含舒马曲坦的阿拉伯胶双层微针贴剂的载药及透皮给药效果评价。

IF 2.8 4区 医学 Q2 PHARMACOLOGY & PHARMACY Current drug delivery Pub Date : 2024-01-01 DOI:10.2174/1567201820666230309140636
Xiaoduo Zhang, Weijun Liu, Wei Wang, Mingli Pi, Beibei Huang, Fanhong Wu
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引用次数: 2

摘要

背景:作为偏头痛患者的急性偏头痛发作,及时缓解头痛并消除相关症状的自我治疗是最佳的。基于此,研制了一种以天然金合欢为原料的快速溶解双层微针。方法:在正交设计试验筛选出的最佳反应条件下,采用阿拉伯胶(GA)进行离子交联,采用规定量的交联复合材料制备针尖负载舒马曲坦的双层微针。测定了猪皮的机械强度和溶解能力以及体外释放。用FT-IR和热分析测定了所得化合物的组分和含量,并用X射线光电子能谱表征了交联剂的键合状态。结果:构建的最大载药量微针的每根针由10.89μg左右的交联阿拉伯胶和1.821μg左右封装的舒马曲坦组成。除了优异的溶解性外,所形成的微针还具有足够的机械刚度来穿透多层链膜。猪皮的组织学切片证实,微针的插入深度可以达到300±28μm,分离猪皮中的针头体积可以在240秒内完全溶解。Franz扩散研究表明,包封药物几乎可以在40分钟内完全释放。交联产生的凝块由阿拉伯胶组分中的葡萄糖醛酸的-COO-和添加的交联剂组成,形成双配位键,交联率达到约13%。结论:所制备的12个微针贴片的药物释放量与皮下注射相当,为偏头痛的治疗提供了新的可能性。
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Evaluation of Gum Arabic Double-layer Microneedle Patch Containing Sumatriptan for Loading and Transdermal Delivery.

Background: As episodes of acute migraine for migraineurs, a self-treatment that promptly relieves headaches and eliminates the associated symptoms would be optimal. Based on the consideration, a rapidly dissolving double-layer microneedles derived from natural acacia was developed.

Methods: Under the optimized reaction conditions that was screened out through orthogonal designing test, acacia (GA) was conducted on the ionic crosslinking, a prescribed amount of cross-linking composites was applied to fabricate the double-layer microneedles loaded with sumatriptan at the tip. The mechanical strength and dissolving capability of penetrating pigskin along with in vitro release were measured. The component and content of the resulting compound were determined with FT-IR and thermal analysis, and the bonding state of cross-linker was characterized using X-ray photoelectron spectroscopy.

Results: Each needle from the constructed microneedles with the maximal drug loading consisted of the crosslinking acacia of around 10.89 μg and the encapsulated sumatriptan of around 1.821 μg. Apart from the excellent solubility, the formed microneedles possessed enough mechanical stiffness to penetrate the multilayer parafilm. The histological section of the pigskin confirmed the insertion depth of the microneedles could reach 300 ± 28 μm, and the needle bulk in the isolated pigskin could be totally dissolved within 240 s. Franz diffusion study displayed that an almost entire release of the encapsulated drug might be realized within 40 min. The coagulum created from crosslinking was composed of -COOof glucuronic acid in the component of acacia and the added crosslinker to form a double coordination bond, and the crosslinking percentage reached about 13%.

Conclusion: The release amount of drug from 12 patches made of the prepared microneedles was comparable to that of subcutaneous injection, providing a new possibility for migraine treatment.

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来源期刊
Current drug delivery
Current drug delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.10
自引率
4.20%
发文量
170
期刊介绍: Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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