Hypocrellin cationic liposome preparation and preparation method and application thereof

A technology of cationic lipid and oleocanthin, which is applied in liposome delivery, pharmaceutical formulation, photodynamic therapy, etc., can solve the problem of not being able to accurately target neovascular endothelium, and not being able to well target lesion malformations. New blood vessels and other problems, to achieve the effect of high dosage form stability, simple preparation process and good biocompatibility

Inactive Publication Date: 2016-04-13
FIRST HOSPITAL AFFILIATED TO GENERAL HOSPITAL OF PLA +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, hypocretin is a fat-soluble molecule. In order to realize its drug delivery in vivo, it is chemically modified to improve its hydrophilicity. The prepared hypocrellin derivatives cannot be well targeted to lesions. The purpose of teratogenic neovascularization (J.Q.Zhao, H.Deng, J.Xie, X.Liu, Y.Zhang, N.Y.Huang and Y.Gu, Towards characteristics of photodynamic drugs specifically yimed at microvascular diseases, Mini-Rev. Med. Chem., 2010, 10, 332-341; H. Deng, X. Liu, J. Xie, R. Yin, N.Y. Huang, Y. Guan and J. Q. Zhao, Quantitative and site-directed chemical modification of hypocrellinstowards direct dug delivery and effective photodynamic activity, J. Med. Chem., 2012, 55, 1910-1919)
Liposome is a microvesicle formed by encapsulating drugs in lipid bilayers. It is a preferred type of drug delivery carrier. It has the advantages of high biocompatibility, good targeting, and fast drug release. However, the existing hypocretin liposome preparations cannot accurately target the neovascular endothelium

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  • Hypocrellin cationic liposome preparation and preparation method and application thereof
  • Hypocrellin cationic liposome preparation and preparation method and application thereof
  • Hypocrellin cationic liposome preparation and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0047] Embodiment 1, prepare hypocrellin cationic liposome preparation

[0048] Hypocretin cationic liposome preparation is prepared according to the following steps:

[0049] (1) Dissolve 50 mg of Hypocretin B, 900 mg of DOTAP, 950 mg of DOPC, 110 mg of cholesterol and 25 mg of STPP in 100 mL (150 g) of chloroform, then place it in a rotary evaporator, and rotate it under a pressure of 8 mbar for 2 hours to prepare a thin film.

[0050] (2) Add 50 mL (50 g) of PBS solution to the film prepared in the above step (1), and shake it at 200 rpm for 4 hours to form multilocular liposomes.

[0051] (3) Place the multilamellar liposome prepared in the above step (2) at 0° C. and ultrasonicate for 45 minutes under the condition of ultrasonic power of 80 W to obtain unilamellar liposomes with a particle size distribution of 57-119 nm.

[0052] (4) Chromatographically separate the unilamellar liposomes prepared in the above step (3) with SephadexG-15 dextran gel (eluent: PBS, pH=7.2~7....

Embodiment 2

[0053] Embodiment 2, prepare hypocrellin cationic liposome preparation

[0054] Hypocretin cationic liposome preparation is prepared according to the following steps:

[0055] (1) Dissolve Hypocretin B 100mg, DPTAP 1850mg, DOPC 1850mg, Cholesterol 220mg and STPP 50mg in 200mL (300g) of chloroform, then place it in a rotary evaporator, and spin evaporate it under 10mbar pressure for 3 hours to prepare a thin film.

[0056] (2) 100 mL (100 g) of PBS solution was added to the film prepared in the above step (1), and shaken at 200 rpm for 4 h to form multilocular liposomes.

[0057] (3) Place the multilamellar liposome prepared in the above step (2) at 4° C., and ultrasonicate for 0.5 h under the condition of ultrasonic power of 120 W, to obtain unilamellar liposomes with a particle size distribution of 55-122 nm.

[0058] (4) Chromatographically separate the unilamellar liposomes prepared in the above step (3) with SephadexG-15 dextran gel (eluent: pH=7.2~7.4, concentration is 0...

Embodiment 3

[0059] Embodiment 3, preparation hypocretin cationic liposome preparation

[0060] Hypocretin cationic liposome preparation is prepared according to the following steps:

[0061] (1) Dissolve Hypocretin B 150mg, DDAB2670mg, DOPC2910mg, Cholesterol 330mg and STPP75mg in 300mL (398g) of dichloromethane, then place it in a rotary evaporator, and rotate it under a pressure of 10mbar for 4 hours to prepare film.

[0062] (2) 150 mL (150 g) of PBS solution was added to the film prepared in the above step (1), and shaken at 200 rpm for 5 h to form multilocular liposomes.

[0063] (3) Put the multilamellar liposome prepared in the above step (2) at 15° C. and ultrasonicate for 1 h under the condition of ultrasonic power of 200 W to obtain unilamellar liposomes with a particle size distribution of 50-120 nm.

[0064] (4) SephadexG-15 dextran gel is used to carry out chromatographic separation of the single-chamber liposomes prepared above, remove the unencapsulated STPP in the liposo...

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Abstract

The invention discloses a hypocrellin cationic liposome preparation and a preparation method and application thereof. The hypocrellin cationic liposome preparation is prepared from hypocrellin, cationic phospholipid, 1-2-dioleoyl phosphatidylcholine, cholesterol and octadecyl triphenylphosphonium bromide. The liposome is a novel hypocrellin liposome designed aiming at macular degeneration photodynamic therapy, the cationic liposome is prepared according to the film-ultrasonic wave dissolving technique, and due to wrapping of octadecyl triphenylphosphonium bromide molecules containing TPP (triphenylphosphine), targeting at new vessel endothelium of a lesion and selectively gathering at a target of endothelial cell mitochondria are realized. In addition, the liposome is technically simple and convenient in preparation and high in stability, biological photodynamic activity of the liposome is more than 2 times of that of parent hypocrellin, and the hypocrellin cationic liposome preparation is a highly potential medicine for macular degeneration photodynamic therapy.

Description

technical field [0001] The invention relates to a hypocretin cationic liposome preparation, a preparation method and application thereof. Background technique [0002] Retinal macular degeneration (Age-related Macular Degeneration, AMD) has become one of the common blinding diseases of the elderly. Its disease types are divided into dry and wet macular degeneration. Studies have shown that about 90% of macular degeneration blinding patients belong to wet macular degeneration. (J. Ambati, B.K. Ambati, S.H. Yoo, S. Lanchulev and A.P. Adamis, Age-related macular degeneration: etiology, pathogenesis, and therapeutic strategies, Surv. Ophthalmol., 2003, 48, 257-293.). The main feature of wet macular degeneration is abnormal abnormal neovascularization (Choroidal Neovascularization, CNV) in the macular area of ​​the retina. Photodynamic therapy (Photodynamic therapy, PDT) has become one of the first-choice treatments for wet macular degeneration. It is safe, efficient, and can be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/127A61P9/10A61P27/02
CPCA61K9/0019A61K9/127A61K41/0057A61K47/28
Inventor 陈虹霞邓虹邹先彪赵井泉
Owner FIRST HOSPITAL AFFILIATED TO GENERAL HOSPITAL OF PLA
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