A photosensitive liposome carrying water-soluble drugs

A photosensitive lipid, water-soluble technology, used in liposome delivery, drug combination, anti-tumor drugs, etc., can solve the problems of slow drug release, incapable of encapsulated drug release, low local drug concentration in tumors, etc.

Active Publication Date: 2015-12-23
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In practical applications, thermosensitive liposomes loaded with water-soluble drugs only rely on local high temperature, which does not allow the encapsulated drugs to be released quickly and in large quantities.
The encapsulated drug is released too slowly, which directly leads to a low local drug concentration in the tumor

Method used

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  • A photosensitive liposome carrying water-soluble drugs
  • A photosensitive liposome carrying water-soluble drugs
  • A photosensitive liposome carrying water-soluble drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Composition of photosensitive liposomes:

[0051] Doxorubicin Hydrochloride (DOX·HCI) 2.76mg

[0052] Dipalmitoylphosphatidylcholine (DPPC ） 31.64mg

[0053] Hydrogenated Soy Lecithin (HSPC) 11.42mg

[0054] Cholesterol 5.0mg

[0055] Polyethylene glycol phospholipids (DSPE-PEG 2000 ) 7.2mg

[0056] OMP-modified hollow gold nanoparticles (OMP-HAuNS) 1.0mg (~2.5×10 12 particles)

[0057] Prescription amounts of DPPC, HSPC, Cholesterol, DSPE-PEG 2000 and OMP-HAuNS (HAuNS:OMP=1:0.0279w / mol), placed in an eggplant-shaped bottle, dissolved in an organic solvent (chloroform:dichloromethane=1:1v / v), and vacuum decompressed in a water bath at 45°C Rotary evaporated overnight, a thin film formed on the vial walls. Add ammonium sulfate solution with pH = 5.4 into the eggplant-shaped bottle, and hydrate in a water bath at 60°C for 1 hour, the film falls off and dissolves to form a multilayered liposome solution. Sonicate the above solution to the desired particle size us...

Embodiment 2

[0075] Composition of photosensitive liposomes:

[0076] Doxorubicin Hydrochloride (DOX·HCI) 2.76mg

[0077] Dipalmitoylphosphatidylcholine (DPPC) 31.64mg

[0078] Hydrogenated Soy Lecithin (HSPC) 11.42mg

[0079] Cholesterol 5.0mg

[0080] Polyethylene glycol phospholipids (DSPE-PEG 2000 ) 7.2mg

[0081] Hollow gold nanoparticles (HAuNS) 1.0mg (~2.5×10 12 particles)

[0082] Prescription amounts of DPPC, HSPC, Cholesterol, DSPE-PEG 2000 and HAuNS were placed in an eggplant-shaped bottle, dissolved in an organic solvent (chloroform: dichloromethane = 1:1 v / v), and evaporated overnight in a 45°C water bath under vacuum under reduced pressure to form a thin film on the bottle wall. Add ammonium sulfate solution with pH = 5.4 into the eggplant-shaped bottle, and hydrate in a water bath at 60°C for 1 hour, the film falls off and dissolves to form a multilayered liposome solution. Sonicate the above solution to the desired particle size using probe sonication. The resultin...

Embodiment 3

[0084] Composition of photosensitive liposomes:

[0085] Doxorubicin Hydrochloride (DOX·HCI) 2.76mg

[0086] Dipalmitoylphosphatidylcholine (DPPC) 31.64mg

[0087] Hydrogenated Soy Lecithin (HSPC) 11.42mg

[0088] Cholesterol 5.0mg

[0089] Polyethylene glycol phospholipids (DSPE-PEG 2000 ) 7.2mg

[0090] Polyethylene glycol phospholipid modified hollow gold nanoparticles (DSPE-PEG 2000 -HAuNS) 1.0mg (~2.5×10 12 particles)

[0091] Prescription amounts of DPPC, HSPC, Cholesterol, DSPE-PEG 2000 and DSPE-PEG 2000 -HAuNS(HAuNS:DSPE-PEG 2000 -SH=1:0.0279w / mol), placed in an eggplant-shaped bottle, dissolved in an organic solvent (chloroform:dichloromethane=1:1v / v), and evaporated in a water bath at 45°C under vacuum and rotary evaporation overnight. Form a thin film. Add ammonium sulfate solution with pH = 5.4 into the eggplant-shaped bottle, and hydrate in a water bath at 60°C for 1 hour, the film falls off and dissolves to form a multilayered liposome solution. Sonic...

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Abstract

The invention provides a photosensitive liposome carrying a water-soluble antitumor drug, which is composed of thermosensitive phospholipids, cholesterol, long-circulation materials and hollow gold nanoparticles. Absorption peak, the particle size distribution range of hollow gold nanoparticles is 20~100nm. In the present invention, a new photosensitive liposome is assembled by encapsulating water-soluble medicine and hollow gold nanoparticles in the thermosensitive liposome. Under the external near-infrared light, the encapsulated hollow gold nanoparticles produce photothermal therapy effect. At the same time, the photothermal effect is used to control the rapid and large-scale localized release of drugs from photosensitive liposomes, effectively damaging blood vessels or Kill tumor cells and play a role in chemotherapy. The drug-loaded liposome of the present invention realizes the therapeutic effect of synchronous photothermal and drug molecules, significantly improves the therapeutic effect on diseases such as tumors, and has clinical applicability and realistic therapeutic significance.

Description

Technical field [0001] The invention involves a new type of water -loading drugs for photoresmal liposome giving system, which involves the preparation method of the photoresist liposomes and its application in anti -tumor in combination with the external infrared light. Background technique [0002] Since Yatvin first published the temperature sensitivity of the two palm -Pharma gallophylsin (DPPC) liposomes and the possibility of the possibility of two palm -alcoholic acid (DPPC) liposomes (DPPC), the possibility of the heating liposomes has been lipids.A hot spot in the field of body targeted research, and it is combined with tumor therapy from the beginning.The thermist liposomes are usually prepared by the temperature -sensitive material of the phase change temperature (41 ° C) such as DPPC (41 ° C).Above the phase change temperature, the liposuop phospholipid bipolar layer changes from a dense liquid to a loose and chaotic liquid crystal state. The permeability of the lipid...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K45/00A61K41/00A61P35/00
Inventor 游剑张培尊胡富强杜永忠袁弘
Owner ZHEJIANG UNIV
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