Integrin receptor target lipidosome drug carrier, preparation method and application thereof

A technology of integrin receptors and targeting liposomes, which is applied in the field of biomedicine and can solve the problems that ordinary liposomes do not have targeting properties

Inactive Publication Date: 2009-12-16
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Ordinary lipos

Method used

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  • Integrin receptor target lipidosome drug carrier, preparation method and application thereof
  • Integrin receptor target lipidosome drug carrier, preparation method and application thereof
  • Integrin receptor target lipidosome drug carrier, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1. Containing RGDF-NHCH 2 (CH 2 ) 14 CH 3 Preparation of liposome (C)

[0025] Prepared by film dispersion method, take phospholipid (80-95%, w / w) and the required RGD conjugate RGDF-NHCH 2 (CH 2 ) 14 CH 3 (5-20%, w / w) was dissolved in chloroform in the round bottom flask, the solvent was removed by rotary evaporation, and a dry and transparent plasma film was formed on the bottle wall, and a required amount of PBS phosphate buffered saline (0.01mol / L), 30C ultrasonic dispersion for 20min. An opalescent liposome solution with a particle size of 200-300 nm and a Zeta-Potential of 20-25 mV was obtained.

Embodiment 2

[0026] Embodiment 2. the preparation that contains paclitaxel liposome (E)

[0027] Referring to the preparation method of Example 1, take an appropriate amount of phospholipids and the required paclitaxel into a round bottom flask and dissolve them in chloroform, remove the solvent by rotary evaporation, and form a dry and transparent plasma film on the wall of the bottle, and add the required amount of PBS phosphate buffered saline solution (0.01mol / L), ultrasonically dispersed at 30°C for 20min. An opalescent liposome solution with a particle size of 200-300 nm and a Zeta-Potential of 25-35 mV was obtained.

Embodiment 3

[0028] Example 3. Containing RGDF-NHCH 2 (CH 2 ) 14 CH 3 Preparation of liposomes with paclitaxel (F)

[0029] The dosage of each component: paclitaxel 5-10%; natural lecithin and RGDF-NHCH 2 (CH 2 ) 14 CH 3 90-95% of the mixture, in the mixture, natural lecithin 80-95% (molar percentage), integrin receptor targeting anchor compound 5-20% (molar percentage);

[0030] With reference to the preparation method of Example 1, get phospholipid and RGDF-NHCH 2 (CH 2 ) 14 CH 3 Dissolve the required paclitaxel in a round bottom flask with chloroform, remove the solvent by rotary evaporation, and form a dry and transparent plasma film on the wall of the bottle, add the required amount of PBS phosphate buffer solution (0.01mol / L), and ultrasonicate at 30°C Disperse for 20min. An opalescent liposome solution with a particle size of 200-300 nm and a Zeta-Potential of 15-20 mV was obtained.

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Abstract

The invention discloses an integrin receptor target lipidosome drug carrier and a preparation method thereof, as well as an application of the drug carrier in preparing antitumor lipidosome drug. Hexadecyl fatty chain is conjugated with RGD peptide segment and is hydrophobic-modified so as to synthesize hexadecyl and RGD peptide conjugate with amphipathy, namely, Arg-Gly-Asp-X-NH-C16H33, and X is selected from valine, serine or phenylalanine. The invention introduces fat-soluble antitumor drug into the conjugate with amphipathy to obtain the antitumor target lipidosome drug, the lipidosome system can increase the concentration of the antitumor drug at the target and can reduce toxic and side effects of the antitumor drug to the non-target part, thereby improving the treatment index of the drug. The invention evaluates the antitumor activity of taxol lipidosome by using a Holland sarcoma S180 mouse as a model, the result shows that the taxol lipidosome has more excellent antitumor activity than each control group.

Description

technical field [0001] The present invention relates to a targeted drug release carrier, in particular to an integrin receptor-targeted liposome drug carrier and its construction method. The present invention also relates to the application of drug carriers in the preparation of targeted anti-tumor liposome drugs, which belongs to biomedicine field. Background technique [0002] The growth and metastasis of many malignant tumors are related to abnormal expression of integrins or changes in molecular structure. Integrins are a large family of transmembrane proteins, consisting of α and β subunits to form heterodimers. At present, it has been found that there are about 18 kinds of α, about 8 kinds of β, and at least 24 kinds of integrin forms of heterodimers. The progression of integrins in tumors may be dual: 1) In the early stage of tumorigenesis, the reduction of integrin expression can weaken the adhesion between tumor cells and basement membrane or ECM components, which...

Claims

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Application Information

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IPC IPC(8): C07K5/09C07K1/107A61K9/127A61K47/42A61P35/00A61K31/337A61K47/18
Inventor 崔国辉崔纯莹付征然孙怡
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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