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Cyclosporine a micellar delivery system for dry eyes

Other Titles
 안구건조증을 위한 사이클로스포린 에이의 미셸 전달 시스템 
Authors
 강한 
Issue Date
2013
Description
Dept. of Pharmacy/석사
Abstract
The aim of this thesis was to develop ophthalmic cyclosporine A micellar delivery system. Cyclosporine A (CsA) is not only an immunosuppressant but also a drug for improving tear production in patients with keratoconjunctivitis sicca, Sjörgren syndrome and dry eye syndrome. But it is difficult to make the stable CsA ophthalmic drug due to the relatively high molecular weight (1202.61) and poor solubility. The CsA micellar delivery systems were prepared only by mixing and homogenizing. Cremophor EL as surfactant and ethanol as cosolvent were chosen by solubility test. pH, osmolarity, particle size and therapeutic efficacy were evaluated. Droplet size was assessed to check critical micelle concentration (CMC) in various micelle formulations. If CsA were sufficiently wetted, micelle formulations were observed about 14nm on size when concentration of Cremophor EL was more than 1%.The stability of CsA micelle solution was assessed as a function of pH, and concentration of Cremophor EL and ethanol by pH meter, osmometer, electrophoretic light scattering spectrophotometer (ELS-Z) and high-performance liquid chromatography (HPLC). These micelle solutions had osmolarity of about 280mOsmol to 320mOsmol and mean size of about 15nm to 25nm. The significant change of pH, osmolarity, droplet size and content measurement are not shown. Also, other visible changes like the aggregation or the phase separation were not shown.Schirmer tear test with New Zealand albino rabbits showed that micelle formulation of this study was more effective comparing with the commercial CsA emulsion on the increasing tear production. Similar with previous commercial formulation, recovery of goblet cell density and epithelium was observed in H&E staining.In conclusion, CsA micellar delivery system for dry eyes can offer a great stability and therapeutic efficacy. Furthermore, CsA micellar delivery system is an advantageous technique for shorter processing time and scale-up.
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/134406
Appears in Collections:
2. Thesis / Dissertation (학위논문) > 5. Others (기타) > Others (기타)
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