a College of Pharmacy and Pharmaceutical Sciences , The University of Toledo Health Science Campus, The University of Toledo , Toledo , OH , USA.
b Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , Ajman University , Ajman , UAE.
Pharm Dev Technol. 2019 Jul;24(6):689-699. doi: 10.1080/10837450.2019.1578371. Epub 2019 Apr 26.
The purpose of this work was to design and characterize a topical formulation of econazole nitrate (EN) with potential for treating Raynaud's phenomenon (RP). Four topical dosage forms (F1_topical solution, F2_HPMC or hydroxypropyl methylcellulose dispersion, F3_VersaBase cream, and F4Lipoderm Activemax™ Cream) containing 3% w/w EN were prepared and characterized for drug content, pH, viscosity, spreadability, drug crystallinity, stability, and in vitro permeation using Franz cells across pig ear skin, and results were compared to the 1% marketed EN cream. All four formulations had acceptable physical and visual characteristics required for topical application, with 3% w/w EN. The order of amount of drug permeated from highest to lowest was F2 (10.27%) > F4 (2.47%) > F1 (2.28%) > F3 (1.47%) > marketed formulation (0.22%). Formulation F2 showed better penetration of the drug into the stratum corneum, epidermis, and dermis layers. The drug concentration in the stratum corneum and epidermis was approximately 10-20 times higher with F2 compared to the marketed formulation. All formulations were found to be stable for up to 6 months. All four EN formulations were found to be better than the 1% marketed cream. Formulation F2HPMC dispersion could be further explored as a treatment option for RP.
本工作旨在设计和表征硝酸益康唑（EN）的局部制剂，以期治疗雷诺现象（RP）。制备并表征了四种含有 3%w/wEN 的局部剂型（F1_局部溶液、F2_HPMC 或羟丙基甲基纤维素分散体、F3_VersaBase 乳膏和 F4Lipoderm Activemax™乳膏），用于药物含量、pH 值、粘度、铺展性、药物结晶度、稳定性以及通过Franz 细胞体外渗透进行评价猪耳朵皮肤，并将结果与 1%市售 EN 乳膏进行比较。所有四种制剂均具有可接受的物理和视觉特征，适用于局部应用，其中含有 3%w/wEN。从最高到最低的药物渗透量依次为 F2（10.27%）>F4（2.47%）>F1（2.28%）>F3（1.47%）>市售制剂（0.22%）。制剂 F2 显示出药物向角质层、表皮和真皮层更好的渗透。与市售制剂相比，F2 中药物在角质层和表皮中的浓度约高 10-20 倍。所有制剂在长达 6 个月的时间内均稳定。所有四种 EN 制剂均优于 1%市售乳膏。F2HPMC 分散体可以进一步探索作为 RP 的治疗选择。
