Abstract Acne vulgaris is the most common dermatological disorder affecting millions of individuals. Acne therapeutic solutions include topical treatment with retinoic acid (RA) which showed a good efficacy in treatment of mild and moderate cases. However, the high prevalence of adverse events, such as skin dryness, shedding and skin irritation affects the patient convenience and obstruct the acne treatment. Thus, the objective of this paper was to produce Span 60 based elastic vesicles enriched with penetration enhancers, and study their influence on the delivery of RA and its skin irritation. RA-loaded nanovesicles, enriched with Transcutol®/Labrasol®, were made using the thin film hydration technique, and assessed for entrapment efficiency, particle size and zeta potential. The optimized RA-loaded nanovesicles (composed of Span 60-Tween 20, and Transcutol®) were morphologically assessed via transmission electron microscopy. Moreover, RA deposition into newborn mice skin was assessed in vitro under non-occlusive conditions, where the optimized RA-loaded nanovesicles showed 2-fold higher RA deposition in the skin compared to the corresponding one lacking Transcutol. The optimized RA-loaded nanovesicles incorporated into 1% carbopol gel was evaluated for in-vivo clinical performance in acne patients, and showed appreciable advantages over the marketed formulation (Acretin®) in the treatment of acne regarding skin tolerability and patient’s compliance.

中文翻译：

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增强视黄酸弹性材料的皮肤靶向性：痤疮患者的体外表征和临床评估。

摘要 寻常痤疮是影响数百万人的最常见的皮肤病。痤疮治疗方案包括使用视黄酸 (RA) 进行局部治疗，在治疗轻度和中度病例方面显示出良好的疗效。然而，皮肤干燥、脱落和皮肤刺激等不良事件发生率高，影响了患者的便利性，阻碍了痤疮的治疗。因此，本文的目的是生产富含渗透促进剂的基于 Span 60 的弹性囊泡，并研究它们对 RA 传递及其皮肤刺激的影响。负载 RA 的纳米囊泡富含 Transcutol®/Labrasol®，使用薄膜水合技术制备，并评估包埋效率、粒径和 zeta 电位。优化的 RA 负载纳米囊泡（由 Span 60-Tween 20 组成，和 Transcutol®) 通过透射电子显微镜进行形态学评估。此外，在非闭塞条件下体外评估新生小鼠皮肤中的 RA 沉积，其中优化的 RA 负载纳米囊泡在皮肤中的 RA 沉积比缺乏 Transcutol 的相应纳米囊泡高 2 倍。将优化的 RA 负载纳米囊泡掺入 1% carbopol 凝胶中，评估了痤疮患者的体内临床性能，并在皮肤耐受性和患者依从性方面显示出优于市售制剂 (Acretin®) 在治疗痤疮方面的明显优势。其中优化的 RA 负载纳米囊泡在皮肤中的 RA 沉积比相应的缺乏 Transcutol 的纳米囊泡高 2 倍。将优化的 RA 负载纳米囊泡掺入 1% carbopol 凝胶中，评估了痤疮患者的体内临床性能，并在皮肤耐受性和患者依从性方面显示出优于市售制剂 (Acretin®) 在治疗痤疮方面的明显优势。其中优化的 RA 负载纳米囊泡在皮肤中的 RA 沉积比相应的缺乏 Transcutol 的纳米囊泡高 2 倍。将优化的 RA 负载纳米囊泡掺入 1% carbopol 凝胶中，评估了痤疮患者的体内临床性能，并在皮肤耐受性和患者依从性方面显示出优于市售制剂 (Acretin®) 在治疗痤疮方面的明显优势。