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Effect of Particle Size and Viscosity of Suspensions on Topical Ocular Bioavailability of Budesonide, a Corticosteroid.
- Source :
-
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics [J Ocul Pharmacol Ther] 2020 Jul/Aug; Vol. 36 (6), pp. 404-409. Date of Electronic Publication: 2020 Jul 14. - Publication Year :
- 2020
-
Abstract
- Purpose: To determine the effect of particle size and viscosity of suspensions on topical ocular bioavailability of budesonide, a corticosteroid drug. Methods: Budesonide microparticle and nanoparticle (MP and NP) suspensions were prepared with or without homogenization and microfluidization. Using different grades of hydroxyl propyl methyl cellulose, low viscosity NP (NP-LV) and low and high viscosity MP (MP-LV and MP-HV) were prepared. Suspensions were characterized for particle size, viscosity, and osmolality. Budesonide suspensions were administered topically to rabbits and aqueous humor was collected and analyzed for budesonide. Budesonide C <subscript>max</subscript> , t <subscript>max</subscript> , and the area under the concentration time curve (AUC <subscript>(0-6h)</subscript> ) values were determined. The geometric mean ratio of AUC and bioequivalence was evaluated using a bootstrap method. Results: The particle sizes for NP and MP were ∼700 and 2,000 nm. The viscosities for low and HV formulations were ∼5 and 50 cP. The geometric mean budesonide C <subscript>max</subscript> values for the suspensions NP-LV, MP-LV, and MP-HV were 0.22, 0.22, and 0.31 μg/g, t <subscript>max</subscript> values were 0.67, 0.60 and 0.53 h, and AUC <subscript>0-6h</subscript> values were 0.72, 0.53, and 0.95 μg h/g, respectively. Bootstrap analysis indicated that the 90% confidence intervals of the geometric mean ratio of AUC <subscript>0-6h</subscript> values were 1.00-1.74 (MP-HV vs. NP-LV), 0.57-0.96 (MP-LV vs. NP-LV), and 0.45-0.70 (MP-LV vs. MP-HV). Conclusions: The 3 budesonide suspensions assessed in this study were not bioequivalent. Results suggested that an increase in viscosity improves the bioavailability of budesonide from the microsuspension formulation.
- Subjects :
- Administration, Topical
Animals
Area Under Curve
Biological Availability
Budesonide administration & dosage
Budesonide adverse effects
Drug Delivery Systems methods
Glucocorticoids administration & dosage
Glucocorticoids adverse effects
Hypromellose Derivatives chemistry
Male
Models, Animal
Nanoparticles administration & dosage
Nanoparticles chemistry
Particle Size
Rabbits
Suspensions administration & dosage
Suspensions chemistry
Therapeutic Equivalency
Budesonide pharmacokinetics
Drug Compounding methods
Glucocorticoids pharmacokinetics
Viscosity drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1557-7732
- Volume :
- 36
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
- Publication Type :
- Academic Journal
- Accession number :
- 32678687
- Full Text :
- https://doi.org/10.1089/jop.2019.0150