Preparation Of JR400 Nanoparticles

In order to expand the preparation system of drug loaded nanoparticles for sustained release,JR400 and CMC based JR400/CMC and CaCl₂/JR400/CMC nanoparticles were prepared.The nanoparticles were characterized and analyzed by Nano Zetasizer,Fu Liye transform infrared spectrometer（FT-IR）,X-ray diffractometer（XRD）,differential scanning calorimeter（DSC）and scanning electron microscope（SEM）.Curcumin（CUR）and berberine hydrochloride（BBR）were selected as the hydrophobic and hydrophilic model drugs,respectively.The loading capacity and release capability in vitro of CUR and BBR were researched by ultraviolet spectrophotometer（UV）.The optimized producing condition of JR400/CMC nanoparticles were that the concentration of JR400 was 0.08%（m/m）,the concentration of CMC was 0.10%（m/m）,and the mass ratio of JR400 to CMC was 1.16:1.JR400/CMC nanoparticles were spherical in shape and the average size was roughly 250-300 nm with the zeta potential of（-43.5±1.7）mV.When CUR to CMC ratio was 10:1（mg/g）,the encapsulation efficiency（EE）and loading capacity（LC）for CUR were（54.27±2.42）%and（12.06±0.45）%,respectively.When BBR to CMC ratio was 60:1（mg/g）,EE and LC for BBR were（18.05±1.15）%and（26.07±1.99）%,respectively.In the in vitro release study,the cumulative release percentage of CUR within the first 4 h was approximately 38%and within 84 h was nearly 91%.The release rate of BBR was fast and BBR was released completely within 12 h.The optimized producing condition of CaCl₂/JR400/CMC nanoparticles were that the concentration of CaCl₂ was 1.00%（m/m）,the amount of added CaCl₂ solution was5.00 g,the concentration of JR400 was 0.08%（m/m）,the concentration of CMC was0.10%（m/m）,and the mass ratio of JR400 to CMC was 0.31:1（m/m）.CaCl₂/JR400complexes were approximately cuboid in shape and the average size was roughly 260nm with the zeta potential of（13.6±2.3）mV.And CaCl₂/JR400/CMC nanoparticles were cuboid in shape and the average size was nearly 260 nm with the zeta potential of（-32.1±0.6）mV.When CUR to CMC ratio was 5.5:1（mg/g）,the EE and LC for CUR were（75.86±4.12）%and（11.92±0.51）%,respectively.When BBR to CMC ratio was120:1（mg/g）,EE and LC for BBR were（11.41±2.36）%and（44.25±4.02）%,respectively.In the in vitro release study,the cumulative release percentage of CUR within the first 12 h was approximately 35%and within 168 h was nearly 99%.The release rate of BBR was fast and BBR was released completely within 12 h.JR400/CMC and CaCl₂/JR400/CMC nanoparticles revealed remarkable sustained release effect for hydrophobic drugs.Meanwhile,CaCl₂/JR400/CMC nanoparticles compared to JR400/CMC nanoparticles exhibited stronger sustained release effect for hydrophobic drugs.CaCl₂/JR400/CMC nanoparticles revealed sustained release effect for hydrophilic drugs.However,JR400/CMC nanoparticles did not reveal sustained release effect for hydrophilic drugs.It was found that hydrophobic drugs loaded CaCl₂/JR400/CMC nanoparticles could release for 7 d.Therefore,CaCl₂/JR400/CMC nanoparticles present considerable potential as the hydrophobic drugs sustained release carrier.