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Ceramide liposome and preparation method and application thereof

A technology of ceramide lipids and ceramides, which is applied in the field of pharmaceutical preparations to achieve the effects of reducing the concentration of chemotherapy drugs, prolonging the survival time of organisms, and improving targeting and bioavailability

Inactive Publication Date: 2012-12-05
陆培华 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no ceramide liposome (including injection or oral dosage forms) that can be used for tumor treatment at home and abroad, so our invention has excellent innovation

Method used

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  • Ceramide liposome and preparation method and application thereof
  • Ceramide liposome and preparation method and application thereof
  • Ceramide liposome and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Ceramide 20mg

[0043] Egg yolk lecithin 20mg

[0044] Cholesterol 200mg

[0045] Ether 10ml

[0046] Taurocholate 30mg

[0047] Preparation method: Dissolve 30mg taurocholate in phosphate buffer (pH 7.4), the weight concentration of taurocholate in phosphate buffer is 15%; mix 20mg ceramide, 20mg egg yolk lecithin and Dissolve 200mg of cholesterol in ether, then slowly inject this solution into phosphate buffer at 50-60℃, stir with an electronic constant speed stirrer at 600r / min until the ether is completely removed, and then dilute with the above phosphate buffer To 100ml, the ceramide liposome is obtained and stored at 4°C.

Embodiment 2

[0049] Ceramide 30mg

[0050] Soy Lecithin 120mg

[0051] Cholesterol 250mg

[0052] Methanol 10ml

[0053] Ethanol 10ml

[0054] Sodium deoxycholate 40mg

[0055] Preparation method: Dissolve 40mg of sodium deoxycholate in an appropriate amount of Tris-HCl (pH7.5, containing 0.15mol / L NaCl) buffer with a molar concentration of 20mmol / L. Sodium deoxycholate in Tris-HCl buffer The weight concentration is 10%; 30mg ceramide is dissolved in 10ml methanol, 120mg lecithin, 250mg cholesterol is dissolved in 10ml ethanol, the two solutions are put together in a rotary evaporator, and the solvent is removed under reduced pressure at 40℃ to form Film, then add the above, and then add the above Tris-HCl buffer dissolved with sodium deoxycholate, ultrasonically treat for 30 minutes, to obtain ceramide liposomes, and spray-dry to obtain a lyophilized preparation of ceramide liposomes . The lyophilized preparation only needs to be fully hydrated and shaken for a short time before use to re-form t...

Embodiment 3

[0057] Ceramide 100mg

[0058] Soy Lecithin 1200mg

[0059] Hydrogenated saturated phospholipids 300mg

[0060] Cholesterol 100mg

[0061] Ganglioside 50mg

[0062] Anhydrous ethanol 50ml

[0063] Vitamin E 50mg

[0064] Preparation method: ultrasonically dissolve 100mg ceramide, 1200mg soy lecithin, 300mg hydrogenated saturated phospholipid, 100mg cholesterol, 50mg ganglioside and 6.5mg vitamin E in 50ml absolute ethanol, and place this solution in a rotary evaporator at 40℃ Remove the solvent under reduced pressure to form a thin film, and then add 20mmol / L Tris-HCl (pH7.5, containing 0.15mol / L NaCl) buffer, ultrasonic treatment for 30min, homogenize 5-6 times with a high-pressure homogenizer, and then pass 0.22μm The microporous filter membrane is packed and sealed to obtain ceramide liposomes, and dried to obtain a lyophilized preparation of ceramide liposomes. The lyophilized preparation only needs to be fully hydrated and shaken for a short time before use, and liposomes can be f...

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Abstract

The invention relates to ceramide liposome and a preparation method and application thereof. The ceramide liposome comprises a therapeutically effective amount of active component and a lipid bilayer film, and is characterized in that the ceramide liposome comprises 0.5 to 20 weight parts of ceramide used as the active component and 10 to 350 weight parts of the lipid bilayer film, wherein the lipid bilayer film comprises the following components in part by weight: 5 to 100 parts of phospholipid substance, 0.5 to 10 parts of cholesterol, 0 to 100 parts of surfactant, 0 to 20 parts of additive and 0.5 to 10 parts of organic solvent. The preparation method comprises the following steps of: fully dissolving the ceramide, the phospholipid substance, the cholesterol and the additive in the organic solvent, dissolving the surfactant in a dispersion medium to prepare the ceramide liposome, and reducing the average particle size of the prepared ceramide liposome to less than 500nm to ensure that the particle sizes are uniformly distributed. The invention also discloses new application of the ceramide liposome to cancer therapy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a short-chain ceramide liposome for targeted drug delivery, a preparation method thereof, and a new application thereof in tumor treatment. Background technique [0002] Malignant tumor has become the disease with the highest mortality rate, and chemotherapy is one of the most important treatment methods. The vast majority of patients with advanced tumors require chemotherapy, which is a more effective method for patients with systemic cancer spread. However, the overall effective rate of chemotherapy in clinical practice is still less than 30%, and almost all chemotherapeutic drugs will produce multidrug resistance during treatment, thereby further reducing the effective rate of chemotherapy. Therefore, how to improve the therapeutic effect of chemotherapy drugs is a key issue in tumor treatment. [0003] Short-chain ceramides (C2, C4, C6, C8, C...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/164A61P35/00
Inventor 陆培华曹聪李晨陈敏斌
Owner 陆培华
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