In present investigation, AND-2-HyP-
β
-CYD (Andrographolide-2-Hydroxypropyl-
β
-cyclodextrin) complex was synthesized and characterized for antiviral and pharmacokinetic profile. The linear host-guest relation suggested synthesis of a 1:1 complex of AND with 2-HyP-
β
-CYD by inclusion mode. The Kc, stability constant of the two phase system of AND with 2-HyP-
β
-CYD computed to be 38.60.x10
-3
M.
1
H NMR spectrum of AND indicated the presence of triplet at 6.63-ppm which was up-fielded in AND-2-HyP-
β
-CYD complex at 6.60-ppm (doublet) confirmed the insertion of AND in cavity of 2-HyP-
β
-CYD through lactone ring. AND-2-HyP-β-CYD complex exhibited the IC
50
of 0.1-
μ
g.mL
-1
(E gene) and 0.29-
μ
g.mL
-1
(N gene) against SARS-CoV-2 infected Vero6 cells. Moreover, a 1.5-fold increment in extent of absorption of AND was noticed post complexation.The bioavailability was estimated to be 15.87±3.84% and 23.84±5.46%, respectively for AND and AND-2-HyP-
β
-CYD complex. AND-2-HyP-
β
-CYD complex may be a prospective candidate for further studies to evolve as a clinically viable formulation against SARS-CoV-2.
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