Preparation and evaluation of solid lipid nanoparticles of XXXX for ocular drug delivery system in vitro and in vivo.

@entity72469 @entity7651 @entity95
PURPOSE: To prepare and evaluate the solid lipid nanoparticles of @entity7651 (BA- @entity72469 ) for ocular drug delivery system. METHODS: The BA- @entity72469 was prepared by emulsification/ultrasonication method. The appearance of BA- @entity72469 was examined by the negative stain method. The mean diameter and zeta potential of BA- @entity72469 were determined using a Zetasizer. The entrapment efficiency of BA- @entity72469 was determined by Sephadex-G50 column. And the solid-state characterization of BA- @entity72469 was analyzed by DSC and X-ray. The release of drug from BA- @entity72469 was evaluated using dialysis bag diffusion technique. The effects of @entity72469 on corneal permeability of @entity7651 were investigated in vitro, using isolated @entity95 corneas. The in vivo ocular irritation of BA- @entity72469 was tested by pathological section observation using @entity95 . The pharmacokinetics was evaluated by microdialysis in the @entity95 aqueous humors. RESULTS: The results showed that the BA- @entity72469 had an average diameter of 91.42    1.02 nm with a zeta potential of -33.5    -1.28 mV and the entrapment efficiency of 62.45    1.67%. In vitro release studies indicated that the BA- @entity72469 retained the drug entity better than the @entity7651 ophthalmic solutions (BA-SOL). In the pharmacokinetics studies, the AUC value of BA- @entity72469 was 4.0-fold versus the BA-SOL (P < 0.01), and the Cmax value of BA- @entity72469 versus the BA-SOL was 5.3-fold (P < 0.01). CONCLUSION: @entity72469 can be used as a carrier to enhance ocular bioavailability of @entity7651 .
