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Preparation method of myricetin-loaded nano-micelle for reducing ovariectomy-induced bone loss by inhibiting formation of osteoclast

A technology for inhibiting osteoclastosis and ovariectomy, applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of low release and bioavailability in vitro, and achieve good bone targeting in vivo and in vitro , good therapeutic effect, and the effect of improving ALP activity

Active Publication Date: 2022-03-18
蒋廷旺
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to solve the problems of poor myricetin water solubility, in vitro release and low bioavailability, etc., to provide a method for preparing myricetin-loaded nanomicelles that can reduce bone loss induced by ovariectomy by inhibiting the formation of osteoclasts. Invented to prepare myricetin with poor water solubility into a bone-targeted micellar preparation, which can significantly improve the solubility and in vitro release of myricetin, and its preparation method is simple

Method used

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  • Preparation method of myricetin-loaded nano-micelle for reducing ovariectomy-induced bone loss by inhibiting formation of osteoclast
  • Preparation method of myricetin-loaded nano-micelle for reducing ovariectomy-induced bone loss by inhibiting formation of osteoclast
  • Preparation method of myricetin-loaded nano-micelle for reducing ovariectomy-induced bone loss by inhibiting formation of osteoclast

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Synthesis of bone targeting material AL-P(LLA-CL)-PEG-P(LLA-CL):

[0031]The compound P(LLA-CL)5 / 5(4500)-PEG(2000)-P(LLA-CL)5 / 5(4500) was ultrasonically dissolved in the DMF solution, and the compound CDI(N,N' was added while stirring -carbonyldiimidazole), reacted at room temperature for 5h. Use dichloromethane-methanol (15:1, v / v) as developing solvent to detect related substances. After the first step reaction finishes, add the mixed solution of alendronate sodium (AL) and tetrabutylammonium hydroxide (molar ratio=1:2; Alendronate sodium, the amount of trihydrate) while stirring in the reaction liquid 10mg, 0.03mmol; tetrabutylammonium hydroxide aqueous solution is 38.9mg, 0.06mmol), heated at 80°C for 5h. The progress of the reaction was monitored by running a plate with dichloromethane:methanol=15:1. After the reaction, use a rotary evaporator to remove DMF (70-80°C), add a small amount of water to wash the remaining reaction solution, and centrifuge to remove t...

Embodiment 2

[0034] Preparation of myricetin-loaded nanomicelles that reduce ovariectomy-induced bone loss by inhibiting osteoclast formation:

[0035] Dissolve the dried AL-P(LLA-CL)-PEG-P(LLA-CL) in ultrapure water at a concentration of 10 mg / mL. Myricetin (MY) was dissolved in absolute ethanol to prepare a solution with a concentration of 10 mg / mL. Take 1, 2, 3, and 4 mL of the prepared MY, and slowly drop them into 20 mL of 10 mg / mL AL-P(LLA-CL)-PEG-P (LLA-CL) aqueous solution under ultrasonic conditions, and ultrasonically mix Uniform (ultrasonic power 200W, ultrasonic time 20min). Remove absolute ethanol by rotary evaporation under reduced pressure, and then filter with a 0.45 μm water filter to obtain AL-P(LLA-CL)-PEG-P(LLA-CL)-MY drug-loaded micelles. The particle size, potential and polydispersity coefficient of the four groups of micelles were measured respectively, and the four groups of micelles were placed in a room temperature environment for 7 days, and the particle size o...

Embodiment 3

[0041] Targeting study of myricetin micelles

[0042] Add nano-scale hydroxyapatite aqueous solution into two 2mL plastic centrifuge tubes respectively, and then add 500uL of myricetin raw material drug and preparation solution (1mg / mL), sonicate for 5min to mix evenly, let it stand at room temperature, and add it at different times Point 5min, 10min, 15min, 30min, 60min, 120min for testing. Take one tube for centrifugation (10000rpm, 5min), take the supernatant, pass through a 0.22um filter, and perform HPLC detection, repeat three times at each time point, take the average value, and calculate the myricetin content; the same method is used, except that nano-scale Aqueous hydroxyapatite solution was used to test the release of formulations at different time points.

[0043] The results showed that after 1 h, the binding rate of myricetin and hydroxyapatite in myricetin-targeted micelles was higher than 80%, while the binding rate of free myricetin and hydroxyapatite was lowe...

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Abstract

The invention provides a preparation method of myricetin-loaded nano-micelles for reducing ovariectomy-induced bone loss by inhibiting formation of osteoclasts, and belongs to the field of pharmaceutical preparations. The invention discloses a myricetin-loaded nano-micelle, and aims to provide a myricetin-loaded nano-micelle capable of improving the drug loading capacity so as to improve the solubility and oral bioavailability of myricetin and reduce ovariectomy-induced bone loss by inhibiting the formation of osteoclasts. According to the key point of the technical scheme, the preparation method of the myricetin-loaded nano-micelle (hereinafter referred to as myricetin micelle) comprises the step of preparing the myricetin bone targeting micelle from a bone targeting material AL-P (LLA-CL)-PEG-P (LLA-CL) and myricetin. The prepared myricetin micelle has smaller particle size and higher encapsulation efficiency, the in-vitro solubility and in-vivo bioavailability of the myricetin micelle are enhanced, the ALP activity of osteoblasts is remarkably improved, and the treatment effect of resisting castrated rat osteoporosis is enhanced. And preliminary information is provided for clinical application of myricetin and other similar water-insoluble compounds.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a method for preparing myricetin-loaded nano-micelles for reducing bone loss induced by ovariectomy by inhibiting the formation of osteoclasts. Background technique [0002] Myricetin (3,5,7,3′,4′,5′-hexahydroxyflavone) is a polyhydroxyflavonol compound found in many natural plants such as bayberry bark and leaves, tea, onion Moderate, with resource advantages in drug research and application. Studies have shown that myricetin has a wide range of pharmacological activities, including hypoglycemic, anti-oxidation, liver protection, anti-inflammatory and analgesic, anti-bacterial and anti-tumor. Studies have also shown that myricetin has the effect of promoting osteogenic activity and inhibiting osteoclastogenic activity. At present, myricetin has been approved by the FDA as an additive to be used in medicine, food, and health care products, and has great de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/352A61K47/34A61P9/10
CPCA61K9/1075A61K31/352A61K47/34A61P9/10
Inventor 蒋廷旺席焱海王伟恒潘文明
Owner 蒋廷旺
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