June 2015
Volume 56, Issue 7
ARVO Annual Meeting Abstract  |   June 2015
Effect of Particle Size and Viscosity of Ophthalmic Suspensions on Ocular Bioavailability
Author Affiliations & Notes
  • David Bourne
    Pharmaceutical Science, CU SOP, Aurora, CO
  • Sunil Vooturi
    Pharmaceutical Science, CU SOP, Aurora, CO
  • Jiban Panda
    Pharmaceutical Science, CU SOP, Aurora, CO
  • Stephanie Choi
    FDA, Washington, DC
  • Hyewon Kim
    FDA, Washington, DC
  • Sarath Yandrapu
    Pharmaceutical Science, CU SOP, Aurora, CO
  • Uday B Kompella
    Pharmaceutical Science, CU SOP, Aurora, CO
  • Footnotes
    Commercial Relationships David Bourne, None; Sunil Vooturi, None; Jiban Panda, None; Stephanie Choi, None; Hyewon Kim, None; Sarath Yandrapu, None; Uday Kompella, None
  • Footnotes
    Support None
Investigative Ophthalmology & Visual Science June 2015, Vol.56, 5722. doi:
  • Views
  • Share
  • Tools
    • Alerts
      This feature is available to authenticated users only.
      Sign In or Create an Account ×
    • Get Citation

      David Bourne, Sunil Vooturi, Jiban Panda, Stephanie Choi, Hyewon Kim, Sarath Yandrapu, Uday B Kompella; Effect of Particle Size and Viscosity of Ophthalmic Suspensions on Ocular Bioavailability. Invest. Ophthalmol. Vis. Sci. 2015;56(7 ):5722.

      Download citation file:

      © ARVO (1962-2015); The Authors (2016-present)

  • Supplements

Purpose: To determine the effect of particle size and viscosity of budesonide suspensions on topical ocular bioavailability.

Methods: Budesonide nanosuspension was prepared by homogenization followed by microfluidization. Budesonide microsuspension was prepared by homogenization. Viscosity of the formulations was adjusted using different grades of hydroxyl propyl methyl cellulose (HPMC). Particle size was measured using a Zetasizer Nano ZS. Viscosity was measured using a Brookfield cone and plate viscometer. Budesonide was analyzed using an LC-MS/MS method, with a C-18 column, triamcinolone internal standard, and a linear gradient. Budesonide suspensions were dosed topically to New Zealand white rabbits, in a 30 µL eye drop, placed in the cul-del-sac of both eyes. Each animal was euthanized at one of six times points and aqueous humor was removed from each eye and stored frozen until analysis. Cmax and tmax values were determined by inspection and the AUC (0-6 hr) values were determined using the linear trapezoidal rule. These data were further analyzed using ANOVA and Duncan’s multiple range test for significance at p = 0.05. Bioequivalence was further evaluated using a bootstrap method.

Results: 1) Nanosuspension (~700 nm) with low viscosity (4.9 cPs), 2) microsuspension (~2000 nm) with low viscosity (4.9 cPs), and 3) microsuspension (~2000 nm) with high viscosity (53 cPs) were prepared and compared for bioavailability. The average Cmax values were 0.26, 0.22, and 0.35 µg/g and tmax values were 0.77, 0.75 and 1.1 hr, respectively, for suspensions 1, 2, and 3. The AUC(0-6 hr) values were 0.73, 0.53 and 0.95 µg.hr/g, respectively. Bootstrap analysis indicated that the 90% confidence intervals of the ratio of AUC (0-6hr) values were 0.605 - 0.991 (2 vs 1), 1.026 - 1.766 (3 vs 1) and 0.465 - 0.702 (2 vs 3), respectively.

Conclusions: The three suspensions assessed were not bioequivalent. An increase in viscosity improved the bioavailability of budesonide dosed as microsuspensions.


This PDF is available to Subscribers Only

Sign in or purchase a subscription to access this content. ×

You must be signed into an individual account to use this feature.