Taxol long-circulating nanoparticle preparation and preparation method thereof

A paclitaxel and nanoparticle technology, which is applied in the field of preparation of the paclitaxel nanoparticle, can solve problems such as inability to complete large-scale production, stay in the laboratory, and immaturity, so as to maintain effective therapeutic concentration, reduce the number of medications, increase release effect

Inactive Publication Date: 2012-11-14
HANGZHOU PUSH KANG BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the technology of paclitaxel long-circulation nanoparticles is still immature, and there is no mature preparation process to prepare ideal long-acting nanoparticles, and many of them are still in the laboratory stage, unable to complete large-scale production

Method used

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  • Taxol long-circulating nanoparticle preparation and preparation method thereof
  • Taxol long-circulating nanoparticle preparation and preparation method thereof
  • Taxol long-circulating nanoparticle preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Implementation Example 1: Preparation of Forward Dropwise Long Circulation Nanoparticles

[0032] 40mg PLGA and 4mg paclitaxel were dissolved together in 10ml acetone solvent as oil phase, 120mg TPGS was dissolved in 50ml double distilled water to form water phase; the organic phase was dropped into the water phase at a speed of 1ml / min and stirred at a low speed of 300r / min to form a shallow phase. The blue nanoemulsion was reacted for 10 minutes, then transferred to a rotary evaporator, and treated for 30 minutes under vacuum rotary evaporation, and the acetone solution was removed to obtain long-circulation nanoparticles. The average particle size measured by the laser dynamic scattering instrument is 105.02±30nm, and the particle size distribution results are as follows: figure 1 shown. The encapsulation efficiency of nanoparticles is 80.2±4%, and the dispersion coefficient is 0.389.

Embodiment 2

[0033] Implementation Example 2: Preparation of Reverse Dropwise Long Circulation Nanoparticles

[0034] 40mg PLGA and 4mg paclitaxel were dissolved in 10ml of acetone solvent as an oil phase, 120mg TPGS was dissolved in 50ml double distilled water to form a water phase; the water phase was dropped into the organic phase at a speed of 5ml / min, and a shallow phase was formed under stirring at a low speed of 300r / min. The blue nano-emulsion, after reacting for 10 minutes, was transferred to a rotary evaporator, processed under vacuum rotary evaporation for 30 minutes, and the acetone solution was removed to obtain long-cycle nanoparticles. The result of diameter distribution is as figure 2 shown. The encapsulation efficiency of nanoparticles is 90.4±3%, and the dispersion coefficient is 0.042.

Embodiment 3

[0035] Implementation Example 3: Preparation of Reverse Dropwise Long Circulation Nanoparticles

[0036] 40mg PLGA and 8mg paclitaxel were dissolved together in 10ml acetone solvent as the oil phase, 120mg TPGS was dissolved in 50ml double-distilled water to form the water phase; the water phase was dropped into the organic phase at a speed of 5ml / min, and stirred at a low speed of 300r / min to form a shallow phase. The blue nanoemulsion, after reacting for 10 minutes, was transferred to a rotary evaporator, and treated for 30 minutes under vacuum rotary evaporation, and the acetone solution was removed to obtain long-cycle nanoparticles. The result of diameter distribution is as figure 2 shown. The encapsulation efficiency of nanoparticles is 84.4±3%, and the dispersion coefficient is 0.108.

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Abstract

The invention discloses taxol long-circulating nanoparticles. The nanoparticle preparation comprises taxol, a copolymer, a cosolvent, water for injection and the like, wherein according to the nanoparticles, the taxol is 5 to 20 percent of the weight of the copolymer. The invention also discloses a method for preparing the taxol long-circulating nanoparticles. A water phase with cosolvent water soluble vitamin E (TPGS) is dropwise added into an oil phase with the taxol and the copolymer by adopting a method for reversely dropwise adding the solvent, and the nanoparticle preparation with uniform particle size, high entrapment efficiency and high stability can be obtained, and the average particle size is less than 200 nm. The nanoparticle preparation can be used for treating malignant tumors; and an animal experiment shows that the nanoparticle preparation is relatively high in safety and effectiveness.

Description

Technical field: [0001] The invention relates to a long-circulation paclitaxel nanoparticle preparation, and at the same time, the invention also relates to a preparation method of the paclitaxel nanoparticle. Background technique: [0002] Paclitaxel is a tetracyclic diterpenoid isolated from the bark of Pacific yew. The molecular formula of paclitaxel is C 47 h 51 o 14 N, molecular mass 853.9, highly lipophilic, insoluble in water, plasma protein binding rate 89% to 98%, half-life 5.3 to 17.4 hours, mainly metabolized by liver, only 5% cleared by kidney. This drug began to be used in clinical research on ovarian cancer and breast cancer in 1983, and was approved by the US FDA in 1992. Clinical studies have confirmed that paclitaxel has an important and significant effect on various solid tumors, including breast cancer, advanced ovarian cancer, lung cancer, brain and neck tumors, and acute leukemia. It has been widely used clinically as a first-line drug. [0003] Pa...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/337A61K47/34A61P35/00
Inventor 余波王国营袁媛
Owner HANGZHOU PUSH KANG BIOTECH CO LTD
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