Chinese Journal of Tissue Engineering Research ›› 2012, Vol. 16 ›› Issue (43): 8018-8022.doi: 10.3969/j.issn.2095-4344.2012.43.009

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Preparation of cyclosporine A nano-particle eye drops and its irritation to the eyes

Zhang Hai-juan1, Xu Qing2, Ma Ke1, Wu Yan2, You Yu-xia1   

  1. 1Beijing Institute of Ophthalmology, Beijing Tongren Eye Center, Beijing Tongren Hospital, Capital Medical University, Beijing 100005, China
    2National Center for Nanoscience and Technology, Beijing 100005, China
  • Received:2012-01-19 Revised:2012-03-15 Online:2012-10-21 Published:2012-10-21
  • Contact: Wu Yan, Associate researcher, National Center for Nanoscience and Technology, Beijing 100005, China wuy@nanoctr.cn
  • About author:Zhang Hai-juan★, Master, Associate researcher, Beijing Institute of Ophthalmology, Beijing Tongren Eye Center, Beijing Tongren Hospital, Capital Medical University, Beijing 100005, China zhanghaijuan1965@yahoo.cn

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Abstract:

BACKGROUND: Cyclosporine A can inhibit the immunological rejection after corneal transplantation. But it cannot be formulated into ophthalmic solution for its insolubility.
OBJECTIVE: To prepare 1% cyclosporine A nano-particle eye drops and to investigate its irritation to the eyes.
METHODS: Cyclosporine A was successfully incorporated into poly (ethylene glycol)-poly (dl-lactide) (PEG-PLA), and 1% cyclosporine A nano-particle eye drops were prepared. The nano-particle eye drop was characterized by using transmission electron microscopy and dynamic light scattering. The irritation of cyclosporine A nano-particle eye drops was observed through single and multiple irritative tests to the eyes in rabbits.
RESULTS AND CONCLUSION: Drug-loading and encapsulation efficiency of cyclosporine A nano-particle eye drops were 21.3% and 85.10%, respectively. The cyclosporine A nano-particles showed sphericity with even dispersion. The average size of cyclosporine A-loaded nano-particle was (296.9±32.06) nm with narrow distribution. Drug release curve in vitro exhibited a sustained drug release of cyclosporine A from the nano-particles. The release amount was 91.3% of cyclosporine A around 20 days. The irritation scores on the conjunctiva, cornea and iris were zero at the period of single and multiple administrations, indicating no irritation was found. These findings suggest that the cyclosporine A nano-particle has no irritation to the eyes.

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