Comprehensive evaluation of formulation factors for ocular penetration of fluoroquinolones in rabbits using cassette dosing technique

Figures & data

Figure 1 Schematic representation of the study design.

Table 1 Spectral masses and different parameters used for the analysis of the fluoroquinolones

FQs	Q1 mass (amu)	Q3 mass (amu)	Dwell (ms)	Declusturing potential	Exit potential	Collision energy	Collision exit potential
Pefloxacin	334.30	205.10	500.00	85.00	10.00	41.70	5.00
Ofloxacin	362.20	221.20	500.00	85.00	10.00	41.70	5.00
Gatifloxacin	376.30	261.10	300.00	85.00	10.00	41.70	5.00
Sparfloxacin	393.30	251.30	300.00	85.00	10.00	41.70	5.00
Gemifloxacin (IS)	390.00	313.40	300.00	85.00	10.00	41.70	5.00

Abbreviations: FQs, fluoroquinolones; Q1, mass filter quadrupole 1; Q3, mass filter quadrupole 3; IS, internal standard.

Figure 2 LC-MS spectra for all the fluoroquinolones.

Notes: Schematic representation of LC–MS spectra for (A) ofloxacin, (B) pefloxacin, (C) sparfloxacin, and (D) gatifloxacin. (E) Chromatogram obtained from standard samples and (F) chromatogram obtained from biosamples for the fluoroquinolones.
Abbreviation: LC–MS, liquid chromatography–mass spectrometry.

Figure 3 Effect of different concentrations at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at volume of instillation of 12.5 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 4 Effect of different concentrations at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at volume of instillation of 25 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 5 Effect of different concentrations at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at volume of instillation of 50 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 6 Effect of different pH on transcorneal penetration of FQs at concentration of 0.025% (A), 0.05% (B), and 0.1% (C) with drop volume of 12.5 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 7 Effect of different pH on transcorneal penetration of FQs at concentration of 0.025% (A), 0.05% (B), and 0.1% (C) with drop volume of 25 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 8 Effect of different pH on transcorneal penetration of FQs at concentration of 0.025% (A), 0.05% (B), and 0.1% (C) with drop volume of 50 μL.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 9 Effect of different volumes of instillation at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at the concentration of 0.025%.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 10 Effect of different volumes of instillation at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at the concentration of 0.05%.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.

Figure 11 Effect of different volumes of instillation at pH 4.5 (A), pH 7.0 (B), and pH 8.0 (C) on transcorneal penetration of FQs at the concentration of 0.1%.

Abbreviations: FQs, fluoroquinolones; AUC, area under curve.