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A drug-loaded liposome co-modified with folic acid and tat peptide and its preparation method

A co-modification and liposome technology, applied in the field of drug-loaded liposomes co-modified with folic acid and TAT peptide and their preparation, can solve the problems of limited application and lack of cell selectivity of cell penetrating peptides, and improve the transport efficiency , the density is easy to control, the effect of reducing steric hindrance

Inactive Publication Date: 2016-08-17
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the lack of sufficient cell selectivity of cell-penetrating peptides, its application in targeted drug delivery is limited to some extent.

Method used

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  • A drug-loaded liposome co-modified with folic acid and tat peptide and its preparation method
  • A drug-loaded liposome co-modified with folic acid and tat peptide and its preparation method
  • A drug-loaded liposome co-modified with folic acid and tat peptide and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Weigh 0.8g of phospholipid soybean lecithin and 0.2g of cholesterol, dissolve it in an organic solvent of chloroform:ethanol=2:1 (volume ratio), spin dry the organic solvent under reduced pressure at 40°C, and obtain a drug-free lipid film ;

[0051] (2) Add pH 7.6 phosphate buffer solution to the drug-free lipid membrane to dissolve, sonicate for 2 minutes, pressurize the 0.22 μm membrane 10 times to obtain blank liposomes, and further adjust the pH to 7.6 with disodium hydrogen phosphate aqueous solution , add 0.15 g of doxorubicin, mix at 70°C for 30 min, and cool to room temperature to prepare drug-loaded liposomes;

[0052] (3) Subsequently, weigh DSPE-PEG 5000 -FA 10g and DSPE-PEG 2000 -TAT 5g, dissolved in phosphate buffer solution, dropwise added to the drug-loaded liposome in step (2), kept at 55°C for 1 hour, and cooled to prepare a dual-target drug-loaded liposome.

[0053] The double-target drug-loaded liposome obtained in Example 1 is tested, and the...

Embodiment 2

[0055] (1) Weigh 0.8g hydrogenated soybean lecithin, 0.2g cholesterol, DSPE-PEG 3400 -FA 1g, DSPE-PEG 3000 - 1g of TAT and 0.2g of hydroxycamptothecin were dissolved in an organic solvent of chloroform:ethanol=2:1 (volume ratio), and then the organic solvent was spin-dried under reduced pressure at 40°C to obtain a drug-containing lipid film;

[0056] (2) Add pH 7.6 phosphate buffer solution to the drug-containing lipid film to dissolve, sonicate for 2 minutes, and filter 10 times with a 0.22 μm membrane to obtain dual-target drug-loaded liposomes.

Embodiment 3

[0058] (1) Weigh 0.8g of lecithin, 0.2g of cholesterol and 0.01g of paclitaxel, dissolve them in an organic solvent of chloroform:ethanol=2:1 (volume ratio), spin dry the organic solvent under reduced pressure at 40°C, and obtain the drug-containing Lipid film;

[0059] (2) Add pH 7.6 phosphate buffer solution to the drug-containing lipid film to dissolve, sonicate for 2 minutes, and filter 10 times with a 0.22 μm membrane to obtain drug-loaded liposomes;

[0060] (3) Weigh DSPE-PEG 1000 -FA 10g and DSPE-PEG 750 -TAT5g, dissolved in phosphate buffer solution, dropwise dropped into the drug-loaded liposome in step (2), kept warm, cooled, to obtain dual-target drug-loaded liposome.

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Abstract

The invention discloses drug-carrying liposome co-modified by folic acid and TAT peptide and a preparation method thereof. The drug-carrying liposome comprises liposome, a long chain targeted membrane material, a short chain targeted membrane material and a drug. Meanwhile, the invention provides the preparation method of the drug-carrying liposome co-modified by folic acid and TAT peptide. The method comprises the following steps: weighing phospholipid, cholesterol, the long chain targeted membrane material, the short chain targeted membrane material and the drug, dissolving the components in an organic solvent, and then carrying out rotary evaporation at 50 DEG C under reduced pressure to remove the organic solvent so as to obtain a medicated liposome membrane; adding a phosphate buffer solution into the medicated liposome membrane for dissolving, carrying out ultrasonic treatment for 2 minutes, and filtering for 10 times by using a 0.22mu m membrane to obtain double-target drug-carrying liposome. According to the drug-carrying liposome disclosed by the invention, the TAT peptide is connected with specific ligands by means of PEG with different weight-average molecular weights to establish a nanometer carrier modified by double ligands, and the prepared drug-carrying liposome can be used for efficiently conveying the drug in tumor cells.

Description

technical field [0001] The invention belongs to the field of drug carriers, in particular to a drug-loaded liposome co-modified with folic acid and TAT peptide and a preparation method thereof. Background technique [0002] Nanocarriers have shown great potential in the tumor-selective delivery of chemotherapeutic drugs. It is worth noting that the antitumor effect of this nanotechnology-based treatment is still very limited, most likely because nanocarriers are not efficient enough to deliver chemotherapeutics. Drug delivery into tumor cells limits the antitumor activity of chemotherapeutic drugs. Nanocarriers enter the tumor interstitium through blood vessels mainly through convection and diffusion. At the same time, the high interstitial pressure (IFP) in the tumor stroma promotes the reverse flow of interstitial fluid into the surrounding tissue, thereby hindering the penetration of nanocarriers into the interior of solid tumors. If the nanocarriers that pass through t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/42A61K47/34A61P35/00
Inventor 程亮朱亚勤李玲程丽芳陈大为
Owner SUZHOU UNIV
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