Enhancement of Dermal Delivery of Finasteride Using Microemulsion Systems.

Saeed Mohammad Soleymani,Anayatollah Salimi

doi:10.15171/apb.2019.067

Saeed Mohammad Soleymani, Anayatollah Salimi

Open Access

https://doi.org/10.15171/apb.2019.067

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Abstract

Purpose: Finasteride is a pharmaceutical agent that treats hair loss and acne with hormonal patterns. Due to its poor water solubility, and the smaller surface area in comparison to total skin surface area, penetration of the drug into hair follicles and skin is low. The aim of this research was to formulate, characterize and evaluate in vitro skin permeability of finasteride microemulsions (MEs). Methods: Finasteride MEs were prepared using a pseudo-ternary phase diagram method with an appropriate ratio of oil mixture, surfactant-co-surfactant mixture and water. MEs containing 1% finasteride were prepared with a suitable amount of oily phase and surfactant and cosurfactant. The physicochemical properties of these MEs and in vitro skin permeability of MEs were evaluated. Results: The results showed that the mean droplet size range of ME samples was 5–17 nm and pH was 5.1–5.7. The viscosity of MEs ranged from 86.4–209.6 cps. The drug release profile showed that 49.510% of the drug was released (ME-F-6) over the 24 hours of the experiment. The kinetics of drug release from all selected MEs were approximately described by Higuchi and first-order modeling. All ME formulations with different compositions and properties significantly increased flux and permeability coefficient from rat skin. The selected MEs exhibit 99.9% finasteride after six months of storage. Conclusion: This study showed that any change in the content and composition of MEs could change the physical and chemical properties in addition to ME permeability parameters. The MEs increased permeability of the skin to finasteride.

Highlights

Hair, in addition to the role of cuticle, is important cosmetically for human beings
The kinetics of drug release from all selected MEs were approximately described by Higuchi and first-order modeling
Testosterone is converted to its active form, DHT, which induces hair loss and is linked to androgenic receptors in hair follicles, which results in compromised growth phase of the hair cycle

Summary

Introduction

In addition to the role of cuticle, is important cosmetically for human beings. It is believed that DHT shortens the growth stage, or anagen, from a typical period of three to six years to several weeks or months This causes the hair follicles to shrink gradually, reducing hair production and making hair smoother. DHT is produced by an enzyme called 5-alpha-reductase.[2] Finasteride is a 5-alphareductase (II) inhibitor which is administered in the treatment of such hair loss and acne by pills that are either 1 or 5 mg in strength. The use of this drug systemically has side effects such as complications like gynecomastia, behavioral disorders and loss of libido.

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