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Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation
摘要： The topical administration route is commonly used for targeting therapeutics to the eye; however, improving the bioavailability of drugs applied directly to the eye remains a challenge. Different strategies have been studied to address this challenge. One of them is the use of aggregates that are formed easily by self-assembly of cyclodextrin (CD)/drug complexes in aqueous solution. The aim of this study was to design a new eye drop formulation based on aggregates formed between CD/drug complexes. For this purpose, the physicochemical properties of the aggregates associated with six CDs and selected water-soluble polymers were analysed. Complex formation was studied using differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and 1H nuclear magnetic resonance spectroscopy (1H-NMR). Results showed that HPβCD performed best in terms of solubilization, while γCD performed best in terms of enhancing nanoaggregate formation. Formation of inclusion complexes was con?rmed by DSC, FT-IR and 1H-NMR studies. A mixture of 15% (w/v) γCD and 8% (w/v) HPβCD was selected for formulation studies. It was concluded that formulations with aggregate sizes less than 1 μm and viscosity around 10–19 centipoises can be easily prepared using a mixture of CDs. Formulations containing polymeric drug/CD nanoaggregates represent an interesting strategy for enhanced topical delivery of nepafenac.
关键词： cyclodextrin,self-assemble,nepafenac,aggregate,polymer,complexation,ocular drug delivery
更新于2025-09-23 15:22:29
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Safety and Efficacy of 0.1% Nepafenac versus 1% Prednisolone Acetate Eye Drops after Laser Iridotomy a?? A Prospective, Randomized Trial
摘要： Purpose: To compare 0.1% nepafenac, a topical non-steroidal anti-inflammatory drop, with 1% prednisolone acetate in controlling inflammation after Nd:YAG laser peripheral iridotomy (LPI) in primary angle closure suspects (PACS). Design: Prospective randomized controlled trial. Participants: One hundred and fifty-two PACS patients undergoing bilateral LPI. Methods: Patients were randomized to 0.1% nepafenac or 1% prednisolone acetate eye drop in both eyes. Medications were given 4 times daily for 7 days, then twice daily for additional 7 days. Investigators were masked to the type of medication. Right eyes in patients with bilateral PACS and the eye with PACS in asymmetrical disease (primary angle closure in fellow eye) were analyzed. Outcome measures: Non-inferior control of inflammation, defined as absence of cell in the anterior chamber at 2weeks and absence of rebound iritis with medication discontinuation, was the primary outcome, while difference in the rise in intraocular pressure (IOP) was a secondary outcome. Results: Both groups were comparable in baseline characteristics, including IOP, and total laser energy. Nepafenac was non-inferior to prednisolone with regards to inflammation control, with one(1.3%) nepafenac-treated patient failing to meet the primary endpoint because of 1+ anterior chamber cell at 2 weeks and 4(5.4%) prednisolone-treated eyes failing to meet the primary endpoint because of rebound iritis (p <0.001). A greater rise in IOP from baseline to 2 weeks was observed in the prednisolone group compared to the nepafenac group (+2.6 vs. +0.6 mmHg; p=0.004), though at 4 weeks IOPs were not significantly different than baseline in either group (p>0.05 for both). Two weeks after LPI, 3 nepafenac-treated eyes and 10 prednisolone-treated eyes demonstrated a 6-15 mmHg IOP elevation from baseline (p=0.10); while 2 prednisolone-treated eyes and no nepafenac-treated eyes had IOP elevation >15 mmHg (p=0.20). Four weeks after LPI, more prednisolone-treated eyes had IOP elevation of 6-15 mmHg as compared to nepafenac-treated eyes (6 vs. 1, p=0.04); no eyes had IOP elevation >15 mmHg. In an unplanned exploratory analysis, 8 prednisolone-treated patients, but no nepafenac-treated patients required repeat LPI (p=0.003). Conclusions: In our study, nepafenac was non-inferior to prednisolone acetate in controlling post-LPI inflammation with less impact on IOP.
关键词： nepafenac,prednisolone acetate,intraocular pressure,laser peripheral iridotomy,inflammation
更新于2025-09-19 17:13:59