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Sialic acid modified dexamethasone palmitate liposome as well as preparation and application thereof

A technology of dexamethasone palmitate and liposomes, which is applied in the field of medicine, can solve problems such as difficult breakthroughs, achieve low cost, improve targeting, and improve the effects of cell targeting in vivo and in vitro

Pending Publication Date: 2021-12-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these designs still have some common problems: ①mainly focus on monocytes / macrophages processing foreign substances; ②single emphasis on inhibiting the immune system’s recognition and processing of nanoparticles entering the body
In the face of a strong immune system, it is difficult to make breakthroughs in the short term by adopting the strategy of "hiding"

Method used

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  • Sialic acid modified dexamethasone palmitate liposome as well as preparation and application thereof
  • Sialic acid modified dexamethasone palmitate liposome as well as preparation and application thereof
  • Sialic acid modified dexamethasone palmitate liposome as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Synthesis of embodiment 1 sialic acid lipid derivatives (LYS-16 and LYS-18) (attached figure 1 A. figure 1 B)

[0054] Add 0.66g (16.5mmol) of 60% sodium hydrogen washed with petroleum ether, 10mL of anhydrous toluene, 2g (8.25mmol) of cetyl alcohol into a 100mL eggplant-shaped bottle, and add 0.94g (9.9mmol) of cetyl alcohol dropwise at 50°C for 1 hour. ) Chloroacetic acid toluene solution 5mL, dripped in 7min, and refluxed for 9 hours. Add 20mL of water, adjust the pH value to 1 with 2N hydrochloric acid, extract 3 times with 30mL ethyl acetate, wash once with 30mL saturated sodium chloride solution, anhydrous MgSO 4 Dry, filter with suction, and evaporate the filtrate to dryness to obtain white 2-(hexadecyloxy)acetic acid solid. Using the same method, white 2-(octadecyloxy)acetic acid solid was obtained from stearyl alcohol and chloroacetic acid as raw materials.

[0055] Add 1g (2.91mmol) of 2-(hexadecyloxy)acetic acid to a 100mL eggplant-shaped bottle, dissolve...

Embodiment 2

[0057] The preparation of embodiment 2 sialic acid modified dexamethasone palmitate liposomes

[0058] (1) Screening of sialic acid derivatives

[0059] Weigh HSPC, cholesterol, sialic acid derivatives and dexamethasone palmitate, add absolute ethanol with a final volume of 10% (v / v) of the preparation, stir and dissolve in a water bath at 60°C. After the solid matter is completely dissolved, open the system, continue stirring to evaporate most of the ethanol, inject 5% Glu preheated to the same temperature, and continue stirring at 60°C for 20 minutes to obtain the primary liposome. After the primary product is ultrasonically dispersed (power and time: 200W×2min+400W×6min, working for 1s and intermittent for 1s), pass through 0.80, 0.45 and 0.22μm microporous membranes in turn to obtain sialic acid-modified (unmodified) DP Liposomes.

[0060] Table 1

[0061]

[0062]

[0063] The results showed that when sialic acid-2-(hexadecyloxy)acetic acid and sialic acid-2-(oct...

example 3

[0075] The cytostatic effect of example 3 DP liposomes (attachment image 3 )

[0076] For the separation and purification method of neutrophils, refer to patent CN201810151125. The cytostatic effect of DP liposome on neutrophils was investigated by CCK8 method.

[0077] 1. Dilute the isolated and purified peripheral blood neutrophils with RPMI 1640 culture medium to make a cell suspension, and adjust the concentration to 6×10 4 cells mL -1 .

[0078] 2. Inoculate the prepared cell suspension into a 96-well culture plate, inoculate 100 μL per well, and place at 37°C, 5% CO 2 Incubate for 1 h in the incubator. All edge wells were filled with 200 μL sterile PBS.

[0079] 3. Add each DP liposome diluted in the culture medium into a 96-well plate, add 10 μL to each well, and the final concentrations are 5, 10, 50, 100, 200 μg·mL -1 , with 3 replicate holes. At the same time, set zero wells (without cells and drugs) and control wells (with cells, without drugs), each with 6...

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Abstract

The invention belongs to the technical field of medicines, and relates to a sialic acid modified dexamethasone palmitate liposome as well as a preparation method and application thereof. The sialic acid derivative modified dexamethasone palmitate liposome disclosed by the invention comprises a sialic acid derivative, phospholipid, cholesterol and dexamethasone palmitate. The sialic acid derivative is selected from one of sialic acid-cholesterol, sialic acid-stearic acid, sialic acid-2-(hexadecyloxy) acetic acid or sialic acid-2-(octadecyloxy) acetic acid. In the sialic acid derivative modified dexamethasone palmitate liposome, the sialic acid derivative accounts for 1%-50% of the total weight of the liposome, preferably 10%-30%; the phospholipid accounts for 50-90%; the cholesterol accounts for 1-40%; and the dexamethasone palmitate accounts for 5-20%. The sialic acid disclosed by the invention can be used for improving in-vivo and in-vitro cell targeting of the liposome.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sialic acid-modified dexamethasone palmitate liposome and a preparation method and application thereof. Background technique [0002] At present, the treatment drugs for rheumatoid arthritis (RA) are mainly divided into four categories (Liu Xuetao, Li Qing. Progress in the treatment of rheumatoid arthritis [J]. Modern Biomedicine Progress, 2015, 15(6) : 1171-3), including nonsteroidal anti-inflammatory drugs (NSAIDs), glucocorticoids (GCs), disease-modifying anti-rheumatic drugs (DMARDs) and biological preparation. Although traditional therapy has achieved certain therapeutic effects, there are still many problems. Biological agents are new drugs for the treatment of RA in recent years, and are considered to be "revolutionary" RA treatment methods (ATZENI F, SARZIPUTTINI P, GORLA R, et al.Switching rheumatoid arthritis treatments: an update[J].Autoimmunity Reviews,2011, 10(7)...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/573A61P5/44A61P19/02C07H1/00C07H13/04
CPCA61K47/6911A61K47/545A61K31/573A61P19/02A61P5/44C07H13/04C07H1/00
Inventor 邓意辉胡玲王硕宋艳志刘欣荣
Owner SHENYANG PHARMA UNIVERSITY
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