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Open AccessArticle

Enhanced Transdermal Delivery of Concentrated Capsaicin from Chili Extract-Loaded Lipid Nanoparticles with Reduced Skin Irritation

1
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand
2
Innovation Center for Holistic Health, Nutraceuticals, and Cosmeceuticals, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand
3
Department of Pharmaceutics, Ernest Mario School of Pharmacy, Center for Dermal Research, Rutgers—The State University of New Jersey, Piscataway, NJ 08854, USA
4
Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmaceutical Sciences, Ubon Ratchathani University, Ubon Ratchathani 34190, Thailand
5
Center for Research and Development of Natural Products for Health, Chiang Mai University, Chiang Mai 50200, Thailand
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2020, 12(5), 463; https://doi.org/10.3390/pharmaceutics12050463
Received: 12 April 2020 / Revised: 11 May 2020 / Accepted: 13 May 2020 / Published: 19 May 2020
(This article belongs to the Section Nanomedicine and Nanotechnology)
The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and −29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDermTM three-dimensional human skin irritation test and hen’s egg test chorioallantoic membrane assay (HET-CAM). View Full-Text
Keywords: capsaicin; chili extract; SLN; NLC; topical delivery system; nanoparticles; irritation capsaicin; chili extract; SLN; NLC; topical delivery system; nanoparticles; irritation
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MDPI and ACS Style

Anantaworasakul, P.; Chaiyana, W.; Michniak-Kohn, B.B.; Rungseevijitprapa, W.; Ampasavate, C. Enhanced Transdermal Delivery of Concentrated Capsaicin from Chili Extract-Loaded Lipid Nanoparticles with Reduced Skin Irritation. Pharmaceutics 2020, 12, 463.

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