A New Approach for Characterizing the Thixotropic Properties of Gel Formulations as Sprayable Agents Based on Rheological Analysis
A New Approach for Characterizing the Thixotropic Properties of Gel Formulations as Sprayable Agents Based on Rheological Analysis
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DOI：
10.1208/s12249-022-02276-y
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发表时间：
2022-04
影响因子：
3.3
通讯作者：
T. Terukina;Yoshiki Uchiyama;Fumiya Kikuma;Saki Fukumitsu;Nana Iwata;T. Kanazawa;H. Kondo
中科院分区：
文献类型：
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作者：
T. Terukina;Yoshiki Uchiyama;Fumiya Kikuma;Saki Fukumitsu;Nana Iwata;T. Kanazawa;H. Kondo
本研究评价了由触变肽两亲物、棕榈酰甘氨酸组氨酸（Pal-GH）和增稠剂、藻酸丙二醇酯（PGA）组成的凝胶制剂的流变学性质，以提出一种适当的方法来设计具有良好喷雾性能和高治疗剂保留率的可喷雾凝胶制剂。滞后环面积（HLA）是一种常规触变性指标，根据含有不同量Pal-GH和PGA的各种配方的剪切应力和剪切速率之间的关系来确定。此外，一种新的评估方法，用于表征的触变性使用的初始结构恢复速度的基础上的时间过程的复杂的模量（G*）的凝胶制剂的结构分解后确定。G* 值随着Pal-GH和PGA的量的增加而增加，表明制剂是不可变形的。此外，当选择具有良好的喷涂性能和高保持力的制剂时，高HLA和高初始结构恢复速度是优选的。由于Pal-GH和PGA的合适组合可以表现出高HLA和高初始结构恢复速度，因此它们是用作具有良好喷雾性能和高保留的可喷雾剂的凝胶制剂的有希望的组分。结果还表明，初始结构恢复速度比HLA更能反映配方的触变性。因此，初始结构恢复速度可以是用于制备可喷雾凝胶制剂的有用尺度。
The present study evaluated the rheological properties of gel formulations composed of the thixotropic peptide amphiphile, palmitoyl-glycine-histidine (Pal-GH), and the thickener, propylene glycol alginate (PGA), to propose a proper approach to design sprayable gel formulations with good spray performance and high retention of a therapeutic agent. The hysteresis loop area (HLA), a conventional index of thixotropy, was determined from the relationship between the shear stress and shear rate of various formulations with different amounts of Pal-GH and PGA. In addition, a new assessment method for characterizing the thixotropy using the initial structure recovery speed was determined based on the time course of the complex modulus (G*) after structural breakdown of the gel formulations. The G* values increased with the increase in the amount of Pal-GH and PGA, indicating that the formulations were not deformable. Additionally, high HLA and high initial structure recovery speed are preferable when selecting a formulation with good spray performance and high retention. As suitable combinations of Pal-GH and PGA could exhibit both high HLA and high initial structure recovery speed, they are promising components for gel formulations to be used as sprayable agents with good spray performance and high retention. The results also suggested that the initial structure recovery speed would reflect the thixotropy for the formulation more appropriately than HLA. Thus, the initial structure recovery speed could be a useful scale for the preparation of sprayable gel formulations.