High-stability phloretin nanosuspension, preparation method thereof and microneedle

A nano-suspension and high-stability technology, applied in the direction of microneedle, nanotechnology, nanotechnology, etc., can solve the problems of uneven quality and curative effect, and achieve the effect of good application effect, good mechanical properties, and simple preparation method

Active Publication Date: 2022-01-14
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the process of production and storage, it is necessary to ensure that the particle size of nanoparticles is uniform and stable within batches and between batches. Unstable nanoparticles will lead to uneven quality and curative effect.

Method used

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  • High-stability phloretin nanosuspension, preparation method thereof and microneedle
  • High-stability phloretin nanosuspension, preparation method thereof and microneedle
  • High-stability phloretin nanosuspension, preparation method thereof and microneedle

Examples

Experimental program
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Effect test

Embodiment 1

[0053] This embodiment provides a phloretin nanosuspension PHL-NIC-NCs, which is prepared by the following method:

[0054] Step 1. Preparation of organic phase solution: Take 10 mg of phloretin (0.036 mmol), dissolve it in 0.5 ml of absolute ethanol, add 4.45 mg of nicotinamide (0.036 mmol), stir and mix thoroughly to obtain an organic phase solution;

[0055] Step 2, preparation of aqueous phase solution: dissolve 20mg of hydroxypropylmethylcellulose HPMC (i.e. the mass ratio of hydroxypropylmethylcellulose to phloretin is 2:1) in 20ml of purified water, and swell at room temperature for 120min , to obtain an aqueous solution;

[0056] Step 3. Under the condition of stirring at 1000rpm, inject the organic phase solution into the aqueous phase solution at a speed of 3-9ml / min, and continue to stir for 0.5min until completely mixed evenly, that is, the phloretin nanosuspension PHL-NIC- NCs.

Embodiment 2-5

[0058] The preparation method of the phloretin nanosuspension provided in Examples 2-5 is roughly the same as that in Example 1, the only difference being that the added molar amounts of nicotinamide are 0.005mmol, 0.02mmol, 0.108mmol and 0.36mmol respectively, That is, in the nanosuspension provided in Examples 1-5, the molar ratios of phloretin and nicotinamide are 1:1, 7.2:1, 1.8:1, 1:3 and 1:10, respectively.

Embodiment 6-8

[0060] The preparation method of the phloretin nanosuspension provided in Examples 6-8 is roughly the same as that in Example 1, the only difference being that the added mass of hydroxypropyl methylcellulose is 5 mg, 10 mg and 50 mg respectively, that is, in In embodiment 1-5, the mass ratio of hydroxypropyl methylcellulose and phloretin is 2:1, and in embodiment 6-8, the mass ratio of hydroxypropyl methylcellulose and phloretin is respectively 1:2, 1:1 and 1:5.

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Abstract

The invention provides a high-stability phloretin nanosuspension, the nanosuspension is prepared from phloretin, a stabilizer and a solvent, the stabilizer comprises nicotinic acid and a derivative thereof, the molar ratio of the nicotinic acid and the derivative thereof to the phloretin is (10: 1)-(1: 10), and the particle size of the phloretin in the phloretin nanosuspension is 10-1000 nm. According to the phloretin nanosuspension provided by the invention, phloretin is prepared into the nanosuspension, the solubility and bioavailability of phloretin serving as a water-insoluble substance are remarkably improved, the phloretin nanosuspension further contains nicotinic acid and derivatives thereof, the nicotinic acid and the derivatives thereof can form hydrogen bonds with hydroxyl in phloretin molecules to stabilize nanocrystals of phloretin, and the effect of improving the stability of the phloretin nanocrystal is achieved.

Description

technical field [0001] The invention relates to the technical field of nano-suspensions, in particular to a high-stability phloretin nano-suspension, its application, preparation method and microneedles made using the phloretin nano-suspension. Background technique [0002] Phloretin, also known as trihydroxyphenolacetone 2,4,6-trihydroxy-3-(4-hydroxyphenyl)propiophenone, is a new type of natural skin whitening agent, mainly distributed in juicy fruits such as apples and pears. In the peel and root bark, it belongs to the polyphenol metabolites of plants. It has various therapeutic effects such as whitening, anti-inflammation, and anti-tumor, as well as a strong antioxidant activity, which can reduce active oxygen during normal oxygen metabolism or exogenous damage. (ROS) formation. Phloretin can be used in facial masks, skin care creams, lotions and essences. It can inhibit the excessive secretion of sebaceous glands and is used to treat acne with exuberant secretion. It c...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/12A61K47/22A61P29/00A61P35/00A61P39/06A61K8/35A61K8/67A61Q19/08A61Q19/02A61Q19/00B82Y5/00B82Y40/00A23L33/105A23L29/00A61M37/00
CPCA61K9/10A61K31/12A61K9/0021A61K47/22A61P29/00A61P35/00A61P39/06A61K8/35A61K8/675A61Q19/08A61Q19/02A61Q19/00B82Y5/00B82Y40/00A23L33/105A23L29/045A61M37/0015A61K2800/592A23V2002/00A61M2037/0046A61M2037/0053A61M2037/0023A61M2037/0061A23V2200/318A23V2200/30A23V2250/2132A23V2250/7046
Inventor苗晓庆向虹葛灿锋
OwnerSHANDONG UNIV