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Testosterone solid lipid microparticles for transdermal drug delivery. Formulation and physicochemical

Amal H El-Kamel¹, Iman M Al-Fagih, Ibrahim A Alsarra

¹Faculty of Pharmacy, Department of Pharmaceutics, King Saud University, Riyadh, Saudi Arabia. amalelkamel@yahoo.com

Journal of Microencapsulation

|June 21, 2007

Summary

This study developed testosterone (TS) solid lipid microparticles (SLM) for transdermal delivery, achieving high entrapment efficiency and promising stability for a potential topical drug delivery system.

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Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems
Nanotechnology

Background:

Transdermal drug delivery offers a non-invasive route for systemic administration.
Testosterone (TS) replacement therapy requires effective and stable delivery systems.
Solid lipid microparticles (SLM) are a promising platform for encapsulating lipophilic drugs like testosterone.

Purpose of the Study:

To formulate and characterize testosterone (TS) solid lipid microparticles (SLM).
To evaluate the potential of these SLMs as a transdermal delivery system.
To assess the stability and release characteristics of TS from the SLMs.

Main Methods:

TS SLMs were prepared using the emulsion melt homogenization technique.
Various lipids (glyceryl monostearate, glyceryl distearate, stearic acid, glyceryl behenate) and TS concentrations were investigated.
Characterization included morphology, particle size, entrapment efficiency, rheology, thermal behavior, and in vitro release studies.

Main Results:

High entrapment efficiency (80.7-95.7%) was achieved for TS SLMs.
Lipid type significantly influenced SLM morphology and particle size.
In vitro release studies indicated varying permeation rates based on formulation, with 10% glyceryl behenate (GB) showing notable potential.
The 10% GB-2.5 mg TS g(-1) SLM formulation demonstrated good stability upon storage at 5°C and trehalose proved effective as a cryoprotectant during freeze-drying.

Conclusions:

The developed testosterone solid lipid microparticles (SLM) show potential as a stable and effective transdermal delivery system.
Further investigation into in vivo performance and optimized formulations is warranted.