Intracorneal melatonin delivery using 2-hydroxypropyl-β-cyclodextrin ophthalmic solution for granular corneal dystrophy type 2
| Autor: | Sung Joo Hwang, Eung Kweon Kim, Su Eon Jin, Sharif Md Abuzar, Jun Hyun Ahn, Ji Yeon Lee, Hyun D. Kim |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
medicine.medical_treatment
Pharmaceutical Science Beta-Cyclodextrins 02 engineering and technology Pharmacology medicine.disease_cause 030226 pharmacology & pharmacy Cornea 03 medical and health sciences Drug Delivery Systems 0302 clinical medicine medicine Animals Solubility Melatonin Corneal epithelium Corneal Dystrophies Hereditary chemistry.chemical_classification Chromatography Cyclodextrin beta-Cyclodextrins Ocular Absorption Eye drop 021001 nanoscience & nanotechnology eye diseases 2-Hydroxypropyl-beta-cyclodextrin medicine.anatomical_structure chemistry Rabbits sense organs Ophthalmic Solutions Irritation 0210 nano-technology |
| Zdroj: | International Journal of Pharmaceutics. 529:608-616 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2017.07.016 |
| Popis: | Melatonin (MT), an effective antioxidant, has therapeutic implications for granular corneal dystrophy type 2 (GCD2) treatment. Eye drop formulations containing cyclodextrins (CDs) were studied with the objective of improving MT solubility, stability, and ocular absorption, while decreasing eye irritation. MT complexes with αCD, βCD, γCD, and 2-hydroxypropyl-βCD (HPβCD) were characterized by phase solubility studies, which demonstrated Higuchi's AL-type phase solubility profiles. The MT/HPβCD complex showed the highest MT solubility (2.75mg/mL). Ocular irritation experiments showed HPβCD inclusion alleviated irritation of the eye. After administration of MT formulations to rabbit corneas, each harvested cornea was separated into corneal epithelium, stroma, and endothelium. MT concentrations in the corneal epithelium, stroma, and endothelium for the F1-treated group were 55.5±9.24, 26.7±2.66, and 21.1±1.77μM while those for the F2-treated group were 127.2±21.01, 43.7±16.93, and 51.0±13.91μM, respectively. Stability studies for 60days showed no significant change in pH, osmolarity, and MT content. In conclusion, MT/HPβCD formulations can lower irritation, enhance MT stability, and improve therapeutic efficacy. |
| Databáze: | OpenAIRE |
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