Department of Pharmaceutical Sciences, Università degli Studi di Milano, via G. Colombo, 71, 20133 Milano, Italy.
Department of Pharmaceutical Sciences, Università degli Studi di Milano, via G. Colombo, 71, 20133 Milano, Italy.
Eur J Pharm Sci. 2018 Jan 1;111:238-246. doi: 10.1016/j.ejps.2017.10.006. Epub 2017 Oct 5.
Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with tributyl citrate (TBC) or triacetin (TRI) in order to design a pressure sensitive adhesive suitable for transdermal patch preparation. The patch adhesive properties (i.e. tack, peel adhesion and shear adhesion) as well as its in vitro biopharmaceutical performances were determined after loading ibuprofen, ketoprofen or flurbiprofen. The addition of 40-60% w/w TBC or 40-50% w/w TRI to EuRL permitted to obtain matrices with the desired adhesive properties. Moreover, the increase of plasticizer content and loading of the drug reduced the relaxation time (τ). Consequently, the shear adhesion values decreased and the in vitro drug release constants (k) increased. Indeed, the k values from patches containing TBC were lower than the corresponding with TRI because of the lower fluidity of such matrices. In conclusion, the 60/40 EuRL/TBC binary blend is suitable for the design of transdermal patches since the in vitro permeability of the three selected drugs appeared comparable to those described in literature for marketed products.
Eudragit® RL（EuRL）基质已被提议用于向皮肤释放药物。然而，关于此类制剂的粘弹性和粘附性能尚无信息。本工作重点评估了不同程度柠檬酸三丁酯（TBC）或三醋酸甘油酯（TRI）塑化的 EuRL 的流变和质地特性，以便设计适合透皮贴剂制备的压敏胶。在载有布洛芬、酮洛芬或氟比洛芬后，测定贴剂的粘合性能（即初粘性、剥离粘合和剪切粘合）及其体外生物药剂学性能。将 40-60wt%w/w TBC 或 40-50wt%w/w TRI 添加到 EuRL 中，可获得具有所需粘合性能的基质。此外，增塑剂含量和药物载量的增加降低了松弛时间（τ）。因此，剪切粘合值降低，体外药物释放常数（k）增加。事实上，由于这些基质的流动性较低，含有 TBC 的贴片的 k 值低于含有 TRI 的相应 k 值。总之，60/40 EuRL/TBC 二元共混物适合透皮贴剂的设计，因为三种所选药物的体外渗透性与文献中报道的市售产品相当。
