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Polymeric micelle for tumor anti-inflammatory treatment and chemotherapy and preparation method thereof

A polymer glue and polymer technology, applied in the field of polymer chemistry and biomedical engineering, can solve the problems of inconvenient preparation and administration, hindering popularization and application, high cost, etc., to enhance anti-tumor effect, improve drug efficacy and Utilization rate, the effect of reducing toxic and side effects

Active Publication Date: 2018-11-16
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PTX has the disadvantages of poor water solubility, the use of polyoxyethylene hydrogenated castor oil (cremophor EL) as a solubilizer can easily cause allergic reactions, and it is inconvenient to prepare and administer.
Albumin-stabilized paclitaxel nanoformulation formulation It is the second type of commercialized nano-preparation without cremophor EL approved by the FDA, but the high cost hinders its popularization and application

Method used

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  • Polymeric micelle for tumor anti-inflammatory treatment and chemotherapy and preparation method thereof
  • Polymeric micelle for tumor anti-inflammatory treatment and chemotherapy and preparation method thereof
  • Polymeric micelle for tumor anti-inflammatory treatment and chemotherapy and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] A kind of polymer micelle and preparation method thereof for tumor anti-inflammation treatment and chemotherapy, the synthesis route process of said polymer micelle is as follows figure 1 shown, including the following steps:

[0058] 1. Synthesis of diblock copolymer allyl polyethylene glycol-polycaprolactone (APEG-PCL-OH)

[0059] Weigh 1.8g of Allyl-PEG-OH (Mw 1.8kDa, 1mmol) into a 50mL reaction flask, dry it in vacuum at 70°C for 2h, add 1 drop of stannous octoate Sn(Oct) 2 Continue drying for 0.5h, then add dry 4.5g caprolactone and 15mL anhydrous toluene. in N 2 Stir the reaction at 110°C for 18 hours, precipitate in excess diethyl ether, filter with suction, and dry to obtain 5.7 g of a white powder product with a yield of 91%. Its composition is APEG 1.8k -PCL 4k -OH.

[0060] 2. Synthesis of APEG-PCL-Ac polymer

[0061] Dissolve 2.9 g of APEG-PCL-OH (Mw 5.8 kDa, 0.5 mmol) in 15 mL of anhydrous CH 2 Cl 2 , at N 2 Add 0.36mL acetyl chloride (5mmol) unde...

Embodiment 2

[0081] A polymer micelle for tumor anti-inflammatory treatment and chemotherapy and a preparation method thereof, steps 1-6 and step 9 are the same as in Example 1, except that the polymer is not coupled to the anti-inflammatory drug molecule CXB. The remaining steps are as follows:

[0082] 7. SA-GGPLGLAGG-Lys (N 3 )-NH 2 Synthesis

[0083] The polypeptide is the substrate of MMP-2, and the synthesis steps are as follows: Weigh a certain amount of Rink Amide resin into a polypeptide solid-phase synthesis column, and wash the resin with DCM and DMF respectively. Weigh Fmoc-Lys (N 3 )-OH was dissolved in DMF in a 50mL centrifuge tube, and activators (HOBT and HBTU) with a degree of substitution of 3.4 times the equivalent of the resin and DIEA with 6 times the equivalent of DIEA were added to react at room temperature for 2 hours, and then the DMF solution was transferred to the peptide solid. Phase synthesis column, continue to stir for 4 ~ 6h. Wash the resin with DMF sol...

Embodiment 3

[0087] A kind of polymer micelle and preparation method thereof for tumor anti-inflammatory treatment and chemotherapy, steps 1 to 7 and step 9 are the same as in Example 1, the difference is that [PPLG-g-(CXB-peptide&mPEG)]-PEG -The proportion of CXB-peptide and mPEG in the PCL-Ac polymer is different, and the mass fraction of CXB is adjusted. The remaining steps are as follows:

[0088] 8. Synthesis of the final polymer [PPLG-g-(CXB-peptide&mPEG)]-PEG-PCL-Ac, namely PCxbP

[0089] Weigh 121mg PPLG-PEG-PCL-Ac (containing 0.3mmol alkyne), 65mg Peptide-Azides (0.05mmol) and 3mg CuSO 4 ·5H 2 O to a 15mL Schlenk bottle, add 4mL DMF to dissolve. Freezing and thawing cycle 2 times basically removes oxygen and replaces it with N 2 Afterwards, 15 mg sodium vitamin C (NaAsc) was added, frozen and thawed once again, sealed, and reacted at 30° C. for 12 hours. Then add 500mg mPEG 1k -N 3 (0.5mmol) and 15mg NaAsc, stir to dissolve, freeze and thaw once to remove oxygen, and react ...

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Abstract

The invention belongs to the technical field of high polymer chemistry and biomedical engineering, and particularly relates to a polymeric micelle for tumor anti-inflammatory treatment and chemotherapy and a preparation method thereof. The polymeric micelle is of a core-shell; polycaprolactone, as a hydrophobic core of the micelle, can load paclitaxel or other hydrophobic pharmaceutical molecules;and a shell layer is formed on the surface of the micelle by a matrix metalloproteinase sensitive polypeptide coupled anti-inflammatory drug and polyethylene glycol together. The polymeric micelle releases the coupled anti-inflammatory drug under the action of matrix metalloproteinase with high expression for solid tumor tissues, implements controllable release of the drug, carries out targeted treatment on the local inflammatory response of tumors, can be used for combined treatment of tumor anti-inflammatory treatment and chemotherapy, and greatly reinforces an anti-tumor effect.

Description

technical field [0001] The invention relates to the technical field of polymer chemistry and biomedical engineering, in particular to a polymer micelle used for tumor anti-inflammatory treatment and chemotherapy and a preparation method thereof. Background technique [0002] Malignant tumors present a high incidence state, seriously endangering people's health and life. Paclitaxel (PTX) is a broad-spectrum first-line chemotherapy drug, which is mainly used in the treatment of ovarian cancer and breast cancer clinically, and is also effective for melanoma, colorectal cancer, lymphoma, head and neck cancer, glioma and lung cancer. It has a certain curative effect. PTX has the disadvantages of poor water solubility, the use of polyoxyethylene hydrogenated castor oil (cremophor EL) as a solubilizer can easily cause allergic reactions, and it is inconvenient to prepare and administer. Albumin-stabilized paclitaxel nanoformulation formulation It is the second type of commercia...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/64A61K47/59A61K45/00A61K31/635A61K47/34A61K31/337A61P35/00A61P29/00
CPCA61K9/1075A61K31/337A61K31/635A61K45/00A61K47/34A61K47/593A61K47/64A61P29/00A61P35/00A61K2300/00
Inventor 帅心涛黄金生徐永敏谢超程度
Owner SUN YAT SEN UNIV
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