Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
Department of Pharmacy, Ram-Eesh Institute of Vocational and Technical Education, Greater Noida, India.
Drug Dev Ind Pharm. 2020 Sep;46(9):1443-1457. doi: 10.1080/03639045.2020.1793998. Epub 2020 Jul 20.
Curcumin (CUR) conventional formulation has poor oral bioavailability due to low solubility and low stability. Also, it extensively undergoes first-pass-metabolism showing low biological activity. The present work focuses on the systematic development and characterization of CUR-loaded Nanostructured Lipid Carrier (CUR-NLCs) having promising topical applications for skin diseases such as psoriasis. CUR-NLCs were prepared by using high-speed homogenization method. Quality by design approach was exploited to select out Critical Process Parameters i.e. homogenization speed (X1), homogenization time (X2), amount of lipid (X3), solid lipids (SL): liquid lipids (LL) (X4), and surfactant conc. (X5) using Plackett-Burman design and for obtaining critical quality attributes i.e. particle size (Y1) and entrapment efficiency (Y2) using Box-Behnken design. The developed NLCs were found to be nano-metric in size (189.4 ± 2.6 nm) with a low polydispersity index (0.262 ± 0.24), zeta potential (-21.45 ± 1.3 mV), and showed good encapsulation efficiency (86.72 ± 09%). Surface morphology determined by SEM and AFM revealed the spherical shape of the NLCs with a smooth surface. XRD studies showed NLCs in the amorphous state. After incorporation of NLCs into a nanogel, it was characterized for pH, rheological behavior, spreadability, occlusion, and release kinetics. The drug release from NLC in 24 h was found to be 60.2 ± 0.45% indicating a sustained release pattern. permeation studies revealed a good permeation flux (0.453 ± 0.76 µg/cm.h) and retention (60.2 ± 0.45%) of CUR in the skin epidermis. Thus, developed CUR-NLCs can be a potential delivery system and a promising therapeutic approach for the effective treatment of psoriasis.
姜黄素（CUR）常规制剂由于溶解度低和稳定性差，口服生物利用度差。此外，它广泛经历首过代谢，表现出低生物活性。本工作重点是开发具有潜在局部应用于皮肤病（如银屑病）的姜黄素载药纳米结构脂质载体（CUR-NLCs）并对其进行表征。CUR-NLCs 是通过高速匀浆法制备的。采用质量源于设计方法，通过 Plackett-Burman 设计选择关键工艺参数，即匀浆速度（X1）、匀浆时间（X2）、脂质量（X3）、固体脂质（SL）：液体脂质（LL）（X4）和表面活性剂浓度（X5），并通过 Box-Behnken 设计获得关键质量属性，即粒径（Y1）和包封效率（Y2）。所开发的 NLC 粒径为纳米级（189.4±2.6nm），具有低的多分散指数（0.262±0.24）、Zeta 电位（-21.45±1.3mV）和良好的包封效率（86.72±09%）。通过 SEM 和 AFM 确定的表面形态表明 NLC 呈球形，表面光滑。XRD 研究表明 NLC 处于无定形状态。将 NLC 掺入纳米凝胶后，对其 pH 值、流变行为、铺展性、封闭性和释放动力学进行了表征。NLC 在 24 小时内的药物释放率为 60.2±0.45%，表明呈持续释放模式。渗透研究表明 CUR 在皮肤表皮中有良好的渗透通量（0.453±0.76µg/cm.h）和保留率（60.2±0.45%）。因此，开发的 CUR-NLCs 可以作为一种有潜力的药物传递系统，并为银屑病的有效治疗提供一种有前途的治疗方法。
