一种用于维持化疗中高剂量甲氨蝶呤递送的口服3D打印聚乳酸-羟基乙酸共聚物-生育酚聚乙二醇琥珀酸酯纳米复合水凝胶
An Oral 3D Printed PLGA-Tocopherol PEG Succinate Nanocomposite Hydrogel for High-Dose Methotrexate Delivery in Maintenance Chemotherapy.
作者信息
Kondiah Pierre P D, Rants'o Thankhoe A, Makhathini Sifiso S, Mdanda Sipho, Choonara Yahya E
机构信息
Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, Johannesburg 2193, South Africa.
出版信息
Biomedicines. 2022 Jun 22;10(7):1470. doi: 10.3390/biomedicines10071470.
High-dose methotrexate (HDMTX) is one of the chemotherapeutic agents used to treat a variety of cancers in both adults and children. However, the toxicity associated with HDMTX has resulted in the spread of infections and treatment interruption. Further, poor bioavailability due to efflux pump activities mediated by P-glycoprotein has also been linked to poor therapeutic effects of methotrexate following oral administrations. D-α-Tocopheryl poly-ethylene glycol 1000 succinate (TPGS) is known to improve the bioavailability of poorly soluble drugs by inhibiting P-gp efflux activities, thus enhancing cellular uptake. Therefore, to achieve improved bioavailability for MTX, this study aimed to design and develop a novel drug delivery system employing TPGS and a biodegradable polymer, i.e., PLGA, to construct methotrexate-loaded nanoparticles fixated in alginate-gelatine 3D printable hydrogel ink to form a solid 3D printed tablet for oral delivery. The results indicated that high accuracy (>95%) of the 3D printed tablets was achieved using a 25 G needle. In vitro, drug release profiles were investigated at pH 1.2 and pH 7.4 to simulate the gastrointestinal environment. The in vitro release profile displayed a controlled and prolonged release of methotrexate over 24 h. The in silico modeling study displayed P-gp ATPase inhibition, suggesting enhanced MTX absorption from the gastrointestinal site. The 3D-printed hydrogel-based tablet has the potential to overcome the chemotherapeutic challenges that are experienced with conventional therapies.
大剂量甲氨蝶呤(HDMTX)是用于治疗成人和儿童多种癌症的化疗药物之一。然而,与HDMTX相关的毒性导致感染扩散和治疗中断。此外,由P-糖蛋白介导的外排泵活性导致的低生物利用度也与口服甲氨蝶呤后的治疗效果不佳有关。已知D-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)通过抑制P-糖蛋白外排活性来提高难溶性药物的生物利用度,从而增强细胞摄取。因此,为了提高甲氨蝶呤的生物利用度,本研究旨在设计和开发一种新型药物递送系统,采用TPGS和可生物降解聚合物(即聚乳酸-羟基乙酸共聚物,PLGA)构建负载甲氨蝶呤的纳米颗粒,固定在藻酸盐-明胶3D可打印水凝胶油墨中,形成用于口服给药的固体3D打印片剂。结果表明,使用25G针头可实现3D打印片剂的高精度(>95%)。在体外,在pH 1.2和pH 7.4条件下研究药物释放曲线以模拟胃肠道环境。体外释放曲线显示甲氨蝶呤在24小时内实现了可控的缓释。计算机模拟研究显示P-糖蛋白ATP酶受到抑制,表明甲氨蝶呤从胃肠道部位的吸收增强。基于3D打印水凝胶的片剂有可能克服传统疗法所面临的化疗挑战。