| 丛萌逸,王海鹏,殷加奇,等.一种新型海洋多糖纳米材料的制备及载药特性研究[J].中国海洋药物,2017,36(1):76-82. |
| 一种新型海洋多糖纳米材料的制备及载药特性研究 |
| Synthesis and Characterization of a Novel Marine Polysaccharide Based Nanoparticle |
| 投稿时间：2016-07-06 修订日期：2016-07-29 |
| DOI： |
| 中文关键词: 海洋多糖 聚甘露糖醛酸 他克莫司 纳米材料 载药胶束 |
| English Keywords:Marine polysaccharide Polymannuronic acid Tacrolimus Nanoparticle material Drug loaded micelle |
| Fund Project: |
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| 中文摘要: |
| 目的 以天然海洋多糖聚甘露糖醛酸(PM)为原料，制备一种生物相容、生物可降解纳米材料，以难溶性药物他克莫司（FK506）为模型药物制备载药胶束，并对其体外释药特性进行考察。方法 以油胺为疏水端，与PM通过酰胺反应制备纳米材料，利用FT-IR、1H-NMR对其结构进行表征。通过超声乳化法制备FK506胶束，利用原子力显微镜与马尔文激光粒度仪分析载药胶束的形态、粒径及zeta-电位。利用高效液相色谱法测定FK506胶束的载药量和包封率。采用体外透析法分析FK506胶束的体外释放特性。结果 油胺与PM等摩尔比投料反应的枝接率为56.8%，FK506胶束外形为球状且分散均匀，粒径大小在 100~150 nm，zeta-电位为?50 mV，多分散系数＜0.2，载药量和包封率分别为17.6±0.21% 和97.7±1.19%。体外释药分为2个阶段，前12 h释放较快，释放药物的64.5±5.8%，后一阶段药物释放较慢，至48 h时可释放药物89.2±6.9%。结论 成功制备生物可降解的PM纳米材料，以其为载体制得的FK506胶束可以提高FK506的溶解性，在体外具有明显的缓释特征，PM纳米材料具有良好的应用前景。 |
| English Summary: |
| To prepare a novel biodegradable and biocompatible nanoparticle material based on modification of polymannuronic acids (PM), which is a marine polysaccharide extracted from seaweed. To prepare tacrolimus (FK506) micelle using this nanoparticle material and characterize its drug loading properties, investigate its physic-chemical properties in vitro. Methods Hydrophobic oleyl amine was used to modify PM, and its structure was confirmed by Fourier-transformed infrared spectrometry (FT-IR) and nuclear magnetic resonance (1 H-NMR). FK506 micelle was prepared by solvent evaporation method. The morphology, particle size and zeta potential of it were characterized by atomic force microscopy (AFM) and malvern laser particle size analyzer. High performance liquid chromatography (HPLC) method was employed to
measure drug loading and encapsulation efficiency. A dialysis method was used to determine the release behaviors of FK506 micelle in vitro. Results The Grafting yield of PM nanoparticles is 56.81%. FK506 micelles are well dispersed as individual nanoscaled micelles with regular spherical shape. The particle size was in the range of 100-150 nm, zeta potential was -50 mV and polydisperse index was below 0.2. Drug loading and encapsulation efficiency were 17.6±0.21% and 97.7±1.19%, respectively. The release behavior of FK506 micelle has two stages, including a relatively fast stage (64.5±5.8% of drug was released in the first 12 h) and a long lasting stage (89.3±6.9% of drug was released in 48 h). Conclusions A biodegradable and biocompatible PM nanoparticles material and FK506 micelle were prepared successfully. FK506 micelle increased the solubility of FK506 and exhibited satisfactory sustained-release characteristics in vitro. The PM nanoparticles material has a potential prospect as a drug carrier. |
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