Thermosensitive silica body and preparing method and application thereof

A siliceous body and heat-sensitive technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of tumor drug resistance, slow drug release, etc., and achieve small side effects , low cost, effective HIFU response performance effect

Inactive Publication Date: 2015-12-30
BEIJING SAMSUNG TELECOM R&D CENT +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this stable silicon body also has the following defects: the drug release is too slow to maintain an effective concentration at the target site, which may lead to drug resistance of the tumor

Method used

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  • Thermosensitive silica body and preparing method and application thereof
  • Thermosensitive silica body and preparing method and application thereof
  • Thermosensitive silica body and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1 Preparation of thermosensitive siliceous body 1

[0059]

[0060] step:

[0061] (1) Hydrolyze the siliceous body-forming lipids in an acidic ethanol solution and incubate at 40° C. for 30 min; wherein the pH of the acidic ethanol solution is 3.0; the acidic ethanol solution is prepared by adding dilute hydrochloric acid to the ethanol solution , adjusted to a pH value of 3.0 with a pH meter.

[0062] (2) The chloroform solution that will be dissolved with dipalmitoylphosphatidylcholine, monostearylphosphatidylcholine and polyethylene glycol 2000-dipalmitoylphosphatidylethanolamine is added in the hydrolyzate of step (1), evenly mix;

[0063] (3) Use a rotary evaporator to remove the solvent in the mixed solution obtained in step (2), and dry it under vacuum overnight;

[0064] (4) Add 100ml of ultrapure water to the solid film obtained in step (3), and hydrate in a water bath at 60°C for 30 minutes; the mixture was vortexed for 20 minutes, and then...

Embodiment 2

[0066] Embodiment 2 Preparation of thermosensitive siliceous body 2

[0067]

[0068] The preparation method is the same as that in Example 1, except that the probe is ultrasonicated for 5-10 minutes (20% amplitude output).

Embodiment 3

[0069] Embodiment 3 Preparation of thermosensitive siliceous body 3

[0070]

[0071] The preparation method is the same as that in Example 1, except that the probe is ultrasonicated for 5-10 minutes (10% amplitude output).

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Abstract

The invention relates to a thermosensitive silica body and a preparing method and application thereof. The thermosensitive silica body and high-intensity focused ultrasound beams (HIFU) are combined and used for controlling release of hydrophobic drugs. The thermosensitive silica body is prepared from, by weight, 41.90-62.90 parts of lipid formed by the silica body, 40.00-60.00 parts of dipalmitoyl phosphatidyl choline, 5.20-8.50 parts of palmitoyl phosphatidyl choline and 14.00-19.50 parts of polyethylene glycol 2000-dipalmitoyl phosphatidyl ethanolamine. The thermosensitive silica body is high in stability and biocompatibility and capable of fast releasing the hydrophobic antineoplastic drugs when combined with HIFU and shows a remarkable therapeutic effect.

Description

technical field [0001] The invention belongs to the field of drug controlled release, in particular, the invention relates to a heat-sensitive siliceous body and its preparation method and application. Background technique [0002] At present, about 40% of the world's marketed drugs and more than 80% of new drugs in research and development are poorly water-soluble drugs. Due to poor water solubility, it is often difficult to achieve the bioavailability required for treatment, or to make preparations for intravenous administration, so that a large number of important drugs cannot fully exert their curative effects, resulting in large drug doses, small curative effects, and serious side effects. The application of poorly water-soluble drugs is limited. [0003] However, the existence of barriers in the tumor microenvironment complicates the uniform and effective delivery of drugs to the tumor site. Clinically, the drug dose required to effectively kill tumor cells at the tum...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/24A61K41/00
Inventor 戴志飞梁晓龙蒋灵冬井立佳谭婵媛金泫伶
Owner BEIJING SAMSUNG TELECOM R&D CENT
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