0 45

Cited 1 times in

Intracorneal melatonin delivery using 2-hydroxypropyl-β-cyclodextrin ophthalmic solution for granular corneal dystrophy type 2

Authors
 Jun-Hyun Ahn  ;  Hyun-Do Kim  ;  Sharif-Md Abuzar  ;  Ji-Yeon Lee  ;  Su-Eon Jin  ;  Eung Kweon Kim  ;  Sung-Joo Hwang 
Citation
 International Journal of Pharmaceutics, Vol.529(1~2) : 608-616, 2017 
Journal Title
 International Journal of Pharmaceutics 
ISSN
 0378-5173 
Issue Date
2017
MeSH
2-Hydroxypropyl-beta-cyclodextrin/chemistry* ; Animals ; Cornea ; Corneal Dystrophies, Hereditary/drug therapy* ; Drug Delivery Systems* ; Melatonin/pharmacology* ; Ophthalmic Solutions/pharmacology* ; Rabbits ; Solubility ; beta-Cyclodextrins
Keywords
2-Hydroxypropyl-β-CD (PubChem CID: 14049689) ; Corneal epithelium ; Cyclodextrin ; Granular corneal dystrophy type 2 ; Melatonin ; Melatonin (PubChem CID: 896) ; Ocular irritation ; Phase solubility ; Potassium chloride (PubChem CID: 4873) ; Sodium chloride (PubChem CID: 5234) ; α-Cyclodextrin (PubChem CID: 444913) ; β-Cyclodextrin (PubChem CID: 444041) ; γ-cyclodextrin (PubChem CID: 5287407)
Abstract
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.
Full Text
https://www.sciencedirect.com/science/article/pii/S0378517317306154
DOI
10.1016/j.ijpharm.2017.07.016
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Ophthalmology (안과학교실) > 1. Journal Papers
Yonsei Authors
김응권(Kim, Eung Kweon) ORCID logo https://orcid.org/0000-0002-1453-8042
Export
RIS (EndNote)
XLS (Excel)
XML
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/160483
사서에게 알리기
  feedback

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

Browse