Enhanced Bioavailability of Nadolol via Cinnamon Oil-Based Microemulsions: Formulation, Characterization, Cell...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Nadolol (NDL) is an antihypertensive medication with poor oral bioavailability.
• Developing effective oral drug delivery systems is crucial for improving NDL's therapeutic efficacy.
• Microemulsions offer potential for enhancing the solubility and permeability of poorly soluble drugs.

Purpose of the Study:

• To formulate and characterize novel nadolol-loaded microemulsions for oral administration.
• To evaluate the cytocompatibility and intestinal permeability of the developed NDL microemulsions.
• To assess the potential of NDL microemulsions as an oral drug delivery system for hypertension.

Main Methods:

• Microemulsions were prepared using cinnamon oil, Tween 20, propylene glycol:ethanol, and water.
• Formulations were characterized for droplet size, PDI, ζ-potential, pH, viscosity, and stability.
• Cytocompatibility was assessed using MTT assays on Caco-2 cells.
• In situ single-pass intestinal perfusion (SPIP) in rats was used to evaluate NDL permeability.

Main Results:

• The optimal NDL microemulsion exhibited a small droplet size (1.01 nm), low PDI (0.46), and negative ζ-potential (-10.26 mV).
• The formulation demonstrated good thermodynamic and storage stability.
• In situ SPIP studies showed a 5.826-fold increase in NDL permeability compared to a pure NDL solution.
• Predicted human absorption was 39.821%, with good cytocompatibility.

Conclusions:

• Developed nadolol-loaded microemulsions are stable and safe for oral delivery.
• These microemulsions significantly enhance NDL permeability and predicted oral absorption.
• NDL microemulsions represent a promising strategy for improving antihypertensive therapy, warranting further clinical investigation.