由于癌症化疗药物面临的障碍，科学家们将吉西他滨 (GEM) 装入脂质体等纳米载体中，该载体以其无毒特性和靶向能力而闻名。含有 GEM 的脂质体纳米结构被岩藻依聚糖 (FU) 包覆，因为它具有针对癌细胞的抗肿瘤特性。由此在最佳条件下采用薄膜水合法制备了四种不同的阳离子脂质体制剂：DOTAP（制剂A）； DPPC/DOTAP（4:1 摩尔比，配方 B）、DPPC/DMPC/DOTAP（4:1:1 摩尔比，配方 C）和 DPPC/DMPC/DOTAP/DSPE-mPEG2000（4:1:1:0.1 摩尔比）比例，配方D)。研究人员对它们进行了研究，以确定能够有效包埋 GEM 并在脂质体表面成功涂覆 FU 的脂质组合物。然后评估其他定性特征，例如粒径、多分散指数、zeta 电位、稳定性和体外药物释放。配方 C 具有最佳的 GEM 包封效率 (EE)，但在涂有 FU 时会形成聚集体，产生不均匀的大尺寸颗粒，因此不适合有效递送。配方 A 和 B 的情况相同。只有配方 D 通过成功包覆来自三种不同藻类的 FU，表现出良好的 GEM-EE (> 80%) 和亲和力。就储存稳定性和药物释放研究而言，涂有 FU 的聚乙二醇化制剂 D 被证明是设计最佳药物递送系统的一种有前途的方法。© 2024。作者获得 Springer Science Business Media 的独家许可， LLC，施普林格自然集团的一部分。

Obstacles facing chemotherapeutic drugs for cancers led scientists to load Gemcitabine (GEM) into nanocarriers like liposomes, known for their nontoxicity profile and targeting capacity. The liposomal nanostructures containing GEM were coated with Fucoidan (FU) due to its anti-tumor properties by targeting cancer cells. Thus four different cationic liposomes formulations were prepared by thin-film hydration method in optimal conditions: DOTAP (formulation A); DPPC/DOTAP (4:1 molar ratio, formulation B), DPPC/DMPC/DOTAP (4:1:1 molar ratio, formulation C) and DPPC/DMPC/DOTAP/DSPE-mPEG2000 (4:1:1:0.1 molar ratio, formulation D). They were studied to identify lipid-compositions offering effective GEM-entrapment and successful coating of FU on the liposome surface. Additional qualitative characteristics, such as particle size, polydispersity index, zeta potential, stability and in vitro drug release were then evaluated. Formulation C gave the best GEM-entrapment efficiency (EE) but formed aggregates when coated with FU, giving non-homogenous large size particles then not suitable for effective delivery. It was the same situation with formulation A and B. Only the formulation D showed a good GEM-EE (> 80%) and affinity by successful coating FU from three different algae species. The PEGylated formulation D coated of FU, with regard to storage stability and drug release studies, revealed to be a promising approach on design of optimal drug delivery system.© 2024. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.