当前位置: X-MOL 学术Pharmaceutics › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
A Screening Study for the Development of Simvastatin-Doxorubicin Liposomes, a Co-Formulation with Future Perspectives in Colon Cancer Therapy
Pharmaceutics ( IF 4.9 ) Pub Date : 2021-09-22 , DOI: 10.3390/pharmaceutics13101526
Cristina Ioana Barbălată 1 , Alina Silvia Porfire 1 , Alina Sesarman 2, 3 , Valentin-Florian Rauca 2, 3 , Manuela Banciu 2, 3 , Dana Muntean 1 , Rareș Știufiuc 4 , Alin Moldovan 4 , Cristian Moldovan 4 , Ioan Tomuță 1
Affiliation  

An increasing number of studies published so far have evidenced the benefits of Simvastatin (SIM) and Doxorubicin (DOX) co-treatment in colorectal cancer. In view of this, the current study aimed to investigate the pharmaceutical development of liposomes co-encapsulating SIM and DOX, by implementing the Quality by Design (QbD) concept, as a means to enhance the antiproliferative effect of the co-formulation on C26 murine colon cancer cells co-cultured with macrophages. It is known that the quality profile of liposomes is dependent on the critical quality attributes (CQAs) of liposomes (drug entrapped concentration, encapsulation efficiency, size, zeta potential, and drug release profile), which are, in turn, directly influenced by various formulation factors and processing parameters. By using the design of experiments, it was possible to outline the increased variability of CQAs in relation to formulation factors and identify by means of statistical analysis the material attributes that are critical (phospholipids, DOX and SIM concentration) for the quality of the co-formulation. The in vitro studies performed on a murine colon cancer cell line highlighted the importance of delivering the optimal drug ratio at the target site, since the balance antiproliferative vs. pro-proliferative effects can easily be shifted when the molar ratio between DOX and SIM changes.

中文翻译:

辛伐他汀-多柔比星脂质体开发的筛选研究,一种具有结肠癌治疗未来前景的复合制剂

迄今为止发表的越来越多的研究证明了辛伐他汀 (SIM) 和多柔比星 (DOX) 联合治疗结直肠癌的益处。鉴于此,目前的研究旨在通过实施质量源于设计 (QbD) 概念来研究共包封 SIM 和 DOX 的脂质体的药物开发,作为增强复合制剂对 C26 鼠类抗增殖作用的一种手段。结肠癌细胞与巨噬细胞共培养。众所周知,脂质体的质量特征取决于脂质体的关键质量属性 (CQA)(药物包埋浓度、封装效率、大小、zeta 电位和药物释放曲线),而这些属性又直接受各种因素的影响。配方因素和加工参数。通过使用实验设计,可以概述与配方因素相关的 CQA 增加的可变性,并通过统计分析确定对复合配方质量至关重要的材料属性(磷脂、DOX 和 SIM 浓度)。对鼠结肠癌细胞系进行的体外研究强调了在目标部位提供最佳药物比例的重要性,因为当 DOX 和 SIM 之间的摩尔比发生变化时,抗增殖与促增殖作用的平衡很容易改变。
更新日期:2021-09-22
down
wechat
bug