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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

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Olive Oil-Based Reverse Microemulsion for Stability and Topical Delivery of Methotrexate: In Vitro.

Mohammad Changez¹, Mohammad Faiyaz Anwar², Hilal Alrahbi¹

¹College of Health Science, University of Buraimi, Al Buraimi 512, Oman.

|February 19, 2024

Summary

This study demonstrates that encapsulating methotrexate (MTX) in a water-in-oil microemulsion significantly enhances its stability and skin permeation. The microemulsion formulation protects MTX from degradation and improves drug delivery through the skin.

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Area of Science:

Pharmaceutical Sciences
Materials Science
Biophysics

Background:

Hydrolysis of active pharmaceutical ingredients can be controlled within confined microemulsion environments.
Methotrexate (MTX), a model drug, stability was investigated in a sodium bis(2-ethylhexyl) sulfosuccinate (AOT) and olive oil microemulsion system.

Purpose of the Study:

To evaluate the physicochemical properties and stability of MTX within an AOT-olive oil reverse microemulsion (MTX-RM).
To assess the in vitro skin permeation of MTX from MTX-RM and elucidate the underlying mechanism.

Main Methods:

Characterization using UV-vis, FT-IR, X-ray diffraction, dynamic light scattering, transmission electron microscopy, and atomic force microscopy.
In vitro skin permeation studies utilizing UV-visible spectrophotometry, confocal laser scanning microscopy (CLSM), differential scanning calorimetry (DSC), and attenuated total reflecting infrared spectroscopy (ATR).

Main Results:

MTX stability in MTX-RM (W₀=5) was significantly higher (~97% over 1 year) compared to MTX-RM (W₀=15) (~72%).
Skin fluxes of MTX were 15.1 to 22.75 times higher from MTX-RM compared to aqueous solutions.
CLSM confirmed enhanced MTX presence in skin layers, hair follicles, and sweat glands, indicating effective permeation.

Conclusions:

The interaction between MTX and the AOT headgroup within the microemulsion enhances MTX stability without compromising molecular integrity.
MTX-RM effectively enhances drug permeation through the skin by interacting with skin lipids and proteins.
The study highlights the potential of microemulsions for improving the delivery and stability of pharmaceutical molecules.