用于银屑病治疗干预的卡兰金负载大豆卵磷脂基乙体纳米凝胶:配方开发、基于因子设计的优化、体外和体内评估。

Md Ali Mujtaba, Purushottam Gangane, Abuzer Ali, Shubham Chaudhari, Mohammed Kaleem, Sachin More, Naiyer Shahzad, Gamal Osman Elhassan, Md Khalid Anwer
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引用次数: 0

摘要

本研究旨在开发和优化卡兰金负载的乙糖体纳米凝胶配方,并评估其在咪喹莫特诱导的动物模型中缓解银屑病症状的疗效。配制这些卡兰金负载的乙糖体纳米凝胶是为了增强药物对皮肤的渗透和表皮的保留。卡兰金具有潜在的抗银屑病活性,因此被用来配制乙糖体。乙素体的配制采用冷冻法,使用 32 个全因子设计来优化配方成分。利用两个自变量 X1(乙醇浓度)和 X2(磷脂浓度)配制了 9 个批次的乙硫体,并选择囊泡大小(Y1)和夹带效率百分比(Y2)作为因变量。所有因变量均具有统计学意义。优化后的乙硫悬浮液(B3)的囊泡大小为 334±2.89 nm,包埋效率为 94.88 ± 1.24%,并显示出良好的稳定性。通过透射电子显微镜(TEM)分析,囊泡的形态呈球形,表面光滑。X 射线衍射(XRD)分析证实,药物在乙素体配方中以无定形状态存在。将优化后的乙素体与 carbopol 934 结合,开发出了易于在皮肤上使用的纳米凝胶。对纳米凝胶的各种参数进行了表征,包括铺展性、粘度、pH 值、挤出性和药物含量百分比。与市售制剂和纯药物相比,乙素体制剂显著增强了卡朗金的皮肤渗透性,并提高了药物在银屑病皮肤表皮的滞留率。皮肤保留研究表明,乙素体纳米凝胶制剂在 6 小时内的表皮保留率为 48.33%。在体内,卡兰金乙糖体纳米凝胶的抗银屑病活性明显改善了银屑病,这表现在皮肤厚度和鳞屑的逐渐减少上,这也反映在 PSI 分级上。因此,制备的乙糖体纳米凝胶是一种改进卡兰金局部给药的潜在载体,可以更好地治疗银屑病。
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Karanjin-loaded soya lecithin-based ethosomal nanogel for the therapeutic intervention of psoriasis: formulation development, factorial design based-optimization,in vitroandin vivoassessment.

This study aimed to develop and optimize karanjin-loaded ethosomal nanogel formulation and evaluate its efficacy in alleviating symptoms of psoriasis in an animal model induced by imiquimod. These karanjin-loaded ethosomal nanogel, were formulated to enhance drug penetration into the skin and its epidermal retention. Karanjin was taken to formulate ethosomes due to its potential ani-psoriatic activity. Ethosomes were formulated using the cold method using 32full factorial designs to optimize the formulation components. 9 batches were prepared using two independent variablesX1: concentration of ethanol andX2: concentration of phospholipid whereas vesicle size (Y1) and percentage entrapment efficiency (Y2) were selected as dependent variables. All the dependent variables were found to be statistically significant. The optimized ethosomal suspension (B3) exhibited a vesicle size of 334 ± 2.89 nm with an entrapment efficiency of 94.88 ± 1.24% and showed good stability. The morphology of vesicles appeared spherical with smooth surfaces through transmission electron microscopy analysis. X-ray diffraction analysis confirmed that the drug existed in an amorphous state within the ethosomal formulation. The optimized ethosome was incorporated into carbopol 934 to develop nanogel for easy application on the skin. The nanogel underwent characterization for various parameters including spreadability, viscosity, pH, extrudability, and percentage drug content. The ethosomal formulation remarkably enhanced the skin permeation of karanjin and increased epidermal retention of the drug in psoriatic skin compared to marketed preparation and pure drug. A skin retention study showed that ethosomal nanogel formulation has 48.33% epidermal retention in 6 h.In vivo,the anti-psoriatic activity of karanjin ethosomal nanogel demonstrated significant improvement in psoriasis, indicated by a gradual decrease in skin thickness and scaling as reflected in the Psoriasis Severity Index grading. Therefore, the prepared ethosomal nanogel is a potential vehicle for improved topical delivery of karanjin for better treatment of psoriasis.

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