Amorphous nano morin outperforms native molecule in anticancer activity and oral bioavailability

Area of Science:

• Pharmacology
• Nanotechnology
• Drug Delivery

Background:

• Naturally occurring phytoconstituents show therapeutic potential but face delivery challenges due to poor solubility and low oral bioavailability.
• Hydrophobic drug delivery requires advanced systems to overcome insolubility and enhance efficacy.
• Nanosuspensions offer a promising nanotechnology approach, avoiding carrier toxicity and scale-up issues.

Purpose of the Study:

• To develop a morin hydrate nanosuspension (MHNS) formulation.
• To enhance the poor physicochemical properties and low oral bioavailability of morin hydrate (MH).
• To evaluate the therapeutic efficacy of the developed MHNS.

Main Methods:

• Investigated various stabilizers and concentrations for nanosuspension preparation.
• Characterized MHNS using DLS, TEM, FTIR, DSC, and powder XRD.
• Evaluated solubility, dissolution, partition coefficient, in-vitro anticancer activity, and pharmacokinetics in rats.

Main Results:

• Optimized MHNS achieved a particle size below 100 nm.
• The nanosuspension significantly increased aqueous solubility, dissolution rate, and oral bioavailability of MH.
• Formulation as MHNS enhanced the in-vitro anticancer efficacy against human lung cancer cells.

Conclusions:

• MHNS formulation effectively improves the physicochemical properties and oral bioavailability of morin hydrate.
• Nanosuspension technology enhances the therapeutic potential of hydrophobic phytoconstituents like morin hydrate.
• MHNS demonstrates increased anticancer activity, highlighting its potential in cancer therapy.