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目的：制备壳聚糖和帕米膦酸双修饰的固体脂质纳米粒。方法：首先利用课题组发表的专利合成帕米膦酸修饰Brij78 的新型非离子表面活性剂（Pa-Brij78），然后以壳聚糖（CS）溶液为水相，Pa-Brij78 为乳化剂，E-Wax 为油相，采用微乳法，利用修饰的帕米膦酸基团与壳聚糖分子链中质子化的氨基交联反应原理，通过一系列实验条件的探索，确定了最佳实验工艺条件，成功制备了壳聚糖和帕米膦酸双修饰的固体脂质纳米粒。通过动态光散射（DLS）粒径仪测定了纳米粒的粒径大小和Zeta 电位；透射电子显微镜（TEM）对CS-Pa-Brij78-SLNs的形貌结构进行了表征。结果：实验结果显示，制备壳聚糖和帕米膦酸双修饰的固体脂质纳米粒的最佳条件为：pH=6.0，壳聚糖浓度分别为0.1 %，0.2 %；反应温度65 ℃，反应时间40 min，在该条件下，制备的壳聚糖和帕米膦酸双修饰的固体脂质纳米粒（CS-Pa-Brij78-SLNs）粒径分别为97.9± 6.6 nm和182.4± 62.2 nm，表面电位分别为（+5.21 ± 1.4 mV）；（+7.94± 0.80 mV），装载姜黄素时，载药量为10 %，包封率在90 %以上，透射电镜下观察其形态圆整，清晰可见壳聚糖包裹的电晕。结论：本文以壳聚糖（CS）溶液为水相，合成的新型非离子表面活性剂Pa-Brij78 为乳化剂，E-Wax 为油相，采用微乳化法，经过最佳实验条件的探索，通过一步法成功制备了稳定的壳聚糖和帕米膦酸双修饰的固体脂质纳米粒（CS-Pa-Brij78-SLNs）。

英文摘要:

Objective:To prepare the chitosan and Pamidronate double-modified solid lipid nanoparticles.Methods:Firstly, a new non-ionic surfactant Pa-Brij78 using pamidronate (Pa) modified Brij78 (polyoxyethylene 20 stearyl ether) based on the patent research our group have published was synthesized. Then, chitosan (CS) solution was used as the aqueous phase, Pa-Brij78 as emulsifier, E-Wax as the oil phase, adopting microemulsion method and the reaction principle of modified pamidronate group (Pa) crosslink with the protonated amino in chitosan molecular chain. Chitosan and pamidronate double-modified solid lipid nanoparticles through exploring a range of experimental conditions and determine the optimumprocess conditions were successfully prepared. The particle size and Zeta potential was measured by Dynamic light scattering (DLS) particle size analyzer. The morphology of CS-Pa-Brij78-SLNs were characterized by transmission electron microscopy (TEM).Results:The results revealed that optimal conditions to prepare chitosan and pamidronate double- modified solid lipid nanoparticles (CS-Pa-Brij78-SLNs) as follows: pH = 6.0, chitosan concentration of 0.1 %, 0.2 %, the reaction temperature is 65 ℃ , reaction time 40min. Under these conditions, the average diameter of chitosan and pamidronate double-modified solid lipid nanoparticles (CS-Pa-Brij78-SLNs )were 97.9± 6.6 nm, 182.4± 62.2 nm and the Zeta potential were (+5.21± 1.4 mV); (+ 7.94 ± 0.80 mV), respectively. The chitosan-coated bisphosphonate (Pa) solid lipid nanoparticles were spherical in shape as shown under transmission electron microscopy.Conclusion:In this paper, we use chitosan (CS) solution as the aqueous phase, the new non-ionic surfactant Pa-Brij78 as emulsifier, E-Wax as the oil phase, adopting microemulsion method, we successfully one-step prepared stable chitosan and pamidronate double-modified solid lipid nanoparticles (CS-Pa-Brij78-SLNs) after exploring the optimal experimental conditions.

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