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Abstract
In this study liposome coated with low molecular weight chitosan (LCH) was proposed
and investigated its in vitro and in vivo properties, and its potential use in ocular
drug delivery was evaluated. LCH with a molecular weight of 8kDa was prepared and
coated on liposome loaded with diclofenac sodium. The LCH coating changed the liposome
surface charge and slightly increased its particle size, while the drug encapsulation
was not affected. After coating, the liposome displayed a prolonged in vitro drug
release profile. LCH coated liposome also demonstrated an improved physicochemical
stability at 25 degrees C in a 30-day storage period. The ocular bioadhesion property
was evaluated by rabbit in vivo precorneal retention, and LCH coated liposome achieved
a significantly prolonged retention compared with non-coated liposome or drug solution.
The LCH coating also displayed a potential penetration enhancing effect for transcorneal
delivery of the drug. In the ocular tolerance study, no irritation or toxicity was
caused by continual administration of LCH coated liposome in a total period of 7 days.
In conclusion, the LCH coating significantly modified the properties of liposome and
brought a series of notable advantages for ocular drug delivery.