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Intelligent response type soluble microneedle and preparation method thereof

A soluble and intelligent technology, applied in pharmaceutical formulations, photodynamic therapy, cosmetic preparations, etc., can solve the problems of poor therapeutic effect, easy aggregation quenching, short incubation time, etc., to inhibit aggregation-induced quenching, avoid photo Degradation, improve the effect of curative effect

Pending Publication Date: 2021-10-22
GUANGZHOU NEWORLD PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with 5-Aminolevulinic acid (5-ALA), a photosensitizer commonly used clinically, ICG has many advantages: the incubation time of ICG-PDT is generally 15-30 minutes shorter; and the current Studies have not shown significant adverse effects of ICG-PDT; ICG is clinically readily available and inexpensive
However, the current use of ICG photosensitizers (such as injections, emulsions, etc.) still has the problems of short half-life in vivo, water instability, and easy aggregation and quenching, and the therapeutic effect is not good.

Method used

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  • Intelligent response type soluble microneedle and preparation method thereof
  • Intelligent response type soluble microneedle and preparation method thereof
  • Intelligent response type soluble microneedle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0071] The preparation of the intelligent responsive nanoparticles comprises the following steps:

[0072] Under stirring conditions (preferred stirring speed is 300rpm, stirring time is 5min), zinc nitrate hexahydrate and photosensitizer are dissolved in organic solvent to obtain solution A;

[0073] Dissolving 2-methylimidazole in an organic solvent to obtain solution B;

[0074] Under stirring conditions (preferably the stirring speed is 300rpm, and the stirring time is 1h), solution B is added to solution A, the resulting mixture is centrifuged, washed, and resuspended to obtain intelligent responsive nanoparticles.

[0075] Preferably, the solvent of solution A and solution B is methanol, which can achieve better drug dissolution and is beneficial to the assembly and formation of nanoparticles. Further, the molar ratio of zinc nitrate hexahydrate in solution A to 2-methylimidazole in solution B is 1:(1-32), preferably 1:(7-9), which helps to obtain a suitable size nanop...

Embodiment 1

[0087] Example 1 Preparation of smart responsive drug-loaded nanoparticles

[0088] Weigh a certain amount of Zn(NO 3 ) 2 ·6H 2 O. Dissolve ICG in methanol solution, stir at room temperature at 300rpm for 5min, and record it as solution A;

[0089] Weigh a certain amount of 2-MeIM and dissolve it in another equal volume of methanol solution, which is recorded as solution B, Zn(NO 3 ) 2 ·6H 2 The molar ratio of O:2-MeIM is 1:8.

[0090] After the solution A was stirred for 5 min, the solution B was dropped into the solution A under the condition of 300 rpm magnetic stirring, and the stirring was continued for 1 h under the condition of magnetic stirring, so as to form uniform drug-loaded nanoparticles.

[0091] The prepared nanoparticle solution was collected, centrifuged at 10,000 rpm and 4°C for 10 min, discarded the supernatant, washed three times with ultrapure water, and centrifuged to remove residual organic solvent. Finally, the nanoparticles were resuspended in u...

Embodiment 2

[0093] Embodiment 2 Determination of drug loading of intelligent responsive nanoparticles

[0094] The standard curve for ICG content determination was established by fluorescence spectroscopy. With the drug concentration as the abscissa and the fluorescence intensity as the ordinate, nonlinear fitting is performed for subsequent ICG content analysis.

[0095] Using a fluorescence spectrometer, the fluorescence intensity of ICG in the supernatant was measured at an excitation wavelength of 763nm, and the drug loading of ZIF-8-ICG nanoparticles was calculated using the standard curve.

[0096]The results are shown in Table 1: ZIF-8-ICG nanoparticles were prepared by an in-situ drug encapsulation method (one-step synthesis). During this process, ICG molecules can form coordination bonds with zinc ions due to the presence of sulfonic acid groups. After adding 2-MeIM ligand, ZIF-8 nanoparticles will form in situ assembly around ICG molecules. It can be seen from Table 1 that wi...

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Abstract

The invention relates to an intelligent response type soluble microneedle and a preparation method thereof. The intelligent response type soluble microneedle comprises a needle tip, a needle body and a substrate; the needle tip is prepared from a raw material comprising a soluble material and intelligent response type nanoparticles; the needle body is prepared from a raw material comprising a soluble material; the substrate is prepared from a raw material comprising a high polymer material; the intelligent response type nanoparticles are a zeolite imidazate framework structure material loaded with a photosensitizer; and the photosensitizer is a cyanine dye with negative electricity. The intelligent response type soluble microneedle provided by the invention is excellent in acne treatment effect, and the photosensitizer has very high load rate and stability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an intelligent responsive soluble microneedle and a preparation method thereof. Background technique [0002] Acne is a chronic inflammatory disease of the pilosebaceous glands. It is commonly known as acne because it often occurs in adolescence. It is one of the most common diseases in dermatology, and its incidence rate shows an increasing trend year by year. Current studies suggest that the pathogenesis of acne is mainly related to the following four factors: excessive sebum secretion, hyperkeratosis at the opening of the pilosebaceous gland duct, propagation of Propionibacterium acnes (P.acnes), and inflammatory response. If timely and effective treatment is not obtained, the best treatment opportunity will be delayed, and sequelae such as pigmentation and scars will often be left behind, which will bring great negative impacts on the life and psychology of patients...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K9/00A61K47/54A61K47/36A61K47/32A61P17/10A61K8/81A61K8/73A61K8/49A61K8/02A61Q19/00
CPCA61K41/0057A61K9/0021A61K47/545A61K47/36A61K47/32A61P17/10A61K8/8176A61K8/735A61K8/4946A61K8/492A61K8/0216A61Q19/00
Inventor 潘昕温婷权桂兰吴传斌陈航平李峰冯地桑杨蓓蓓
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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