TY - JOUR
T1 - Amorphous nano morin outperforms native molecule in anticancer activity and oral bioavailability
AU - Jangid, Ashok Kumar
AU - Agraval, Hina
AU - Gupta, Nitin
AU - Jain, Poonam
AU - Yadav, Umesh C.S.
AU - Pooja, Deep
AU - Kulhari, Hitesh
N1 - Publisher Copyright:
© 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2020/7/2
Y1 - 2020/7/2
N2 - In the past decade, naturally occurring phytoconstituents have emerged as potential therapeutic agents and alternative to synthetic drugs. However, efficient delivery of hydrophobic phytoconstituents into the body with desired therapeutic efficacy is a key challenge for the pharmaceutical industries due to their insolubility in water and low oral bioavailability. Nanosuspension formulations have shown promises to improve the delivery of the hydrophobic molecules with simultaneously avoiding the drawbacks like carrier toxicity and scale-up issues of other nanotechnology-based drug delivery systems. In this study, we have used morin hydrate (MH), a flavonol, and developed MH nanosuspension formulation (MHNS) to improve its poor physiochemical properties and low oral bioavailability. Different stabilizers with varying concentrations were investigated for preparing nanosuspension. MHNS was characterized by DLS, TEM, FTIR, DSC, powder XRD and was evaluated for its solubility, dissolution, partition coefficient, in-vitro anticancer activity and pharmacokinetics in rats. The optimized nanosuspension formulation, with a size of <100 nm, is capable of increasing aqueous solubility, dissolution rate, and oral bioavailability of MH. Moreover, the therapeutic efficacy, in terms of cytotoxicity to human lung cancer cells, of MH was also increased after formulating into nanosuspension form.
AB - In the past decade, naturally occurring phytoconstituents have emerged as potential therapeutic agents and alternative to synthetic drugs. However, efficient delivery of hydrophobic phytoconstituents into the body with desired therapeutic efficacy is a key challenge for the pharmaceutical industries due to their insolubility in water and low oral bioavailability. Nanosuspension formulations have shown promises to improve the delivery of the hydrophobic molecules with simultaneously avoiding the drawbacks like carrier toxicity and scale-up issues of other nanotechnology-based drug delivery systems. In this study, we have used morin hydrate (MH), a flavonol, and developed MH nanosuspension formulation (MHNS) to improve its poor physiochemical properties and low oral bioavailability. Different stabilizers with varying concentrations were investigated for preparing nanosuspension. MHNS was characterized by DLS, TEM, FTIR, DSC, powder XRD and was evaluated for its solubility, dissolution, partition coefficient, in-vitro anticancer activity and pharmacokinetics in rats. The optimized nanosuspension formulation, with a size of <100 nm, is capable of increasing aqueous solubility, dissolution rate, and oral bioavailability of MH. Moreover, the therapeutic efficacy, in terms of cytotoxicity to human lung cancer cells, of MH was also increased after formulating into nanosuspension form.
KW - A549 cell line
KW - Morin hydrate
KW - nanosuspension
KW - pharmacokinetic study
KW - surfactants
UR - http://www.scopus.com/inward/record.url?scp=85087031784&partnerID=8YFLogxK
U2 - 10.1080/03639045.2020.1776318
DO - 10.1080/03639045.2020.1776318
M3 - Article
C2 - 32469607
AN - SCOPUS:85087031784
SN - 0363-9045
VL - 46
SP - 1123
EP - 1132
JO - Drug Development and Industrial Pharmacy
JF - Drug Development and Industrial Pharmacy
IS - 7
ER -