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Glutathione sensitive bone targeted liposome and preparation method thereof

A technology of glutathione and liposomes, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., which can solve the problems of short half-life, low blood flow, and reduced drug treatment. Efficiency and other issues to achieve the effect of reducing toxic side effects and increasing long circulation

Inactive Publication Date: 2020-03-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the problems of high hardness, low blood flow, and poor permeability of bone tissue, it is difficult for general chemotherapy drugs to reach the target site, and the drug usually needs to be administered systemically to achieve an effective therapeutic concentration in bone tissue, which not only reduces the The therapeutic efficiency, and will have certain toxic side effects on other normal tissues
[0003] Cytarabine is a water-soluble drug with a short half-life in the body. To exert an anti-tumor effect, a large amount of administration is required. It is difficult for the drug to reach the site of action by oral administration or injection, and it will also cause certain damage to normal tissues.

Method used

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  • Glutathione sensitive bone targeted liposome and preparation method thereof
  • Glutathione sensitive bone targeted liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Weigh 160 mg of soybean lecithin, 16 mg of cholesterol, and 5 mg of PEG into a 100 mL eggplant-shaped bottle, add 20 mL of dichloromethane to dissolve, spin dry at 48 °C and 50 r / min, and then add 10 mL of water The membrane was washed, the probe was sonicated for 30 min to obtain blank liposomes, and then co-incubated with cytarabine solution (40 mg / mL, 10 mL) and dialyzed to obtain cytarabine liposomes. Take 1mL cytarabine liposomes in a vial, and then prepare 2 mg / mL bone-targeting material ALN-HA-CYS-Chol, heat and co-incubate in a vial, and the incubation temperature should be higher than that of the liposome phase. Change the temperature, and after it cools down, pass through 0.45 μm and 0.22 μm filters in turn to obtain bone-targeted liposomes.

Embodiment 2

[0043] Weigh 160 mg of soybean lecithin, 16 mg of cholesterol, 5 mg of PEG, and 20 mg of bone-targeted substance in an eggplant-shaped bottle, add 20 mL of dichloromethane to dissolve, spin dry at 48 °C at 50 r / min, and then Add 10 mL of water to wash the membrane, sonicate the probe for 30 min to obtain blank bone-targeted liposomes, then co-incubate with cytarabine solution (40 mg / mL, 10 mL), and finally dialyze to remove free arabinose Cytidine yields bone-targeted cytarabine liposomes.

Embodiment 3

[0045] Weigh 160 mg of soybean lecithin, 16 mg of cholesterol, 5 mg of PEG, and dissolve 20 mg of bone-targeting substance in tetrahydrofuran, then slowly drop it into 10 mL of PBS and keep stirring, after the tetrahydrofuran volatilizes, you can get Bone-targeted blank liposomes, and finally co-incubated cytarabine aqueous solution (40 mg / mL, 10 mL) with blank liposomes and dialyzed to obtain cytarabine bone-targeted liposomes.

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Abstract

The invention discloses glutathione sensitive bone targeted liposome and a preparation method thereof. The bone targeted liposome is prepared by modifying amphipathic materials of alendronate-hyaluronic acid-aminiform-cholesterol on a phosphatide dimolecular layer framework of liposome. The glutathione sensitive bone targeted liposome disclosed by the invention is prepared by modifying a glutathione sensitive bone targeted material to the liposome, so that bone tissue can be targeted, besides, disulfide bonds can be embedded into the liposome and can be rapidly cracked in tumor cells rich in glutathione, and medicines can be released out.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a glutathione-sensitive bone-targeting liposome and a preparation method thereof. Background technique [0002] Bone tumors include bone tumors in situ, bone metastases, and leukemia. Due to the problems of high hardness, low blood flow, and poor permeability of bone tissue, it is difficult for general chemotherapy drugs to reach the target site, and the drug usually needs to be administered systemically to achieve an effective therapeutic concentration in bone tissue, which not only reduces the The treatment efficiency, and will have certain toxic side effects on other normal tissues. [0003] Cytarabine is a water-soluble drug with a short half-life in the body. To exert its anti-tumor effect, it needs to be administered in large quantities. It is difficult for the drug to reach the site of action by oral administration or injection, and it will...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/36A61K47/28A61K47/24A61K47/20A61K31/7068A61P35/00
CPCA61K9/127A61K31/7068A61K47/20A61K47/24A61K47/28A61K47/36A61P35/00
Inventor 柯学吴豪邹丹璐慈天元
Owner CHINA PHARM UNIV
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