Preparation and In Vitro and In Vivo Evaluation of Sirolimus Ophthalmic Micelles
WANGLing1, SUNRu-ru2, TANGZhan1, WANGQiao1*
1. Institute of Materia Medica, Zhejiang Academy of Medical Sciences, Hangzhou 310013, China; 2. Zhejiang Jingxin Pharmaceutical Co., Ltd., Xinchang 312500, China
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.
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WANGLing, SUNRu-ru, TANGZhan, WANGQiao. Preparation and In Vitro and In Vivo Evaluation of Sirolimus Ophthalmic Micelles. Chinese Pharmaceutical Journal, 2019, 54(8): 638-645.
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2019, Vol. 54 
