In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect ...In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect and preliminary stability.APT011-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique.The L9(34)orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation.Microscope photographs showed that APT011-loaded microspheres were spherical,and the particle size was^90μm with uniform size distribution.XRD results indicated that APT011 existed in the microspheres in an amorphous form.DSC results showed that there was no significant interaction between APT011 and blank microspheres.APT011-loaded microspheres had a significant sustained-release effect,which maintained release for at least 2 months.Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.展开更多
基金National Science&Technology Major Project“Key New Drug Creation and Manufacturing”(Grant No.2019ZX09201001-003-007)。
文摘In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect and preliminary stability.APT011-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique.The L9(34)orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation.Microscope photographs showed that APT011-loaded microspheres were spherical,and the particle size was^90μm with uniform size distribution.XRD results indicated that APT011 existed in the microspheres in an amorphous form.DSC results showed that there was no significant interaction between APT011 and blank microspheres.APT011-loaded microspheres had a significant sustained-release effect,which maintained release for at least 2 months.Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.
