Health Information Technology Department, Jeddah Community College, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia.
Department of Medical Laboratory Technology, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia.
PLoS One. 2018 Mar 20;13(3):e0193451. doi: 10.1371/journal.pone.0193451. eCollection 2018.
Ursolic acid (UA) is a promising molecule with anti-inflammatory, analgesic and potential anti-arthritic activity.
This study was undertaken to make formulation and evaluation of Ocimum sanctum L. leaf extract (OLE) loaded nano-structured lipid carriers (OLE-NLCs) for improved transdermal delivery of UA. Different surfactants, solid lipids and liquid lipids were used for the preparation of NLCs. The NLCs were developed using emulsion solvent diffusion and evaporation method. Different physicochemical properties, entrapment efficacy, in vitro release evaluation, and ex vivo permeation studies of the prepared NLCs were carried out. The in vivo anti-arthritic activity of OLE-loaded NLC gel and control gel formulation (OLE free NLC gel) against Complete Freund's Adjuvant (CFA) induced arthritis in wister albino rats was also carried out.
OLE-NLCs were composed of spherical particles having a mean particle size of ~120 nm, polydispersity index of ~0.162 and zeta potential of ~ -27 mV. The high entrapment efficiency (EE) of UA ~89.56% was attained. The in vitro release study demonstrated a prolonged release of UA from the NLCs up to 12 h. The developed formulation was found to be significantly better with respect to the drug permeation amount with an enhancement ratio of 2.69 as compared with marketed formulation. The in vivo biological activity investigations, studies showed that the newly prepared NLCs formulation of OLE showed excellent anti-arthritic activity and the results were found at par with standard marketed diclofenac gel for its analgesic and anti-arthritic activities. These results were also supported by radiological analysis and molecular docking studies.
The overall results proved that the prepared OLE-NLCs were very effective for the treatment of arthritis and the results were found at par with standard marketed the standard formulation of diclofenac gel.
熊果酸（UA）是一种有前途的分子，具有抗炎、镇痛和潜在的抗关节炎活性。
本研究旨在制备负载荜茇叶提取物（OLE）的纳米结构脂质载体（OLE-NLCs）并进行评价，以提高 UA 的经皮传递。使用不同的表面活性剂、固体脂质和液体脂质来制备 NLCs。NLCs 是通过乳化溶剂扩散和蒸发方法制备的。对制备的 NLCs 的不同理化性质、包封效率、体外释放评价和体外渗透研究进行了研究。还对负载 OLE 的 NLC 凝胶和对照凝胶制剂（无游离 OLE 的 NLC 凝胶）对 Wister 白化大鼠完全弗氏佐剂（CFA）诱导关节炎的体内抗关节炎活性进行了研究。
OLE-NLCs 由平均粒径约为 120nm、多分散指数约为 0.162 和 Zeta 电位约为-27mV 的球形颗粒组成。UA 的高包封效率（EE）达到了~89.56%。体外释放研究表明，UA 从 NLCs 中的释放可延长至 12h。与市售制剂相比，所开发的制剂在药物渗透量方面具有显著优势，其增强比为 2.69。体内生物学活性研究表明，OLE 的新型 NLCs 制剂表现出优异的抗关节炎活性，其结果与标准市售双氯芬酸钠凝胶的镇痛和抗关节炎活性相当。这些结果也得到了放射学分析和分子对接研究的支持。
总的来说，这些结果证明，所制备的 OLE-NLCs 非常有效地治疗关节炎，其结果与标准市售双氯芬酸钠凝胶的标准制剂相当。
