College of Pharmacy, Chung-Ang University , Seoul, Korea.
College of Pharmacy, Dankook University , Cheonan, Korea.
Expert Opin Drug Deliv. 2020 Nov;17(11):1555-1572. doi: 10.1080/17425247.2020.1810016. Epub 2020 Sep 4.
Intravesical instillation is preferred over the systemic route of administration, as an efficient route of drug administration to treat bladder cancer. However, the periodic voiding of urine washes out the instilled drugs, eventually resulting in reduced drug exposure. Moreover, the presence of the bladder permeability barrier limits drug permeation into tumor tissues. It is therefore important to develop a novel delivery system that not only promotes prolonged retention of drugs in the bladder but also enables drugs to penetrate the barrier.
This review addresses the limitations of conventional therapeutic regimens and reports the use of polymeric hydrogels and nano/microcarriers for enhanced intravesical drug delivery in bladder cancer. Strategies to prolong residence time in the bladder and enhance cell penetration and target-cell specificity are discussed.
Although promising results have been obtained in the field of intravesical drug delivery, numerous questions remain unanswered in terms of therapeutic efficacy. Specialized function covering extended drug exposure and/or enhanced drug uptake should be considered. Assessment protocols that adequately mimic the human bladder environment in vitro and in vivo experiments are needed to expedite formulation development.
与全身给药途径相比,膀胱内给药是治疗膀胱癌的首选方法,因为这是一种有效的药物给药途径。然而,尿液的定期排空会冲洗掉灌注的药物,最终导致药物暴露减少。此外,膀胱通透性屏障的存在限制了药物渗透到肿瘤组织中。因此,开发一种新的给药系统非常重要,该系统不仅能促进药物在膀胱中的长时间滞留,还能使药物穿透屏障。
本综述讨论了传统治疗方案的局限性,并报告了聚合物水凝胶和纳米/微载体在膀胱癌增强膀胱内药物输送中的应用。讨论了延长在膀胱中停留时间以及增强细胞穿透和靶细胞特异性的策略。
尽管在膀胱内药物输送领域已经取得了有希望的结果,但在治疗效果方面仍有许多问题尚未得到解答。应考虑具有延长药物暴露和/或增强药物摄取功能的专门制剂。需要开发评估方案来充分模拟体外和体内实验中的人类膀胱环境,以加速制剂的开发。