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Curcumin Containing PEGylated Solid Lipid Nanoparticles for Systemic Administration: A Preliminary Study
Molecules ( IF 4.2 ) Pub Date : 2020-06-30 , DOI: 10.3390/molecules25132991
Debora Santonocito 1 , Maria Grazia Sarpietro 1 , Claudia Carbone 1 , Annamaria Panico 1 , Agata Campisi 1 , Edy Angela Siciliano 1 , Giovanni Sposito 1 , Francesco Castelli 1 , Carmelo Puglia 1
Affiliation  

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.

中文翻译:

用于全身给药的含有姜黄素的聚乙二醇化固体脂质纳米颗粒:一项初步研究

姜黄素 (CUR) 具有广泛的药理特性,包括抗炎和抗氧化活性,它可以被认为是潜在治疗中枢神经系统 (CNS) 病理的良好候选者,尽管其在临床实践中的应用受到了影响因其高亲油性。固体脂质纳米颗粒 (SLN) 是众所周知的纳米载体,代表了一种用于递送亲脂性化合物的综合方法,但由于其半衰期短,其全身应用受到限制。隐形 SLN (pSLN) 的制定可能是克服这一限制的有效策略。姜黄素负载 pSLNs 是通过溶剂蒸发法制备的。制剂的特征在于它们的平均尺寸、zeta 电位、尺寸分布和形态。通过氧自由基吸收能力(ORAC)测定评估药物抗氧化活性。最后,在长期稳定性方面对获得的制剂进行分析。经 TEM 图像证实,负载姜黄素的 pSLN 显示出良好的技术参数,平均粒径低于 200 nm,zeta 电位值约为 -30 mV,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 pSLN 表面上 PEG 的位置。因此,这些初步研究表明,所制备的制剂可被视为一种有前途的全身给药载体。经 TEM 图像证实,负载姜黄素的 pSLN 显示出良好的技术参数,平均粒径低于 200 nm,zeta 电位值约为 -30 mV,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 pSLN 表面上 PEG 的位置。因此,这些初步研究表明,所制备的制剂可被视为一种有前途的全身给药载体。经 TEM 图像证实,负载姜黄素的 pSLN 显示出良好的技术参数,平均粒径低于 200 nm,zeta 电位值约为 -30 mV,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 pSLN 表面上 PEG 的位置。因此,这些初步研究表明,所制备的制剂可被视为一种有前途的全身给药载体。
更新日期:2020-06-30
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