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Open AccessArticle

In Situ Gelling Systems Using Pluronic F127 Enhance Corneal Permeability of Indomethacin Nanocrystals

1
Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan
2
Okamoto Eye Clinic, 5-11-12-312 Izumicho, Suita, Osaka 564-0041, Japan
3
Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo 105-8512, Japan
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(19), 7083; https://doi.org/10.3390/ijms21197083
Received: 3 September 2020 / Revised: 17 September 2020 / Accepted: 22 September 2020 / Published: 25 September 2020
We previously designed an ophthalmic dispersion containing indomethacin nanocrystals (IMC-NCs), showing that multiple energy-dependent endocytoses led to the enhanced absorption of drugs from ocular dosage forms. In this study, we attempted to prepare Pluronic F-127 (PLF-127)-based in situ gel (ISG) incorporating IMC-NCs, and we investigated whether the instillation of the newly developed ISG incorporating IMC-NCs prolonged the precorneal resident time of the drug and improved ocular bioavailability. The IMC-NC-incorporating ISG was prepared using the bead-mill method and PLF-127, which yielded a mean particle size of 50–150 nm. The viscosity of the IMC-NC-incorporating ISG was higher at 37 °C than at 10 °C, and the diffusion and release of IMC-NCs in the IMC-NC-incorporating ISG were decreased by PLF-127 at 37 °C. In experiments using rabbits, the retention time of IMC levels in the lacrimal fluid was enhanced with PLF-127 in the IMC-NC-incorporating ISG, whereby the IMC-NC-incorporating ISG with 5% and 10% PLF-127 increased the transcorneal penetration of the IMCs. In contrast to the results with optimal PLF-127 (5% and 10%), excessive PLF-127 (15%) decreased the uptake of IMC-NCs after instillation. In conclusion, we found that IMC-NC-incorporating ISG with an optimal amount of PLF-127 (5–10%) resulted in higher IMC corneal permeation after instillation than that with excessive PLF-127, probably because of the balance between higher residence time and faster diffusion of IMC-NCs on the ocular surface. These findings provide significant information for developing ophthalmic nanomedicines. View Full-Text
Keywords: nanoparticles; indomethacin; Pluronic F-127; in situ gelling system; ophthalmic delivery system nanoparticles; indomethacin; Pluronic F-127; in situ gelling system; ophthalmic delivery system
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MDPI and ACS Style

Nagai, N.; Isaka, T.; Deguchi, S.; Minami, M.; Yamaguchi, M.; Otake, H.; Okamoto, N.; Nakazawa, Y. In Situ Gelling Systems Using Pluronic F127 Enhance Corneal Permeability of Indomethacin Nanocrystals. Int. J. Mol. Sci. 2020, 21, 7083. https://doi.org/10.3390/ijms21197083

AMA Style

Nagai N, Isaka T, Deguchi S, Minami M, Yamaguchi M, Otake H, Okamoto N, Nakazawa Y. In Situ Gelling Systems Using Pluronic F127 Enhance Corneal Permeability of Indomethacin Nanocrystals. International Journal of Molecular Sciences. 2020; 21(19):7083. https://doi.org/10.3390/ijms21197083

Chicago/Turabian Style

Nagai, Noriaki; Isaka, Takumi; Deguchi, Saori; Minami, Misa; Yamaguchi, Mizuki; Otake, Hiroko; Okamoto, Norio; Nakazawa, Yosuke. 2020. "In Situ Gelling Systems Using Pluronic F127 Enhance Corneal Permeability of Indomethacin Nanocrystals" Int. J. Mol. Sci. 21, no. 19: 7083. https://doi.org/10.3390/ijms21197083

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