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对载扑热息痛纳米孔二氧化硅纳米粒子的经皮给药系统的研究。

Investigation of Paracetamol Entrapped Nanoporous Silica Nanoparticles in Transdermal Drug Delivery System.

机构信息

School of Materials Science and Nanotechnology, Jadavpur University, Kolkata, India.

Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.

出版信息

Appl Biochem Biotechnol. 2023 Aug;195(8):4712-4727. doi: 10.1007/s12010-023-04576-w. Epub 2023 Jun 5.

Abstract

An effort was made to administer paracetamol drug through transdermal patch, as no such formulation of this drug has been developed yet. The primary cause for the lack of such formulations is paracetamol's poor aqueous solubility. As a result, the current research concentrated on preparing nanomedicines, or drug-loaded nanoparticles, for delivery via transdermal formulations. Nanoparticles can improve the solubility of weakly aqueous soluble or even aqueous insoluble drugs by changing the crystalline structure of loaded medicines to an amorphous state and serving as drug permeation boosters. Silica nanoparticles (SNPs) were synthesized through sol-gel technique to achieve the aforementioned goal. DLS data revealed that the average particle size was around 100-200 nm, which was sufficient to penetrate the skin barrier. XRD analysis showed that the SNPs were amorphous, and the drug molecules lost their crystallinity after encapsulation into the nanoparticles, causing the enhancement of dissolution of drug molecules in physiological pH (pH-7.4). Different kinetic models were employed for the ex vivo dissolution data to evaluate the suitable kinetic model followed by the drug release in both burst and sustained phase. In vivo analgesic study was executed on mice applying each of the transdermal formulations to examine the performances of the patches.

摘要

曾尝试通过透皮贴剂给药,但目前尚未开发出这种药物的制剂。缺乏此类制剂的主要原因是对乙酰氨基酚的水溶性差。因此,目前的研究集中于制备纳米药物或载药纳米粒子,通过透皮制剂进行递送。纳米粒子可以通过将负载药物的晶体结构转变为无定形状态来提高弱水溶性甚至水不溶性药物的溶解度,并作为药物渗透促进剂。通过溶胶-凝胶技术合成了硅纳米粒子 (SNP) 以实现上述目标。DLS 数据显示平均粒径约为 100-200nm,足以穿透皮肤屏障。XRD 分析表明 SNPs 为无定形,药物分子在封装到纳米粒子后失去结晶度,导致药物分子在生理 pH(pH-7.4)下的溶解增强。采用不同的动力学模型对体外溶解数据进行拟合,以评估合适的动力学模型,随后在突释和持续阶段进行药物释放。对小鼠进行体内镇痛研究,应用每种透皮制剂来考察贴剂的性能。

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