School of Pharmacy, University of Reading, Whiteknights, Reading RG6 6AD, United Kingdom; Faculty of Chemistry and Chemical Technology, Al-Farabi Kazakh National University, Almaty 050040, Kazakhstan.
School of Pharmacy, University of Reading, Whiteknights, Reading RG6 6AD, United Kingdom; Pharmaceutical Development of Green Innovations Group, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Eur J Pharm Sci. 2018 Jan 1;111:83-90. doi: 10.1016/j.ejps.2017.09.039. Epub 2017 Sep 27.
Intravesical drug administration is used to deliver chemotherapeutic agents via a catheter to treat bladder cancer. The major limitation of this treatment is poor retention of the drug in the bladder due to periodic urine voiding. In this work, maleimide-functionalised PEGylated liposomes (PEG-Mal) were explored as mucoadhesive vehicles for drug delivery to the urinary bladder. The retention of these liposomes on freshly excised porcine bladder mucosa in vitro was compared with conventional liposomes, PEGylated liposomes, two controls (dextran and chitosan), and evaluated through Wash Out (WO) values. PEG-Mal liposomes exhibited greater retention on mucosal surfaces compared to other liposomes. The penetration abilities of conventional, PEG-Mal-functionalised and PEGylated liposomal dispersions with encapsulated fluorescein sodium into the bladder mucosa ex vivo were assessed using a fluorescence microscopy technique. PEGylated liposomes were found to be more mucosa-penetrating compared to other liposomes. All liposomes were loaded with fluorescein sodium salt as a model drug and the in vitro release kinetics was evaluated. Longer drug release was observed from PEG-Mal liposomes.
经尿道给药是通过导管将化疗药物递送至膀胱以治疗膀胱癌的一种方法。这种治疗方法的主要局限性是由于定期排尿导致药物在膀胱中的保留效果不佳。在这项工作中，马来酰亚胺功能化的聚乙二醇化脂质体（PEG-Mal）被探索作为递送至膀胱的药物的黏附载体。通过 Wash Out（WO）值比较了这些脂质体在新鲜离体猪膀胱黏膜上的保留情况与常规脂质体、聚乙二醇化脂质体、两种对照物（葡聚糖和壳聚糖）的保留情况。与其他脂质体相比，PEG-Mal 脂质体在黏膜表面的保留效果更好。使用荧光显微镜技术评估了载有荧光素钠的常规、PEG-Mal 功能化和聚乙二醇化脂质体分散体在离体膀胱黏膜中的穿透能力。与其他脂质体相比，聚乙二醇化脂质体具有更好的黏膜穿透能力。所有脂质体均负载荧光素钠盐作为模型药物，并评估了体外释放动力学。从 PEG-Mal 脂质体中观察到更长时间的药物释放。
