Evaluation of formulation properties and skin penetration in the same additive-containing formulation

Abstract

The aim of this study is to examine the physicochemical properties of the external preparation, the effect on the skin permeability and the human senses. Miconazole nitrate cream formulation (MCZ-A: bland name and MCZ-B, −C, −D: generics) to measure the physicochemical properties, was performed by the skin permeation test and human sensory test. The flattening, viscoelasticity, and water content of each cream were measured and each cream was subjected to near-infrared (NIR) absorption spectroscopy and human sensory testing. The yield value was calculated based on measured flattening and was 734.8 dynes/cm² for MCZ-A, 1198.9 dynes/cm² for MCZ-B, 461.3 dynes/cm² for MCZ-C and 3112.3 dynes/cm² for MCZ-D. Measurement of viscoelasticity and viscosity revealed that MCZ-C had a smaller tanδ than the other 3 creams at 25 °C. NIR absorption spectroscopy revealed that MCZ-A had the highest absorption peak due to hydroxyl groups, followed by MCZ-C, −B, and then −D. Measurement of water content revealed that MCZ-A had a water content of 65.9%, MCZ-B, −C, and −D had a water content of around 56.3%. Human sensory testing revealed differences between MCZ-A and MCZ-C and between MCZ-B and MCZ-D in terms of spreadability and feel. These findings indicate that differences in water and oil content and emulsification resulted in the creams having different physical properties, such as flattening, internal structure, and dynamic viscoelasticity. NIR absorption spectroscopy, which allows non-destructive measurement of a sample’s physicochemical properties, and measurement of viscoelasticity and viscosity, which allows measurement of a sample’s dynamic viscoelasticity, revealed differences in the physical properties of creams. The skin permeation test, skin MCZ amount was 7.48 µg/cm² for MCZ-A, 5.11 µg/cm² for MCZ-B, 12.08 µg/cm² for MCZ-C and 3.75 µg/cm² for MCZ-D. In addition, since the drug spread is good about the skin migration, spreadability is affecting the potential dermal transfer.