Tyagi Pradeep, Kashyap Mahendra, Majima Tsuyoshi, Kawamorita Naoki, Yoshizawa Tsuyoshi, Yoshimura Naoki
Department of Urology, University of Pittsburgh, Pittsburgh, Pennsylvania, USA.
Department of Urology, Nagoya University Graduate School of Medicine, Nagoya, Aichi, Japan.
Int J Urol. 2017 Apr;24(4):262-271. doi: 10.1111/iju.13317. Epub 2017 Mar 4.
Over the past two decades, there has been lot of interest in the use of liposomes as lipid-based biocompatible carriers for drugs administered by the intravesical route. The lipidic bilayer structure of liposomes facilitates their adherence to the apical membrane surface of luminal cells in the bladder, and their vesicular shape allows them to co-opt the endocytosis machinery for bladder uptake after instillation. Liposomes have been shown to enhance the penetration of both water-soluble and insoluble drugs, toxins, and oligonucleotides across the bladder epithelium. Empty liposomes composed entirely of the endogenous phospholipid, sphingomyelin, could counter mucosal inflammation and promote wound healing in patients suffering from interstitial cystitis. Recent clinical studies have tested multilamellar liposomes composed entirely of sphingomyelin as a novel intravesical therapy for interstitial cystitis. In addition, liposomes have been used as a delivery platform for the instillation of botulinum toxin in overactive bladder patients. The present review discusses the properties of liposomes that are important for their intrinsic therapeutic effect, summarizes the recently completed clinical studies with intravesical liposomes and covers the latest developments in this field.
在过去二十年中，人们对使用脂质体作为膀胱内给药的基于脂质的生物相容性载体产生了浓厚兴趣。脂质体的脂质双层结构有助于它们粘附在膀胱腔细胞的顶端膜表面，其囊泡形状使它们能够利用内吞机制在灌注后被膀胱摄取。脂质体已被证明可增强水溶性和非水溶性药物、毒素及寡核苷酸穿过膀胱上皮的渗透能力。完全由内源性磷脂鞘磷脂组成的空脂质体可以对抗黏膜炎症，并促进间质性膀胱炎患者的伤口愈合。最近的临床研究测试了完全由鞘磷脂组成的多层脂质体作为间质性膀胱炎的一种新型膀胱内治疗方法。此外，脂质体已被用作膀胱过度活动症患者注射肉毒杆菌毒素的递送平台。本综述讨论了对脂质体内在治疗效果重要的特性，总结了最近完成的膀胱内脂质体临床研究，并涵盖了该领域的最新进展。
