Institute of Biomedical Engineering, Chinese Academy of Medical Sciences, Peking Union Medical College, The Key Laboratory of Biomedical Material of Tianjin, Tianjin 300192, PR China.
Drug Deliv. 2010 Sep-Oct;17(7):552-8. doi: 10.3109/10717544.2010.490250.
To develop pullulan acetate nanoparticles (PANs) as a drug nanocarrier, pullulan acetate (PA) was synthesized and characterized. Its acetylation degree determined by the proton nuclear magnetic resonance ((1)H NMR) was 2.6. PANs were prepared by the solvent diffusion method and characterized by transmission electron microscope (TEM), size distribution, and zeta potential techniques. PANs had nearly spherical shape with a size range of 200-450 nm and low zeta potentials both in distilled water and in 10% FBS. The storage stability of PANs was observed in distilled water. PANs were stored for at least 2 months with no significant size and zeta potential changes. The safety of PANs was studied through single dose toxicity test in mice, and the result showed that PANs were well tolerated at the dose of 200 mg/kg in mice. Epirubicin-loaded PANs (PA/EPI) were also prepared and characterized in this study. Moreover, the in vivo pharmacokinetics of PA/EPI was investigated. Compared with the free EPI group, the PA/EPI group exhibited higher plasma drug concentration, longer half-life time (t(1/2)) and the larger area under the curve (AUC). All results suggested that PANs were stable, safe, and showed a promising potential on improving the bioavailability of the loaded drug of the encapsulated drug.
为了开发用作药物纳米载体的支链淀粉醋酸酯纳米粒（PANs），合成并表征了支链淀粉醋酸酯（PA）。通过质子核磁共振（1H NMR）确定其乙酰化程度为 2.6。通过溶剂扩散法制备了 PANs，并通过透射电子显微镜（TEM）、粒径分布和zeta 电位技术对其进行了表征。PANs 具有近乎球形的形状，粒径范围为 200-450nm，在蒸馏水和 10% FBS 中的 zeta 电位均较低。在蒸馏水中观察到了 PANs 的储存稳定性。PANs 在至少 2 个月内保持稳定，粒径和 zeta 电位没有明显变化。通过小鼠单次毒性试验研究了 PANs 的安全性，结果表明 PANs 在 200mg/kg 剂量下在小鼠中具有良好的耐受性。本研究还制备并表征了载表阿霉素的 PANs（PA/EPI）。此外，研究了 PA/EPI 的体内药代动力学。与游离 EPI 组相比，PA/EPI 组表现出更高的血浆药物浓度、更长的半衰期（t1/2）和更大的曲线下面积（AUC）。所有结果表明，PANs 稳定、安全，并显示出在提高封装药物的载药生物利用度方面具有广阔的应用前景。
