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Lyophobic and modified glucan-modified long circulating liposome and preparation method thereof

A long-circulating liposome and hydrophobic modification technology, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, and pharmaceutical formulations, can solve the problems of high cost and difficult functional modification, and achieves low cost, The effect of improving active targeting function and enhancing stability

Inactive Publication Date: 2012-03-07
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the PEG molecular chain only contains a small amount of active groups, it is difficult to functionalize the modification, resulting in limitations such as high cost in the actual production and application of PEG-modified liposomes

Method used

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  • Lyophobic and modified glucan-modified long circulating liposome and preparation method thereof
  • Lyophobic and modified glucan-modified long circulating liposome and preparation method thereof
  • Lyophobic and modified glucan-modified long circulating liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Hydrophobically modified dextran modified liposomes

[0045] Accurately weigh 40 mg of soybean lecithin or egg yolk lecithin and 15 mg of cholesterol, and dissolve them in 2 mL of chloroform solvent. Weigh 6 mg of hydrophobically modified dextran and dissolve it in 1 mL of methanol solvent, mix the two in a 50 mL round-bottomed flask, and remove the organic solvent by rotary evaporation until the dry lipid film is evenly deposited on the bottle wall. Hydrate with deionized water (or PBS, ammonium sulfate solution), and sonicate at 37° C. for 2 hours to obtain a bluish opalescent suspension. Then filter twice with 0.45 μm and 0.2 μm filter membranes respectively to obtain a stable hydrophobically modified dextran-modified liposome suspension.

[0046] The average particle diameter of the liposome liquid is 105 nm, and the polydispersity coefficient is 0.15.

Embodiment 2

[0048] Hydrophobic Modified Dextran Modified Liposomes Loading Ibuprofen and Other Substances

[0049] First, accurately weigh 40 mg of soybean lecithin or egg yolk lecithin, 15 mg of cholesterol, and dissolve them in 2 mL of chloroform; weigh 6 mg of hydrophobically modified dextran and dissolve them in 0.5 mL of methanol; weigh a certain amount of ibuprofen solution In 0.5mL of methanol, the three were mixed in a 50mL round bottom flask to remove the organic solvent by rotary evaporation until the dry lipid film was evenly deposited on the bottle wall. Then hydrated, and ultrasonicated at 37°C for 2 hours to obtain a liposome suspension loaded with ibuprofen.

[0050] The method for encapsulating ibuprofen as above was used to encapsulate other various substances, and the specific results are shown in Table 1.

[0051] Table 1 The loading of hydrophobically modified dextran liposomes on various substances such as ibuprofen

[0052]

Embodiment 3

[0054] Preparation of hydrophobically modified dextran liposomes loaded with doxorubicin by ammonium sulfate gradient method

[0055] The modified dextran liposome loaded with doxorubicin first makes the liposome modified by hydrophobically modified dextran with example 1, wherein 250mM (NH 4 ) 2 SO 4 Solution, get the liposome liquid at 45 ℃, dialyze in PBS (pH7.4, 50mM) for 24 hours, remove the unencapsulated (NH 4 ) 2 SO 4 . Take out the dialysate in a volumetric flask, weigh different amounts of doxorubicin, dissolve it in deionized water, add it to the volumetric flask, and dilute to the required amount with PBS, and incubate at 45°C for 1 hour to obtain hydrophobically modified dextran. Adriamycin liposomal fluid.

[0056] The average particle size of the doxorubicin-loaded modified dextran-modified liposome is about 100-150 nm, the encapsulation efficiency is as high as over 95%, and the maximum drug-loading capacity can reach 56%.

[0057] The above method was u...

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Abstract

The invention belongs to the field of medicinal preparation, and particularly relates to a lyophobic and modified glucan-modified long circulating liposome, a preparation method thereof and application thereof. The liposome consists of phospholipids, cholesterol and lyophobic and modified glucan. The liposome is characterized in that the lyophobic chain segment part of the lyophobic and modified glucan enters into the lyophobic layer of the liposome due to the drive of entropy so as to improve the stability of the inner structure of the liposome; and the hydrophilic chain segment part is positioned at the hydrophilic outer layer of the liposome so as to play a part in three-dimensional stability and internal long circulation. The yophobic and modified glucan can be prepared by the reaction between oleamide and carboxymethyl glucan. The liposome is applied to various carriers of medicines, nutrient substances, perfumes and dyes, has high packing rate, mean grain diameter, good stability and good redispersibility, and can be stored by means of freeze-drying. Compared with the existing PEG-modified long circulating liposome, the liposome has the advantages of low cost and being more convenient in further modifying the targeted function.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to hydrophobically modified dextran-modified long-circulation liposomes and a preparation method thereof. Background technique [0002] Liposome is a new dosage form of targeted drug delivery system, which is a closed vesicle with a water phase in the interior composed of a lipid bilayer. As an intelligent drug delivery carrier, liposome has remarkable advantages such as targeting, biocompatibility, improving drug stability and reducing toxic and side effects, so it has attracted more and more attention. Although ordinary liposomes can improve the curative effect of drugs, they are quickly swallowed by the reticuloendothelial system after entering the body, and are mainly targeted at organs of the reticuloendothelial system such as liver, spleen, and bone marrow. The residence time of drugs in the body is short, and In the body, it is susceptible to leakage du...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K9/127
Inventor 李娟刘又年宁顺花黄启瑜黄可龙张翼
Owner CENT SOUTH UNIV
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