Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Pharmaceutical Sciences Research Centre, Haemoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran.
J Biomater Sci Polym Ed. 2022 Dec;33(18):2325-2352. doi: 10.1080/09205063.2022.2103626. Epub 2022 Jul 25.
Terbinafine (TER) is a promising candidate medication for the topical treatment of fungal infections. However, its solubility in water and skin permeability are limited. To overcome these limitations, a Terbinafine niosome and niosomal gel was developed. The impact of cholesterol:surfactants on terbinafine incorporated niosome (terbinasome) preparations was examined. Differential scanning calorimetry (DSC), photon correlation spectroscopy (PCS), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy were used to assess the morphological features of terbinasome and the physicochemical characteristics of TER in terbinasome. The obtained results has shown that Chol enhanced the diameter of the terbinasome from 123.20 ± 2.86 to 701.93 ± 17.72 nm. The highest encapsulation of terbinafine was estimated to be around 66% due to the cholesterol:surfactants ratio in the terbinasome was 1:3 and 1:6. Additional examination has revealed that changes in the cholesterol:surfactants ratio can result in a change in the PDI value of between 0.421 ± 0.004 and 0.712 ± 0.011. The terbinasome gel was prepared and tested for pharmaceutical testing, including pH, viscosity, spreadability, and stability. The percentage of TER dissolution from terbinasome were determined more than 80% and showed quickest drug release. In a cutaneous permeability examination, the quantity of TER in the cutaneous layers and the receiver compartment were higher for the terbinasome gel than for the TER simple gel. The terbinasome's cell viability was around 90% (HFF cell line) and MTT experiment demonstrated that the terbinasome was not cytotoxic. The MIC of the terbinasome was lower than pure drug against , and . The terbinasomal gels were non-irritant (score < 2) in the cutaneous irritation examination performed on Wistar rats. The research suggests that the optimized terbinasome may be used as a nano-vesicle for TER drug administration, hence opening up new possibilities for the treatment of cutaneous infections.
特比萘芬（TER）是一种有前途的候选药物，可用于局部治疗真菌感染。然而，其在水中的溶解度和皮肤渗透性有限。为了克服这些限制，开发了特比萘芬的脂囊和脂囊凝胶。研究了胆固醇：表面活性剂对含有特比萘芬的脂囊（terbinasome）制剂的影响。差示扫描量热法（DSC）、光子相关光谱法（PCS）、扫描电子显微镜（SEM）和衰减全反射-傅里叶变换红外光谱（ATR-FTIR）光谱用于评估terbinasome 的形态特征和 terbinasome 中特比萘芬的物理化学性质。结果表明，胆固醇使脂囊的直径从 123.20±2.86nm 增加到 701.93±17.72nm。由于胆固醇：表面活性剂在 terbinasome 中的比例为 1:3 和 1:6，因此估计特比萘芬的最高包封率约为 66%。进一步的研究表明，胆固醇：表面活性剂的比例变化会导致 PDI 值在 0.421±0.004 和 0.712±0.011 之间变化。制备了 terbinasome 凝胶并进行了药物测试，包括 pH 值、粘度、铺展性和稳定性。从 terbinasome 中测定的特比萘芬的溶解百分比超过 80%，显示出最快的药物释放。在皮肤渗透性研究中，terbinasome 凝胶在皮肤层和接受室中的特比萘芬含量高于特比萘芬简单凝胶。terbinasome 的细胞活力约为 90%（HFF 细胞系），MTT 实验表明 terbinasome 无细胞毒性。与对照相比，terbinasome 的 MIC 值低于纯药物，对，和。在 Wistar 大鼠进行的皮肤刺激性研究中，terbinasomal 凝胶无刺激性（评分<2）。研究表明，优化后的 terbinasome 可作为特比萘芬药物输送的纳米囊泡，为皮肤感染的治疗开辟了新的可能性。
