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Effect of Different Pressure-Sensitive Adhesives on Performance Parameters of Matrix-Type Transdermal Delivery Systems

机译:不同的压敏胶粘剂对基质型透皮给药系统性能参数的影响

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摘要

Matrix-type transdermal delivery systems (TDS) are comprised of the drug dissolved or dispersed in a pressure-sensitive adhesive (PSA) matrix and are designed to provide a controlled delivery through the skin and into systemic circulation. PSAs can directly affect the permeation, release, and performance characteristics of the system. In this study we aimed to design and characterize transdermal delivery systems formulated with lidocaine—as the model drug—loaded in different PSAs, including silicone, polyisobutylene (PIB), and acrylate. TDS containing lidocaine at its saturation points were prepared by the solvent casting method. In vitro permeation studies across dermatomed porcine ear skin were performed using Franz diffusion cells. In vitro release studies were carried out using USP apparatus 5 (paddle over disk). The cumulative amount permeated from the acrylate was significantly higher than silicone and PIB. The acrylate TDS contained a ten times higher drug amount than silicone TDS, but the permeation flux was only two folds higher. Results also showed the release of drug does not linearly correlate to saturation, as the silicone TDS comprising of the lowest amount of drug loading, showed the highest percentage release indicating the choice of PSA affected the drug release and permeation profile.
机译:基质型透皮给药系统(TDS)由溶解或分散在压敏胶粘剂(PSA)基质中的药物组成,旨在提供通过皮肤和全身循环的受控给药。 PSA可以直接影响系统的渗透,释放和性能特征。在这项研究中,我们旨在设计和表征由利多卡因配制的透皮递送系统(作为模型药物),将其装入不同的PSA中,包括有机硅,聚异丁烯(PIB)和丙烯酸酯。通过溶剂浇铸法制备在饱和点含有利多卡因的TDS。使用Franz扩散池进行了猪皮皮肤的体外渗透研究。使用USP装置5(桨在磁盘上)进行了体外释放研究。从丙烯酸酯渗透的累积量显着高于有机硅和PIB。丙烯酸酯TDS的药物量是有机硅TDS的十倍,但渗透通量仅高两倍。结果还显示药物的释放与饱和度不线性相关,因为包含最低载药量的有机硅TDS显示最高的释放百分比,表明PSA的选择会影响药物的释放和渗透曲线。

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