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Paclitaxel-entrapped biodegradable nanocomposite and preparation method thereof

A nanocomposite, paclitaxel technology, applied in the field of biodegradable nanocomposites loaded with anti-tumor drug paclitaxel and its preparation, can solve the problems of slow degradation rate, research and application limitations, strong hydrophobicity of PTMC, etc., to achieve extended Half-life, increased healing, and effects that prevent devouring

Inactive Publication Date: 2012-12-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The PTMC can be erosively degraded in vivo or in the presence of enzymes without producing acidic substances, and has better biocompatibility than other types of polyesters; however, PTMC has strong hydrophobicity and slow degradation rate. Its research and application in the field of biomedicine are greatly restricted

Method used

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  • Paclitaxel-entrapped biodegradable nanocomposite and preparation method thereof
  • Paclitaxel-entrapped biodegradable nanocomposite and preparation method thereof
  • Paclitaxel-entrapped biodegradable nanocomposite and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Take by weighing 40mg PEG (1000)-PTMC (6000) copolymer, 2mg paclitaxel, add 1ml dichloromethane, ultrasound makes carrier material and medicine fully dissolved; Said solution is added in the 2% polyvinyl alcohol solution of 5ml, Ultrasonic with ice-bath probe, ultrasonic power is 300W, ultrasonic time is 5s, ultrasonic interval is 5s, and the number of ultrasonics is 20 times; colostrum is obtained after ultrasonication, and the colostrum is added dropwise to 25ml of 1% polyvinyl alcohol solution , magnetically stirred at 100 r / min, and after stirring for 1 min, at 37° C., the dichloromethane was removed by rotary evaporation to obtain the paclitaxel PEG-PTMC nanocomposite preparation.

[0047] The particle size measurement results showed that the average particle size of the prepared PEG-PTMC nanocomposite was 96±28.1 nm.

Embodiment 2

[0049] Take by weighing 40mg PEG (3000)-PTMC (6000) copolymer, 2mg paclitaxel, add 1ml dichloromethane, ultrasound makes carrier material and medicine fully dissolve; Said solution is added in the 0.6% sodium cholate solution of 5ml, Ultrasonic with an ice bath probe, the ultrasonic power is 300W, the ultrasonic time is 5s, the ultrasonic interval is 5s, and the number of ultrasonics is 20 times; the colostrum is obtained after ultrasonication, and the colostrum is added dropwise to 25ml of 0.3% sodium cholate solution , magnetically stirred at 100 r / min, and after stirring for 1 min, at 37° C., the dichloromethane was removed by rotary evaporation to obtain the paclitaxel PEG-PTMC nanocomposite preparation.

[0050] The particle size measurement results showed that the average particle size of the prepared PEG-PTMC nanocomposite was 49±8.1 nm.

Embodiment 3

[0052] Take by weighing 40mg PEG (3000)-PTMC (9000) copolymer, 2mg paclitaxel, add 1ml dichloromethane, ultrasound makes carrier material and medicine fully dissolve; This solution is added in the 0.6% sodium cholate solution of 5ml, ice Bath probe ultrasonication, ultrasonic power is 300W, ultrasonic time is 5s, ultrasonic interval time is 5s, and the number of ultrasonic waves is 15 times; the colostrum is obtained after the ultrasonic wave is completed, and the colostrum is added dropwise to 25ml of 0.3% sodium cholate solution, Magnetic stirring was performed at 100 r / min. After stirring for 1 min, dichloromethane was removed by rotary evaporation at 37° C. to obtain paclitaxel PEG-PTMC nanocomposite preparation.

[0053] The particle size measurement results showed that the average particle size of the prepared PEG-PTMC nanocomposite was 79±18.8 nm.

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Abstract

The invention belongs to the technical field of biological medicines and relates to a paclitaxel-entrapped biodegradable nanocomposite and a preparation method thereof. A paclitaxel polyethylene glycol-poly trimethylene carbonate (PEG-PTMC) nanocomposite is prepared by adopting an emulsification / solvent evaporation method, and by taking a PEG-PTMC copolymer as a carrier, paclitaxel is entrapped in a hydrophobic core of PTMC. The solubility of the paclitaxel can be effectively increased by the prepared paclitaxel PEG-PTMC nanocomposite, and a PEG long chain of a carrier material can take effect of invisibility, and thereby, the phagocytosis of an in-vivo reticulo-endothelial system is avoided. The nanocomposite has a long circulation effect, and the half-life period of the nanocomposite in blood can be prolonged. Moreover, through controlling the grain size of the nanocomposite, a passive targeting effect on a tumor tissue is realized, and thereby, a treatment effect is improved. As the nanocomposite does not contain Cremophor El or ethanol, compared with commercially available paclitaxel injections, the toxic and side effects of the nanocomposite can be reduced, and the safety of the nanocomposite in clinical application is enhanced.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a biodegradable nanocomposite loaded with an antitumor drug paclitaxel and a preparation method thereof. technical background [0002] Studies have disclosed that Paclitaxel is a new anti-microtubule antineoplastic drug, which promotes the assembly of microtubules, inhibits depolymerization, maintains the stability of tubulin, and inhibits cell mitosis by promoting the polymerization of spindle tubulin; The above effects can also occur in the absence of mediators (such as guanosine triphosphate, GTP) required for normal microtubule assembly, resulting in the formation of stable, non-functional microtubules. In vitro experiments have proved that paclitaxel has a significant radiosensitizing effect, which may cause cells to stop in the G2 and M phases that are sensitive to radiotherapy; clinically it is mainly used for breast cancer, non-small cell lung cancer, pancreatic cancer,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K47/34A61P35/00
Inventor 方晓玲姜新义沙先谊
Owner FUDAN UNIV
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