Andrographolide/Phospholipid/Cyclodextrin Complex-Loaded Nanoemulsion: Preparation, Optimization, in Vitro and in...

Area of Science:

• Pharmacology
• Drug Delivery
• Materials Science

Background:

• Andrographolide (AG) has limited oral bioavailability due to poor solubility, stability, and absorption.
• Phospholipid (PC) and hydroxypropyl-β-cyclodextrin (HPCD) show potential for enhancing drug solubility and absorption.
• Nanoemulsions (NE) are effective enhancers for oral drug bioavailability.

Purpose of the Study:

• To synthesize an Andrographolide/HPCD/PC complex (AHPC).
• To optimize and prepare AHPC-loaded nanoemulsion (AHPC-NE) for improved oral delivery.
• To evaluate the physicochemical properties, sustained-release effect, and oral bioavailability of AHPC-NE.

Main Methods:

• Synthesis of AHPC complex.
• Optimization and preparation of AHPC-NE using central composite design and response surface methodology.
• Characterization of AHPC-NE droplet size, polydispersity index (PDI), loading capacity, encapsulation efficiency, and morphology via transmission electron microscopy.
• In vivo release studies and oral bioavailability assessment compared to AG suspension.

Main Results:

• Optimized AHPC-NE exhibited an average droplet size of 116.50 ± 5.99 nm and a PDI of 0.29 ± 0.03.
• High loading capacity (0.32 ± 0.01%) and encapsulation efficiency (96.43 ± 2.27%) were achieved.
• AHPC-NE demonstrated sustained-release properties in vivo.
• A significant enhancement in AG absorption was observed, with a relative bioavailability of 550.71% compared to AG suspension.

Conclusions:

• AHPC-NE formulation is a promising strategy for enhancing the oral bioavailability of Andrographolide.
• The developed nanoemulsion system offers sustained-release benefits.
• This approach holds potential for improving the therapeutic efficacy of poorly bioavailable natural products.