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A Microemulsion for Oral Delivery of Nintedanib - QbD-Enabled Formulation Development, In-Vitro Characterization &
Dnyandev Gadhave1, Mural Quadros1, Mimansa Goyal1
1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, New York, 11439, USA.
The AAPS Journal
|August 11, 2025
Summary
This study developed a novel Nintedanib-loaded microemulsion (Nint-ME) to improve oral delivery for idiopathic pulmonary fibrosis (IPF) treatment. The optimized Nint-ME formulation significantly enhanced Nintedanib
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Nintedanib (Nint) is crucial for idiopathic pulmonary fibrosis (IPF) but suffers from poor solubility and low oral bioavailability (<5%).
- Existing Nintedanib delivery methods face challenges due to its rapid metabolic degradation.
- Overcoming these limitations is essential for effective Nintedanib therapy in IPF patients.
Purpose of the Study:
- To formulate and optimize a Nintedanib-loaded microemulsion (Nint-ME) for enhanced oral delivery.
- To evaluate the physicochemical properties, in vitro release, and in vivo pharmacokinetic profile of the Nint-ME.
- To assess the therapeutic potential of Nint-ME in overcoming Nintedanib's delivery constraints.
Main Methods:
- Nint-ME was prepared using low-energy oil-in-water (O/W) emulsification and aqueous titration, optimized via a Quality by Design (QbD) approach.
- Characterization included globule size, PDI, encapsulation efficiency, transmittance, surface charge, and viscosity.
- In vitro release kinetics, Caco-2 cell permeability, and in vivo pharmacokinetic studies were conducted.
Main Results:
- Optimized Nint-ME exhibited desirable characteristics: 23.8 nm globule size, 0.18 PDI, 99.8% encapsulation efficiency, and -0.7 mV surface charge.
- High Nintedanib release (94.5%) over 72 hours followed first-order kinetics, indicating controlled release.
- In vitro studies showed significant Caco-2 cell permeation, and in vivo studies revealed a 2-fold increase in oral bioavailability compared to Nintedanib suspension.
Conclusions:
- Successful development of an oral Nintedanib-loaded microemulsion (Nint-ME) formulation.
- Nint-ME demonstrates improved solubility, stability, and significantly enhanced oral bioavailability of Nintedanib.
- This novel formulation offers a promising strategy for safe and effective Nintedanib delivery in IPF treatment.
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