School of Pharmacy, Queen's University of Belfast, Belfast, Antrim, Northern Ireland, United Kingdom.
School of Pharmacy, Queen's University of Belfast, Belfast, Antrim, Northern Ireland, United Kingdom.
Carbohydr Polym. 2021 Mar 15;256:117512. doi: 10.1016/j.carbpol.2020.117512. Epub 2020 Dec 15.
This study questioned whether rheological properties can predict drug (metronidazole) release from Hydroxypropylcellulose (HPC) platforms. Viscometric and viscoelastic properties of aqueous, alcohols/diols and mixed solvent HPC solutions and gels were determined using viscometry and oscillatory analysis. Drug release was conducted at pH 7.4 under sink conditions. Relationships between rheological parameters and drug release were modelled using multiple linear stepwise regression. Viscometry identified ethanol and water as good solvents for HPC. Diol solvents were predicted to exhibit greater interactions with HPC (COSMO modelling) but possessed lowest intrinsic viscosities. Pentanediol or ethylene glycol prepared gels exhibited greatest elasticity. No relationships were observed between dilute solution properties and initial gel viscoelasticity. Drug release from HPC gels occurred via gel erosion and diffusion. No relationships were observed between initial gel viscoelasticity and drug release and thus, for gel platforms that undergo erosion in aqueous media, drug release cannot be predicted from initial gel viscoelasticity.
本研究质疑流变性能是否可以预测羟丙纤维素（HPC）基质中药物（甲硝唑）的释放。使用粘度计和振荡分析测定了水相、醇/二醇和混合溶剂 HPC 溶液和凝胶的粘度和粘弹性。在溶出条件下，在 pH 7.4 下进行药物释放。使用多元逐步线性回归对流变参数与药物释放之间的关系进行建模。粘度计将乙醇和水鉴定为 HPC 的良溶剂。二醇溶剂预计与 HPC 具有更大的相互作用（COSMO 建模），但具有最低的固有粘度。戊二醇或乙二醇制备的凝胶表现出最大的弹性。在稀溶液性质和初始凝胶粘弹性之间未观察到关系。HPC 凝胶中的药物释放是通过凝胶侵蚀和扩散发生的。在初始凝胶粘弹性和药物释放之间未观察到关系，因此，对于在水性介质中经历侵蚀的凝胶平台，不能从初始凝胶粘弹性预测药物释放。
