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Genistein positive ion nano lipid carrier and preparation method thereof

A technology of nano-lipid carrier and genistein, which can be applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. The problems of drug dosage and low solubility of genistein have achieved good industrialization prospects, good market prospects, and the effect of increasing drug loading.

Active Publication Date: 2013-09-04
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the low solubility of genistein in the conventional oil phase, less than 1mg / g, this greatly limits the drug loading capacity of genistein in the nano-lipid carrier
According to the law of Ostwald ripening, the uneven particle size distribution will lead to the development of polarization of ion particle size, thus affecting the stability of the preparation

Method used

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  • Genistein positive ion nano lipid carrier and preparation method thereof
  • Genistein positive ion nano lipid carrier and preparation method thereof
  • Genistein positive ion nano lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Accurately weigh 10 mg of genistein, 150 mg of glyceryl behenate, 100 mg of glyceryl caprylate, and 20 mg of macrogolglyceride neodecanoate, mix evenly, and heat to 85°C to form an oil phase; Weigh 100mg of soybean lecithin, 300mg of polyoxyethylene castor oil and ultrapure water (the final concentration of phospholipids is 0.75%, w / v) and mix evenly at 85°C to form a water phase; stir at 90°C at 400-600r / min Slowly add the water phase to the oil phase and mix under the high speed. After the dropwise addition, continue to stir and emulsify for 10 minutes. While maintaining the temperature of the colostrum system, use an ultrasonic breaker with a power of 200w to perform ultrasonic crushing for 2 minutes; transfer the sonicated colostrum to an ice bath for low-temperature solidification. Slowly add the prepared nano-lipid carrier dropwise at a stirring speed of 400-600r / min to a concentration of 0.1mg / mL of methacrylic acid and methacrylate copolymer (ethyl ac...

Embodiment 2

[0040] Example 2: Accurately weigh 10 mg of genistein, 120 mg of glyceryl monostearate, 80 mg of soybean oil, and 20 mg of macrogolglyceride neodecanoate, mix evenly, and heat to 85°C to form an oil phase; Soybean lecithin 75mg, polyethylene glycol lauryl hydroxystearate 250mg and ultrapure water (the final concentration of phospholipids is 0.5%, w / v) are mixed uniformly at 85°C to form a water phase; At a stirring speed of 1 / min, slowly add the water phase to the oil phase and mix, after the dropwise addition, continue to stir and emulsify for 10 min. While maintaining the temperature of the colostrum system, use an ultrasonic breaker with a power of 400w to perform ultrasonic crushing for 2 minutes; transfer the sonicated colostrum to an ice bath for low-temperature solidification. Slowly add the prepared nano-lipid carrier dropwise at a stirring speed of 400-600r / min to ethyl enoate, methyl methacrylate and trimethylethyl methacrylate at a concentration of 0.5 mg / mL (1:2:0...

Embodiment 3

[0041] Example 3: Accurately weigh 5 mg of genistein, 80 mg of glycerol palmitostearate, 50 mg of oleic acid, and 10 mg of macrogol glycerol oleate, mix evenly, and heat to 85° C. to form an oil phase; accurately weigh Soybean lecithin 50mg, Tween-80225mg and ultrapure water (the final concentration of phospholipids is 0.75%, w / v) are uniformly mixed at 85°C to form a water phase; The water phase was slowly added into the oil phase for mixing, and after the dropwise addition was completed, the stirring and emulsification was continued for 10 minutes. While maintaining the temperature of the colostrum system, use an ultrasonic breaker with a power of 200w to perform ultrasonic crushing for 2 minutes; transfer the sonicated colostrum to an ice bath for low-temperature solidification. The prepared nano-lipid carrier was slowly added dropwise at a stirring speed of 400-600r / min to a concentration of 1.0mg / mL ethyl acrylate methyl methacrylate and trimethylaminoethyl methacrylate c...

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Abstract

The invention discloses a genistein positive ion nano lipid carrier and a preparation method thereof. Every 100ml of nano lipid carrier comprises the following components: 0.01-0.1g of genistein, 0.8-1.5g of solid lipid material, 0.5-1g of liquid lipid material, 0.1-0.2g of PEG (polyethylene glycol) modified liquid lipid material, 2-4g of emulsifier, 0.1-1g of copolymer of methacrylic acid and methacrylate and the balance of water. The prepared genistein positive ion nano lipid carrier is round in appearance and uniform in mass, encapsulation efficiency is more than 85%, and biocompatibility and biodegradability are good. By adopting the genistein positive ion nano lipid carrier, solubility of genistein is improved, in vitro release of genistein is prolonged, and the aims of prolonging intraocular preparation retention time and reducing toxic and side effects of a medicine are achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a genistein cationic nano lipid carrier and a preparation method thereof. technical background [0002] Genistein, also known as genistein or 5,7,4'-trihydroxyisoflavone, is an isoflavone compound widely present in legumes. Genistein has extensive inhibitory activity on cell proliferation, and can bind to the Scr tyrosine kinase region in growth factor receptors during cell division to inhibit its activity, thereby inhibiting cell division and proliferation. Studies have shown that when genistein acts on rabbit and human lens epithelial cells, it can inhibit the expression of P21 protein and promote the expression of CyclinD1 protein, thereby blocking the division of lens epithelial cells in S phase and inducing Cells arrested in S phase undergo apoptosis. Genistein has a strong inhibitory effect on tyrosine kinase, which plays a key role in blo...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/352A61K47/34A61K47/32A61P27/12A61J3/07
Inventor 潘卫三张文骥孔郡李雪东陈奋于世慧李静李三鸣
Owner SHENYANG PHARMA UNIVERSITY
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