A novel skin penetration enhancer: evaluation by membrane diffusion and confocal microscopy

Area of Science:

• Dermatology and Pharmaceutical Sciences
• Drug Delivery Systems
• In Vitro Efficacy Studies

Background:

• Transdermal drug delivery aims to enhance therapeutic outcomes by delivering active pharmaceutical ingredients through the skin.
• Oil/water emulsions are a common vehicle for topical formulations, but their transdermal efficiency can vary.
• Investigating novel formulations for improved drug penetration is crucial for effective topical treatments.

Purpose of the Study:

• To evaluate the in vitro transdermal efficacy of Meyer Zall Laboratories (MZL) oil/water emulsions.
• To compare the release rates and penetration characteristics of MZL formulations containing coal tar (Exorex) and diclofenac sodium (Athru-Derm) against comparator products.
• To elucidate the penetration mechanisms of MZL formulations using advanced microscopy techniques.

Main Methods:

• In vitro release rate studies using an enhancer cell system.
• Confocal and electron microscopy to analyze penetration characteristics in human skin and a melanoma cell line.
• Comparison of MZL formulations (Exorex, Athru-Derm) with four comparator products.

Main Results:

• MZL formulations (Exorex, Athru-Derm) exhibited significantly higher in vitro release rates for coal tar and diclofenac sodium compared to comparators.
• Microscopy identified emzaloid particles (50 nm to 1 micrometer) in MZL lotion.
• Emzaloid particles were detected in the epidermis of human skin and penetrated melanoma cells, including the nucleus.

Conclusions:

• The oil/water base in MZL formulations acts as a highly efficient transdermal vehicle.
• These formulations effectively transport various actives to their intended sites of action.
• MZL formulations show promise for enhanced topical drug delivery.