Department of Herbal Nanotechnology, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), 751003, Bhubaneswar, Odisha, India.
Department of Medicine, Pandit Raghunath Murmu Medical College, and Hospital, Baripada, Odisha, India.
AAPS PharmSciTech. 2024 Mar 12;25(3):57. doi: 10.1208/s12249-024-02774-1.
Psoriasis is a complex and persistent autoimmune skin disease. The present research focused on the therapeutic evaluation of betulin-loaded nanostructured lipid carriers (BE-NLCs) towards managing psoriasis. The BE-NLCs were synthesized using the emulsification cum solidification method, exhibiting a spherical shape with a particle size of 183.5±1.82nm and a narrow size distribution window (PDI: 0.142±0.05). A high zeta potential -38.64±0.05mV signifies the relative stability of the nano-dispersion system. BE-NLCs show a drug loading and entrapment efficiency of 47.35±3.25% and 87.8±7.86%, respectively. In vitro release study, BE NLCs show a cumulative percentage release of 90.667±5.507% over BE-sol (57.334±5.03%) and BD-oint (42±4.58%) for 720min. In an ex vivo 24-h permeation study, % cumulative amount permeated per cm was found to be 55.667±3.33% from BE-NLCs and 32.012±3.26% from BE-sol, demonstrating a better permeability of 21.66% when compared to the standard formulation BD-oint. The in vivo anti-psoriatic activity in the IMQ-induced model shows topical application of BE-sol, BE-NLCs, and BD-oint resulted in recovery rates of 56%, 82%, and 65%, respectively, based on PASI (Psoriasis Area and Severity Index) score. Notably, BE-NLCs demonstrated a more significant reduction in spleen mass, indicating attenuation of the local innate immune system in psoriatic mice. Reductions in TNF-α, IL-6, and IL-17 levels were observed in both BE-sol and BE-NLCs groups compared to the disease control (DC) group, with BE-NLCs exhibiting superior outcomes (74.05%, 44.76%, and 49.26% reduction, respectively). Soy lecithin and squalene-based NLCs could be better carrier system for the improvement of the therapeutic potential of BE towards management of psoriasis.
银屑病是一种复杂且持久的自身免疫性皮肤病。本研究专注于评估桦木醇负载的纳米结构化脂质载体(BE-NLCs)在治疗银屑病方面的疗效。BE-NLCs 是通过乳化固化法合成的,呈现出球形,粒径为 183.5±1.82nm,粒径分布窗口较窄(PDI:0.142±0.05)。高的 ζ 电位-38.64±0.05mV 表明纳米分散体系具有相对稳定性。BE-NLCs 的药物载药量和包封效率分别为 47.35±3.25%和 87.8±7.86%。体外释放研究表明,在 720min 内,BE-NLCs 的累积释放百分比为 90.667±5.507%,而 BE-sol(57.334±5.03%)和 BD-oint(42±4.58%)的累积释放百分比分别为 90.667±5.507%。在 24 小时离体渗透研究中,发现从 BE-NLCs 中渗透的累积量为 55.667±3.33%,从 BE-sol 中渗透的累积量为 32.012±3.26%,与标准制剂 BD-oint 相比,渗透能力提高了 21.66%。在咪喹莫特诱导的模型中,体内抗银屑病活性研究表明,在基于 PASI(银屑病面积和严重程度指数)评分的情况下,局部应用 BE-sol、BE-NLCs 和 BD-oint 后,恢复率分别为 56%、82%和 65%。值得注意的是,与疾病对照组相比,BE-NLCs 组的脾脏质量显著降低,表明其对银屑病小鼠局部固有免疫系统的抑制作用更强。与疾病对照组相比,BE-sol 和 BE-NLCs 组的 TNF-α、IL-6 和 IL-17 水平均有所降低,其中 BE-NLCs 组的降低更为显著(分别降低 74.05%、44.76%和 49.26%)。基于大豆卵磷脂和角鲨烯的 NLCs 可能是提高桦木醇治疗银屑病疗效的更好载体系统。