Preparation, characterization and in vitro evaluation of melatonin-loaded porous starch for enhanced bioavailability

Yuanyuan Li; Xiuhua Zhao; Lingling Wang; Yanjie Liu; Weiwei Wu; Chen Zhong; Qian Zhang; Jianhang Yang

doi:10.1016/j.carbpol.2018.08.127

Preparation, characterization and in vitro evaluation of melatonin-loaded porous starch for enhanced bioavailability

Carbohydr Polym. 2018 Dec 15:202:125-133. doi: 10.1016/j.carbpol.2018.08.127. Epub 2018 Aug 30.

Authors

Yuanyuan Li¹, Xiuhua Zhao², Lingling Wang¹, Yanjie Liu¹, Weiwei Wu¹, Chen Zhong³, Qian Zhang¹, Jianhang Yang¹

Affiliations

¹ Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China.
² Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China. Electronic address: xiuhuazhao@nefu.edu.cn.
³ College of Life Science, Northeast Forestry University, Harbin 150040, Heilongjiang, China.

PMID: 30286985
DOI: 10.1016/j.carbpol.2018.08.127

Abstract

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_max of 134.26 and 291.77 ng/mL at 15 and 20 min, respectively. The AUC_0-360min of the formulated MPS-treated group was approximately 2.34-fold higher than that of raw MLT.

Keywords: Bioavailability; Cellular antioxidant activity; Melatonin (PubChem CID: 896); Porous starch; Release.