Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China.
Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China.
Carbohydr Polym. 2018 Dec 15;202:125-133. doi: 10.1016/j.carbpol.2018.08.127. Epub 2018 Aug 30.
The present work aimed to apply porous starch (PS) as carrier to improve the oral bioavailability of poorly soluble drug melatonin (MLT). The drug loading and encapsulation efficiency of MLT-loaded porous starch (MPS) were optimized. The characteristics of MPS were analyzed using scanning electron microscopy, Brunauer-Emmett-Teller surface area, Fourier-transform infrared spectroscopy, x-ray diffraction, differential scanning calorimetry and thermo gravimetric analysis. Most MLT transformed into their amorphous form in the PS pores. MPS showed higher MLT solubility and cumulative release rate compared with raw MLT in SGF and SIF. MPS exhibited a higher inhibition to DCFH-DA-oxidized peroxyl radicals at a lower EC50 than that of the raw MLT. Furthermore, the plasma concentrations of MLT and MPS reached a C of 134.26 and 291.77 ng/mL at 15 and 20 min, respectively. The AUC of the formulated MPS-treated group was approximately 2.34-fold higher than that of raw MLT.
本工作旨在应用多孔淀粉（PS）作为载体来提高难溶性药物褪黑素（MLT）的口服生物利用度。优化了载 MLT 的多孔淀粉（MPS）的载药量和包封效率。使用扫描电子显微镜、BET 比表面积、傅里叶变换红外光谱、X 射线衍射、差示扫描量热法和热重分析对 MPS 的特性进行了分析。大部分 MLT 在 PS 孔隙中转化为无定形形式。与 SGF 和 SIF 中的原 MLT 相比，MPS 显示出更高的 MLT 溶解度和累积释放率。MPS 在较低的 EC50 下对 DCFH-DA 氧化过氧自由基的抑制作用高于原 MLT。此外，MPS 组的血浆 MLT 和 MPS 浓度在 15 和 20 分钟时分别达到 134.26 和 291.77ng/mL。与原 MLT 相比，配方 MPS 处理组的 AUC 约高 2.34 倍。
