Intracellular delivery mediated by an ethosomal carrier

Area of Science:

• Biotechnology
• Materials Science
• Cell Biology

Background:

• Ethosomes are advanced phospholipid vesicular carriers containing ethanol, designed for enhanced molecule delivery.
• Investigating ethosomes' transcellular delivery efficiency is crucial for developing novel drug and cosmetic delivery systems.

Purpose of the Study:

• To evaluate the transcellular delivery efficiency of ethosomes for molecules with diverse physicochemical properties into fibroblasts and nude mouse skin.
• To compare the efficacy of ethosomes against traditional liposomes and hydroethanolic solutions for molecule penetration.

Main Methods:

• Utilized fluorescent probes (D-289, RR, PC*) to track molecule penetration into 3T3 fibroblasts.
• Employed Confocal Laser Scanning Microscopy (CLSM) and Flow Cytometry (FACS) for quantitative analysis of intracellular probe distribution.
• Conducted skin permeation studies with hydrophilic calcein and lipophilic RR on nude mouse skin.

Main Results:

• Ethosomes demonstrated significantly enhanced penetration of all tested probes into fibroblasts, evidenced by high fluorescence intensity.
• Intracellular presence of probes was observed within 3 minutes, with D-289 reaching the fibroblast nucleus.
• Ethosomal delivery resulted in greater depth penetration for calcein (160 µm) and higher fluorescence intensity for RR (150 AU) in nude mouse skin compared to controls.
• Fibroblast viability assays confirmed the non-toxic nature of the ethosomal carrier.

Conclusions:

• Ethosomes are highly effective carriers for transcellular delivery of molecules into cells and through the skin.
• The ethanol content in ethosomes plays a key role in enhancing the penetration of both hydrophilic and lipophilic substances.
• Ethosomes represent a safe and efficient platform for topical and transdermal delivery applications.