Soluplus solutions as thermothickening materials for topical drug delivery
Soluplus solutions as thermothickening materials for topical drug delivery
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DOI：
10.1002/app.46915
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发表时间：
2019-01-05
影响因子：
3
通讯作者：
Cook, M. T.
中科院分区：
文献类型：
--
作者：
Salah, I.;Abou Shamat, M.;Cook, M. T.
Soluplus是一种主要用于生产固体分散体的药用辅料。该聚合物在水溶液中也表现出令人感兴趣的流变性，随着溶液升温，粘度增加。这种材料可以应用于局部药物递送到包括皮肤、阴道、直肠或鼻粘膜的部位，其中粘度的增加允许改善的保留。然而，存在非常少的信息围绕这个“热增稠”现象和溶液组成对温度依赖性流变学的影响。在这项研究中，soluplus浓度，盐的夹杂物，乙醇添加，和pH值对温度依赖性流变学的影响进行了测量。溶液的流变性在皮肤耐受的范围内（pH 4-7）不受pH影响，但包含乙醇迅速否定了热增稠效应。溶液的“盐析”导致凝胶化温度的降低，以及溶液的储存模量和损耗模量的增加。在1 M NaCl或KCl中的30%（w/v）soluplus被鉴定为用于局部药物递送的潜在热增稠剂。(c)2018 Wiley Periodicals，Inc. J.应用聚合物Sci. 2019，136，46915。
Soluplus is a pharmaceutical excipient used primarily in the manufacture of solid dispersions. The polymer also exhibits interesting rheology in aqueous solution, increasing in viscosity as the solution is warmed. This material could have application topical drug delivery to sites including the skin, vagina, rectum or nasal mucosa, where the increase in viscosity allows for improved retention. However, there exists very little information surrounding this "thermothickening" phenomenon and the effect of solution composition on temperature-dependent rheology. In this study, the effect of soluplus concentration, salt inclusion, ethanol addition, and pH on temperature-dependent rheology was measured. The rheology of the solutions was unaffected by pH over the range tolerated by the skin (pH 4-7), but the inclusion of ethanol rapidly negated the thermothickening effect. "Salting out" of the solutions resulted in a depression of gelation temperatures, and an increase in both storage and loss moduli of the solutions. 30% (w/v) soluplus in 1 M NaCl or KCl was identified as a potential thermothickening agent for topical drug delivery. (c) 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019, 136, 46915.