The Effect of Polymers on Drug Release Kinetics in Nanoemulsion In Situ Gel Formulation

Glaucoma is an ocular condition characterized by elevated intraocular pressure (IOP). Conventional treatments of glaucoma face poor corneal permeability and bioavailability. To address these issues, a nanoemulsion in situ gel of Timolol maleate was developed in this study by adding the polymer Carbopol 934p. Using Carbopol 934p, a novel ophthalmic pH-induced nanoemulsion in situ gel was formulated. The formulation was liquid at pH 4 and quickly gelled when the pH was raised to 7.4 (Lacrimal pH).

The pH-triggered in situ gelling mechanism demonstrated continuous drug release over a 24 h cycle. A total of nine trial formulations were prepared (NEI₁–NEI₉) and subjected to various physicochemical and in vitro evaluations. According to the in vitro release kinetics, the drug release of Timolol maleate nanoemulsion in situ gel NEI₅ followed zero-order kinetics, with a release exponent value of 0.902, indicating that the mechanism of release was non-Fickian diffusion regulated. In vivo results showed that Timolol maleate nanoemulsion in situ gel NEI₅ provided a better-sustained release of the drug, compared with the Timolet OD eye drops. The formulation is stable in storage, with no distinguishable change in appearance, physical properties, quality, and percentage drug release.

NEI₅ also reduces drug administration frequency, which improves patient compliance. Timolol maleate nanoemulsion in situ gel NEI₅ achieved the goal of controlled drug delivery with extended-release and cost-effectiveness, lowering the dosage and frequency of drug administration, and thus may improve patient compliance. In conclusion, the stable nanoemulsion in situ gel of Timolol maleate NEI₅ decreases intraocular pressure (IOP) over a prolonged period.

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Article information: Vijaya Rani, K.R.; Rajan, S.; Bhupathyraaj, M.; Priya, R.K.; Halligudi, N.; Al-Ghazali, M.A.; Sridhar, S.B.; Shareef, J.; Thomas, S.; Desai, S.M.; Pol, P.D. The Effect of Polymers on Drug Release Kinetics in Nanoemulsion In Situ Gel Formulation. Polymers 2022, 14, 427. https://doi.org/10.3390/polym14030427