Influence of chitosan thioglycolic acid conjugate in improving bioavailability of an antiparkinson drug; Rasagiline Mesylate from transdermal patch

Abstract

Objective

Parkinson disease (PD) is a chronic disorder of central nervous system mainly affecting the motor systems. The drug of choice to treat PD is Rasagiline Mesylate (RM) and it belongs to BCS class III drug. The objective of the present study was the preparation of transdermal drug delivery system for RM. Several permeation enhancers were screened to be included in the formulation. To achieve desired flux a new strategy was developed by including in-house prepared CTC to enhance the permeation of RM.

Methods

The CTC was prepared by reaction between chitosan and thioglycolicacid, characterized by determining physical properties and applying analytical tools. Seven permeation enhancers with different mechanisms were screened. The transdermal patches were prepared with chitosan along with permeation enhancer IPM, various proportions of CTC and evaluated for physical and permeation studies. The optimized transdermal patch was obtained by two factors and three responses to obtain the design space and further evaluated for pharmacokinetic studies.

Results

The results of the present study confirmed the formation of CTC, IPM was best permeation enhancer among all. The presence of CTC in the formulations significantly improved the permeation of RM to achieve desired steady-state flux. The relative bioavailability of optimized transdermal patch was determined and it was observed that improved bioavailability as compared to marketed conventional tablets.

Conclusion

The study was concluded that CTC has significant influence on permeation enhancing ability of IPM.

Keywords:

• Antiparkinson
• rasagiline
• transdermal patch
• chitosan conjugate
• optimization
• LCMS/MS

Acknowledgements

The authors express thanks to M/s Apotex Research Pvt Ltd, Bangalore for providing gift samples of RM pure drug with a certificate of analysis. The authors are grateful to Dr. K. P. Channabasavaraja, Principal, Government College of Pharmacy, Karnataka, India for providing required facilities to carry out the experiment.

Disclosure statement

No potential conflict of interest was reported by the author(s).