Department of Pharmaceutical Sciences, Ibn Sina National College of Medical Studies, Jeddah 21418, Saudi Arabia.
Department of Basic Sciences, Ibn Sina National College of Medical Studies, Jeddah 21418, Saudi Arabia.
J Adv Res. 2016 May;7(3):453-61. doi: 10.1016/j.jare.2016.03.003. Epub 2016 Mar 15.
The present study investigates the entrapment of terbinafine hydrochloride (TH) in ethosomal vesicles via unsonicated and sonication method. Carbopol 934P was incorporated in the best formulation, F6, obtained by sonication method. The formulated ethosomal gel obtained as such i.e. F6(∗) was exploited to achieve a zero order release profile of TH. The composition includes phospholipid, ethanol and propylene glycol. Drug entrapment efficiency (DEE), in-vitro and ex-vivo drug diffusion studies, FT-IR and stability studies of the prepared ethosomes were investigated. The size and shape of F6 ethosomes vesicles were characterized by SEM. In-vitro drug release studies were performed using sigma dialysis membrane in phosphate buffer, pH 7.4 for 12 h while drug content was determined by HPLC. DEE was ranked from 55.33 ± 1.32% to 69.11 ± 2.11%. Highest DEE was seen with F6 ethosomal formulation with a vesicle size of 248 ± 1.02 nm. FT-IR studies confirmed that there was no chemical interaction between drug and excipients used in the formulation. Ex-vivo result suggested that drug diffusion observed after 12 h from F6(∗) and marketed cream (MR) formulations was 74.01 ± 0.62% and 61.45 ± 0.86%, respectively. The results of similarity factor (f 2 values) for MR and F6(∗) ethosomal gel were 85.14 and 42.63, respectively. It revealed that F6(∗) showed dissimilar dissolution profiles. Transdermal flux value for F6(∗) and MR was found to be 144.61 ± 1.28 μg/cm(2)/h and 121.6 ± 1.16 μg/cm(2)/h, respectively. This study disclosed that F6(∗) resides at targeted site for a relatively longer period of time thereby signifying the improved patient compliance.
本研究通过非超声和超声法考察了盐酸特比萘芬（TH）在醇质体囊泡中的包封。将 Carbopol 934P 掺入通过超声法获得的最佳配方 F6 中。如此获得的配制醇质体凝胶，即 F6（∗），用于实现 TH 的零级释放曲线。该组合物包含磷脂、乙醇和丙二醇。考察了所制备的醇质体的药物包封效率（DEE）、体外和离体药物扩散研究、傅里叶变换红外光谱（FT-IR）和稳定性研究。通过 SEM 对 F6 醇质体囊泡的大小和形状进行了表征。在磷酸盐缓冲液，pH7.4 中进行了 12 小时的体外药物释放研究，同时通过 HPLC 测定了药物含量。DEE 的范围为 55.33±1.32%至 69.11±2.11%。F6 醇质体制剂的 DEE 最高，其囊泡大小为 248±1.02nm。FT-IR 研究证实药物与制剂中使用的赋形剂之间没有化学相互作用。离体结果表明，F6（∗）和市售乳膏（MR）制剂在 12 小时后观察到的药物扩散分别为 74.01±0.62%和 61.45±0.86%。MR 和 F6（∗）醇质体凝胶的相似因子（f 2 值）分别为 85.14 和 42.63，表明 F6（∗）显示出不同的溶出曲线。F6（∗）和 MR 的透皮通量值分别为 144.61±1.28μg/cm(2)/h 和 121.6±1.16μg/cm(2)/h。本研究表明，F6（∗）在靶向部位停留时间相对较长，从而提高了患者的依从性。
