期刊
EXPERT OPINION ON DRUG DELIVERY
卷 17, 期 9, 页码 1305-1319出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/17425247.2020.1783236
关键词
Dry age-related macular degeneration; astragaloside-IV; lipid nanocapsules; eye drops; ultra-small size
资金
- National Mega-project for Innovative Drugs [2019ZX09721001]
- Major Project of National Science and Technology 'Creation of Major New Drugs' from China [2018ZX09721002-002]
- China Postdoctoral Science Foundation [2019M651149]
- Liaoning Revitalization Talents Program [XLYC1907111, XLYC1908031]
- Liaoning Province Doctoral Start-up Fund Program [2019BS-226]
- Liaoning Province Natural Science Fund Project [20180551031]
- Overseas Returnees Start-up Fund from Shenyang Pharmaceutical University [GGJJ2018102]
Background Age-related macular degeneration (AMD) is a major cause of severe visual loss in elderly people. The treatments for dry AMD (dAMD) are severely limited so far. In this work, we aim to develop an eye drop to protect retinal functions against oxidative stress and apoptosis for improving dAMD management. Methods Astragaloside-IV (ASIV) was prepared into phospholipid complex and loaded into three sizes (20, 50 and 90 nm) of ASIV lipid nanocapsules (ASIV-LNCs). The penetration and distribution of LNCs were investigated. DAMD mice model was induced by NaIO3, and therapeutic effect was evaluated by electroretinography (ERG), histological examination, apoptosis and ROS detection. Results The ocular penetration and pharmacokinetic studies corroborated the feasibility of the LNCs to reach the fundus, and ultra-small-size LNCs (ASIV-LNCs-20) had the best delivery effect. ASIV-LNCs-20 was able to decrease ROS production and reduce the apoptosis rate from 5.12% to 0.533%. ERG and H&E staining results confirmed ASIV-LNCs-20 had a good protective effect on the morphology and function of the retina. Conclusions These results suggest that ASIV-LNCs can be a promising therapy approach for dAMD, and this research also offers new possibilities for further applications of LNCs as a drug delivery system for other eye diseases.
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