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Liposome gel preparation and preparation method and application thereof

A technology of liposome gel and liposome, which is applied in the direction of liposome delivery, antibody delivery, liquid delivery, etc. It can solve the problems of prominent toxic and side effects, affecting the metabolism and activity of skin tissue cells, etc., achieving less toxic and side effects, regulating Skin immune cytokines, the effect of improving poor water solubility

Active Publication Date: 2012-10-03
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therapeutic drugs mainly include steroid hormones (local injection or smear), anti-metabolite drugs (local injection or oral administration) and silicon preparations (smear or spray), among which hormonal drugs are effective quickly, but long-term application will cause local side effects and systemic reactions. Such as skin atrophy, local telangiectasia and pigmentation, etc.; anti-metabolite drugs are generally anti-cancer preparations, with prominent toxic and side effects, affecting the metabolism and activity of normal skin tissue cells; silicon preparations have no side effects and good patient compliance, but only for maintenance Effective on areas of pressure (such as extremities)

Method used

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  • Liposome gel preparation and preparation method and application thereof
  • Liposome gel preparation and preparation method and application thereof
  • Liposome gel preparation and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0036] Embodiment 1: Paeonol transdermal gel preparation

[0037] Formula: paeonol 40mg, egg yolk lecithin 400mg, ethanol 8mL, cholesterol 200mg, Avastin-PEG-DOPE 20mg, phosphate buffer (pH 7.4) 10mL, carbomer 934 3g, glycerin 0.3g.

[0038] Preparation method: Dissolve paeonol in ethanol, add egg yolk lecithin, cholesterol and Avastin-PEG-DOPE, heat and stir in a water bath at 50-60°C to dissolve, and form a clear solution. Slowly inject into phosphate buffer (pH 7.4) in liquid flow through a syringe needle with a fine pore size, magnetically stir, the stirring speed is controlled at 300rpm, and N is introduced during the injection process. 2 Remove most of the ethanol. The resulting liquid was ultrasonically pulverized 3 times, each time for 1 minute, at a frequency of 300 Hz. Add Carbomer 934 to the above liposome solution, after the swelling is complete, add glycerin, grind evenly, pack separately, apply on the mounting material, and sterilize to get the product.

Embodiment 2

[0039] Embodiment 2: Paeonol transdermal gel preparation

[0040] Formula: paeonol 42mg, hydrogenated soybean lecithin 400mg, ether 5mL, cholesterol 200mg, Avastin-PEG-DOPE 20mg, phosphate buffer (pH 7.4) 10mL, carbomer 980 2.5g, glycerol 0.3g.

[0041] Preparation method: Dissolve paeonol with ether, add hydrogenated soybean lecithin, cholesterol and Avastin-PEG-DOPE to dissolve and form a clear solution. Slowly inject into phosphate buffer (pH 6.5) in liquid flow through a syringe needle with a fine pore diameter, stir magnetically at a speed of 300 rpm, form a milky white liquid, and then ultrasonically pulverize 3 times, each time for 1 minute, with a frequency of 300 Hz. Add Carbomer 980 into the above liposome solution, after the swelling is complete, add glycerin, grind evenly, pack separately, apply on the mounting material, and sterilize to get the product.

Embodiment 3

[0042] Embodiment 3: Paeonol transdermal gel preparation

[0043] Formula: paeonol 4g, hydrogenated soybean lecithin 40g, ethanol 800mL, cholesterol 20g, Avastin-PEG-DOPE 2g, phosphate buffer (pH 7.4) 1 L, poloxamer 188 2Kg, glycerin 300g.

[0044] Preparation method: Dissolve paeonol in ethanol, add hydrogenated soybean lecithin, cholesterol and Avastin-PEG-DOPE, heat and stir in a water bath at 50-60°C to dissolve, and form a clear solution. Slowly inject into phosphate buffer (pH 7.4) in liquid flow through a micropipeline with a fine pore size, magnetically stir, the stirring speed is controlled at 250rpm, and N is introduced during the injection process. 2 Remove most of the ethanol. The obtained liquid was high-pressure emulsified three times under the condition of 10 bar to obtain a liposome solution. Add poloxamer 188 into the above liposome solution, after the swelling is complete, add glycerin, grind evenly, dispense, apply on the mounting material, and sterilize...

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Abstract

The invention provides a liposome gel preparation for treating hypertrophic scars. The liposome gel preparation comprises liposome, gel material and glycerol, wherein the liposome is encapsulated with paeonol, and the surface of the liposome is bonded with vascular endothelial growth factor (VEGF) antibodies through polyethylene glycol. The invention provides a preparation method and application of the gel preparation at the same time. The gel preparation is encapsulated by using a material such as phospholipid with good physiological compatibility with the human body, so that the problems of poor water solubility and low stability of the paeonol are effectively solved. The VEGF antibodies are used for modifying the surface of the liposome, lipid particles enter the dermis through the epidermis by using the permeation promoting effect of liposome carriers and are directionally bonded with VEGF receptors of the pathological change skin part, and the encapsulated medicament is released at the same time, so that positioned retention of the medicament in the scar hyperplasia part is realized. Compared with other reported scar hyperplasia resistant medicament preparations or treatment schemes, the invention has the advantages that the liposome gel preparation is low in relapse rate, reduces the occurrence rate of the toxic or side effect and can be applied to any scar hyperplasia part of the body.

Description

technical field [0001] The invention mainly relates to a liposome gel preparation, in particular to a paeonol immune liposome gel preparation. The invention also relates to the preparation method and application of the gel preparation. Background technique [0002] Hypertrophic scars (Hypertrophic scars, HS) is a progressive, pathological and irreversible skin disease, often occurs in the repair process of deep trauma (such as surgery, burns and scalds), caused by a large number of micro-vascularization, fibroblast proliferation , Excessive deposition of collagen leads to excessive fibrosis of the dermis. Medical research results have shown that the degree of scar hyperplasia is positively correlated with the density of microvessels in the wounded skin, in which vascular endothelial growth factor (vascular endothelial growth factor, VEGF) plays a key role in physiological and pathological angiogenesis. After tissue trauma, factors such as inflammation, allergic reaction, h...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/127A61K47/48A61K39/44A61P17/02A61K31/12
Inventor 时军
Owner GUANGDONG PHARMA UNIV
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