Mesoporous sponge spicule as well as preparation method and application of mesoporous sponge spicule

A technology of sponge and bone spicules, applied in pharmaceutical formulations, medical preparations with non-active ingredients, inorganic non-active ingredients, etc., can solve the problems of insufficient convenience, reduced SHS penetration effect, etc. Effect

Active Publication Date: 2021-01-19
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still many deficiencies in the use of SHS for skin drug delivery: 1) The penetration-promoting effect of SHS decreases sharply with the increase of the molecular weight of the drug; 2) The entire drug delivery step is divided into two steps, which is not convenient enough

Method used

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  • Mesoporous sponge spicule as well as preparation method and application of mesoporous sponge spicule
  • Mesoporous sponge spicule as well as preparation method and application of mesoporous sponge spicule
  • Mesoporous sponge spicule as well as preparation method and application of mesoporous sponge spicule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Mesoporous silica modified on the surface of bee sponge spicules

[0043]Bee sponge spicules: For the preparation method, see CN201610267764.6 "Preparation method of high-purity sponge spicules"

[0044] The following method can be used to prepare the surface-modified mesoporous silica of bee sponge spicules:

[0045] ①100mg of bee sponge spicules, add 35ml of deionized water, 80mg of cetyltrimethylammonium bromide (CTAB) or cetyltrimethylammonium chloride (CTAC), concentrated ammonia water (also hydrogen Sodium oxide or hydrochloric acid) (3-10ul, 20-50wt%), ethanol (10-100ml), stirred for 30min to form a uniform solution;

[0046] ② Add 30-100ul methyl orthosilicate (also can be ethyl orthosilicate or propyl orthosilicate) dropwise, then react statically at 30-100°C for 20-100 hours, wash with water to remove by-products, 100-120 Aging overnight at ℃;

[0047] ③ Remove the surfactant by solvent extraction, wherein the solvent can be a mixture of ethanol solution an...

Embodiment 2

[0055] Coumarin 6 was used as a fat-soluble model drug to study the effect of mSHS on Coumarin 6 drug loading and transdermal administration.

[0056] ①Drug loading process: Dichloromethane was used as a solvent to prepare Coumarin 6 solutions with different concentrations; weigh 10 mg mSHS and place it in a centrifuge tube, add 600 μl of Coumarin 6 with different concentrations, rotate and shake for 12 hours, and then mix mSHS and Coumarin 6 The mixed solution was centrifuged to remove all the supernatant drug solution, and the drug-loaded mSHS was placed in a fume hood to dry naturally to prepare the mSHS loaded with Coumarin 6 (mSHS@Coumarin 6). See Figure 4 .

[0057] Put mSHS@Coumarin 6 in a certain amount of ethanol solution, place it on a shaker for 12h (28°C, 200rpm), and then calculate the drug loading corresponding to mSHS according to the content of Coumarin 6 in the ethanol solution. See the result Figure 7 .

[0058] Quantitative results of drug loading

[...

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Abstract

The invention discloses a mesoporous sponge spicule. The mesoporous sponge spicule is prepared by modifying the surface of the sponge spicule with a mesoporous material. The sponge spicule, especiallya sponge haliclona spicule (SHS), can penetrate into the cuticle of the skin to open the skin barrier, and stay in the cuticle of the skin for a long time to form a large number of continuous micro-channels which are far longer than the duration of the micro-channels after the traditional micro-needles act on the skin. The mesoporous sponge spicule (mSS), especially the surface of the mesoporoussponge haliclona spicule (mSHS), is modified with the mesoporous material, so that various drugs, especially insoluble drugs or bioactive components, can be adsorbed and loaded, and the drug loading capacity is improved. In this way, loaded medicines or bioactive components can enter the skin along with the mesoporous spicule and then are released to the deep layer of the skin from the mesoporouslayer.

Description

technical field [0001] The invention relates to a mesoporous spicule (surface modified sponge spicules with mesoporous silica, mSS). Background technique [0002] Skin Drug Delivery has many unique advantages compared to other drug delivery routes, mainly reflected in: avoiding the liver first-pass effect; drug absorption is not affected by the digestive tract environment and gastrointestinal function; slow release or controlled drug release; patient compliance with treatment; and so on. However, the essence of the skin is a biofilm barrier. Except for a very small number of drug molecules (with a molecular weight less than 500Da and a moderate oil-water partition coefficient) that can pass through the stratum corneum barrier of the skin, most of the drug molecules are difficult to penetrate and absorb through the skin. Therefore, How to overcome the skin barrier and safely and effectively transdermally deliver various biomacromolecular drugs or active substances with diffe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/46A61K47/04A61K31/37
CPCA61K9/0021A61K47/46A61K47/02A61K31/37C01B33/18C01B33/12A61K9/143A61K9/148A61K9/0014A61K47/24
Inventor 陈铭张佳良梁雪娇
Owner XIAMEN UNIV
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