Department of Pharmaceutics & Pharmaceutical Technology, Faculty of Pharmacy, Pharos University in Alexandria, Alexandria, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Int J Pharm. 2022 Mar 5;615:121523. doi: 10.1016/j.ijpharm.2022.121523. Epub 2022 Jan 30.
Vitiligo is a depigmentation disorder that affects 0.5-2% of the world population. It has a severe impact on a patient's quality of life and even causes suicidal attempts. Up to date, no curative therapy is available which have created a substantial demand for novel vitiligo treatments. Berberine (BRB) is an isoquinoline alkaloid with promising pharmacological effects. However, it suffers from poor membrane permeability hindering its topical application. The current work is the first to design and assess topical BRB-loaded hyalurosomes for targeted vitiligo treatment. BRB-hyalurosomes are hyaluronan-immobilized phospholipid nanovesicles that showed promising invitro physicochemical properties. Novel ex vivo studies were performed using full-thickness human skin to mimic its dermal application. Furthermore, in-vivo studies were conducted using a vitiligo-induced mouse model followed by biochemical, histological and immunohistochemical investigations. In addition, gene expression of skin inflammatory markers was assessed using quantitative reverse-transcription PCR. Biological studies showed significant improvement of the biochemical markers in BRB-hyalurosomes group compared to the vitiligo-model group and BRB conventional gel. It is worthy to mention that placebo hyalurosomes demonstrated significant enhancement in the biological activity confirming its intrinsic activity. Conclusively, BRB-hyalurosomes is considered a novel nanodermatological tool that paving the way for its clinical application for vitiligo treatment.
白癜风是一种影响全球 0.5-2%人口的脱色素疾病。它严重影响患者的生活质量，甚至导致自杀企图。迄今为止，尚无有效的治疗方法，这就产生了对新型白癜风治疗方法的巨大需求。小檗碱（BRB）是一种具有良好药理作用的异喹啉生物碱。然而，它的细胞膜通透性差，限制了其在局部的应用。目前的工作是首次设计和评估用于靶向白癜风治疗的局部 BRB 载 hyalurosomes。BRB-hyalurosomes 是一种固定在透明质酸上的磷脂纳米囊泡，具有良好的体外理化性质。使用全厚人皮肤进行了新的离体研究，以模拟其在皮肤中的应用。此外，还使用白癜风诱导的小鼠模型进行了体内研究，随后进行了生化、组织学和免疫组织化学研究。此外，还使用定量逆转录聚合酶链反应评估了皮肤炎症标志物的基因表达。生物研究表明，与白癜风模型组和 BRB 常规凝胶组相比，BRB-hyalurosomes 组的生化标志物显著改善。值得一提的是，赋形剂透明质酸囊泡显示出显著增强的生物活性，证实了其内在活性。总之，BRB-hyalurosomes 被认为是一种新型的纳米皮肤病学工具，为其在白癜风治疗中的临床应用铺平了道路。
