Self-assembly hyaluronic acid-indissolvable prodrug-coated active medicine-encapsulated liposome nano administration system and preparation method thereof

A technology of hyaluronic acid and active drugs, which is applied in the field of self-assembled nano-liposome complex and its preparation, to achieve the effect of improving anti-tumor ability, reducing toxic and side effects, and improving targeting

Inactive Publication Date: 2017-12-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a compound, hyaluronic acid-insoluble prodrug is difficult to successfully reach the vicinity of tumor tissue through its own blood circulation

Method used

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  • Self-assembly hyaluronic acid-indissolvable prodrug-coated active medicine-encapsulated liposome nano administration system and preparation method thereof
  • Self-assembly hyaluronic acid-indissolvable prodrug-coated active medicine-encapsulated liposome nano administration system and preparation method thereof
  • Self-assembly hyaluronic acid-indissolvable prodrug-coated active medicine-encapsulated liposome nano administration system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] prescription:

[0025] Hyaluronic Acid-Paclitaxel Prodrug 10mg

[0026] Temperature Responsive Liposomes 20mg

[0027] Marimastat 1mg

[0028] Preparation:

[0029] A temperature-responsive liposome loaded with 1 mg of Marimastat was prepared by thin film dispersion-probe ultrasonic method, ready for use. Add 10 mg of hyaluronic acid-paclitaxel prodrug into the temperature-responsive liposome solution loaded with 1 mg of Marimastat, and vortex for half a minute. The mixed solution of hyaluronic acid-prodrug and temperature-responsive liposomes loaded with 1 mg Marimastat was left to stand to obtain self-assembled hyaluronic acid-poorly soluble prodrug-coated liposome nano-administration of active drugs system.

[0030] Utilize the particle size of the liposome nano drug delivery system of the self-assembled hyaluronic acid-poorly soluble prodrug coating of embodiment 1 prepared by dynamic light scattering nano particle size meter, polydispersity coefficient, The Z...

Embodiment 2

[0032] prescription:

[0033] Hyaluronic Acid-Paclitaxel Prodrug 10mg

[0034] Temperature-responsive cationic liposome 20mg

[0035] Preparation:

[0036] The temperature-responsive cationic liposome was prepared by thin film dispersion-probe ultrasonic method, ready for use. Add 10 mg of hyaluronic acid-paclitaxel prodrug into the temperature-responsive cationic liposome solution, and vortex for half a minute. The mixed solution of hyaluronic acid-prodrug and temperature-responsive cationic liposome is left to stand to obtain a self-assembled hyaluronic acid-poorly soluble prodrug-coated liposome nano drug delivery system coated with active drugs.

Embodiment 3

[0038] prescription:

[0039] Hyaluronic Acid-Paclitaxel Prodrug 10mg

[0040] Long Circulation Liposomes 20mg

[0041] Preparation:

[0042] Prepare long-circulating liposomes by thin film dispersion-probe ultrasonic method, ready for use. Add 10 mg hyaluronan-paclitaxel prodrug to the long-circulating liposome solution and vortex for half a minute. The mixed solution of hyaluronic acid-prodrug and long-circulation liposome is left to stand to obtain a self-assembled hyaluronic acid-poorly soluble prodrug-coated liposome nano drug delivery system coated with active drugs.

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Abstract

The invention provides a self-assembled hyaluronic acid-poorly soluble prodrug-coated liposome nano drug delivery system and a preparation method thereof, belonging to the field of pharmaceutical preparations. It is made from the following ingredients: active drug, hyaluronic acid-insoluble prodrug, liposomes. Based on the self-assembled hyaluronic acid-insoluble prodrug-coated liposome nano-drug delivery system itself as a nano-preparation, it can effectively and quickly deliver active drugs and prodrugs to tumor sites through the EPR effect, reducing It can reach the amount of drug in normal tissue; based on the active targeting of the self-assembled hyaluronic acid-insoluble prodrug-coated liposome nano drug delivery system, after it reaches the vicinity of the tumor site, it will pass through the hyaluronic acid Binding to the highly expressed CD44 receptor on the surface of tumor cells mediates drug transport into the cell, enhances the amount of drug entering the cell, and significantly improves the anti-tumor ability of the drug. The present invention is characterized in that two drugs with synergistic effects are simultaneously delivered on the same carrier, which has the consistency of space and time, improves tumor targeting, and improves the curative effect of drugs.

Description

technical field [0001] The invention relates to a self-assembled nano liposome complex and a preparation method thereof. In particular, it relates to a self-assembled hyaluronic acid-poorly soluble prodrug-coated liposome nano drug delivery system coated with active drugs and a preparation method thereof. Background technique [0002] At present, with the development of contemporary material science, cell biology and molecular biology, the nano drug delivery system is gradually developed, which can use the special properties of tumor tissue in the process of tumor treatment to relatively concentrate the drug in the tumor tissue And produce minor side effects. In recent years, nanoliposomes, which have been researched hotter and have higher safety, encapsulate active drugs in lipid bilayers, and release drugs through the decomposition of carriers by enzymes. But at present, only encapsulating active drugs in liposomes greatly limits the drug loading and the types of drugs t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/36A61P35/00A61K31/16
CPCA61K9/1271A61K9/1277A61K31/16A61K31/337A61K47/36
Inventor 尹莉芳何伟吕雅琪
Owner CHINA PHARM UNIV
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