Abstract In our study, the potential of bilosomes as novel vesicular carrier for the cutaneous delivery of the sulphone compound, Dapsone, for topical treatment of acne was investigated. The effect of different formulation variables (type and concentration of bile salt, and molar ratio of Span 60:cholesterol) on the properties of DPS-loaded bilosomes was investigated using a full factorial design. Design Expert software was used for data analysis and optimization of DPS-loaded bilosomes. The optimized bilosomes, chosen on the basis of their superior properties giving maximum entrapment, in vitro release after different time intervals and RE% with minimum vesicle size. Results showed that the bilosome system prepared using Span® 60: Cholesterol (5:1) and containing 0.25 M sodium deoxycholate as the bile salt was found to obey these criteria, with a desirability value of 0.637. Therefore, this system was chosen for further assessment for its morphological properties, zeta potential, thermal analysis using differential scanning calorimetry and X-ray diffractometry. Results revealed that the chosen bilosomes were spherical in shape with no aggregation, and contained DPS in a molecularly dispersed amorphous form. Finally, the capability of the optimized DPS-loaded bilosomes to deliver DPS through rat skin layers will be investigated and compared with that of DPS alcoholic solution. Results showed that the amounts of DPS retained in the skin treated with DPS-loaded bilosomes, and DPS alcoholic solution after 24 h were found to be 170.57 ± 55.12 and 120.24 ± 10.7 µg/mL, respectively, representing about 1.5-fold higher drug retained in the bilosomes-treated skin. Finally, the safety and the tolerability of the prepared bilosomes were assessed using histopathological examination, and revealed that the control untreated skin sections and skin sections treated with DPS-loaded bilosomes showed normal histological structures characterized by absence of defects or inflammation. Such results can be considered a good addition in the field of pharmaceutical drug delivery for effective topical therapy of acne.

中文翻译：

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Bilosomes 作为一种新型载体，用于氨苯砜的皮肤递送，作为痤疮的潜在治疗方法：制备、表征和体内皮肤沉积测定

摘要 在我们的研究中，研究了胆囊体作为新型囊泡载体的潜力，用于皮肤递送砜化合物氨苯砜，用于局部治疗痤疮。使用全因子设计研究了不同配方变量（胆汁盐的类型和浓度，以及 Span 60: 胆固醇的摩尔比）对加载 DPS 的胆囊体特性的影响。Design Expert 软件用于对加载 DPS 的双糖体进行数据分析和优化。优化的胆囊体，根据其优异的特性进行选择，可提供最大的截留率、不同时间间隔后的体外释放和最小囊泡尺寸的 RE%。结果表明，发现使用 Span® 60: 胆固醇 (5:1) 制备并含有 0.25 M 脱氧胆酸钠作为胆汁盐的胆体系统符合这些标准，合意性值为 0.637。因此，该系统被选择用于进一步评估其形态特性、zeta 电位、使用差示扫描量热法和 X 射线衍射法的热分析。结果表明，所选择的胆汁体是球形的，没有聚集，并且含有分子分散的无定形形式的 DPS。最后，将研究优化的 DPS 负载胆囊体通过大鼠皮肤层递送 DPS 的能力，并与 DPS 酒精溶液进行比较。结果表明，用负载 DPS 的胆囊体和 DPS 酒精溶液处理的皮肤中保留的 DPS 量在 24 小时后分别为 170.57 ± 55.12 和 120.24 ± 10.7 µg/mL，代表药物保留率高约 1.5 倍在双糖体处理的皮肤中。最后，使用组织病理学检查评估了制备的胆汁体的安全性和耐受性，结果表明对照未处理的皮肤切片和用负载 DPS 的胆汁体处理的皮肤切片显示正常的组织学结构，特征是没有缺陷或炎症。这样的结果可以被认为是有效局部治疗痤疮的药物递送领域的一个很好的补充。