Esposito Tiziana, Sansone Francesca, Auriemma Giulia, Franceschelli Silvia, Pecoraro Michela, Picerno Patrizia, Aquino Rita P, Mencherini Teresa
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano (SA), Italy.
Pharmaceutics. 2020 Jul 17;12(7):671. doi: 10.3390/pharmaceutics12070671.
The administration of natural antioxidants is considered to be a prevention strategy for chronic diseases and a useful tool for the healthcare system to reduce the administration of expensive and often not effective treatments. The chemical characterization of a methanolic extract (AJ) of L. was performed, and its antioxidant activity was evaluated. AJ and the major compounds, characterized by chromatographic techniques as phenylpropanoids and iridoids, were able to reduce the Reactive Oxygen Species levels in cancer cell lines (melanoma, A375, cervical cancer, HeLa, and alveolar adenocarcinoma, A549), stimulated by lipopolysaccharide. However, a clinical translation of these results encountered a significant limitation represented by the poor water solubility and bioavailability of the extract and compounds. Consequently, a hydro-soluble powder system (AJEP) was developed by spray-drying encapsulating AJ into a multi-component solid matrix that is based on L-proline and hydroxyethylcellulose as loading and coating agents, and lecithin as solubility enhancer. The technological approach led to a satisfactory process yield (71.5%), encapsulation efficiency (99.9%), and stability. The in vitro water dissolution rate of the bioactive compounds appeared to be improved with respect to the extract, suggesting higher feasibility in the manufacturing and administration; even the in vitro biological activity of the produced multi-component AJEP was clearly enhanced.
天然抗氧化剂的施用被认为是一种慢性疾病预防策略,也是医疗保健系统减少昂贵且往往无效的治疗方法施用的有用工具。对L.的甲醇提取物(AJ)进行了化学表征,并评估了其抗氧化活性。AJ以及通过色谱技术鉴定为苯丙素类和环烯醚萜类的主要化合物,能够降低脂多糖刺激的癌细胞系(黑色素瘤、A375、宫颈癌、HeLa和肺泡腺癌、A549)中的活性氧水平。然而,这些结果的临床转化遇到了一个重大限制,即提取物和化合物的水溶性和生物利用度较差。因此,通过喷雾干燥将AJ封装到基于L-脯氨酸和羟乙基纤维素作为负载和包衣剂以及卵磷脂作为增溶剂的多组分固体基质中,开发了一种水溶性粉末系统(AJEP)。该工艺方法产生了令人满意的工艺产率(71.5%)、包封效率(99.9%)和稳定性。生物活性化合物的体外水溶解速率相对于提取物似乎有所提高,表明在制造和施用方面具有更高的可行性;所生产的多组分AJEP的体外生物活性也明显增强。