Honokiol nanoparticles and preparation method thereof

A honokiol and nanoparticle technology, applied in the field of pharmaceutical preparations, can solve the problems of poor water solubility, low oral bioavailability, and low drug loading, and achieve the effects of facilitating treatment, improving tissue distribution in the body, and improving drug distribution

Inactive Publication Date: 2014-04-09
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Poor water solubility and low oral bioavailability limit its clinical application and curative effect to a large extent. Most of the reports on the preparati

Method used

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  • Honokiol nanoparticles and preparation method thereof
  • Honokiol nanoparticles and preparation method thereof
  • Honokiol nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Add 100mg of hydroxypropyl methylcellulose into 20mL of water, stir to dissolve it completely, completely dissolve 40mg of honokiol in 2mL of acetone, slowly add this solution dropwise into 20mL of aqueous solution with a syringe, 200W ultrasonic for 10min, The temperature of the water bath was room temperature. Obtain honokiol initial suspension, remove acetone by rotary evaporation under reduced pressure, namely obtain honokiol nanoparticles, the average particle diameter is 353nm ( figure 1 ).

Embodiment 2

[0031] Add 200mg of Poloxamer P188 into 20mL of water, stir to dissolve it completely, completely dissolve 100mg of honokiol in 3mL of acetone, slowly add this solution dropwise into 20mL of aqueous solution with a syringe, stir for 10min, and the temperature of the water bath is room temperature . Obtain the initial suspension of honokiol, remove the acetone by rotary evaporation under reduced pressure, obtain honokiol nanoparticles, and the average particle diameter is 189nm ( figure 1 ).

Embodiment 3

[0033] Add 40mg of Tween-80 into 20mL of water, stir to dissolve it completely, completely dissolve 40mg of honokiol in 1mL of acetone, quickly drop this solution into 20mL of aqueous solution with a syringe, 250W ultrasonic for 8min, and the temperature of the water bath is 0°C. Obtain honokiol initial suspension, remove acetone by rotary evaporation under reduced pressure, namely obtain honokiol nanoparticles, the average particle diameter is 151nm ( figure 1 ).

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Abstract

The invention belongs to the technical field of medicines, and relates to honokiol nanoparticles and a preparation method thereof. The honokiol nanoparticles are prepared by adopting an ultrasonic-precipitation method in combination with a freeze-drying technology, and the composition of prescription is as follows: the combination ratio of honokiol to a stabilizer is 1:(0.05-50). According to the honokiol nanoparticles and the preparation method thereof, through prescription optimization, povidone (PVP) and bovine serum albumin (BSA) are screened as the best stabilizer combination. The prepared honokiol nanoparticles are high in drug loading, stable in nature, simple in prescription composition, easy, convenient and feasible in preparation process, and the particle size range is 100nm-300nm; and through the preparation of the nanoparticles, the dissolution of honokiol can be obviously promoted, the oral bioavailability is improved, and tissue distribution in the body is improved. In addition, the honokiol nanoparticles can be freeze-dried, and a suitable excipient is added into the obtained freeze-dried powder for further preparing different dosage forms such as oral liquid, tablets, granules and capsules, and also can be prepared into injection for subcutaneous, muscle or intravenous drug delivery so as to be convenient for clinical application.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to honokiol nanoparticles, a preparation method and application. Background technique [0002] Honokiol (Honokiol) is a small molecular bioactive substance containing phenolic hydroxyl extracted from the traditional Chinese medicine Magnolia officinalis. Its molecular formula is C18H18O2, its molecular weight is 266.33, and its water solubility is poor. Domestic and foreign studies have reported that honokiol has strong antioxidant, antibacterial, antithrombotic, anti-inflammatory, anti-anxiety and anti-tumor effects. [0003] Poor water solubility and low oral bioavailability limit its clinical application and curative effect to a large extent. Most of the reports on the preparation and activity of honokiol are limited to liposomes and micelles, and the drug loading is relatively low. relatively low, and there are relatively few studies on it in vivo. [0004] Nanoparti...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/19A61K31/05A61P39/06A61P31/04A61P7/02A61P29/00A61P25/22A61P35/00A61P9/00
Inventor 韩美华王向涛于鑫
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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