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Preliminary In Vivo Safety Evaluation of a Tacrolimus Eye Drop Formulation Using Hydroxypropyl Beta Cyclodextrin After Ocular Administration in NZW Rabbits

Authors Mahmoudi A, Malaekeh-Nikouei B, Hanafi-Bojd MY, Toloei M, Hosseini M, Nikandish M

Received 11 September 2019

Accepted for publication 11 March 2020

Published 27 March 2020 Volume 2020:14 Pages 947—953

DOI https://doi.org/10.2147/OPTH.S229405

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Editor who approved publication: Dr Scott Fraser


Asma Mahmoudi, 1 Bizhan Malaekeh-Nikouei, 2, 3 Mohammad Yahya Hanafi-Bojd, 4, 5 Mojtaba Toloei, 6 Mehran Hosseini, 6 Malihe Nikandish 7

1Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; 2Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; 3Nanotechnology Research Center, Institute of Pharmaceutical Technology, Mashhad University of Medical Sciences, Mashhad, Iran; 4Cellular and Molecular Research Center, Birjand University of Medical Sciences, Birjand, Iran; 5Department of Nanomedicine, Faculty of Medicine, Birjand University of Medical Sciences, Birjand, Iran; 6Cellular and Molecular Research Center, Department of Anatomy, Birjand University of Medical Sciences, Birjand, Iran; 7Ophthalmology Department, Valiasr Hospital, Birjand University of Medical Sciences, Birjand, Iran

Correspondence: Malihe Nikandish
Ophthalmology Department, Valiasr Hospital, Birjand University of Medical Sciences, P. O. Box:9717853577, Birjand, Iran
Tel +9856 32395000
Fax +9856 32430076
Email malihenikandish@yahoo.com

Aim: Tacrolimus is an immunosuppressive drug with higher potency compared to cyclosporine A (as a useful immunosuppressant). We prepared an ophthalmic solution formulation of Tacrolimus using hydroxypropyl beta cyclodextrin (HP-ßCD). In the present study, safety of this formulation was investigated in rabbits.
Materials and Methods: Formulation containing HP-ßCD, Tacrolimus, Polyvinyl alcohol (PVA) and Benzalkonium Chloride in PBS 7.4 was prepared. Tacrolimus concentration in ophthalmic preparation was 0.05% w/v. Ten male New Zealand white rabbits were housed in clean separated cages. One drop of Tacrolimus prepared formulation and a placebo formulation were applied every 12 hrs in the right and left eyes respectively, for 28 days.
Results: This new aqueous formulation of Tacrolimus could improve Tacrolimus solubility about 42 times. Clinical examinations on the  1st, 3rd, 7th, 14th and 28th days of study showed transient redness and conjunctivitis in some cases of both control and intervention groups that was not persistent. At the end of the study, there were no statistical differences between the two groups in corneal epithelial defect, redness or pathological evaluations.
Conclusion: The results of this study suggest that eye drop formulation of CD-Tacrolimus is safe in preliminary evaluations and can be useful for further studies.

Keywords: Tacrolimus, hydroxypropyl beta cyclodextrin (HP-BCD), animal study, ocular administration, safety

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