摘要

pH-sensitive lappaconitine-loaded kappa-carrageenan microparticle (LA-KCG-MP), a degradable, high-load, ionic biopolymer, was prepared using a two-step self-assembly method. Cation exchange resin was selected to degrade kappa-carrageenan (KCG). By investigating the reaction time, temperature, and resin dose, the optimum reaction conditions were determined. Degraded KCG was then easily loaded with a hydrophobic drug, lappaconitine (LA), forming lappaconitine-loaded kappa-carrageenan (LA-KCG) by electrostatic self-assembly. LA-KCG-MP can be prepared by LA-KCG using secondary self-assembly by dialysis subsequently. The loading capacity, release behavior, and pH sensitivity of LA as well as its analgesic properties were determined. Results showed that KCG could be a novel natural polymeric carrier to load a hydrophobic alkaloid, since no synthetic polymer was involved. Furthermore, the loading capacity reached up to 26 % (w/w). Also, LA loaded with KCG was released faster in an acidic environment than that in a neutral environment. The loading capacity and pH sensitivity increased with a decrease in the molecular weight of KCG. In addition, animal analgesic experiments showed that LA-KCG-MP of low molecular weight had earlier onset time and longer duration. These results suggested that KCG of low molecular weight had great potential to achieve the synergistic effect of LA.