Improved Ocular Delivery of Nepafenac by Cyclodextrin Complexation
| Autor: | Forrest Smith, Eva M. Abarca, R. Jayachandra Babu, Makenzie Grant, Haley Shelley |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
genetic structures
Swine Benzeneacetamides Pharmaceutical Science 02 engineering and technology Aquatic Science Eye Nepafenac Permeability 03 medical and health sciences 0302 clinical medicine Ciliary body Cornea Drug Discovery medicine Animals Solubility Ecology Evolution Behavior and Systematics Phenylacetates Chromatography Aqueous solution Ecology Chemistry Anti-Inflammatory Agents Non-Steroidal beta-Cyclodextrins General Medicine Permeation 021001 nanoscience & nanotechnology eye diseases Sclera medicine.anatomical_structure Drug delivery 030221 ophthalmology & optometry sense organs Ophthalmic Solutions 0210 nano-technology Agronomy and Crop Science medicine.drug |
| Zdroj: | AAPS PharmSciTech. 19(6) |
| ISSN: | 1530-9932 |
| Popis: | Nepafenac is a nonsteroidal anti-inflammatory drug (NSAID), currently only available as 0.1% ophthalmic suspension (Nevanac®). This study utilized hydroxypropyl-β-cyclodextrin (HPBCD) to increase the water solubility and trans-corneal permeation of nepafenac. The nepafenac-HPBCD complexation in the liquid and solid states were confirmed by phase solubility, differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), and nuclear magnetic resonance spectroscopy (NMR) analyses. Nepafenac 0.1% ophthalmic solution was formulated using HPBCD (same pH and osmolality as that of Nevanac®) and pig eye trans-corneal permeation was studied versus Nevanac®. Furthermore, nepafenac content in cornea, sclera, iris, lens, aqueous humor, choroid, ciliary body, retina, and vitreous humor was studied in a continuous isolated pig eye perfusion model in comparison to the suspension and Nevanac®. Permeation studies using porcine corneas revealed that the solution formulation had a permeation rate 18 times higher than Nevanac®. Furthermore, the solution had 11 times higher corneal retention than Nevanac®. Drug distribution studies using porcine eyes revealed that the solution formulation enables detectable levels in various ocular tissues while the drug was undetectable by Nevanac®. The ocular solution formulation had a significantly higher drug concentration in the cornea compared to the suspension or Nevanac®. |
| Databáze: | OpenAIRE |
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