Ingallina Cinzia, Costa Pedro M, Ghirga Francesca, Klippstein Rebecca, Wang Julie T, Berardozzi Simone, Hodgins Naomi, Infante Paola, Pollard Steven M, Botta Bruno, Al-Jamal Khuloud T
Institute of Pharmaceutical Science, Faculty of Life Sciences & Medicine, King's College London, Franklin-Wilkins Building, London, SE1 9NH, UK.
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Rome, Italy.
Nanomedicine (Lond). 2017 Apr;12(7):711-728. doi: 10.2217/nnm-2016-0388. Epub 2017 Mar 21.
With the purpose of delivering high doses of glabrescione B (GlaB) to solid tumors after systemic administration, long-circulating GlaB-loaded oil-cored polymeric nanocapsules (NC-GlaB) were formulated.
MATERIALS & METHODS: Synthesis of GlaB and its encapsulation in nanocapsules (NCs) was performed. Empty and GlaB-loaded NCs were assessed for their physico-chemical properties, in vitro cytotoxicity and in vivo biodistribution.
GlaB was efficiently loaded into NCs (∽90%), which were small (∽160 nm), homogeneous and stable upon storage. Further, GlaB and NC-GlaB demonstrated specific activities against the cancer stem cells. Preliminary studies in tumor-bearing mice supported the ability of NC to accumulate in pancreatic tumors.
This study provides early evidence that NC-GlaB has the potential to be utilized in a preclinical setting and justifies the need to perform therapeutic experiments in mice.
为了在全身给药后将高剂量的毛蕊异黄酮B（GlaB）递送至实体瘤，制备了长循环载毛蕊异黄酮B的油核聚合物纳米胶囊（NC-GlaB）。
进行了GlaB的合成及其在纳米胶囊（NCs）中的包封。对空白和载GlaB的NCs进行了物理化学性质、体外细胞毒性和体内生物分布评估。
GlaB被高效载入NCs（约90%），其粒径小（约160 nm），均一且储存稳定。此外，GlaB和NC-GlaB对癌症干细胞表现出特异性活性。在荷瘤小鼠中的初步研究支持了NC在胰腺肿瘤中蓄积的能力。
本研究提供了早期证据，表明NC-GlaB有潜力用于临床前研究，并证明有必要在小鼠中进行治疗实验。
