Gennari Chiara G M, Casiraghi Antonella, Selmin Francesca, Cilurzo Francesco
Department of Pharmaceutical Sciences, Università degli Studi di Milano, via G: Colombo, 71, 20133 Milano, Italy.
Pharmaceutics. 2025 Jan 11;17(1):88. doi: 10.3390/pharmaceutics17010088.
BACKGROUND/OBJECTIVES: The objective of this paper is to design a novel film-forming system (FFS) based on Eudragit E PO (EuE) polymeric solutions, differing in volatile solvents (i.e., isopropanol and ethanol) and plasticizers (i.e., tributylcitrate, glycerine, triacetin and PEG 400).
The physicochemical and mechanical properties of the FFS and dried films were evaluated in terms of formation time, stickiness, T, tensile strength, break elongation and Young's modulus. The in vitro skin permeation studies were conducted on formulations containing caffeine and testosterone.
The FFS, consisting of EuE and PEG400 in isopropyl alcohol and ethanol (80:20, /), exhibited rapid film formation within about 5 min and the dried film allowed a high skin permeability compared to other formulations due to the ability to increase the thermodynamic activity of both drugs. When triiodothyronine (T3) was loaded as a model of a very low soluble drug, tocopherol polyethylene glycol succinate (TPGS) was added as a co-solvent and it allowed for the improvement of T3 retention in the skin.
Among the formulative variables, the nature and the amount of plasticizer represent the most critical variables to obtain an EuE-based film with satisfying physical and biopharmaceutical properties.
背景/目的：本文的目的是设计一种基于尤特奇E PO（EuE）聚合物溶液的新型成膜系统（FFS），该系统在挥发性溶剂（即异丙醇和乙醇）和增塑剂（即柠檬酸三丁酯、甘油、三醋精和聚乙二醇400）方面有所不同。
根据形成时间、粘性、T、拉伸强度、断裂伸长率和杨氏模量评估FFS和干膜的物理化学和机械性能。对含有咖啡因和睾酮的制剂进行体外皮肤渗透研究。
由EuE和聚乙二醇400在异丙醇和乙醇（80:20，/）中组成的FFS在约5分钟内表现出快速成膜，并且与其他制剂相比，干膜由于能够增加两种药物的热力学活性而具有较高的皮肤渗透性。当将三碘甲状腺原氨酸（T3）作为极低溶性药物的模型负载时，添加生育酚聚乙二醇琥珀酸酯（TPGS）作为助溶剂，它可以提高T3在皮肤中的保留率。
在配方变量中，增塑剂的性质和用量是获得具有令人满意的物理和生物药剂学性质的基于EuE的薄膜的最关键变量。
