Aqueous penetration of topical tacrolimus
Samir S Shoughy, Faisal M Aljassar, Khalid F Tabbara, Samir S Shoughy, Faisal M Aljassar, Khalid F Tabbara
Abstract
Purpose: To evaluate the penetration of topical tacrolimus 0.05% into the aqueous humor.
Observations: A total of four patients scheduled for routine cataract surgery were included prospectively. We excluded patients with corneal pathology or ocular surface diseases. Topical tacrolimus 0.05% was compounded at our facility. It was dosed every 1 min for 5 min an hour before the aqueous was sampled. Aqueous samples were collected at the time of cataract surgery and were subjected to detection of presence and level of tacrolimus. There were 2 male and 2 female patients. The age range was 58-73 years with a mean age of 66 years. Tacrolimus was detected in the aqueous humor in all patients. The concentration of tacrolimus in the aqueous ranged from 2.6 to 5.6 ng/ml (mean 4.15 ± 1.18 ng/ml). In all patients, the aqueous tacrolimus concentration was greater than the minimal therapeutic level. The study was registered at clinicaltrials.gov (registration number is NCT02794610).
Conclusions and importance: Tacrolimus was detected in the aqueous humor following topical application. Topical tacrolimus may be a promising steroid-sparing modality for the treatment of anterior uveitis.
Keywords: Ocular inflammation; Ocular penetration; Topical tacrolimus.
Conflict of interest statement
The following authors have no financial disclosures: SS,FJ, KT.
© 2020 The Authors.
References
- Shoughy S.S. Topical tacrolimus in anterior segment inflammatory disorders. Eye Vis. 2017;4:7.
- Mochizuki M., Masuda K., Sakane T. A multicenter clinical open trial of FK506 in refractory uveitis, including Behcet's disease. Transplant Proc. 1991;23:3343–3346.
- Ishioka M., Ohno S., Nakamura S. FK506 treatment of noninfectious uveitis. Am J Ophthalmol. 1994;118:723–729.
- Sloper C.M., Powell R.J., Dua H.S. Tacrolimus (FK506) in the treatment of posterior uveitis refractory to cyclosporine. Ophthalmology. 1999;106:723–728.
- Shoughy S.S., Jaroudi M.O., Tabbara K.F. Efficacy and safety of low-dose topical tacrolimus in vernal keratoconjunctivitis. Clin Ophthalmol. 2016;10:643–647.
- Shoughy S.S., Tabbara K.F. Topical tacrolimus solution in autoimmune polyglandular syndrome-1-associated keratitis. Br J Ophthalmol. 2017 Sep;101(9):1230–1233.
- Thomson A.W. Interspecies comparison of the immunosuppressive efficacy and safety of FK506. Transplant Proc. 1990;22:100–105.
- Pleyer U., Lutz S., Jusko W.J. Ocular absorption of topically applied FK506 from liposomal and oil formulations in the rabbit eye. Investig Ophthalmol Vis Sci. 1993;34(9):2737–2742.
- Yuan J., Zhai J.J., Chen J.Q., Ye C.T., Zhou S.Y. Preparation of 0.05% FK506 suspension eyedrops and its pharmacokinetics after topical ocular administration. J Ocul Pharmacol Ther. 2009;25(4):345–350.
- Hikita N., Chan C.C., Whitcup S.M., Nussenblatt R.B., Mochizuki M. Effects of topical FK506 on endotoxin-induced uveitis (EIU) in the Lewis rat. Curr Eye Res. 1995;14:209–214.
- Whitcup S.M., Pleyer U., Lai J.C., Lutz S., Mochizuki M., Chan C.C. Topical liposome-encapsulated FK506 for the treatment of endotoxin-induced uveitis. Ocul Immunol Inflamm. 1988;6:51–56.
- Yalçındağ F.N., Batıoğlu F., Arı N., Özdemir Ö. Aqueous humor and serum penetration of tacrolimus after topical and oral administration in rats: an absorption study. Clin. Ophthalmol. (Auckland, NZ) 2007;1(1):61–64.
- Yalçindağ F.N., Batioğlu F., Ozdemir O. Penetration of topically applied tacrolimus into the aqueous humor in Behçet’s disease. Ann Ophthalmol. 2007;39(1):15–17.
- Garg V., Jain G.K., Nirmal J., Kohli K. Topical tacrolimus nanoemulsion, a promising therapeutic approach for uveitis. Med Hypotheses. 2013;81(5):901–904.
- Silva-Cunha A., da Silva G.R., de Castro W.V., Fialho S.L. Evaluation of the pharmacokinetics and ocular tolerance of a microemulsion containingtacrolimus. J Ocul Pharmacol Ther. 2014 Feb;30(1):59–65.
Source: PubMed