New generation of amphiphilic vesicles known as aspasomes were investigated as potential carriers for transdermal delivery of tizanidine (TZN). Using full factorial design, an optimal formulation was developed by evaluating the effects of selected variables on the properties of the vesicles with regards to entrapment efficiency, vesicle size and cumulative percentage released. The optimal formula (TZN-AS 6) consisting of 20 mg TZN, 50 mg ascorbyl palmitate (AP), 50 mg cholesterol (CH) and 50 mg Span 60, represented well dispersed spherical vesicles in the nanorange sizes and exhibited excellent stability under different storage conditions. Ex-vivo permeation studies using excised rat skin showed a 4.4-fold increase of the steady state flux in comparison to the unformulated drug (p < 0.05). The pharmacokinetic parameters obtained from the in-vivo study using Wistar rats, showed that the bioavailability of TZN was enhanced significantly (p < 0.05) when compared to the oral market product of TZN, Sirdalud®. Moreover, skin irritancy tests confirmed that the vesicles were noninvasive and safe for the skin. Based on the results obtained, the optimized aspasomes formula represents a promising Nano platform for TZN to be administered transdermally, thus improving the therapeutic efficacy of this important muscle relaxant.

中文翻译：

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开发装载替扎尼定的 Aspasomes 作为透皮递送系统：体外和体内评估

被称为 aspasomes 的新一代两亲性囊泡被研究作为替扎尼定 (TZN) 透皮递送的潜在载体。使用全因子设计，通过评估所选变量对囊泡特性的影响，如包埋效率、囊泡大小和累积释放百分比，开发了最佳配方。由 20 mg TZN、50 mg 抗坏血酸棕榈酸酯 (AP)、50 mg 胆固醇 (CH) 和 50 mg Span 60 组成的最佳配方 (TZN-AS 6) 在纳米范围内表现出良好分散的球形囊泡，并在不同条件下表现出优异的稳定性。贮藏条件。使用离体大鼠皮肤进行的体外渗透研究表明，与未配制的药物相比，稳态通量增加了 4.4 倍（p < 0.05）。从使用 Wistar 大鼠进行的体内研究中获得的药代动力学参数表明，与 TZN 的口服市场产品 Sirdalud® 相比，TZN 的生物利用度显着提高（p < 0.05）。此外，皮肤刺激性测试证实，这些囊泡对皮肤无创且安全。基于获得的结果，优化的 aspasomes 配方代表了 TZN 经皮给药的有前途的纳米平台，从而提高了这种重要的肌肉松弛剂的治疗效果。