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Preparation, characterization and in vitro evaluation of melatonin-loaded porous starch for enhanced bioavailability
Carbohydrate Polymers ( IF 11.2 ) Pub Date : 2018-08-30 , DOI: 10.1016/j.carbpol.2018.08.127
Yuanyuan Li , Xiuhua Zhao , Lingling Wang , Yanjie Liu , Weiwei Wu , Chen Zhong , Qian Zhang , Jianhang Yang

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 Cmax of 134.26 and 291.77 ng/mL at 15 and 20 min, respectively. The AUC0–360min of the formulated MPS-treated group was approximately 2.34-fold higher than that of raw MLT.



中文翻译:

褪黑素多孔淀粉的制备,表征和体外评价以提高生物利用度

本工作旨在应用多孔淀粉(PS)作为载体,以改善难溶性褪黑激素(MLT)的口服生物利用度。优化了载有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,Brunauer-Emmett-Teller表面积,傅立叶变换红外光谱,X射线衍射,差示扫描量热法和热重分析法分析了MPS的特征。大多数MLT在PS孔中转变为无定形形式。与SGF和SIF中的原始MLT相比,MPS显示出更高的MLT溶解度和累积释放速率。与原始MLT相比,MPS对DCFH-DA氧化的过氧自由基的抑制作用更高,EC50更低。此外,MLT和MPS的血浆浓度达到C max在15和20分钟时分别达到134.26 ng / mL和291.77 ng / mL。配制MPS处理组的AUC 0–360min大约比原始MLT高2.34倍。

更新日期:2018-08-31
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