Maximization of the In Vitro transcorneal release and the In Vivo IOP-lowering effects of Latanoprost Ophthalmic gel formulations using Azone as a penetration enhancer and Carbopol-974 as a mucoadhesive
AbstractThe objectives of this study were to maximize; a) the in vitro transcorneal release, b) the IOP-lowering effect and, c) the duration of action, of Latanoprost acid (LAT) ophthalmic gels. Method. The in vitro transcorneal release of LAT from a 1st set of gel formulations that containing different concentrations of Azone™ (as enhancer) with fixed concentration of C-974® (as mucoadhesive) were studied. Then, formulation that showed greatest permeability parameters at lowest Azone™ concentration was selected for preparation of a 2nd set of ocular gels containing various C-974® concentrations. Similarly, their in vitro permeabilities were evaluated, and the best C-974® concentration required for preparation of formulation(s) that can be conceded as ideal ophthalmic LAT gel(s) was pinpointed. Thereafter, the in vivo IOP-lowering efficacy study for the scaled-up formulations from both sets of the test formulations was conducted using TONO-PEN™ AVIA tonometer in rabbits for 4-consecutive days. Finally, how long such IOP-lowering effect does persist? To answer this question, the most effective formulations were used for a single-dose study, and the IOP was assessed at predetermined time interval till re-establishing the IOP base-line. Results. Majority of tested formulations have showed significant but varied augmentations in both, in vitro and in vivo results. Formulations (GAZ-4) & GC-4 have shown the highest therapeutic IOP lowering effects; i.e., (7.8±1.8), (6.5±2.1), respectively. Particularly noteworthy with both formulations the IOP base-line didn’t re-established after 24 hours, and their durations of action in the single-dose study were 47±2.25, and 48±1.5, respectively. Conclusion. The in vitro release, onset, magnitude & duration of action of action of LAT gels have been enhanced and extended for up to 2-day with two gel formulations. Nonetheless, the success in developing a novel ophthalmic formulation depended for great extent upon the crucial net outcomes of a very sensitive interplay/balance between the drug and additives.
How to Cite
AFOUNA, Mohsen I.. Maximization of the In Vitro transcorneal release and the In Vivo IOP-lowering effects of Latanoprost Ophthalmic gel formulations using Azone as a penetration enhancer and Carbopol-974 as a mucoadhesive. Journal of Excipients and Food Chemicals, [S.l.], v. 7, n. 2, p. 20-34, june 2016. ISSN 21502668. Available at: <https://ojs.abo.fi/ojs/index.php/jefc/article/view/259>. Date accessed: 27 oct. 2020.
Original Research Articles
Azone; Corneal transport; Ocular delivery; Ocular enhancers; Carbopol-974; Glaucoma; IOP lowering effect; Mucoadhesive; Thixotropy
Authors who publish with this journal agree to the following terms: Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal. Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal. Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).