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Drug delivery system for targeting co-delivery of photosensitizer and chemotherapeutic drug

A chemotherapeutic drug and photosensitizer technology, applied in the field of new drug delivery system, can solve the problems of reducing drug loading and encapsulation efficiency, high drug accumulation, poor stability of photosensitizer, etc., to achieve high drug loading efficiency in the inner core, low Critical micelle concentration, effect of increasing accumulation

Active Publication Date: 2017-05-03
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although nanotechnology can be used for the co-encapsulation of photosensitizers and chemotherapy drugs to a certain extent, there are still some serious problems in practical applications, such as: the physical stability of photosensitizers encapsulated by polymer carriers is poor, and it is easy to Leakage; co-encapsulation of photosensitizers and chemical drugs in nanocarriers will reduce the drug loading and encapsulation efficiency of both; nanocarriers cannot achieve high accumulation of drugs in tumor sites only relying on passive targeting, etc.

Method used

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  • Drug delivery system for targeting co-delivery of photosensitizer and chemotherapeutic drug
  • Drug delivery system for targeting co-delivery of photosensitizer and chemotherapeutic drug
  • Drug delivery system for targeting co-delivery of photosensitizer and chemotherapeutic drug

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Embodiment 1

[0031] Example 1 Preparation and characterization of nanoparticles co-encapsulating doxorubicin and chlorin e6

[0032] Preparation of nanoparticles by nanoprecipitation method, including: weighing doxorubicin hydrochloride and adding it to the mixture of acetone and tetrahydrofuran, and adding triethylamine (the molar ratio of doxorubicin to triethylamine is 1:3) to seal the reaction overnight, and the reaction The liquid was spin-dried in a vacuum to obtain desalted doxorubicin, which was co-dissolved in acetone (1 mL) with TPGS-Ce6, TPGS-PLA, and TPGS at a mass ratio of 6:3:1 to prepare a 10 mg / mL polymer acetone solution. Add the polymer solution dropwise into rapidly stirred 0.1M phosphate buffer (pH 7.4) with a 1mL syringe at room temperature (volume ratio of organic phase to aqueous phase is 1:2), and after rapid stirring for 3 h, use coagulation The gel column was used to separate and remove unencapsulated doxorubicin to obtain NP, which was stored at 4°C for later use...

Embodiment 2

[0034] Qualitative and quantitative results of nanoparticle uptake by embodiment 2 HUVEC cells

[0035] HUVEC cells were seeded in a 96-well plate at a density of 5000 cells / well, placed in a 5% carbon dioxide incubator and cultured for 24 hours, and the original medium was replaced with doxorubicin group, NP group, NP+light group, tLyP-1- NP group, tLyP-1-NP+ light group, and set the concentration gradient to 0.4, 0.6, 0.8, 1, 2, 3 μg / mL, after 30 minutes of dark incubation, use a laser probe emitting 660nm near-infrared wavelength at 0.6 J / cm 2 (22mW / cm 2 , 30s) to irradiate the well plate, continue to incubate in the incubator at 37°C for 2h, wash the plate 3 times with warm PBS (0.1M phosphate buffered saline solution, pH7.4), add paraformaldehyde Fix for 15 minutes, stain the nucleus with 2 μg / mL Hochest33258 for 10 minutes, and finally add 200 μL PBS to each well to quantitatively analyze the cellular uptake of the drug with a high-content instrument; observe and take pi...

Embodiment 3

[0037] Qualitative and quantitative results of nanoparticle uptake by embodiment 3MCF-7 / ADR cells

[0038] MCF-7 / ADR cells were seeded in 96-well plates at a density of 5000 / well, placed in a 5% carbon dioxide incubator and cultured for 24 hours, and the original medium was replaced with doxorubicin group, NP group, NP+light group, tLyP-1-NP group, tLyP-1-NP+light group, and set the concentration gradient to 0.4, 0.6, 0.8, 1, 2, 3 μg / mL, after 30min of dark incubation, use a laser emitting 660nm near-infrared wavelength Probe at 0.6J / cm 2 (22mW / cm 2 , 30s) to irradiate the well plate, continue to incubate at 37°C for 2 hours, wash the plate three times with warm PBS, add paraformaldehyde to fix for 15 minutes, 2 μg / mL Hochest33258 to stain the nuclei for 10 minutes, and finally Add 200 μL PBS to each well, and use a high-content instrument to quantitatively analyze the cellular uptake of the drug; observe and take pictures with an inverted fluorescence microscope;

[0039] ...

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Abstract

The invention belongs to the field of pharmaceutical preparations and relates to a drug delivery system for targeting co-delivery of a photosensitizer and a chemotherapeutic drug. According to the drug delivery system, a nanometer preparation is prepared from vitamin E polyethylene glycol succinate-L-polylactic acid as a raw material, a chemotherapeutic drug adriamycin is wrapped in a hydrophobic inner core of the nanometer preparation, simultaneously, a photosensitizer chlorin e6 is connected to vitamin E polyethylene glycol succinate (TPGS) through a covalent bond, then the compound is inserted into a shell structure of the nanometer preparation so that efficient and stable coating of the chemotherapeutic drug and the photosensitizer is realized, and a polypeptide tLyp-1 having a targeting function modifies the surface of the nanometer preparation through a covalent bond so that nanometer preparation vascular permeability and tumor penetrability are promoted. Results of in-vitro and in-vivo experiments show that the drug delivery system is used for treatment on tumors resisting multiple drugs, has the characteristics of good targeting ability, high efficiency and low toxicity, and has a clinical application prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug delivery system for targeted co-delivery of photosensitizers and chemotherapeutic drugs to tumor sites, in particular to a drug delivery system with active targeting function and capable of simultaneously efficiently and stably carrying photosensitizers and chemotherapeutic drugs A novel drug delivery system combining photodynamic therapy and chemotherapy. Background technique [0002] The prior art discloses that chemotherapy is one of the first choices for clinical treatment of tumors. However, the occurrence of multidrug resistance leads to a decrease in the accumulation of chemotherapeutic drugs in tumor sites, thereby causing chemotherapy failure and tumor recurrence. Studies have shown that the emergence of multidrug resistance is mainly due to the following reasons: the reduction of drug uptake by tumor cells, the increase of drug efflux by tumor cells, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K41/00A61K47/34A61K45/06A61P35/00
Inventor 陈钧姜頔羊梦诗康婷冯兴业姚建辉
Owner FUDAN UNIV
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