Purpose:
To develop a novel injectable FK-506 micelles and the potential application in the treatment of uveoretinitis was primarily evaluated in rat model.
Methods:
Briefly, PEG-PCL diblock copolymer was prepared by ring-opening copolymerization of e-CL initiated by MPEG at 130oC using Sn(Oct)2 as catalyst.To improve the water solubility of FK506, thin-film method was employed to develop a novel FK506 nanoformulation based on MPEG-PCL copolymer.Briefly, 0.2g of FK506 and 0.8g of MPEG-PCL copolymer were co-dissolved into 10ml acetone solution, and then evaporated by a rotary evaporation at 37oC. Finally,the product was re-suspended into 40ml water solution at 55oC to obtain FK506 nanoformulation. The obtained FK 506 nanoformulation was lyophilized and storage at 4oC for further usage. In the rate model, rats were intravitreally injected with saline, FK506, FK506 nanoformulation and its efficiency on the inflammation was evaluated.
Results:
Due to the solubilization of MPEG-PCL co-polymer, the water solubility of FK506 was greatly improved,and the obtained FK506 nanoformulation could be freeze-dried into a power state while could re-dissolved into the water solution. As presented in Fig.1, the obtained FK506 nanoformulation were uniform particle size (about 50nm) and monodisperse with no aggregation. Meanwhile, the preliminary study on the rate model revealed that the application of FK506 nanoformulation could significantly reduce the intraocular inflammation and markedly inhibite the development of uveoretinitis .
Conclusions:
In the presented paper, a novel FK 506 micelles was developed and its potential application in the treatment of uveoretinitis was investigated. The results suggested that the application of FK506 nanoformulation could significantly reduce the intraocular inflammation and markedly inhibite the development of uveoretinitis .
Keywords: drug toxicity/drug effects