TY - JOUR
T1 - Inulin-pluronic-stearic acid based double folded nanomicelles for pH-responsive delivery of resveratrol
AU - Jangid, Ashok Kumar
AU - Patel, Krunal
AU - Jain, Poonam
AU - Patel, Sunita
AU - Gupta, Nitin
AU - Pooja, Deep
AU - Kulhari, Hitesh
N1 - Publisher Copyright:
© 2020
PY - 2020/11/1
Y1 - 2020/11/1
N2 - Herein, we introduce a novel amphiphilic bioconjugate (INU-F68-SA), synthesized by functionalization of pluronic F68 with a polysaccharide inulin (INU) and a lipid stearic acid (SA). The synthesis of INU-F68-SA was confirmed by FTIR and 1H-NMR analysis. INU-F68-SA can self-assemble into nanomicelles and therefore, its application in delivering of hydrophobic resveratrol (RSV) was investigated. The RSV-loaded INU-F68-SA nanomicelles (RSNM) had about 172 nm size, spherical shape, 0.237 polydispersity index, and −18 mV zeta potential. More importantly, the RSNM showed high drug entrapment efficiency, controlled drug release and protection of drug during storage. The RSNM significantly enhanced the cytotoxicity of RSV against colorectal cancer cells by inducing apoptosis and changing mitochondrial membrane potential. Further, in-vivo pharmacokinetic experiment indicated an improvement in pharmacokinetics of RSV after administering as RSNM. Thus, the use of self-assembled nanomicelles of amphiphilic INU-F68-SA bioconjugate could be a better alternative to overcome the poor in-vitro and in-vivo performance of RSV.
AB - Herein, we introduce a novel amphiphilic bioconjugate (INU-F68-SA), synthesized by functionalization of pluronic F68 with a polysaccharide inulin (INU) and a lipid stearic acid (SA). The synthesis of INU-F68-SA was confirmed by FTIR and 1H-NMR analysis. INU-F68-SA can self-assemble into nanomicelles and therefore, its application in delivering of hydrophobic resveratrol (RSV) was investigated. The RSV-loaded INU-F68-SA nanomicelles (RSNM) had about 172 nm size, spherical shape, 0.237 polydispersity index, and −18 mV zeta potential. More importantly, the RSNM showed high drug entrapment efficiency, controlled drug release and protection of drug during storage. The RSNM significantly enhanced the cytotoxicity of RSV against colorectal cancer cells by inducing apoptosis and changing mitochondrial membrane potential. Further, in-vivo pharmacokinetic experiment indicated an improvement in pharmacokinetics of RSV after administering as RSNM. Thus, the use of self-assembled nanomicelles of amphiphilic INU-F68-SA bioconjugate could be a better alternative to overcome the poor in-vitro and in-vivo performance of RSV.
KW - Colorectal cancer
KW - INU-F68-SA bioconjugate
KW - Inulin
KW - pH-triggered release
KW - Pharmacokinetics
KW - Resveratrol
UR - http://www.scopus.com/inward/record.url?scp=85087803035&partnerID=8YFLogxK
U2 - 10.1016/j.carbpol.2020.116730
DO - 10.1016/j.carbpol.2020.116730
M3 - Article
C2 - 32829852
AN - SCOPUS:85087803035
SN - 0144-8617
VL - 247
JO - Carbohydrate Polymers
JF - Carbohydrate Polymers
M1 - 116730
ER -