Gel formulations containing catanionic vesicles composed of alprenolol and SDS: Effects of drug release and skin penetration on aggregate structure
Gel formulations containing catanionic vesicles composed of alprenolol and SDS: Effects of drug release and skin penetration on aggregate structure
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DOI：
10.1016/j.colsurfb.2011.08.022
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发表时间：
2012-01-01
影响因子：
5.8
通讯作者：
Bjork, Erik
中科院分区：
文献类型：
--
作者：
Dew, Noel;Edwards, Katarina;Bjork, Erik
为了充分利用凝胶制剂的延长接触时间，研究了一种新型的含有阳离子聚集体的药物制剂，该药物具有延长药物释放和皮肤渗透的作用。本研究旨在进一步探讨凝胶中阳离子囊泡的药物释放过程。由阿普萘洛尔和十二烷基硫酸钠形成了阳离子囊泡。使用了由阳离子囊泡和SoftCAT聚合物组成的物理凝胶以及共价卡波尔凝胶。采用改进的USP桨片法测定体外药物释放量，并采用水平乌辛室安装的猪耳皮肤进行皮肤透入研究。用低温透射电镜观察了药物释放和透皮过程中聚集体的结构。研究结果表明，在整个药物释放过程中以及在临床相关的皮肤应用时间内，制剂中都存在阳离子囊泡。因此，皮肤渗透速率的降低源于药物从凝胶中释放的时间延长。流变学研究表明，即使原料药被释放，凝胶体积减小，物理交联凝胶的凝胶结构仍保持不变。这些发现表明，像这样的公式的适用性是未来的可能性。(C) 2011 Elsevier B.V.版权所有
To fully utilize the extended contact time of gel formulations a novel formulation with drug containing catanionic aggregates offering prolonged drug release and skin penetration were investigated. This study aimed to further explore the drug release process from catanionic vesicles in gels.Catanionic vesicles were formed from alprenolol and sodium dodecyl sulphate. Physical gels composed of catanionic vesicles and a SoftCAT polymer were used as well as covalent Carbopol gels. Drug release was measured in vitro using a modified USP paddle method and the skin penetration was studied using dermatomized pig ear skin mounted in horizontal Ussing chambers.The aggregate structure was visualized with cryo-TEM during the drug release and skin penetration process. The study results show that catanionic vesicles are present in the formulations throughout the drug release process and during the clinically relevant skin application time. Hence, the decreased skin penetration rate stems from the prolonged release of drug substance from the gels. The rheological investigation shows that the gel structure of the physically cross-linked gels is maintained even as the drug substance is released and the gel volume is decreased. These findings indicate that the applicability of formulations like these is a future possibility. (C) 2011 Elsevier B.V. All rights reserved.