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Paclitaxel nano liposomes of dual targeting tumor and method for preparing paclitaxel nano liposomes

A nano-liposome, dual-targeting technology, used in the field of medicine to achieve the effect of inhibiting tumor growth and strong specific binding ability

Inactive Publication Date: 2011-08-31
SHANGHAI PULMONARY HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether the new dosage form of paclitaxel can improve the prognosis of cancer patients compared with the traditional dosage form of paclitaxel is still unknown.

Method used

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  • Paclitaxel nano liposomes of dual targeting tumor and method for preparing paclitaxel nano liposomes
  • Paclitaxel nano liposomes of dual targeting tumor and method for preparing paclitaxel nano liposomes
  • Paclitaxel nano liposomes of dual targeting tumor and method for preparing paclitaxel nano liposomes

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Example 1: Synthesis steps of dual targeting tumor polypeptides

[0037] The dual-targeting tumor peptide was synthesized by 9-fluorenylmethyloxycarbonyl (FMOC) solid-phase synthesis method, purified by high performance liquid chromatography (HPLC), and identified by mass spectrometry. Concrete synthetic steps are as follows:

[0038] 1) Resin swelling: put FMOC-AA-Wang-Resin resin into the reaction tube, add dimethylformamide (N, N-dimethylformamide, DMF) (15ml / g) for 30min;

[0039] Deprotection: discard DMF, add 20% piperidine DMF solution (15ml / g) for 5min, then add 20% piperidine DMF solution (15ml / g) for 15min;

[0040] 2) Detection: Take out the piperidine solution, take more than a dozen resins, wash them three times with ethanol, add ninhydrin, potassium cyanide, and phenol solution one drop each, heat at 105°C-110°C for 5 minutes, and turn dark blue as a positive reaction.

[0041] 3) Washing: DMF (10ml / g) twice, methanol (10ml / g) twice, DMF (10ml / g) twice; ...

Embodiment 2

[0050]Example 2: Preparation of non-targeting, single-targeting and dual-targeting tumor paclitaxel liposomes

[0051] Preparation of Paclitaxel Liposomes by Thin Film Ultrasonic Dispersion

[0052] Non-active targeting paclitaxel liposome formula: PC: CHOL: mPEG-DSPE: PTX9: 1: 0.5: 0.33, active targeting paclitaxel liposomes added different lipid polypeptides (ARYCRGDCFDG-KGG, ARYCRGDCFDATWLPPR- KGG) (to the total fat molar ratio is 1: 542). Since in the patent 1 embodiment, the polypeptide ATWLPPR and ATWLPPR-fluorescent liposomes do not show specific affinity to cells better than the polypeptides ARYCRGDCFDG, ARYCRGDCFDG-fluorescent liposomes and polypeptides ARYCRGDCFDATWLPPR, ARYCRGDCFDATWLPPR-fluorescent liposomes, therefore Not synthesized and not used in subsequent experiments.

[0053] The above formula was dissolved in chloroform, filtered through a 0.2 μm plate filter, placed in a rotary evaporator at 37°C to form a film, and then vacuumed for 1 hour to further re...

Embodiment 3

[0055] Embodiment 3: Paclitaxel liposome release experiment in vitro

[0056] 3ml of reconstituted non-active targeting paclitaxel liposomes, paclitaxel liposomes with single and dual targeting tumors, and Taxol were placed in a dialysis bag with a molecular weight of 14KD, and 20ml containing 45g / L bovine serum white was added to the bag Protein sterilized water simulates the internal environment, stirred with a constant temperature magnetic stirrer (300rpm), and 80μL of dialysate was taken out at 30min, 1h, 2h, 4h, 6h, 8h, and 24h for use, and at the same time, 80μL containing 45g / L cattle was added back to the dialysis bag. Serum albumin in sterile water. Add 320 μL of chromatographic grade methanol solution to the dialysate taken out to precipitate protein, vortex and mix, then centrifuge at 13000g×10min at high speed, and take the supernatant to detect paclitaxel content by HPLC. At the same time, the concentration of paclitaxel in each paclitaxel liposome and Taxol solu...

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Abstract

The invention belongs to the field of biomedicine. In particular, the invention discloses paclitaxel nano liposomes of dual targeting tumor. The dual targeting paclitaxel nano liposomes consist of three parts: polypeptides of dual targeting tumor, lipid attachments and paclitaxel liposomes. The invention also discloses a method for preparing the paclitaxel nano liposomes of dual targeting tumor and application of paclitaxel nano liposomes to preparation of a tumor-inhibiting medicament.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically, the invention discloses a nano-liposome with dual targeting tumors and a preparation method thereof. Background technique [0002] In recent years, the morbidity and mortality of malignant tumors have shown an obvious upward trend, and have become a major disease that threatens human health and life. According to a report by the International Agency for Research on Cancer, the number of cancer cases worldwide doubled between 1975 and 2000, with approximately 12 million new cases and more than 7 million deaths each year. In 2010, cancer will become the leading cause of death in the world. In 2030, the number of cancer patients will triple, and the number of new cases will increase to 20-26 million. [0003] Chemotherapy is one of the main methods in the comprehensive treatment of malignant tumors. A reasonable chemotherapy strategy can significantly prolong the survival time of canc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/48A61P35/00A61K47/64A61K47/65A61K47/69
Inventor 周彩存孟淑燕周蔚粟波李玮宋胤
Owner SHANGHAI PULMONARY HOSPITAL
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