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Nanosized ethosomes bearing ketoprofen for improved transdermal delivery
Manish K Chourasia1, Lifeng Kang2, Sui Yung Chan2
1Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore ; Pharmaceutics Division, Central Drug Research Institute, CSIR, Lucknow 226001, India.
Results in Pharma Sciences
|March 11, 2015
Summary
Ethosomes effectively deliver ketoprofen through the skin, enhancing drug permeation and achieving therapeutic levels. These novel vesicles offer sustained release, improving upon traditional hydroalcoholic solutions for transdermal drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Dermatology
Background:
- Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) commonly used for pain and inflammation.
- Traditional topical formulations often face challenges with skin penetration and achieving therapeutic drug concentrations.
- Ethosomes offer a promising lipid-based nanocarrier system for enhanced transdermal drug delivery.
Purpose of the Study:
- To evaluate the potential of ethosomes for transdermal ketoprofen delivery.
- To optimize and characterize ethosomal formulations for improved drug permeation.
- To compare the in vitro and in vivo efficacy of ethosomal ketoprofen with hydroalcoholic solutions.
Main Methods:
- Ethosomes were prepared using soya phosphatidyl choline (SPC) and ethanol, then optimized.
- Vesicular characteristics (size, shape, entrapment efficiency) were assessed using techniques like dynamic light scattering and transmission electron microscopy.
- In vitro drug release, permeation studies across human skin, and confocal microscopy were performed.
Main Results:
- Ethosomal formulations showed variable vesicle sizes (120.3–410.2 nm) and entrapment efficiencies (42–78%).
- Sustained in vitro drug release and significantly enhanced skin permeation and transdermal flux were observed with ethosomes compared to hydroalcoholic solutions.
- In vivo estimations indicated therapeutic plasma concentrations from ethosomes, unlike sub-therapeutic levels from hydroalcoholic solutions.
Conclusions:
- Ethosomes are effective carriers for transdermal ketoprofen delivery, demonstrating improved permeation and sustained release.
- Optimized ethosomal formulations can achieve therapeutic drug levels in vivo, offering a superior alternative to conventional methods.
- Confocal microscopy confirmed enhanced skin penetration of ethosomal formulations.
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