Nanoemulsion-Based Strategy for Maximizing Nitrofurantoin Absorption: In-vitro and In-vivo Investigations

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Gastrointestinal (GI) intolerance and absorption variability limit Nitrofurantoin (NFT) efficacy.
• Developing advanced drug delivery systems is crucial for improving oral drug performance.

Purpose of the Study:

• To formulate a nanoemulsion (NE) of Nitrofurantoin (NFT) to enhance absorption and minimize GI intolerance.
• To evaluate the physicochemical properties and in vitro performance of the optimized NFT-NE.

Main Methods:

• Selected soybean oil, Transcutol HP, and Labrafil M1944CS based on NFT solubility for NE formulation.
• Utilized pseudoternary phase diagrams to determine optimal surfactant/co-surfactant (S_mix) ratios.
• Characterized the optimized formulation (NF5) for globule size, zeta potential, and drug release.

Main Results:

• The optimized NFT-NE (NF5) exhibited significantly improved membrane permeability (2.30x vs. pure drug, 1.43x vs. marketed suspension).
• NF5 demonstrated comparable cell viability and toxicity in Caco-2 cell lines to the marketed suspension.
• Relative bioavailability of NFT-NE was enhanced (1.10x vs. marketed, 1.17x vs. pure drug suspension).

Conclusions:

• The optimized NFT nanoemulsion formulation significantly enhances membrane permeability and relative bioavailability.
• The NE formulation shows potential for overcoming oral absorption variability and GI intolerance associated with Nitrofurantoin.
• Nanoemulsion technology offers a promising strategy for improving the therapeutic profile of poorly absorbed drugs like Nitrofurantoin.