Department of Drug Sciences, University of Catania, Viale Andrea Doria n°6, 95125 Catania, Italy.
Molecules. 2020 Jun 30;25(13):2991. doi: 10.3390/molecules25132991.
Curcumin (CUR) has a wide range of pharmacological properties, including anti-inflammatory and antioxidant activities, and it can be considered a good candidate for the potential treatment of central nervous system (CNS) pathologies, although its use in clinical practice is compromised due to its high lipophilicity. Solid lipid nanoparticles (SLNs) are well-known nanocarriers representing a consolidated approach for the delivery of lipophilic compounds, but their systemic use is limited due their short half-life. The formulation of stealth SLNs (pSLNs) could be a valid strategy to overcome this limit. Curcumin-loaded-pSLNs were prepared by the solvent evaporation method. Formulation was characterized for their mean size, zeta potential, size distribution, and morphology. Drug antioxidant activity was evaluated by Oxygen Radical Absorbance Capacity (ORAC) assay. Finally, the obtained formulations were analyzed in terms of long-term stability. Curcumin-loaded-pSLNs showed good technological parameters with a mean particle size below 200 nm, as confirmed by TEM images, and a zeta potential value around -30 mV, predicting good long-term stability. Differential Scanning Calorimetry (DSC) analysis confirmed that PEG micelles interacted with the SLN surface; this suggests the location of the PEG on the pSLN surface. Therefore, these preliminary studies suggest that the produced formulation could be regarded as a promising carrier for the systemic administration.
姜黄素 (CUR) 具有广泛的药理特性,包括抗炎和抗氧化活性,因此可以被认为是治疗中枢神经系统 (CNS) 疾病的潜在候选药物,尽管由于其高亲脂性,其在临床实践中的应用受到限制。固体脂质纳米粒 (SLN) 是众所周知的纳米载体,代表了递送亲脂性化合物的一种成熟方法,但由于其半衰期短,其系统应用受到限制。隐形 SLN(pSLN)的配方可能是克服这一限制的有效策略。通过溶剂蒸发法制备载姜黄素的 pSLN。对其平均粒径、zeta 电位、粒径分布和形态进行了表征。通过氧自由基吸收能力 (ORAC) 测定法评估药物的抗氧化活性。最后,对获得的制剂进行了长期稳定性分析。载姜黄素的 pSLN 表现出良好的技术参数,平均粒径低于 200nm,TEM 图像证实,zeta 电位值约为-30mV,预示着良好的长期稳定性。差示扫描量热法 (DSC) 分析证实 PEG 胶束与 SLN 表面相互作用;这表明 PEG 位于 pSLN 表面。因此,这些初步研究表明,所制备的制剂可以被认为是一种有前途的用于系统给药的载体。