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Nano micro ball with taxol capable of biologically degradating high molecule and its preparing method

A biodegradable, nano-microsphere technology, used in drug combination, powder delivery, anti-tumor drugs, etc., can solve the problems of reduced drug efficacy, toxic side effects, rodent carcinogenesis, etc., and achieves convenient use, small side effects, and low dosage Effect

Inactive Publication Date: 2005-01-12
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the dissolved DEHP enters the human body, it will cause toxic and side effects, because animal experiments have shown that DEHP can cause liver cell toxicity in animals and cause cancer in rodents
In addition, although the preparation was maintained at 4°C under sealed conditions for 5 years without deterioration before dilution, the stability after dilution was very poor and could only be maintained for a few hours. After 24 hours, small particles were precipitated and used after filtration. Significantly reduced potency
[0006] Due to the poor water solubility of paclitaxel, and there are many problems in the existing paclitaxel preparations, the development of new paclitaxel preparations with good water solubility has always been a hot spot of people's research.

Method used

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  • Nano micro ball with taxol capable of biologically degradating high molecule and its preparing method
  • Nano micro ball with taxol capable of biologically degradating high molecule and its preparing method
  • Nano micro ball with taxol capable of biologically degradating high molecule and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] 15mg of paclitaxel and 85mg of polylactide-polyethylene glycol diblock copolymer, diblock molecular weights are 60,000 and 5000 respectively dissolved in 5ml of dichloromethane, the dichloromethane solution was added to 40ml of 2% polyvinyl alcohol solution , phacoemulsification for 90 seconds, emulsification power of 70W. Then the obtained emulsion was diluted to 500ml with distilled water, volatilized under reduced pressure for 2 hours, collected nano-microspheres at 18,000 rpm, washed four times with distilled water, redispersed in water, and freeze-dried to obtain nano-microspheres containing paclitaxel.

[0028] The electron micrograph of the nanometer microsphere that gained is coated with paclitaxel is shown in figure 2 (a), its particle size is 760 ± 35nm, the drug loading is 12.5% ​​(w / w), its paclitaxel release behavior in vitro see image 3 (a) Line.

Embodiment 2

[0030] 10mg of paclitaxel and 67mg of polylactide-polyethylene glycol diblock copolymer, the molecular weight of the two blocks are 30,000 and 5000 respectively dissolved in 4ml of dichloromethane, the dichloromethane solution was added to 40ml of 2% polyvinyl alcohol solution , phacoemulsification for 75 seconds, emulsification power of 60W. Then the obtained emulsion was diluted to 400ml with distilled water, volatilized under reduced pressure for 2 hours, collected nano-microspheres at 20,000 rpm, washed four times with distilled water, redispersed in water, and freeze-dried to obtain nano-microspheres containing paclitaxel.

[0031] The electron micrograph of the nanometer microsphere that gained is coated with paclitaxel is shown in figure 2 (b), its particle size is 520 ± 42nm, drug loading is 11.4% (w / w), the release behavior of paclitaxel in vitro see image 3 (b) Line.

Embodiment 3

[0033]8mg of paclitaxel and 53mg of polylactide-polyethylene glycol diblock copolymer, the molecular weights of the two blocks are 10,000 and 5000 respectively dissolved in 3ml of dichloromethane, and the dichloromethane solution was added to 40ml of 2% polyvinyl alcohol solution , phacoemulsification for 60 seconds, emulsification power is 40W. Then the obtained emulsion was diluted to 400ml with distilled water, volatilized under reduced pressure for 2 hours, collected nano-microspheres at 20,000 rpm, washed four times with distilled water, redispersed in water, and freeze-dried to obtain nano-microspheres containing paclitaxel.

[0034] The electron micrograph of the nanometer microsphere that gained is coated with paclitaxel is shown in figure 2 (c), its particle size is 340 ± 50nm, drug loading is 9.8% (w / w), the release behavior of paclitaxel in vitro see image 3 (c) Line.

[0035] In the above three examples, the particle size, encapsulation rate and drug loading da...

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Abstract

A biodegradable high-molecular nanoball is prepared from the block copolymer of polylactone and polyethanediol and taxusol through dissolving them in organic solvent, adding the solution to the aqueous solution of polyvinyl alcohol or gelatin, ultrasonic emulsifying, and vacuum volatilization of organic solvent.

Description

technical field [0001] The invention belongs to biodegradable macromolecular nano microspheres loaded with paclitaxel and a preparation method thereof. Background technique [0002] Paclitaxel is a diterpene natural product, which was first isolated from the bark of Pacific yew tree and Taxus brevifolia by Wani et al. in 1971 (J.AM.Chem. Soc.), 93:2325 (1971)), and its structure was determined by chemical and X-ray crystallographic methods. It has been found to be effective in the treatment of various tumors, such as ovarian cancer, breast cancer, non-small cell lung cancer, head cancer and neck cancer. [0003] The biological activity of paclitaxel is related to its effect on cell division. It can promote the assembly of microtubule dimers into microtubules during cell division, and then increase the stability of microtubules by preventing the multimerization process, thereby inhibiting the normalization of the microtubule network. Kinetic reorganization, thereby affectin...

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 景遐斌张雪飞陈学思徐效义胡俊丽边新超杨立新
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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