Abstract: A novel chitosan amphiphilic derivative with high degree of substitution, N,N-dilauryl-3,6-O-sulfopropyl chitosan (SPDLCS), was synthesized. PTX-loaded SPDLCS micelles were prepared by a dialysis method. The impact of the feed ratio of SPDLCS to PTX on drug-loading concentration and its efficiency, together with the mean diameter and Zeta potential were investigated. The morphology and stability of micelles were further studied. The results show that SPDLCS self-assembled nanomicelle with amorphous PTX inside was successfully prepared. The drug loading concentration (DLC) and drug loading efficiency(DLE) of PTX-loaded SPDLCS micelles with the average size of 141.1 nm, zeta potential of -34.1 mV and spherical shape were as high as 50.36 % and 92.2 % respectively under the optimal feed ratio of SPDLCS∶PTX = 1∶1.1. The results of stability test show that the micelles system with the DLC of 50.36 % displays good stability and the PTX concentration of 6.08 mg/mL was found in this aqueous solution, which has not been reported yet. It suggests that the product SPDLCS may be used as a carrier material with a high solubilization capacity for hydrophobic drug.

Key words: amphiphilic chitosan, polymeric micelles, paclitexel, solubilization

摘要： 合成高取代度的N,N-双十二烷基-3,6-O-磺丙基壳聚糖（SPDLCS）双亲性衍生物，通过透析法制备了SPDLCS载紫杉醇（PTX）胶束，考察了投料比对载药量、包封率、胶束粒径和Zeta电位的影响，并对胶束形态及其稳定性进行了研究。结果表明，紫杉醇以无定形态包载于胶束的疏水内核中，最优投料比为SPDLCS∶PTX=1∶1.1，载药量为50.36 %，包封率为92.2 %，对紫杉醇的增溶能力达6.08 mg/mL。载药胶束呈现分散性良好的球形颗粒，平均粒径为141.1 nm，Zeta电位为?34.1 mV。稳定性实验表明SPDLCS载紫杉醇胶束具有良好的稳定性，SPDLCS是潜在的疏水药物高增溶载体材料。

关键词: 双亲性壳聚糖衍生物, 聚合物胶束, 紫杉醇, 增溶