=50:50) mixture and dissolve in 100ml of dichloromethane, chloroform, dichloromethane / chloroform 1:1 mixture , magnetic stirring at room temperature until completely dissolved, adding 0.3 g of paclitaxel, and continuing magnetic stirring for 10 minutes until uniformly dissolved, forming an organic phase. Weigh 30g of polyvinyl alcohol and dissolve it in 1000ml of water, dissolve at high temperature for 1 hour until completely dissolved and cool to room temperature to form a water phase. Take out 40ml of the above-mentioned organic phase and 200ml of the aqueous phase and place them in a dry beaker, and perform ultrasonic treatment at 100W for 10 minutes (work for 3 seconds, rest for 3 seconds) to form an emulsion. Immediately pour the emulsion into a rotary evaporator to remove the organi...

Embodiment 3

[0049] The effect of the concentration of polymer materials in the organic phase on paclitaxel / polylactic acid nanoparticles was investigated. Weigh 0.5g, 1g, 2g, 3g of polyhydroxybutyric acid\polylactic acid (polyhydroxybutyric acid:polylactic acid=50:50) mixture and dissolve in 100ml dichloromethane / chloroform 1:1 mixture , magnetically stirred at room temperature until completely dissolved, then added 0.3 g of paclitaxel, and continued to magnetically stir for 10 minutes until uniformly dissolved and an organic phase was formed. Weigh 30g of polyvinyl alcohol and dissolve it in 1000ml of water, dissolve at high temperature for 1 hour until completely dissolved and cool to room temperature to form a water phase. Take out 10ml of the above-mentioned organic phase and 200ml of the aqueous phase and place them in a dry beaker, and perform ultrasonic treatment at 100W for 10 minutes (work for 3 seconds, rest for 3 seconds) to form an emulsion. Immediately pour the emulsion into...

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Abstract

The invention discloses a paclitaxel polymer nanoparticle. The paclitaxel polymer nanoparticle can be used as a slow-release carrier of a paclitaxel medicament and is characterized in that the particle size of the nanoparticle is 50-800nm, a composition of the paclitaxel polymer nanoparticle contains the components of a biodegradable polymer material, the paclitaxel medicament and a stabilizing agent; the encapsulation rate of the paclitaxel medicament is within 2.0-6.0%; and the paclitaxel polymer nanoparticle has a paclitaxel slow-release effect. The invention also discloses a preparation method of the nanoparticle. The paclitaxel can be scattered in the nanoparticle prepared from the biodegradable polymer material under the condition of maintaining the original biological activity of the paclitaxel. Pure physical effects are played in the whole process, side effects brought by residue of other reagents in the chemical synthesis process can be effectively avoided, and the prepared nanoparticle can effectively play a role in medicament slow release. Compared with a conventional method, the preparation method does not need chemical reaction, and is simple in preparation process, relatively low in cost and relatively energy-saving.

Description

technical field [0001] The invention relates to a polymer nanoparticle and a preparation method, in particular to a paclitaxel polymer nanoparticle and a preparation method, which are used in the clinical treatment of tumors. Background technique [0002] Paclitaxel is one of the most clinically effective broad-spectrum antineoplastic drugs so far. However, its poor water solubility and clinical side effects caused by high local concentration during in vivo administration greatly limit its wide clinical application. In order to further solve the problem of poor solubility of paclitaxel and avoid the side effects of one-time local large amount of drug toxicity, it is the best method to prepare paclitaxel as a sustained-release medicament. [0003] At present, publicly reported paclitaxel sustained-release agents include liposomes, emulsions, polymer microspheres and nanoparticles, etc. With the deepening of research and clinical trials, it is found that the existing paclitaxe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K47/34A61P35/00
Inventor 魏岱旭钟建闫志强何丹农
Owner SHANGHAI NAT ENG RES CENT FORNANOTECH
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