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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
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Nanoemulsions Containing Megestrol Acetate: Development, Characterization, and Stability Evaluation
Tahir Emre Yalcin1, Emre Tuncel2, Cigdem Yucel3
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330, Yenimahalle, Ankara, Turkey. emreyalcin@gazi.edu.tr.
AAPS Pharmscitech
|May 10, 2022
Summary
This study developed novel nanoemulsions (NEs) for megestrol acetate (MGA), a poorly soluble drug. These MGA-loaded NEs demonstrated excellent encapsulation efficiency and stability, improving oral delivery potential.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery
Background:
- Many active pharmaceutical ingredients (APIs) exhibit poor water solubility, limiting oral bioavailability and therapeutic efficacy.
- Megestrol acetate (MGA), a hydrophobic drug, suffers from limited oral absorption influenced by food intake.
- Nanoemulsions (NEs) offer a promising strategy for oral delivery of hydrophobic APIs by encapsulating them within the oil phase.
Purpose of the Study:
- To develop and characterize megestrol acetate (MGA)-loaded nanoemulsions (NEs) for enhanced oral delivery.
- To investigate the impact of various excipients on NE properties and stability.
- To evaluate the in vitro performance and cytotoxicity of the developed MGA-loaded NEs.
Main Methods:
- MGA-loaded NEs were prepared using the spontaneous emulsification technique.
- Excipients including ethanol, Tween 80, Lipoid E80, and medium-chain triglyceride (MCT) were screened for optimal NE formulation.
- Characterization involved droplet size analysis, zeta potential measurement, encapsulation efficiency determination, in vitro dissolution, and stability studies.
- The effect of polyvinylpyrrolidone (PVP) coating on NE properties was also assessed.
Main Results:
- Optimized MGA-loaded NEs (F20) exhibited nanometer-sized droplets (166.9 ± 3.0 nm) and a negative zeta potential (-12.2 ± 1.1 mV).
- Encapsulation efficiency exceeded 99%, indicating effective loading of MGA.
- NEs demonstrated good stability across a pH range of 1.2 to 6.8 and maintained stability at 4°C for 12 weeks.
- PVP-coated NEs (PVP-2) also showed favorable characteristics and enhanced cytotoxicity on MCF-7 cells.
Conclusions:
- Nanoemulsions are effective for delivering poorly soluble drugs like MGA, improving their oral bioavailability.
- Droplet size, surface charge, and stability are critical parameters for successful NE formulation and effectiveness.
- The developed MGA-loaded NEs, particularly PVP-coated ones, show potential as an improved oral drug delivery system with enhanced efficacy.
