Positively charged amphiphilic chitosan derivative for the transscleral delivery of rapamycin

摘要: Purpose We explored the potential of an amphiphilic chitosan derivative to facilitate transscleral delivery rapamycin, a multitherapeutic agent with poor water solubility. Methods The derivative, O-octanoyl-chitosan-polyethylene glycol (OChiPEG) graft copolymer, was analyzed using Fourier-transform infrared spectroscopy (FT-IR). OChiPEG micelles were prepared via thin film method and characterized for their size dynamic light scattering (DLS), zeta laser Doppler velocimetry (LDV), morphology transmission electron microscopy (TEM), drug entrapment efficiency (EE), loading (DL) reversed-phase high performance liquid chromatography (RP-HPLC), critical micelle concentration (CMC) spectrofluorometry, thermal properties differential scanning calorimetry (DSC) x-ray powder diffraction (XRPD). Scleral permeation retention rapamycin from drug-loaded determined in porcine sclera clamped Ussing chambers, RP-HPLC. Results Conjugation hydrophilic hydrophobic groups confirmed FT-IR. Rapamycin-loaded particle 40.6 nm + 6.84 mV successfully. These carriers exhibited EE DL 85.6 16.3%, respectively, CMC 16.6 μM. showed scleral (14.8 ± 0.81 μg/g) successful (5.57 1.04 × 10(-8) cm(2) · s(-1)). Conclusions Positively charged loaded therefore may be useful topical other agents.