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Targeting liposome drug delivery system for multidrug resistant tumors

A multi-drug resistance, targeting liposome technology, applied in anti-tumor drugs, liposome delivery, drug combination and other directions, can solve the problems of encapsulating vincristine and no liposomes yet

Inactive Publication Date: 2013-12-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports of folic acid-modified liposomes encapsulating vincristine

Method used

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  • Targeting liposome drug delivery system for multidrug resistant tumors
  • Targeting liposome drug delivery system for multidrug resistant tumors
  • Targeting liposome drug delivery system for multidrug resistant tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation and Characterization of Folic Acid-Polyethylene Glycol-Liposome

[0048] 1. Preparation and Characterization of Folic Acid-PEG-Liposome / 5-Carboxyfluorescein

[0049] Polyethylene glycol-liposome membrane material is formulated as hydrogenated soybean lecithin / cholesterol / methoxypolyethylene glycol 2000- Distearoylphosphatidylethanolamine (55:45:2, mol / mol), folate-modified polyethylene glycol-liposome membrane material formulated as hydrogenated soybean phospholipid / cholesterol / methoxypolyethylene glycol 2000- Distearoyl Phosphatidylethanolamine / Folic Acid-Polyethylene Glycol 3350- Distearoylphosphatidylethanolamine (55:45:2:1, mol / mol). Weigh the above membrane material and dissolve it in chloroform, remove the organic solvent by rotary evaporation under reduced pressure to obtain a uniform lipid membrane, and dry it in vacuum for 24 hours. Add 5-carboxyfluorescein aqueous solution for hydration, and shake in a water bath at 65°C for 2 hours to...

Embodiment 2

[0054] Example 2 In vivo and in vitro targeting evaluation of folic acid-polyethylene glycol-liposome

[0055] 1. Targeting evaluation of folic acid-polyethylene glycol-liposome / 5-carboxyfluorescein on multidrug-resistant tumor cells in vitro

[0056] Take monolayer cultured KBv200 cells in the logarithmic growth phase, digest the monolayer cultured cells with 0.25% trypsin and 0.025% disodium edetate, and prepare single cell suspension with DMEM medium containing 15% fetal bovine serum , with 1 x 10 per well 5 Cells were inoculated in a 24-well culture plate with a volume of 1 ml per well, and the culture plate was moved into a carbon dioxide incubator, and cultured overnight at 37°C, 5% carbon dioxide and saturated humidity to allow the cells to adhere to the wall. On the next day, prepare a series of different concentrations of PEG-liposome / 5-carboxyfluorescein and folic acid-polyethylene glycol-liposome / 5-carboxyfluorescein in DMEM medium containing 1% fetal bovine serum ...

Embodiment 3

[0060] In vivo and in vitro pharmacodynamic evaluation of folic acid-polyethylene glycol-liposome

[0061] 1. Evaluation of growth inhibitory effect of folic acid-polyethylene glycol-liposome / vincristine on multidrug-resistant tumor cells in vitro

[0062] KBv200 cells in the logarithmic growth phase were digested with 0.25% trypsin and 0.025% disodium ethylenediaminetetraacetic acid, counted cells, and added 200 microliters of cell suspension (2×10 3 cells), set aside three wells plus cell-free culture medium as blank wells, and adhere to the wall for 24 hours. Dilute free vincristine solution, polyethylene glycol-liposome / vincristine and folic acid-polyethylene glycol-liposome / vincristine with cell culture medium to a series of vincristine solutions with different concentration gradients , suck off the cell culture medium in the 96-well plate, and add 200 microliters of liposome liquids with a series of concentrations to each well. After cultivating for 2 hours, dump the d...

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Abstract

Belonging to the fields of pharmacy and clinical pharmacy, the invention relates to a folic acid modified and vincristine encapsulated active targeting liposome drug delivery system, a preparation method and application in multidrug resistant tumor targeted drug delivery. The invention discloses a preparation method of a folic acid modified and vincristine encapsulated liposome. Cell specific uptaking and living animal imaging tests show that the drug delivery system has good in vitro and in vivo tumor cell targeting. 3-(4, 5-dimethylthiazole)-3, 5-diphenyltetrazolium bromide (MTT) analysis indicates that the drug delivery system has a good effect for inhibiting the in vitro growth of tumor cells. Pharmacodynamic results show that the drug delivery system has a good effect for inhibiting the in vivo growth of multidrug resistant tumors. The drug delivery system can enter the whole body blood circulation through intravenous injection dosing, then can be targeted to multidrug resistant tumor sites through tumor EPR effect and folic acid mediation and enter the tumor cells.

Description

technical field [0001] The invention belongs to the field of pharmacy and clinical pharmacy, and relates to a liposome drug delivery system for targeted drug delivery to multidrug-resistant tumors, in particular to an active targeting lipid modified by folic acid and loaded with vincristine Body drug delivery system, preparation method and medical application thereof. Background technique [0002] Multidrug resistance is the main reason for the failure of cancer chemotherapy. For most antitumor drugs, after a period of chemotherapy, tumor cells will produce multidrug resistance, but there is no unified view on the mechanism of drug resistance. One of the more popular views is that P-glycoprotein Mediated drug efflux. Therefore, many researchers at home and abroad are trying to co-pack P-glycoprotein inhibitors (such as verapamil, etc.) effect, and can reduce drug side effects. However, because the first, second and third generation P-glycoprotein inhibitors all have non-...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/475A61K47/34A61K47/22A61P35/00
Inventor 陆伟跃王晨瑜俸灵林杨向坤王飞
Owner FUDAN UNIV
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