Planta Med 2019; 85(13): 1114-1123
DOI: 10.1055/a-0978-5172
Formulation and Delivery Systems of Natural Products
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Capsaicin and Piperine as Functional Excipients for Improved Drug Delivery across Nasal Epithelial Models

Werner Gerber
1  Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Dewald Steyn
1  Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Awie Kotzé
1  Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Hanna Svitina
1  Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Ché Weldon
2  Unit for Environmental Sciences and Management, North-West University, Potchefstroom, South Africa
,
Josias Hamman
1  Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
› Author Affiliations
Further Information

Publication History

received 23 April 2019
revised 05 July 2019

accepted 09 July 2019

Publication Date:
24 July 2019 (online)

Abstract

The fruit from various pepper plants has been employed for the seasoning of food, as perfuming agents, and also as traditional medicines. Phytochemicals isolated from different pepper species have been found to modulate the pharmacokinetics of orally administered drugs. This study investigated the possibility to apply capsaicin and piperine (extracted alkaloids) as modulators for drug delivery across the nasal epithelium. Both a nasal epithelial cell line (RPMI 2650) and excised sheep nasal tissue were used as models to investigate the effects of the selected pepper compounds on drug permeation. FITC-dextran 4400 (MW 4400 Da) was used as a large molecular weight marker compound for paracellular transport, while rhodamine 123 was used as a marker compound that is a substrate for P-glycoprotein-mediated efflux. From the permeation results, it was clear that capsaicin inhibited P-glycoprotein efflux to a larger extent, while piperine showed drug permeation enhancement via other mechanisms. The cell cytotoxicity studies indicated that capsaicin was noncytotoxic up to a concentration of 200 µM and piperine up to a concentration of 500 µM as indicated by cell viability above 80%. The histological analysis of the excised nasal tissue and cultured RPMI 2650 cell layers indicated that some damage occurred after treatment with 200 µM capsaicin, but no changes were observed for piperine up to a concentration of 50 µM.