Targeted lipidosome decorated by pH sensitive polypeptide

A technology targeting liposome and polypeptide modification, which is applied in liposome delivery, medical preparations of non-active ingredients, non-active ingredients of polymer compounds, etc., and can solve problems such as strong toxicity and side effects

Inactive Publication Date: 2014-02-26
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the lack of selectivity of membrane-penetrating peptides, the cell penetration

Method used

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  • Targeted lipidosome decorated by pH sensitive polypeptide
  • Targeted lipidosome decorated by pH sensitive polypeptide
  • Targeted lipidosome decorated by pH sensitive polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1. Preparation of DSPE-PEG2000-A

[0047] In a 25ml round bottom flask, add 10ml chloroform, then add DSPE-PEG2000-Mal 10.0mg, triethylamine 3μL, and then add polypeptide A (sequence is LH L LH H L LH HLL H LL, in the sequence, L is leucine, H is histidine; the underline indicates that the amino acid is a D-type amino acid,) 9.1mg is dissolved in 5ml methanol and added to a round bottom flask, and reacted at room temperature in the dark for 48h, and the reaction solution Spin-dry under reduced pressure to obtain the initial product, add chloroform to dissolve, filter, and then spin-dry under reduced pressure to obtain 15.0 mg (89.3%) of DSPE-PEG2000-A as a colorless oily compound.

[0048]

Embodiment 2

[0049] Example 2. Preparation of liposomes modified by DSPE-PEG2000-A

[0050] Polypeptide A modified targeting liposomes were prepared from soybean phospholipids, cholesterol, DSPE-PEG2000, and DSPE-PEG2000-A. Weigh 1.42 mg of soybean lecithin, 0.40 mg of cholesterol, 0.28 mg of DSPE-PEG2000, and 0.78 mg of DSPE-PEG2000-A, dissolve in an appropriate amount of chloroform, and remove the chloroform by rotary evaporation under reduced pressure in a water bath at 37°C to form a uniform lipid film. Add 1ml of PBS buffer solution for hydration for 1h, and probe sonication (5s, 5s, 15 times). Sequentially extrude through 400nm, 200nm and 100nm polycarbonate membranes to obtain DSPE-PEG2000-A modified liposomes.

[0051]

Embodiment 3

[0052] Example 3. Preparation of liposomes modified by DPPE-PEG-A

[0053] Polypeptide A modified targeting liposomes were prepared from soybean phospholipids, cholesterol, DPPE-PEG3000 and DPPE-PEG3000-A. Weigh soybean lecithin 1.42mg, cholesterol 0.40mg, DPPE-PEG3000 0.26mg, DPPE-PEG3000-A 0.75mg, dissolve in appropriate amount of chloroform, 37 ℃ water bath, vacuum rotary evaporation to remove chloroform, form a uniform lipid film, Add 1ml of PBS buffer solution for hydration for 1h, and probe sonication (5s, 5s, 15 times). Sequentially extrude through 400nm, 200nm and 100nm polycarbonate membranes to obtain DPPE-PEG3000-A modified liposomes.

[0054]

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Abstract

The invention relates to an anti-tumor targted lipidosome decorated by pH sensitive polypeptide. The lipidosome is mainly prepared by phospholipid, cholesterol, lipid-polyethylene glycol and lipid-polyethylene glycol-pH sensitive polypeptide. The pH sensitive polypeptide can have enhanced transmembrane capacity in an acidified environment of tumor tissue, and the lipidosome can be mediated to efficiently enter a cell on a tumor part.

Description

technical field [0001] The invention relates to a targeting liposome, in particular to an anti-tumor targeting liposome modified with a pH-sensitive polypeptide and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] The morbidity and mortality of malignant tumors have been increasing year by year, becoming one of the diseases that seriously threaten human health. Although there are various means of treating tumors, chemotherapy is still the most commonly used treatment. However, chemotherapy drugs often lack selectivity between normal tissues and tumor tissues, so their therapeutic effect and application range are often limited. [0003] At present, the development of tumor-targeted nano-drug delivery system has brought new breakthroughs to the treatment of tumors. Among them, liposome, as a nano-scale carrier with good biocompatibility, has attracted widespread attention, and the liposome modified w...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/22A61K47/42A61K47/34A61P35/00
Inventor 何勤张倩玉刘亚圆
Owner SICHUAN UNIV
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