Freeze drying has emerged as an important technique for the storage and transportation of pharmaceutical compounds. It has also been widely used in the formulation and development of diagnostic reagents, including those for COVID-19 testing. In this work, researchers use Linkam’s FDCS196 to look at how freeze drying can be used to characterise the antipsychotic drug, Risperidone, and pave the way for new transdermal drug delivery systems.

*This is the first study of its kind reporting on the enhancement of skin permeability of risperidone (RIS) using eutectic systems.*

The study, undertaken at the University of Petra in Jordan and published in AAPS PharmSciTech, describes the formation of room temperature therapeutic deep eutectic solvent (THEDES) of RIS, an antipsychotic drug that is used in the treatment of schizophrenia, mixed and manic states associated with bipolar disorder, and irritability in children and adolescents with autism. This is the first study of its kind.

RIS is commercially available in several forms, as a conventional tablet, disintegrating tablet, oral liquid solution and long-acting intramuscular injection. It is thought that creating a transdermal drug delivery system (TDDS) for RIS may help improve its bioavailability, which is typically low. The conversion of the active pharmaceutical agent (API) into liquid form using deep eutectic solvents (DES) to form THEDES has been reported to have many formulation advantages, including enhanced skin permeation for transdermal drug delivery.

In this ground-breaking study aimed at enhancing the skin permeability of RIS using eutectic systems, the researchers were able to achieve the formation of room temperature compounds (THEDES of RIS and some fatty acids) using a simple method for preparation – potentially opening up opportunities for formulation innovation for this important pharmaceutical drug.

Freeze drying microscopy (FDM) can be used to determine the crystallisation, collapse and eutectic temperatures of pharmaceutical solutions intended to be freeze dried. In this study, FDM was successfully used to follow the eutectic phase changes for the THEDES of RIS. These changes were captured using a Linkam FDCS196 temperature and vacuum control stage.

Faisal T. Al-Akayleh [Source: ResearchGate]

Faisal T. Al-Akayleh, Associate Professor at the University of Petra comments on the role of the Linkam stage in this research: “Eutectic systems’ phase changes are temperature-dependant, which we were able to control and monitor with the Linkam FDCS196 stage. The stage provided valuable information regarding the phase change and transitions the drug undergoes as a function of temperature, clarifying the interpretation of the differential thermal analysis results.”

Located in West Amman in Jordan, the University of Petra's campus houses 8024 undergraduate and graduate students in the faculties of Arts and Sciences, Administrative & Financial Sciences, Pharmacy & Medical Sciences, Information Technology, Architecture & Design, Law and Mass Communication and Faculty of Engineering. The University is a hub for creating knowledge through research, developing skills, applying knowledge to new technologies and technology transfer.

The FDCS196 played an important role in the development of a novel liquid pharmaceutical formulation of RIS to overcome problems of poor drug solubility, dissolution and permeation. This research could potentially lead to new formulations of RIS that will benefit patients around the world. The FDCS196 is used in a wide range of research, from increasing the shelf life of drugs and vaccines, to food processing and preservation.

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