Preparation and In Vitro and In Vivo Evaluation of Sirolimus Ophthalmic Micelles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare sirolimus micelles for the purpose of improving the solubility and applicability in the eye. METHODS: Sirolimus micelles were prepared by thin-film dispersion with Tween-80 and polyoxyethylene stearate (P40S) as carriers. Size distribution, X-ray diffraction spectra, IR spectra and encapsulation efficiency were used to evaluated the character of micelles. The in vitro release and scleral permeability were investigated, and the pharmacokinetics of micelles formulation in rabbit aqueous humor was preliminarily studied. RESULTS: The average particle size was (12.36±0.21) nm, the mean potential was (-6.08±0.98) mV, and the entrapment efficiency was (99.6±0.20)%. Both X-ray diffraction and IR spectra showed that there was almost no free drug. The in vitro release and scleral permeation profiles were in accordance with Higuchi equation. The pharmacokinetic RESULTS: of aqueous humor showed that sirolimus micelles could reach and maintain the therapeutic concentration in the eye for a long time. CONCLUSION: The prepared sirolimus ophthalmic micelles is suitable for ocular administration and is expected to become a promising formulation in the treatment of immune rejection for corneal transplantation.