渗透促进剂对Eudragit®RS100聚合物基质型药物拉莫三嗪在粘性贴片中的体外释放和透皮给药的影响。

IF 4.4 3区 医学 Q2 ENGINEERING, BIOMEDICAL Progress in Biomaterials Pub Date : 2019-06-01 Epub Date: 2019-05-08 DOI:10.1007/s40204-019-0114-9
Ifrah Jafri, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Fatima Ramzan Ali
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引用次数: 22

摘要

采用油酸、PG、柠檬油和芦荟等不同的渗透促进剂,研制了拉莫三嗪的DIA型基质贴剂,并对其体外释放和渗透性能进行了评价。拉莫三嗪长期以来一直被用作抗癫痫、情绪稳定剂,用于治疗成人双相情感障碍,并被用作抗抑郁药。通过将溶液倾倒在背衬膜(3M-9720)上制备由Eudragit®RS100(速率控制聚合物)和DuroTak®387-2510(粘合剂)组成的拉莫三嗪基质贴片。120µm的厚度通过微米薄膜涂布器进行调整。USP装置V用于评估释放曲线,该曲线被拟合到各种数学模型中。通过重量变化、水分含量、水分吸收和药物含量评估来确定贴片的质量特征。FTIR研究药物赋形剂的兼容性;采用Franz扩散池研究了渗透通量、滞后时间和ER等体外渗透参数,并对优化后的贴剂进行了皮肤敏感性研究。由PG和油酸组成的贴剂的释放量最大,即96.24 ± 1.15%和91.12 ± 分别为1.11%。制剂(A1-A5)表现出Makoid-Banakar释放曲线。与增强率为3.55的其他增强剂相比,由油酸组成的制剂A3由于增强了药物在皮肤上的渗透而得到优化。皮肤敏感性研究表明,贴片是安全和非过敏性的。研究表明,油酸可作为基质型贴片透皮给药拉莫三嗪的合适渗透促进剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from Eudragit®RS100 polymer matrix-type drug in adhesive patches.

The drug-in-adhesive (DIA)-type matrix patches of lamotrigine are developed using variable permeation enhancers (oleic acid, PG, lemon oil and aloe vera), and drug in vitro release and its permeation are evaluated. Lamotrigine has been long used as an anti-epileptic, mood stabilizer, to treat bipolar disorder in adults and off label as an antidepressant. lamotrigine matrix patches comprising of Eudragit®RS100 (rate-controlling polymer) and DuroTak® 387-2510 (adhesive) were prepared by pouring the solution on backing membrane (3M-9720). The thickness of 120 µm was adjusted through micrometer film applicator. USP Apparatus V was used for the evaluation of release profile, which was fitted into various mathematical models. Quality characteristics of patches were determined through weight variation, moisture content, moisture uptake and drug content evaluation. FTIR studies were performed for drug-excipient compatibility; Franz diffusion cell was employed for studying in vitro permeation parameters such as flux, lag time, and ER. Skin sensitivity study of optimized patch was also performed. The release from patches comprising of PG and oleic acid was maximum, i.e., 96.24 ± 1.15% and 91.12 ± 1.11%, respectively. Formulations (A1-A5) exhibited Makoid-Banakar release profile. Formulation A3 consisting of oleic acid was optimized due to enhanced permeation of drug across skin compared to other enhancers with enhancement ratio of 3.55. Skin sensitivity study revealed patch as safe and non-allergenic. The study demonstrates that oleic acid can be used as a suitable permeation enhancer for transdermal delivery of lamotrigine from matrix-type patches.

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来源期刊
Progress in Biomaterials
Progress in Biomaterials MATERIALS SCIENCE, BIOMATERIALS-
CiteScore
9.60
自引率
4.10%
发文量
35
期刊介绍: Progress in Biomaterials is a multidisciplinary, English-language publication of original contributions and reviews concerning studies of the preparation, performance and evaluation of biomaterials; the chemical, physical, biological and mechanical behavior of materials both in vitro and in vivo in areas such as tissue engineering and regenerative medicine, drug delivery and implants where biomaterials play a significant role. Including all areas of: design; preparation; performance and evaluation of nano- and biomaterials in tissue engineering; drug delivery systems; regenerative medicine; implantable medical devices; interaction of cells/stem cells on biomaterials and related applications.
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