Weng Yu-Hua, Ma Xiao-Wei, Che Jing, Li Chan, Liu Juan, Chen Shi-Zhu, Wang Yu-Qin, Gan Ya-Ling, Chen Hao, Hu Zhong-Bo, Nan Kai-Hui, Liang Xing-Jie
Chinese Academy of Sciences (CAS) Center for Excellence in Nanoscience National Center for Nanoscience and Technology Beijing 100190 P. R. China.
Laboratory of Controllable Nanopharmaceuticals CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety National Center for Nanoscience and Technology Beijing 100190 P. R. China.
Adv Sci (Weinh). 2017 Nov 10;5(1):1700455. doi: 10.1002/advs.201700455. eCollection 2018 Jan.
Ocular inflammations are common diseases that may lead to serious vision-threatening obstacles. Eye drops for antiinflammation therapy need to be administered multiple times daily at a high dosage due to the rapid precorneal removal and low bioavailability of drugs. To overcome these problems, a cRGD-functionalized DSPE-PEG nanomicelle (DSPE-PEG-cRGD) encapsulated with flurbiprofen is proposed. The tailored nanomicelles trigger specific binding to integrin receptors on the ocular surface, which leads to rapid and robust mucoadhesion, superior ocular surface retention, and transcorneal penetration behaviors of nanomicelles. Due to the enhanced drug delivery on ocular surface and in aqueous humor, the functionalized nanoformulation significantly improves ocular antiinflammation efficacy at a low dosage by blocking the synthesis of inflammatory mediators and cytokines. The present study demonstrates a promising strategy that uses a functional peptide combined with nanomicelles for targeted delivery to the eye in ophthalmologic applications.
眼部炎症是常见疾病，可能导致严重的视力威胁障碍。由于药物在角膜前的快速清除和低生物利用度，用于抗炎治疗的眼药水需要每天多次高剂量给药。为了克服这些问题，提出了一种包裹氟比洛芬的cRGD功能化DSPE-PEG纳米胶束（DSPE-PEG-cRGD）。定制的纳米胶束触发与眼表整合素受体的特异性结合，导致纳米胶束快速而牢固的粘膜粘附、卓越的眼表滞留和角膜穿透行为。由于在眼表和房水中药物递送的增强，功能化纳米制剂通过阻断炎症介质和细胞因子的合成，在低剂量下显著提高了眼部抗炎效果。本研究证明了一种有前景的策略，即在眼科应用中使用功能肽与纳米胶束相结合用于眼部的靶向递送。
