Inclusion complexes of nateglinide with HP–β–CD and L-arginine for solubility and dissolution enhancement: preparation, characterization, and molecular docking …
Journal of Pharmaceutical Innovation, 2017•Springer
Purpose The objective of present study was to increase solubility and dissolution
performance of a poorly water soluble antidiabetic drug, Nateglinide (NAT), through
formation of inclusion complexes with hydroxypropyl-beta-cyclodextrin (HP–β–CD). The
effect of L-arginine (ARG), an amino acid, on the complexation efficiency and solubility
enhancing power of HP–β–CD was investigated by preparing ternary inclusion complexes.
Methods The binary and ternary inclusion complexes were prepared by physical mixing …
performance of a poorly water soluble antidiabetic drug, Nateglinide (NAT), through
formation of inclusion complexes with hydroxypropyl-beta-cyclodextrin (HP–β–CD). The
effect of L-arginine (ARG), an amino acid, on the complexation efficiency and solubility
enhancing power of HP–β–CD was investigated by preparing ternary inclusion complexes.
Methods The binary and ternary inclusion complexes were prepared by physical mixing …
Purpose
The objective of present study was to increase solubility and dissolution performance of a poorly water soluble antidiabetic drug, Nateglinide (NAT), through formation of inclusion complexes with hydroxypropyl-beta-cyclodextrin (HP–β–CD). The effect of L-arginine (ARG), an amino acid, on the complexation efficiency and solubility enhancing power of HP–β–CD was investigated by preparing ternary inclusion complexes.
Methods
The binary and ternary inclusion complexes were prepared by physical mixing, kneading, co-evaporation, and spray drying methods containing NAT, HP–β–CD, and ARG. The complexes were characterized by FTIR, DSC, PXRD, and 1H–NMR. Molecular modeling study revealed that introduction of ternary agent ARG have improved the interactions of NAT and HP–β–CD.
Results
The complex prepared by spray drying method showed the highest increase in solubility and dissolution rate compared to other methods. Molecular docking study revealed that ARG interactions plays an essential role in increasing the stability and solubility of the complex.
Conclusions
The present study demonstrated increase in solubility and dissolution of NAT. Hence, ternary complexes of NAT can be used as an efficient tool for the delivery of insoluble drug, NAT.
Springer
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