A Novel Eyes Topical Drug Delivery System: CsA-LNC for the Treatment of DED.

The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed by a validated UPLC-MS/MS method. The efficacy of CsA-LNCs (25 nm, 50 nm, 85 nm) was evaluated using the tear breakup time, fluorescein staining, tear production, inflammatory cytokines and histopathology tests. The safety of CsA-LNCs was study by the score of ocular irritation and histological examination study. CsA-LNCs(20-100 nm) were successfully prepared, An in vivo PK study showed significant improvement of the bioavailability (4.20-fold (25 nm), 2.15-fold (50 nm) and 2.33-fold (85 nm)) in bulbar conjunctiva, and great permeability was observed in the cornea for CsA-LNCs compared with CsA emulsion. An in vivo PD study showed that CsA-LNCs have great efficacy for DED, and the effect was improved over CsA emulsion. CsA-LNCs were safe and not cause significant irritation to the eyes surface of rabbits. This work has demonstrated CsA-LNCs, in particular small sizes CsA-LNC, are safe and effective with promising potential to treat DED. Grapical abstract.

Citation

Anan Zhang, Rong Sun, Meixin Ran, Yaxin Deng, Ying Ge, Yunjing Zhu, Xiumei Tao, Lixia Shang, Jingxin Gou, Haibing He, Tian Yin, Yanjiao Wang, Yu Zhang, Xing Tang. A Novel Eyes Topical Drug Delivery System: CsA-LNC for the Treatment of DED. Pharmaceutical research. 2020 Jul 14;37(7):146

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PMID: 32666340

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