Department of Pharmaceutics and Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, PO Box: 14155-6153, Tehran, Iran.
Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Pharm Res. 2020 Jun 3;37(6):119. doi: 10.1007/s11095-020-02818-8.
Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this strategy is hampered by several hurdles, namely premature clearance of small-sized molecules from the peritoneum, limited distribution within the peritoneal space and inadequate penetration into the target tissues. To address these challenges, incorporation of therapeutic agents into the particulate-based drug delivery systems has brought new hope in this direction. Nonetheless, as yet, there has been no formulation specifically approved for IP delivery. To gain this goal, it is crucial to have a detailed understanding of the correlation between the physicochemical characteristics of particle-based carriers and their biological fate and anticancer efficacy after IP administration. The main focus of this review, therefore, concerns the significance of these characteristics, namely composition, particle size, charge, coating and presence of targeting moieties in the design of carriers for successful IP delivery. Graphical Abstract Physicochemical characteristics of particle-based carriers influence their peritoneal residence time, biological fate and anticancer efficacy after intraperitoneal administration.
在过去的几十年中，腹腔内（IP）局部药物递送通过在腹腔内提供高药物浓度和延长保留时间，为治疗危及生命的腹膜疾病（如腹膜癌病（PC））开辟了新的前景。然而，这种策略的临床转化受到几个障碍的阻碍，即小分子从腹膜过早清除、在腹膜空间内的分布有限以及对目标组织的渗透不足。为了解决这些挑战，将治疗剂纳入基于颗粒的药物递送系统为这一方向带来了新的希望。尽管如此，迄今为止，还没有专门批准用于 IP 给药的制剂。为了实现这一目标，详细了解基于颗粒的载体的物理化学特性与其在 IP 给药后的生物命运和抗癌疗效之间的相关性至关重要。因此，本篇综述的主要重点是这些特性（即组成、粒径、电荷、涂层和靶向部分的存在）在成功的 IP 递药载体设计中的重要性。
图摘要 基于颗粒的载体的物理化学特性影响其在腹腔内给药后的腹膜停留时间、生物命运和抗癌疗效。
