The impact of active substance on the adhesiveness of medicated patches containing liquid additives

IF 4.3 3区 医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutical Sciences Pub Date : 2024-12-23 DOI:10.1016/j.ejps.2024.106997
Bartosz Maciejewski , Barbara Mikolaszek , Joanna Dłabiszewska , Małgorzata Sznitowska
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Abstract

Adhesiveness of dermal patches can be modified in the presence of active substances. The effect is more complex when liquid components are also present in the matrix. Commercial grade pressure sensitive adhesive (PSA) polyacrylates (three types) and silicones (two types) were used to prepare adhesive matrices and liquid additives were propylene glycol, polyoxyethylene glycol, isopropyl myristate, triacetin, triethyl citrate or low viscosity silicone oil. Drug-in-adhesive patches were prepared with model active substances (5% w/w): indomethacin or cytisine. The effect of the suspended or dissolved drug on adhesiveness was evaluated with probe tack test and 90° peel test. Most of the acrylate patches loaded with dissolved indomethacin showed acceptable level of adhesiveness. In case of cytisine, suspension type patches were often formed and only in some patches sufficient adhesiveness was retained. Adhesion of silicone based matrices was altered profoundly by the simultaneous drug and excipient addition. Only one matrix with indomethacin and silicone oil showed acceptable quality in both tack and peel tests (S1, Bio-PSA MD7–4502). In the course of the data analysis of the adhesiveness, the relevance of film formation mechanism was noted. It was observed, that if the film formation occurs by solvent evaporation in patches where drug particles are suspended, the impact of the particles on adhesion might be greater than in the case of patches with the dissolved drug. It was concluded, that a choice of a suitable polymer-liquid mixture for a particular active substance requires an experimental work in case of an adhesive properties adjustment. Due to complex physicochemical interaction between the components reliable theoretical predictions are considered as questionable.

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活性物质对含液体添加剂药贴黏附性的影响。
在活性物质的存在下,皮肤贴片的粘附性可以被改变。当基质中也存在液体成分时,效果更为复杂。采用工业级压敏胶(PSA)聚丙烯酸酯(三种类型)和有机硅(两种类型)制备胶粘剂基质,液体添加剂为丙二醇、聚氧乙烯醇、肉豆酸异丙酯、三乙酸酯、柠檬酸三乙酯或低粘度硅油。以吲哚美辛或胞氨酸为模型活性物质(5% w/w)制备药物贴。用探针粘连试验和90°剥离试验评价悬浮剂和溶解剂对粘连性的影响。大多数丙烯酸酯贴片加载溶解吲哚美辛显示出可接受的粘附水平。在胞氨酸的情况下,经常形成悬浮型贴片,只有部分贴片保留了足够的粘附性。药物和赋形剂的同时加入使硅基基质的粘附性发生了深刻的变化。只有一种含有吲哚美辛和硅油的基质在粘接和剥离试验中均表现出可接受的质量(S1, Bio-PSA MD7-4502)。在黏附性的数据分析过程中,注意到成膜机理的相关性。我们观察到,如果在药物颗粒悬浮的贴片中通过溶剂蒸发形成薄膜,那么颗粒对粘附的影响可能比溶解药物的贴片更大。结论是,在粘合剂性能调整的情况下,为特定活性物质选择合适的聚合物-液体混合物需要进行实验工作。由于组分之间复杂的物理化学相互作用,可靠的理论预测被认为是有问题的。
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来源期刊
CiteScore
9.60
自引率
2.20%
发文量
248
审稿时长
50 days
期刊介绍: The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.
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