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Development, Characterization, and Evaluation of CAGE-based Ionic Liquid Systems for Transdermal Delivery
Published on: September 26, 2025
Episodic transdermal delivery of testosterone
Ritu Malik1, K S Venkatesh, Anil Kumar Dwivedi
1Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, 226001, India.
Molecular Pharmaceutics
|April 27, 2012
Summary
New transdermal systems deliver testosterone episodically. This research demonstrates pulsatile testosterone delivery via lotions and patches, offering potential for hormone therapy and contraception.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Endocrinology
Background:
- Testosterone (T) therapy often requires specific dosing regimens.
- Current transdermal systems may not provide pulsatile delivery.
- Developing novel delivery systems for controlled T release is crucial.
Purpose of the Study:
- To investigate the feasibility of achieving episodic transdermal delivery of testosterone (T).
- To develop and characterize novel film-forming lotions, precast films, and adhesive patches for pulsatile T release.
- To evaluate the in vivo pharmacokinetic profile of T from selected transdermal formulations.
Main Methods:
- Formulation of transdermal systems (lotions, films, patches) using vinylic, acrylic, and cellulosic polymers.
- In vitro drug release studies to assess T release kinetics and periodicity.
- In vivo pharmacokinetic studies in female rats, comparing transdermal application with intravenous administration.
- Pharmacokinetic analysis including deconvolution and noncompartment analysis.
Main Results:
- Composition-dependent differences in in vitro T release and periodicity were observed.
- Selected transdermal formulations demonstrated episodic T release in vivo, with multiple serum concentration peaks.
- Peak serum T concentrations and durations varied significantly between lotion and patch formulations.
- Pharmacokinetic analysis confirmed the pulsatile nature of T delivery from the tested systems.
Conclusions:
- Transdermal systems, including lotions and patches, can be formulated for episodic testosterone delivery.
- The developed systems show potential for achieving pulsatile T release in vivo.
- These findings suggest the feasibility of using transdermal systems for pulsatile T delivery in clinical applications like hormone supplementation and male contraception.
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