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Targeted lipidosome with pH and temperature dual responsiveness and preparation method of targeted lipidosome

A targeting liposome, responsive technology, applied in the field of pharmacy, to achieve the effect of enhancing the therapeutic effect, enhancing the function, and improving the availability of the drug

Inactive Publication Date: 2018-11-23
JINGCHU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The contradictory requirements of targeting and long circulation in vivo are well resolved by the pH-responsive "uncoating" behavior

Method used

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  • Targeted lipidosome with pH and temperature dual responsiveness and preparation method of targeted lipidosome
  • Targeted lipidosome with pH and temperature dual responsiveness and preparation method of targeted lipidosome
  • Targeted lipidosome with pH and temperature dual responsiveness and preparation method of targeted lipidosome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation method of genistein liposomes with pH and temperature dual responsiveness

[0022] Step 1: Synthesis of cholesterol-benzoic imine-PEG (Chol-benzoic imine-PEG)

[0023] 1) Preparation of benzimide polyethylene glycol (compound 1): 1 mole part of polyethylene glycol monomethyl ether (mPEG2000) was dissolved in 25 mL of dichloromethane, and then 1.2 mole parts of p-aldehyde benzoic acid, 1.3 Mole parts of dicyclohexylcarbodiimide (DCC) and catalytic amount (0.1g) of 4-dimethylaminopyridine (DMAP), under the protection of nitrogen, shielded from light and magnetically stirred for 48 hours, evaporated most of the solvent under reduced pressure, The concentrated solution was added dropwise to 100ml of isopropanol, stirred and precipitated, left to stand overnight at 0°C, filtered with suction, and washed three times with cold isopropanol. The filter cake was redissolved in 8 ml of dichloromethane, precipitated in isopropanol again, and filtered with suc...

Embodiment 2

[0029] Example 2 Preparation method of genistein liposomes with pH and temperature dual responsiveness

[0030] The difference from Example 1 is that single-chain phospholipids (MSPC) are added to the membrane material, wherein dipalmitoylphosphatidylcholine (DPPC): hydrogenated soybean phospholipids (HSPC): cholesterol-benzimide-polyethylene glycol The mass ratio of alcohol: cell penetrating peptide Stearyl-R8: genistein: single-chain phospholipid (MSPC) is 8: 3: 2: 0.1: 1: 1.5, and the uniformity and stability of liposomes obtained by this method are obtained. improve. The particle size of the liposome is 110.21nm, and the PDI is 0.112.

Embodiment 3

[0031] Example 3 Preparation method of genistein liposomes with dual responsiveness to pH and temperature

[0032] Different from Example 1, vitamin E (tocopherol) is added to the film material, and the quality of genistein is increased by 50%, and the formula ratio is dipalmitoylphosphatidylcholine (DPPC): hydrogenated soybean phosphatidylcholine (HSPC) : cholesterol-benzimide-polyethylene glycol: cell-penetrating peptide Stearyl-R8: genistein: single-chain phospholipid (MSPC): tocopherol with a mass ratio of 8:3:2:0.1:1.5:1.5 :3. The drug loading capacity of the liposome prepared by the method is increased by 50%, the size of the liposome is 132.65 nanometers, and the PDI is 0.124.

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Abstract

The invention discloses a targeted lipidosome with pH and temperature dual responsiveness. The targeted lipidosome comprises a lipidosome carrier and lipotropic medicine, wherein the lipidosome carrier is prepared from the following raw materials in parts by weight: 8 parts of dipalmitoyl phosphatidyl choline, 1-3 parts of hydrogenated soybean phosphatide, 0.5-2 parts of cholesterol-benzimide-polyethylene glycol, 0-1.5 parts of single-chain phospholipid, 0.01-0.1 part of cell penetrating peptide Stearyl-R8 and 0-3 parts of vitamin E. Polyethylene glycol and the cell penetrating peptide are adopted to jointly modify the lipidosome, trigger type active targeting is realized through pH responsiveness, the requirements on targeting performance and in-vivo long circulation are taken into consideration, meanwhile, a temperature-sensitive lipidosome is adopted to be serve as a membrane material, and the rapid release of the medicine can be realized through local thermal therapy.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to targeted preparations, in particular to a targeted liposome with dual responsiveness to pH and temperature and a preparation method thereof. Background technique [0002] At present, liposomes have been widely used as drug carriers, and various preparations such as adriamycin liposomes, daunorubicin liposomes, and paclitaxel liposomes have been on the market for many years. If it is used as an anticancer drug carrier, the traditional ordinary liposomes can no longer meet the needs of medication, and three key problems need to be solved: (1) Targeted delivery problem: ordinary liposomes rely on the EPR effect to enrich at the tumor site, target (2) long-circulating in vivo: liposomes are easily captured by the endothelial reticulum system (RES) and rapidly metabolized leading to drug The commonly used method is to modify polyethylene glycol (PEG) on the liposome surface to prepare "stealth l...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K9/127A61K45/00A61K47/42A61K47/69A61K31/352A61P35/00
CPCA61K9/1271A61K31/352A61K45/00A61K47/42A61K47/60A61K47/6911A61P35/00
Inventor 范伟伟彭佩李强杨洋
Owner JINGCHU UNIV OF TECH
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