Department of Health Sciences, University Magna Græcia of Catanzaro, Germaneto-Catanzaro, Italy.
Eur J Pharm Biopharm. 2012 Sep;82(1):94-102. doi: 10.1016/j.ejpb.2012.06.001. Epub 2012 Jun 15.
Supramolecular vesicular aggregates (SVAs), made up by self-assembling liposomes and polyasparthydrazide co-polymers conjugated to folic acid molecules were extensively investigated in this manuscript as potential active targeting formulation for anticancer drug delivery. Folate-targeted systems (FT-SVAs) were used to treat breast cancer and to further proof the potential in vivo administration of these systems for the therapeutic treatment for several aggressive solid tumors. The physicochemical and technological parameters of FT-SVAs are suitable for their potential in vivo administration. The chemotherapeutic activity of GEM-loaded FT-SVAs was increased during in vivo experiments. NOD-SCID mice bearing MCF-7 human xenograft is used as breast cancer model. The measurement of the volume and weight of tumor masses decreased when animal models are treated by using GEM-loaded FT-SVAs, compared to data obtained by using GEM-loaded mPEG-SUVs and the free form of GEM. An almost complete regression of the tumor (≈ 0.2 cm(3)) was observed in NOD-SCID mice bearing MCF-7 human xenografts treated by GEM-loaded FT-SVAs due to the noticeable improvement of GEM pharmacokinetic parameters provided by FT-SVAs with respect to native anticancer drug. The obtained data showed that supramolecular systems could represent an innovative drug delivery system by self-assembling liposomes and biocompatible polymers to be potentially used for anticancer treatment.
本文研究了由自组装脂质体和与叶酸分子缀合的聚天冬酰肼共聚物组成的超分子囊泡聚集体（SVAs），作为抗癌药物传递的潜在主动靶向制剂。叶酸靶向系统（FT-SVAs）被用于治疗乳腺癌，并进一步证明这些系统在体内给药治疗几种侵袭性实体瘤方面的潜力。FT-SVAs 的物理化学和技术参数适合其潜在的体内给药。在体内实验中，载有 GEM 的 FT-SVAs 的化疗活性增加。使用 MCF-7 人异种移植的 NOD-SCID 小鼠作为乳腺癌模型。与使用载有 GEM 的 mPEG-SUVs 和游离 GEM 获得的数据相比，当使用载有 GEM 的 FT-SVAs 治疗动物模型时，肿瘤体积和重量的测量值降低。在接受载有 GEM 的 FT-SVAs 治疗的携带 MCF-7 人异种移植的 NOD-SCID 小鼠中，肿瘤几乎完全消退（≈0.2cm3），这是由于 FT-SVAs 提供的 GEM 药代动力学参数的显著改善相对于天然抗癌药物。所得数据表明，超分子系统可以通过自组装脂质体和生物相容性聚合物来代表一种创新的药物传递系统，有望用于癌症治疗。
