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Preparation method of double-drug-loading thermosensitive liposome and application thereof

A heat-sensitive liposome and dual drug-loading technology, applied in the field of medicine, can solve the problems of short half-life of 2-ME, lower drug concentration, and low bioavailability, and achieve high bioavailability, less administration times, and stable good sex effect

Inactive Publication Date: 2021-04-20
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although 2-ME has been proved to have good anti-tumor activity, it can be dehydrogenated rapidly in vivo to produce inactive metabolites, which reduces its drug concentration in plasma; in addition, due to the short half-life of 2-ME, The disadvantages of low solubility, poor oral absorption and low bioavailability severely limit its clinical application

Method used

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  • Preparation method of double-drug-loading thermosensitive liposome and application thereof
  • Preparation method of double-drug-loading thermosensitive liposome and application thereof
  • Preparation method of double-drug-loading thermosensitive liposome and application thereof

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Experimental program
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Effect test

Embodiment 1

[0026] When the present invention is concretely implemented, specifically comprise the following steps:

[0027] 1) Weigh dipalmitoylphosphatidylcholine (DPPC) 18mg, cholesterol (Chol) 4mg, phospholipid polyethylene glycol-RGD peptide (cRGD-DSPE-PEG2K) 2.5mg, 2-methoxyestradiol (2 -ME) 1mg and indocyanine green (ICG) 0.25mg in a 100mL round-bottomed flask, then dissolve the above mixture in a mixed solution of 22mL chloroform and 4mL methanol for ultrasonic dissolution and mixing, at 45°C, 120rpm Rotary evaporation under reduced pressure;

[0028] 2) After the round bottom flask forms a light green transparent lipid film, add 1.5ml of PBS solution to the round bottom flask, and carry out hydration treatment on a rotary evaporator at room temperature;

[0029] 3) After the light green lipid film is completely hydrated to form a light green transparent solution, dip it in the ice bath for more than 10 times, each time for 3 seconds, with an interval of 5 seconds;

[0030] 4) D...

Embodiment 2

[0033] When the present invention is concretely implemented, specifically comprise the following steps:

[0034] 1) Weigh dipalmitoylphosphatidylcholine (DPPC) 21.322mg, cholesterol (Chol) 5.029mg, phospholipid polyethylene glycol-RGD peptide (cRGD-DSPE-PEG2K) 3.649mg, 2-methoxyestradiol (2-ME) 1.5mg and indocyanine green (ICG) 0.75mg in a 100mL round bottom flask, then dissolve the above mixture in a mixed solution of 25mL chloroform and 5mL methanol for ultrasonic dissolution and mixing, at 45°C , rotary evaporation under reduced pressure under the condition of 120rpm;

[0035] 2) After the round bottom flask forms a light green transparent lipid film, add 2ml of PBS solution to the round bottom flask, and carry out hydration treatment on a rotary evaporator at room temperature;

[0036] 3) After the light green lipid film is completely hydrated to form a light green transparent solution, dip it in the ice bath for more than 10 times, each time for 3 seconds, with an interv...

Embodiment 3

[0040] When the present invention is concretely implemented, specifically comprise the following steps:

[0041] 1) Weigh dipalmitoylphosphatidylcholine (DPPC) 24mg, cholesterol (Chol) 6mg, phospholipid polyethylene glycol-RGD peptide (cRGD-DSPE-PEG2K) 4.5mg, 2-methoxyestradiol (2 -ME) 2mg and indocyanine green (ICG) 1mg in a 100mL round bottom flask, then dissolve the above mixture in a mixed solution of 28mL chloroform and 6mL methanol for ultrasonic dissolution and mixing, at 45°C, 120rpm Rotary evaporation under reduced pressure;

[0042] 2) After the round-bottomed flask forms a light green transparent lipid film, add 2.5ml of PBS solution to the round-bottomed flask, and carry out hydration treatment on a rotary evaporator at room temperature;

[0043] 3) After the light green lipid film is completely hydrated to form a light green transparent solution, dip it in the ice bath for more than 10 times, each time for 3 seconds, with an interval of 5 seconds;

[0044] 4) Di...

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Abstract

The invention relates to a preparation method of a double-drug-loading thermosensitive liposome and application thereof. Early diagnosis of tumors can be quickly realized, effective absorption of tumor cells to drugs is increased, the half-life period of the drugs in vivo is prolonged, and bioavailability of the drugs is improved. According to the technical scheme, the preparation method comprises the steps that dipalmitoyl phosphatidylcholine, cholesterol, phospholipid polyethylene glycol-RGD peptide, 2-methoxyestradiol and indocyanine green are weighed in a round-bottom flask, then the mixture is dissolved in a mixed solution of chloroform and methanol to be subjected to ultrasonic dissolution, and a PBS solution is added in the round-bottom flask to be subjected to hydration treatment on a rotary evaporator at room temperature; finally, the double-drug-loading thermosensitive liposome is obtained after polycarbonate membrane extrusion. The preparation method of the double-drug-loading thermosensitive liposome is simple, production and preparation are easy, and the prepared liposome is good in stability, long in drug effect, high in cancer treatment targeting performance, small in adverse reaction, few in drug administration frequency, high in bioavailability and beneficial to being used by patients and is an innovation of the double-drug-loading thermosensitive liposome.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method and application of a double-loaded thermosensitive liposome. Background technique [0002] 2-Methoxyestradiol (2-ME), as an endogenous antitumor drug, has no estrogenic intrinsic activity, and has attracted widespread attention. Compared with conventional chemotherapy and radiotherapy, 2-ME has become a class of antitumor drugs with great development potential because of its advantages of high efficiency, low toxicity, and good drug resistance. In recent years, a large number of in vitro and in vivo studies on 2-ME have shown that it mainly exerts its anti-tumor effect by inhibiting cell apoptosis and proliferation, and has high biological safety. At present, it has been applied in the phase II clinical trials for the treatment of melanoma, ovarian cancer, breast cancer and other tumors. [0003] Indocyanine Green (ICG) is the only tricarbocyanine dye approved by th...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/565A61K41/00A61K49/00A61P35/00
Inventor 张楠冯楠楠辛向英高鸣张艳陈慧张俊伟吴德巧徐玥霍鹏超徐霞封全灵张振中
Owner ZHENGZHOU UNIV
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