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Folic acid modified norcantharidin stealth niosome and preparation method thereof

The technology of norcantharidin and folic acid is applied to the preparation of vesicles and the field of folic acid-modified invisible vesicles, which can solve the problems of easy hydrolysis, low drug bioavailability, and low norcantharidin, and achieves improved efficacy, The effect of high efficiency and low toxicity in the treatment of cancer and enhanced anticancer activity

Active Publication Date: 2013-08-28
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, norcantharidin tablets and norcantharidin injections are mainly used clinically, both of which are common preparations, have no selectivity for tumor tissues and tumor cells, and have low bioavailability of drugs, so there is serious liver and kidney toxicity. It is easy to produce drug resistance, and it is easily hydrolyzed into norcantharidic acid with low drug efficacy.

Method used

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  • Folic acid modified norcantharidin stealth niosome and preparation method thereof
  • Folic acid modified norcantharidin stealth niosome and preparation method thereof
  • Folic acid modified norcantharidin stealth niosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation and verification of poloxamer 407-cholesterol

[0048] 1. Preparation and characterization of poloxamer 407-cholesterol:

[0049] 1.1. Preparation of poloxamer 407-cholesterol

[0050] According to macromolecular substances such as PEG and Poloxamer 407, which have terminal -OH, the synthetic route can be adopted: PEG-OH+(CH 3 CO) 2 O+CH 3 SOCH 3 → PEGOCH 2 CHO yields polymer acetals (called polymer-aldehydes). Namely: Weigh 5.123g of Poloxamer 407 into a 50ml round bottom flask, add 0.4g of acetic anhydride and 15ml of dimethyl sulfoxide (DMSO), and react at RT for 30h with electromagnetic stirring, drop into 150ml of anhydrous ether, shake well, Add dichloromethane dropwise to make the solution homogeneous, then add an appropriate amount of diethyl ether to precipitate, place at 4°C until the precipitate is completely precipitated, filter under reduced pressure, and dry in vacuum to constant weight to obtain a white loose solid: Poloxamer ...

Embodiment 2

[0069] Example 2 Preparation and Analysis of Folic Acid Modified Norcantharidin Stealth Vesicle Novel Drug Delivery System

[0070] 3. Preparation of a novel delivery system of folic acid-modified norcantharidin stealth vesicles

[0071] 3.1 Preparation of folic acid-modified norcantharidin invisible vesicle suspension (abbreviation: folic acid vesicle)

[0072] Each milliliter suspension contains 3.8 mg of norcantharidin, 20.0 mg of poloxamer 407-cholesterol (a), 1.2 mg of folic acid-polymer (b), and 29.4 mg of surfactant (c). Carrier materials a, b, and c are completely dissolved with organic solvents, mixed with norcantharidin for ultrasonication, and then mixed with PBS preheated at 60°C by injection method, stirred at 20-70°C and ultrasonicated until the organic solvent volatilizes Get it later.

[0073] 3.2 Preparation of folic acid modified norcantharidin / Rd B stealth vesicle suspension (abbreviation: folic acid vesicle’)

[0074] Adopt "3.1" method, but add fluoresc...

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Abstract

The invention relates to a folic acid modified norcantharidin stealth niosome and a preparation method thereof. The niosome is a surface hydrophilic and folic acid modified stealth niosome which is formed by entrapping norcantharidin with a poloxamer 407-cholesterol compound and a folic acid-polymer as major carrier materials; and the stealth niosome contains no free cholesterol. The entrapment rate of the niosome is (52.30+ / -2.16)%, the mean grain size of the niosome is (100.87+ / -0.23)nm and the zeta potential of the niosome is -25.96 mV; the drug release rate in vitro of the niosome is obviously lower than that of a crude drug; t1 / 2 released by the niosome in an environment in which the pH of 7.4 of the normal tissue is simulated is 1.98 times of that released by the niosome in an environment in which the pH of 5.0 of the normal tissue is simulated; and the folic acid modified norcantharidin stealth niosome is obvious in slow release effect and advantageous for releasing in target cells. Besides, the niosome is capable of obviously increasing the growth inhibition ratio and drug taking quantity of tumor cells, and generating active targeting effect at molecular level, and therefore, the efficacy of the drug is improved, treatment of cancer at high efficiency and low toxicity is facilitated.

Description

technical field [0001] The invention relates to a drug delivery system, in particular to a folic acid-modified drug stealth vesicle, and also relates to a preparation method of the vesicle. Background technique [0002] Targeted drug delivery system is a drug delivery system that uses special carrier materials and is prepared through specific processes and technologies. Intracellular targets play a role, so as to overcome the common problems in current clinical treatment, such as large doses of anticancer drugs, fast metabolism, small amount of drugs entering tumor cells, lack of selectivity in killing tumor cells, and damage to normal cells leading to severe toxic and side effects. The characteristics usually required for the targeted drug delivery system are: A. It can avoid the clearance of the reticuloendothelial system in the body, and has stealth characteristics. The general particle size is <200nm, and the surface is modified by hydrophilic chain polymers, which c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/22A61K47/34A61K47/28A61K31/34C08G65/00A61P35/00A61K47/10
Inventor 杨红刘洪月陈华兵冒华建韩楠楠顾睿南马雪莹武艺静
Owner SUZHOU UNIV
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