Altay Benetti Ayça, Thwin Ma Thinzar, Suhaimi Ahmad, Liang Ryan Sia Tze, Ng Lisa Fong-Poh, Lum Fok-Moon, Benetti Camillo
Department of Pharmacy and Pharmaceutical Sciences, National University of Singapore, Singapore 117544, Singapore.
A*STAR Infectious Diseases Labs (A*STAR ID Labs), Agency for Science, Technology and Research (A*STAR), Singapore 138648, Singapore.
Pharmaceutics. 2024 Jul 26;16(8):994. doi: 10.3390/pharmaceutics16080994.
Given the increasing aging population and the rising prevalence of musculoskeletal diseases due to obesity and injury, urgent research is needed to formulate new treatment alternatives, as current options remain inadequate. Viruses can exacerbate arthritis and worsen symptoms in patients with pre-existing osteoarthritis. Over the past decade, the chikungunya virus (CHIKV) has emerged as a significant public health concern, especially in Asia and South America. Exploring natural products, such as berberine, has shown promise due to its anticatabolic, antioxidative, and anti-inflammatory effects. However, berberine's low stability and bioavailability limit its efficacy. We hypothesized that encapsulating berberine into a proniosome gel, known for its ease of preparation and stability, could enhance its bioavailability and efficacy when applied topically, potentially treating CHIKV infection. Our investigation focused on how varying berberine loads and selected excipients in the proniosome gel influenced its physical properties, stability, and skin permeability. We also examined the biological half-life of berberine in plasma upon topical administration in mice to assess the potential for controlled and sustained drug release. Additionally, we analyzed the antioxidant stress activity and cell viability of HaCaT keratinocytes and developed a lipopolysaccharide-stimulated cell culture model to evaluate anti-inflammatory effects using pro-inflammatory cytokines. Overall, the research aims to transform the treatment landscape for arthritis by leveraging berberine's therapeutic potential.
鉴于人口老龄化加剧以及肥胖和损伤导致肌肉骨骼疾病的患病率不断上升,由于目前的治疗选择仍然不足,迫切需要开展研究以制定新的治疗方案。病毒会加重关节炎,并使已有骨关节炎患者的症状恶化。在过去十年中,基孔肯雅病毒(CHIKV)已成为一个重大的公共卫生问题,尤其是在亚洲和南美洲。探索天然产物,如黄连素,因其具有抗分解代谢、抗氧化和抗炎作用而显示出前景。然而,黄连素的低稳定性和生物利用度限制了其疗效。我们假设将黄连素封装到以易于制备和稳定性著称的前体脂质体凝胶中,局部应用时可提高其生物利用度和疗效,有可能治疗基孔肯雅病毒感染。我们的研究重点是前体脂质体凝胶中不同的黄连素负载量和选定的辅料如何影响其物理性质、稳定性和皮肤渗透性。我们还研究了小鼠局部给药后黄连素在血浆中的生物半衰期,以评估药物控释和持续释放的潜力。此外,我们分析了HaCaT角质形成细胞的抗氧化应激活性和细胞活力,并建立了脂多糖刺激的细胞培养模型,以使用促炎细胞因子评估抗炎作用。总体而言,该研究旨在利用黄连素的治疗潜力改变关节炎的治疗格局。