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Perfluocarbon silicon plastid as well as preparation method and application thereof

A technology of siliceous body and carbon fluoride, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as complex synthesis

Active Publication Date: 2021-03-26
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These encapsulation agents have limited drug loading stability and are complex to synthesize

Method used

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  • Perfluocarbon silicon plastid as well as preparation method and application thereof
  • Perfluocarbon silicon plastid as well as preparation method and application thereof
  • Perfluocarbon silicon plastid as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Preparation of siliceous body entrapped carbon fluoride preparation

[0076] (1) Dissolve 9.5 μmol complex lipid A, 0.5 μmol DSPE-mPEG2000, 4 μmol small molecule drug doxorubicin and 20 μL perfluorohexane in 2 mL ethanol, and inject it into 20 mL PBS. Within minutes, 20 mL of PBS was sonicated using a water bath sonicator (Prima, UK, model PM3-900TL). After that, use a probe-type ultrasonic instrument (Qsonica Company, USA, model Q700) to continue ultrasonication for 10 minutes at an output power of 50% in an ice bath. Through a high-pressure extruder (U.S. Northern Lipid Company), the liquid was repeatedly extruded 3 times with a polycarbonate filter membrane (pore size 100 nm, U.S. Whatman Company) to obtain a preparation with an average particle diameter of about 100 nm.

[0077] (2) In order to remove the doxorubicin that is not encapsulated in the siliceous body preparation, first filter the preparation obtained in step (1) with a 0.45 μm filter, and the...

Embodiment 2

[0080] Example 2 Preparation of carbon fluoride preparations entrapped in siliceous bodies

[0081] (1) 6 μmol complex lipid B was hydrolyzed in acidic ethanol at 40° C. for 30 minutes. The acidic ethanol solution is prepared by adding dilute hydrochloric acid into the ethanol solution, and adjusting the pH value to 3.0 with a pH meter.

[0082] (2) Dissolve 1 μmol of the small-molecule drug paclitaxel, 4 μmol of Si-free phospholipid components (including 3 μmol of hydrogenated soybean lecithin (HSPC) and 1 μmol of DSPE-mPEG2000) in 2 mL of chloroform, and add the hydrolysis of step (1) evaporate the liquid to form a phospholipid film, dry it in vacuum overnight, add 5mL ultrapure water and 20μL perfluorocrown ether, shake and hydrate for 60 minutes, use a probe-type ultrasonic instrument (Qsonica, USA, model Q700), and place in an ice bath , with 50% output power, continue ultrasonication for 10 minutes, and obtain a preparation with an average particle size of about 200 nm....

Embodiment 3

[0085] Example 3 Preparation of Fluorocarbon Preparation Carried by Silica Body with Tumor Targeting Molecules

[0086] (1) Dissolve 9.5 μmol complex lipid A, 0.2 μmol DSPE-mPEG2000, 4 μmol small molecule drug doxorubicin, 20 μL perfluorohexane, 0.3 μmol DSPE-mPEG2000-Maleimide in 2 mL ethanol, inject into 20 mL PBS, inject During the process and within 15 minutes after injection, 20 mL of PBS was sonicated using a water bath sonicator (Prima, UK, model PM3-900TL). Afterwards, using a probe-type ultrasonic instrument (Qsonica, USA, model Q700), the ultrasonic was continued for 10 minutes at an output power of 50% in an ice bath. Through a high-pressure extruder (U.S. Northern Lipid Company), the liquid was repeatedly extruded 3 times with a polycarbonate filter membrane (pore size 100 nm, U.S. Whatman Company) to obtain a preparation with an average particle diameter of about 100 nm.

[0087] (2) Add 0.6 μmol of tumor-targeting molecule var7 polypeptide to the preparation (va...

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Abstract

The invention discloses a silicon plastid-entrapped perfluocarbon preparation as well as a preparation method and application thereof. The prepared preparation can be used as an oxygen and drug delivery system to synchronously deliver oxygen and drugs to tumors in a targeted manner, and under the stimulation of high-intensity focused ultrasound, oxygen and drugs can be quickly released at tumor parts, the hypoxic microenvironment of tumors is improved, and the drug effect of the drugs is improved. A silicate network structure on the surface of the silicon plastid enables the preparation to have good structural stability and drug loading stability, early leakage of drugs in a blood circulation system can be reduced, and toxic and side effects of the drugs are reduced. The preparation can also enhance the effect of ultrasonic imaging and realize drug delivery and drug release under image monitoring.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a perfluorocarbon preparation entrapped in siliceous body and its preparation method and application. Background technique [0002] Tumor hypoxia is one of the most prevalent features of solid tumors. Hypoxia is a malignant feature of the tumor microenvironment, which is closely related to tumor resistance to various therapies, including chemotherapy, radiotherapy and photodynamic therapy. Especially for chemotherapy resistance, hypoxia may lead to tumor multidrug resistance (multidrug resistance), which may eventually lead to chemotherapy failure. In the process of multidrug resistance, tumor hypoxia will first increase the relative expression level of hypoxia-inducible factor-1α (HIF-1α) in tumor cells, thereby increasing the transcription level of multidrug resistance gene 1 (MDR1), Finally, the protein expression level of P-glycoprotein (P-gp) is increased, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/00A61K45/06A61K31/704A61K31/337A61K47/02A61K47/06A61K47/24A61P35/00A61K49/22
CPCA61K33/00A61K45/06A61K31/704A61K31/337A61K47/02A61K47/06A61K47/24A61P35/00A61K49/22A61K2300/00
Inventor 王凡梁晓龙马晓途史继云姚美男
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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