A novel delivery system comprising -succinic anhydride (N-SAA) and D-fructose -conjugated chitosan (NSCF)-modified polymeric liposomes (NSCF-PLip) were designed to enhance oral delivery of paclitaxel (PTX) by targeting monocarboxylate transporters (MCT) and glucose transporters (GLUT). The synthesized NSCF was characterised by FT-IR and H NMR spectra. The prepared 30.78 % (degree of substitution of N-SAA) NSCF-PTX-PLip were approximately 150 nm in size, with a regular spherical shape, the zeta potential of −25.4 ± 5.13 mv, drug loading of 2.35 % ± 0.05 %, and pH-sensitive and slow-release characteristics. Compared with PTX-Lip, 30.78 % NSCF-PTX-PLip significantly enhanced Caco-2 cellular uptake co-mediation of MCT and GLUT, showing relatively specific binding of propionic acid and MCT. Notably, the NSCF modification of PTX-Lip had no appreciable influence on their original cellular uptake pathway. The fructose modification of 30.78 % NSC-PTX-PLip significantly increased the concentration after t, indicating their continuous and efficient absorption. Compared with PTX-Lip, the 30.78 % NSCF-PTX-PLip resulted in a 2.09-fold extension of MRT, and a 6.06-fold increase of oral bioavailability. It significantly increased tumour drug distribution and tumour growth inhibition rate. These findings confirm that 30.78 % NSCF-PLip offer a potential oral delivery platform for PTX and targeting the dual transporters of MCT and GLUT is an effective strategy for enhancing the intestinal absorption of drugs.

中文翻译：

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靶向双重转运蛋白的聚合物脂质体可高效口服紫杉醇

一种由琥珀酸酐 (N-SAA) 和 D-果糖缀合壳聚糖 (NSCF) 修饰的聚合物脂质体 (NSCF-PLip) 组成的新型递送系统，旨在通过靶向单羧酸转运蛋白 (MCT) 来增强紫杉醇 (PTX) 的口服递送和葡萄糖转运蛋白（GLUT）。合成的 NSCF 通过 FT-IR 和 1H NMR 谱进行了表征。制备的30.78%（N-SAA取代度）NSCF-PTX-PLip尺寸约为150 nm，形状规则球形，zeta电位为-25.4±5.13 mv，载药量为2.35%±0.05%，以及pH敏感和缓释特性。与PTX-Lip相比，30.78％NSCF-PTX-PLip显着增强了Caco-2细胞对MCT和GLUT的摄取共介导，显示出丙酸和MCT的相对特异性结合。值得注意的是，PTX-Lip 的 NSCF 修饰对其原始细胞摄取途径没有明显影响。 30.78% NSC-PTX-PLip 的果糖修饰显着提高了 t 后的浓度，表明其连续有效的吸收。与PTX-Lip相比，30.78% NSCF-PTX-PLip导致MRT延长2.09倍，口服生物利用度增加6.06倍。显着增加肿瘤药物分布和肿瘤生长抑制率。这些发现证实，30.78% NSCF-PLip 为 PTX 提供了潜在的口服递送平台，并且靶向 MCT 和 GLUT 的双重转运蛋白是增强药物肠道吸收的有效策略。