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Development and optimization of kaempferol loaded ethosomes using Box-Behnken statistical design: In vitro and
Shraddha Singh Raghav1, Bhavna Kumar1, Neeraj Kumar Sethiya1
1Faculty of Pharmacy, DIT University, Dehradun, Uttarakhand, India.
This study developed kaempferol (KMP) ethosomal formulations for diabetic foot ulcers. Optimized KMP ethosomes demonstrated enhanced drug release and skin permeation, offering a promising delivery system.
Area of Science:
- Pharmacology and Drug Delivery
- Materials Science
- Biotechnology
Background:
- Diabetic foot ulcers (DFUs) are a severe complication of diabetes mellitus, often requiring advanced therapeutic strategies.
- Flavonoids, such as kaempferol (KMP), possess therapeutic properties but suffer from poor bioavailability and skin penetration.
- Ethosomes, a novel vesicular system, offer enhanced drug delivery due to their deformability and ability to penetrate the skin.
Purpose of the Study:
- To formulate and optimize ethosomal carriers for kaempferol (KMP) delivery.
- To evaluate the potential of KMP ethosomes for treating diabetic foot ulcers.
- To investigate the physicochemical properties, in vitro release, and ex vivo permeation of KMP ethosomes.
Main Methods:
- Kaempferol (KMP) was formulated into ethosomes using the cold method.
- Box-Behnken design (BBD) was employed for optimization of formulation variables: KMP concentration, soylecithin content, and ethanol percentage.
- Characterization included Transmission Electronic Microscopy (TEM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) spectroscopy, in vitro release, and ex vivo permeation studies.
Main Results:
- Optimized KMP ethosomes exhibited a vesicle size of 283 nm, zeta potential of -29.67 mV, and high entrapment efficiency (91.02%).
- In vitro drug release of KMP ethosomes (88.2%) was significantly higher than pure KMP (49.9%).
- Ex vivo permeation studies showed a substantially increased apparent permeation coefficient for KMP ethosomes (356.25 μg/cm²) compared to pure KMP (118.46 μg/cm²).
Conclusions:
- Ethosomal formulation represents a cutting-edge strategy for enhanced delivery of kaempferol.
- Optimized KMP ethosomes demonstrate potential for prolonged and targeted distribution, suitable for various dosage forms.
- This approach offers a promising new delivery method for managing diabetic foot ulcers and other conditions requiring effective KMP delivery.
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