Abstract

Capsaicin has known health beneficial and therapeutic properties. It is also able to enhance the permeability of drugs across epithelial tissues. Unfortunately, due to its pungency the oral administration of capsaicin is limited. To this end, we assessed the effect of nanoencapsulation of capsaicin, under the hypothesis that this would reduce its pungency. Core-shell nanocapsules with an oily core and stabilized with phospholipids were used. This system was used with or without chitosan coating. In this work, we investigated the in vitro release behavior of capsaicin-loaded formulations in different physiological media (including simulated saliva fluid). We also evaluated the influence of encapsulation of capsaicin on the cell viability of buccal cells (TR146). To study the changes in pungency after encapsulation we carried out a sensory analysis with a trained panel of 24 students. The in vitro release study showed that the systems discharged capsaicin slowly in a monotonic manner and that the chitosan coating had an effect on the release profile. The cytotoxic response of TR146 cells to capsaicin at a concentration of 500 μM, which was evident for the free compound, was reduced following its encapsulation. The sensory study revealed that a chitosan coating results in a lower threshold of perception of the formulation. The nanoencapsulation of capsaicin resulted in attenuation of the sensation of pungency significantly. However, the presence of a chitosan shell around the nanoformulations did not mask the pungency, when compared with uncoated systems.

Highlights

  • Capsaicin (N-(4-hydroxy-3-methoxybenzyl)-8-methyl-trans-6nonenamide) is a pungent alkaloid found in plants of the genus Capsicum in concentrations between 0.3–0.5% [1]

  • In the present study we investigated the in vitro release behavior of the formulations in simulated saliva fluid, evaluated the cytotoxicity of free and encapsulated capsaicin to buccal cells (TR146) and carried out a sensory analysis to study the effect of encapsulation on sensation of pungency to evaluate their feasibility for oral administration

  • To evaluate the effect of encapsulation on the pungency of capsaicin we investigated the physicochemical properties of two different systems, studied their interaction with cells using in vitro experiments and conducted a sensory analysis to study the influence on pungency sensation

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Summary

Introduction

Capsaicin (N-(4-hydroxy-3-methoxybenzyl)-8-methyl-trans-6nonenamide) is a pungent alkaloid found in plants of the genus Capsicum (for example chili peppers) in concentrations between 0.3–0.5% [1]. Capsaicin is an agonist to TRPV1 receptors causing burn and pain sensations on skin and mucus membranes [2]. Taken orally, it influences the cardiovascular system, induces an increase of salivation and gastric secretion and gastrointestinal disorders in higher dosages [3,4]. Capsaicin is known for its antioxidant, anti-inflammatory, anticarcinogenic and antifungal effects [5,6]. It is known as promoter of PLOS ONE | DOI:10.1371/journal.pone.0141017. It is known as promoter of PLOS ONE | DOI:10.1371/journal.pone.0141017 October 22, 2015

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