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Aqueous humor pharmacokinetics of Benzalkonium chloride free bimatoprost formulated in tight junction modulation technology compared to Benzalkonium chloride preserved bimatoprost 0.01% ophthalmic solution in rabbit eyes

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Original Article

Author Details : Arindam Halder, Vinod Burade, Ajay J Khopade*, Monali Vakharia

Volume : 7, Issue : 2, Year : 2021

Article Page : 321-326

https://doi.org/10.18231/j.ijceo.2021.064

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Abstract

Purpose: This study was undertaken with an objective to compare the aqueous humor pharmacokinetics (PKs) of bimatoprost and bimatoprost free acid of innovator bimatoprost 0.01% (BAK-Bimatoprost) and the novel formulation, Tight Junction Modulation technology based bimatoprost 0.01% (TJM-bimatoprost) containing polyhexamethylene Biguanide hydrochloride (PHMB) as a preservative.
Materials and Methods: All animals in the study were assigned to one of two treatment arms: either a single dose of BAK-Bimatoprost (n=28) or a TJM-bimatoprost ophthalmic solution (n=28). Time points for aqueous humor collection were 0.5, 1, 2, 4, 8, 12 and 24 Hrs after drug administration.
Results: The mean Cmax of 11.93± 2.70 vs 10.92± 3.84 ng/ml was comparable (P>0.05, one-way ANOVA) across TJM bimatoprost and BAK-bimatoprost treatment arms. Results of other PK parameters pertaining to bimatoprost+ bimatoprost free acid concentration were as follows: time to maximum concentration (T_max) was 1.75± 2.0 vs 1.50 ± 1.16 hr and half-live (T_half) was 2.13 ± 0.58 vs 2.47 ± 0.79 hr in the TJM- bimatoprost and BAK-bimatoprost treatment arms respectively. Overall, there was no difference between TJM-bimatoprost and BAK-bimatoprost treatment arms in the PK end points.
Conclusions: The results taken in totality support the hypothesis that pharmacokinetics TJM-bimatoprost 0.01%, containing PHMB preservative, is comparable to BAK-bimatoprost 0.01%.
Key messages: A new formulation of bimatoprost 0.01% using Tight Junction Modulation technology is pharmacokinetically comparable to marketed formulation of bimatoprost containing benzalkonium chloride preservative.

Keywords: Aqueous humor, Bimatoprost 0.01%, Gel free reservoir technology, Glaucoma, Pharmacokinetics, Polyhexamethylene biguanide, Tight junction modulator.

How to cite : Halder A, Burade V, Khopade A J, Vakharia M, Aqueous humor pharmacokinetics of Benzalkonium chloride free bimatoprost formulated in tight junction modulation technology compared to Benzalkonium chloride preserved bimatoprost 0.01% ophthalmic solution in rabbit eyes. Indian J Clin Exp Ophthalmol 2021;7(2):321-326

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