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Programmable targeted liposome for cascade delivery of single drug and chemical drug combined therapy

A technology targeting liposomes and liposomes, which is applied in the field of biomedical technology and nanotechnology, and can solve the problems of large toxic side effects and poor curative effect

Active Publication Date: 2018-08-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional chemotherapy methods have poor curative effect and severe side effects. Therefore, scientists are devoting themselves to the study of liver-targeted drug delivery systems

Method used

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  • Programmable targeted liposome for cascade delivery of single drug and chemical drug combined therapy
  • Programmable targeted liposome for cascade delivery of single drug and chemical drug combined therapy
  • Programmable targeted liposome for cascade delivery of single drug and chemical drug combined therapy

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preparation example Construction

[0025] The invention discloses a novel program targeting liposome design, construction, preparation method, drug in vitro characterization, pharmacozoological property research; preparation of liver targeting ligand, in vitro cell uptake characteristics; preparation of mitochondrial targeting drug , in vitro cell colocalization properties. The preparation of program targeting mixed liposomes in the present invention comprises: (1) liver targeting ligand DSPE-PEG2000 -Synthesis of LA; (2) synthesis of mitochondrial targeting drug TPP-PTX; (3) preparation of procedurally targeted mixed liposomes.

[0026] The program-targeted mixed liposome prepared by the present invention is to pack PTX and TPP-PTX into the liposome respectively; and then physically mix the two kinds of liposomes in different volume ratios; the lipid material is lecithin , cholesterol and DSPE-PEG 2000 -LA is prepared by mixing in a certain proportion. The size of the programmed targeting mixed liposomes pre...

Embodiment 1

[0027] Example 1 Preparation of Novel Program Targeting Mixed Liposomes

[0028] 1. Liver targeting ligand DSPE-PEG 2000 - Synthesis of LA:

[0029] Weigh an appropriate amount of DSPE-PEG 2000 -NH 2 Dissolve in DMSO, add lactobionic acid, stir at room temperature for 2 hours, add appropriate amount of EDCI and NHS to the mixed solution, add catalytic amount of triethylamine TEA to adjust the pH to near neutral, and stir the reaction solution at room temperature with a magnetic stirrer About 20h. Transfer the crude product to a dialysis bag for dialysis to remove uncoupled lactobionic acid, TEA, EDCI, NHS, freeze-dried at -20°C and then lyophilized.

[0030] 2. Synthesis of mitochondrial targeting drug TPP-PTX:

[0031] Synthesis of 2'-TBS-PTX: Take appropriate amount of tert-butyldimethylsilyl chloride (TBSCl), and dissolve imidazole in dimethylformamide (DMF) as a stock solution; dissolve the above stock solution with appropriate amount of paclitaxel (PTX) , stirred at...

Embodiment 2

[0037] Embodiment 2 The characterization of program-targeted mixed liposomes

[0038] Particle size distribution and potential measurement:

[0039] Take freshly prepared liver-targeted paclitaxel liposomes, liver-mitochondria-targeted paclitaxel liposomes, program-targeted mixed liposomes 3:1, program-targeted mixed liposomes 1:1, program-targeted mixed lipids Body 1:3 200 μL each, diluted to 3 mL with distilled water. The mixing time was set to 0 min, and the hydrated particle size and potential of the liposome preparation were measured on a particle size potentiometer at 5 min, 15 min, and 30 min after mixing.

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Abstract

The invention belongs to the field of biomedical technology and nanotechnology and particularly relates to a preparation method and an application of a novel programmable targeted mixed liposome preparation. The programmable targeted mixed liposome is prepared through two steps as follows: liposome with LA (lactobionic acid) DSPE-PEG2000-LA added is taken as a shell, and a liver targeted PTX (paclitaxel) liposome and a liver-mitochondrion targeted PTX liposome are prepared independently and then mixed. The solubility of an entrapment drug and the bioavailability of the drug can be improved, programmable delivery of the drug towards tumor tissue-cell-organelle is realized, the antitumor treatment effect of the drug is improved, and the liposome can be used for intravenous infusion tumor diagnosis and treatment research.

Description

technical field [0001] The invention belongs to the fields of biomedical technology and nanotechnology, and specifically relates to the design, construction and application of a novel program targeting liposome. The system combines the characteristics of nano-drug delivery system, cell targeting and organelle targeting to add lactobionic acid-modified DSPE-PEG 2000 -LA liposomes are used as carriers, which act as a delivery system and target liver tumor cells; The role of tubulin and mitochondria in cells. In the mixed liposome prepared by physically mixing the two in a certain ratio, it can improve the bioavailability and pharmacokinetic properties of the drug, endow the drug with good solubility, liver targeting and mitochondrial targeting properties, and can be used for intravenous Injection tumor diagnosis and treatment research. Background technique [0002] Liver cancer is one of the three major malignant tumors in the world, which seriously threatens human health. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/54A61K47/26A61P35/00
CPCA61K9/1271A61K31/337A61K47/26A61K47/54A61P35/00
Inventor 丁娅杨功俊侯晓双马宇刘爱赟
Owner CHINA PHARM UNIV
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