Gaafar Passent M E, Abbas Haidy, Aboukilila HussamElDin Y, Kamal Miranda F, Zewail Mariam
Department of Pharmaceutics, Division of Pharmaceutical Sciences, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, P.O. Box 1029, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy University, Damanhour University 22511, Egypt.
Int J Pharm. 2025 Aug 20;681:125895. doi: 10.1016/j.ijpharm.2025.125895. Epub 2025 Jun 24.
Skin photoaging induced by ultraviolet B (UVB) radiation involves oxidative stress, inflammation, and extracellular matrix degradation. L-Carnosine (CAR) possesses potent anti-inflammatory, antioxidant, and anti-wrinkling characteristics, but its topical delivery is limited by poor skin penetration. Development and evaluation of CAR-loaded hya-ascorposomes (CAR-HA-ASP) for enhanced efficacy against UVB-induced photoaging was the main aim of the study. CAR-HA-ASP were prepared using the phospholipid hydration method. The optimized formulation exhibited favorable colloidal properties: a particle size of 192.6 ± 0.56 nm, a negative zeta potential of -16 ± 1.34 mV confirming HA coating, and a high encapsulation efficiency of 85.23 ± 1.89 %. TEM micrographs revealed spherical vesicles with a distinct HA layer. A sustained drug release over 24 h was observed. Ex vivo permeation study revealed that CAR-HA-ASP could significantly enhance CAR flux and permeation coefficient compared with CAR gel. In a rat model of UVB-induced photoaging, topical application of CAR-HA-ASP (0.2 % CAR) significantly reduced skin damage compared to untreated UVB-irradiated and the conventional CAR gel group. Biochemical analysis showed CAR-HA-ASP treatment significantly increased skin superoxide dismutase levels (62.35 ± 1.09 U/g tissue) compared to the positive control (12.3 ± 0.87 U/g) and CAR gel (32.4 ± 1.09 U/g). Furthermore, levels of interleukin-6 and matrix metalloproteinase-9 in the CAR-HA-ASP group were comparable to the negative control group. Histopathological examination revealed normal epidermal and dermal structures in the CAR-HA-ASP-treated group.These results demonstrate that CAR-HA-ASP effectively delivers CAR into the skin, providing enhanced protection against UVB-induced photoaging, highlighting its potential as a novel advanced topical anti-aging formulation.
紫外线B(UVB)辐射引起的皮肤光老化涉及氧化应激、炎症和细胞外基质降解。L-肌肽(CAR)具有强大的抗炎、抗氧化和抗皱特性,但其局部给药受皮肤渗透性差的限制。本研究的主要目的是开发和评估负载CAR的透明质酸抗坏血酸脂质体(CAR-HA-ASP),以增强其对UVB诱导的光老化的疗效。采用磷脂水化法制备CAR-HA-ASP。优化后的制剂表现出良好的胶体性质:粒径为192.6±0.56nm,ζ电位为-16±1.34mV,证实有HA包衣,包封率高达85.23±1.89%。透射电子显微镜照片显示为具有明显HA层的球形囊泡。观察到药物在24小时内持续释放。体外渗透研究表明,与CAR凝胶相比,CAR-HA-ASP可显著提高CAR通量和渗透系数。在UVB诱导的光老化大鼠模型中,局部应用CAR-HA-ASP(0.2%CAR)与未处理的UVB照射组和传统CAR凝胶组相比,显著减少了皮肤损伤。生化分析表明,与阳性对照组(12.3±0.87U/g组织)和CAR凝胶组(32.4±1.09U/g)相比,CAR-HA-ASP处理显著提高了皮肤超氧化物歧化酶水平(62.35±1.09U/g组织)。此外,CAR-HA-ASP组白细胞介素-6和基质金属蛋白酶-9的水平与阴性对照组相当。组织病理学检查显示,CAR-HA-ASP处理组的表皮和真皮结构正常。这些结果表明,CAR-HA-ASP能有效地将CAR递送至皮肤,增强对UVB诱导的光老化的保护作用,突出了其作为一种新型先进局部抗老化制剂的潜力。