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Impregnation of collagen corneal shields with liposomes: Uptake and release of hydrophilic and lipophilic marker substances

 

作者: GrammerJoachim B.,   KortümFlorence A.,   WolburgHartwig,   LüdtkeRainer,   HeinzKarl,   JürgenHans,   PleyerUwe,  

 

期刊: Current Eye Research  (Taylor Available online 1996)
卷期: Volume 15, issue 8  

页码: 815-823

 

ISSN:0271-3683

 

年代: 1996

 

DOI:10.3109/02713689609017622

 

出版商: Taylor&Francis

 

关键词: carboxyfluorescein;collagen corneal shield;liposomes;phosphatidylethanolamine-rhodamine B;release kinetics

 

数据来源: Taylor

 

摘要:

PurposeLiposomes and collagen corneal shields (CCS) have been used as ophthalmic drug delivery devices. With regard to a possibly combined application, we studied the effects of surface charge and bilayer fluidity of liposomes on their uptake and release by CCS.Methods12-hours-CCS were soaked in large unilamellar liposomes, which had been labelled with 4,5-carboxyfluorescein (CF) and N-(lissamine rhodamine B sulfonyl)-diacylphosphatidylethanolamine (PE-RhB) in the aqueous space and in the liposome bilayer, respectively. Released fluorophores were determined fluorometrically in the elution buffer at intervals from 1 to 240 min after immersion.ResultsThe CF concentration in the CCS soaked in a CF solution was two to seven times higher than immersion in the liposome suspensions. Among those, the negatively charged, cholesterol-containing preparation led to the highest CF concentration in the CCS. The PE-RhB concentration was highest after soaking the CCS in neutral, cholesterol-free liposomes. All types of liposomes were found inside the CCS by freeze fracture electron microscopy. The release kinetics data indicate a first order release. More than 90% of CF was released by the CCS within the first 30 min. This was equal after soaking the CCS in the CF solution or in liposomes. With DOPC-liposomes, the maximal release was already attained after 10 min. In general, the differences in the release kinetics of both hydrophilic and lipophilic markers, obtained by the various liposome types were small.ConclusionsOur results indicate that surface charge and bilayer fluidity are of minor importance for the interaction with collagen corneal shields. However, since the release kinetics of a liposomeencapsulated hydrophilic or lipophilic substance are similar to the release of a non-encapsulated drug, the combination of liposomes with collagen shields may be useful mainly with respect to the encapsulation of drugs which do not penetrate the ocular surface as well as to prolong corneal contact time of the liposomes. Curr. Eye Res. 15: 815–823, 1996.

 

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