Investigation of Silicone-Containing Semisolid in Situ Film-Forming Systems Using QbD Tools.

Nikolett Kis,Mária Budai-Szűcs,Ildikó Csóka,Attila Gácsi,Szilvia Berkó,Erzsébet Csányi,Anita Kovács

doi:10.3390/pharmaceutics11120660

Abstract

The aim of our research work was to develop dermally applicable, semisolid film-forming systems (FFSs) containing silicones, which form a film on the skin in situ, with suitable mechanical properties for skin application. FFSs were developed and investigated by means of the Quality by Design (QbD) methodology. With this QbD approach, the initial risk assessment defines the critical quality attributes (CQAs), the critical material attributes (CMAs) and the critical process parameters (CPPs) to ensure the required quality. Different semisolid systems were formed with or without silicones. During the initial risk assessment, three CQAs, namely skin adhesion, film flexibility and burst strength, were found to be critical attributes, while film appearance, film integrity and the drying time of the semisolid system, were found to be medium attributes. These parameters were investigated. The initial risk assessment also showed that there are three high CMAs: the type of silicones, film-forming excipients, drying excipients, and that there was one medium CMA: viscosity-enhancing excipients. Based on our results, the silicone content had a great effect on the film-forming systems. Different silicones affected the mechanical properties of the films in varying ways, decreased the drying time and showed promising results regarding the drying mechanism.

Highlights

The dermal route of drugs has high potential in the health care system
Our study focuses on the determination of critical quality parameters, which have the highest influence on the formulation, using Quality by Design (QbD) tools
The quality target product profile (QTPP) of the film-forming systems (FFSs)-containing silicones includes the route of administration, dosage form, site of activity, appearance of drug delivery system, stability, silicone content, packaging material type and mechanical properties of the film for skin application

Summary

Introduction

One of the most important advantages of this route is the possibility to achieve a high concentration of the drug on the application site, which is promising for local anesthesia, arthritis or acne treatment. It gives good patient compliance, as it is a comfortable and painless administration route. The outermost layer of the epidermis is the stratum corneum (SC), which is the most important layer to protect the skin It has many functions, such as, to inhibit excessive water loss to ensure optimal skin hydration, and to defend the body from microbial pathogens, such as bacteria, and from various toxins as well [3]

Methods

Results

Conclusion