Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 588, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119683
Keywords
Prodrug nanomedicine; Anti-oxidant; Anti-inflammtory; Dry eye; Ocular drug delivery
Categories
Funding
- Zhejiang Provincial Natural Science Foundation of China [LR18H300002]
- National Natural Science Foundation of China [31671022, 81971732]
- Zhejiang Medicines Health Science and Technology Program [WKJ-ZJ-1529]
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In the present study, a pterostilbene-peptide amphiphile (PS-GA-RGD) that can spontaneously self-assemble into prodrug nanomedicine, was rationally designed and developed as a novel ophthalmic formulation for the potential management of dry eye. The formed PS-GA-RGD nanomedicine was characterized by dynamic latter scattering (DLS) and transmission electron microscopy (TEM). After esterase treatment, active pterostilbene (PS) sustainably released from the PS-GA-RGD nanomedicine within 48 h, as indicated by an in vitro release study. In comparison with native PS, the formed PS-GA-RGD nanomedicine caused minimal cytotoxicity towards RAW 264.7 and HCEC cells in the 0-20 mu M range and did not delay wound healing of HCEC monolayer within 6 h. Furthermore, PS-GA-RGD nanomedicine effectively reduced the intracellular reactive oxygen species (ROS) level in H2O2 challenged RAW264.7 macrophages and remarkably suppressed the secretion of inflammatory cytokines (e.g., NO, TNF-alpha, and IL-6) in lipopolysaccharide (LPS) activated RAW264.7 macrophages. Ocular tolerance to the proposed PS-GA-RGD nanomedicine was good after a single instillation in in vivo ocular irritation tests. Overall, the proposed PS-GA-RGD nanomedicine had potent anti-oxidant capacity and anti-inflammatory efficacy, which may be a promising ophthalmic formulation for the management of dry eye.
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