Preparation of lappaconitine-loaded chitosan/sodium β-glycerophosphate injectable thermosensitive hydrogels and research on its properties / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare lappaconitine (LA)-loaded chitosan/sodium β-glycerophosphate (CS/β-GP) thermosensitive hydrogels and investigate its phase transition mechanism of gel formation process and release properties in vitro. METHODS: The injectable CS/β-GP thermosensitive hydrogels were prepared with biodegradable CS as carrier material and β-GP as coagulation accelerator.The release behavior in vitro was studied by dynamic dialysis, and the phase transition mechanism of gel formation process was further investigated by rheologieal method. RESULTS: The optimized process condition was as follows;the concentration of β-GP and CS was 560 and 22 mg·mL-1, respectively, CS was dissolved by 0.1 mol·L-1 HOAc, and the valume ratio of CS to β-GP was 8.751.25 (V/V), the gelation time of CS/β-GP thermosensitive hydrogels with volume ratio of 8.751.25 (V/V) at 37℃ was 5 min 38 s.The in vitro release study showed that these injectable CS/β-GP thermosensitive hydrogels had sustained release effect for LA, and the release behavior could be well described by the Higuchi model and Korsmeyer-Peppas model.The mechanism of LA releasing from CS/β-GP thermosensitive hydrogels was attributed to drug dissolution and diffusion.Rheologieal studies showed that the CS/β-GP thermosensitive hydrogels belonged to thixotropic system and exhibited non-Newtonian and shear-thinning fluid behavior as well as "solid-like" gelatin behavior. CONCLUSION: LA-Loaded CS/β-GP injectable thermosensitive hydrogels with good elasticity and gel strength properties are prepared successfully, and they show sustained release effect of LA in vitro.