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Published on: November 24, 2021
Phloretin Transfersomes for Transdermal Delivery: Design, Optimization, and In Vivo Evaluation
Jiawen Wang1, Yuanyuan Zhao2, Bingtao Zhai1
1State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), and Shaanxi Key Laboratory of Chinese Medicine Fundamentals and New Drugs Research, and Shaanxi Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Shaanxi University of Chinese Medicine, Xi'an 712046, China.
This study developed a phloretin transfersome gel (PTG) for improved transdermal delivery. The PTG formulation enhances phloretin
Area of Science:
- Pharmacology
- Materials Science
- Dermatology
Background:
- Phloretin (Phl), a flavonoid with antioxidant and anticancer properties, suffers from poor water solubility and low bioavailability.
- Limited clinical applications of Phl necessitate strategies to enhance its solubility and efficacy for skin health.
- Developing effective transdermal delivery systems is crucial for combating skin aging and oxidative damage.
Purpose of the Study:
- To develop and evaluate a phloretin transfersome gel (PTG) for enhanced transdermal drug delivery.
- To improve the bioavailability and anti-aging potential of phloretin.
- To create a stable and effective topical antioxidant product.
Main Methods:
- Phloretin transfersomes (Phl-TFs) were prepared using thin-film dispersion-ultrasonication.
- Characterization involved TEM, DSC, FTIR, and XRD; solubility was assessed via Log P.
- In vitro skin penetration (Franz cell), in vivo pharmacokinetics in rats, and antioxidant activity in a D-gal rat model were evaluated.
Main Results:
- Optimized Phl-TFs were successfully prepared with specific ratios and parameters.
- Phl-TFs exhibited significantly higher Log P (2.26) compared to phloretin.
- The PTG formulation demonstrated enhanced cumulative skin penetration (842.73 μg/cm²), increased Cmax (1.39-fold) and AUC (1.97-fold) versus controls, and superior antioxidant effects in aging rats.
Conclusions:
- Successfully developed stable and safe phloretin transfersomes (Phl-TFs) and phloretin transfersome gel (PTG) preparations.
- In vivo studies confirmed the transdermal penetration and antioxidant efficacy of the PTG formulation.
- The developed PTG provides a promising foundation for future anti-aging and antioxidant topical product development.
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