Abstract
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).
Highlights
At the present time, the use of the herbal extract, chili oleoresin, is a prerequisite for alternative pain medicine, because of the effectiveness, aroma, and hot sensation of the oleoresin
The results show that the formulations composed of Glyceryl monostearate (GMS) and cetyl alcohol (COH) as the solid lipids yielded higher %EE and %Loading Capacity (LC), and the nanostructured lipid carriers (NLCs) formulations exhibited significantly higher %EE and %LC than solid lipid nanoparticles (SLN)-based formulations due to the less-ordered lipid structure and more amorphous area provided in NLC than in SLN
Lipid-based nanocarriers with green chemistry production using the selection of a lipid core mixture and hot high-pressure homogenization for chili oleoresin entrapment were successfully developed
Summary
The use of the herbal extract, chili oleoresin, is a prerequisite for alternative pain medicine, because of the effectiveness, aroma, and hot sensation of the oleoresin. Products with highly concentrated capsaicin (≥0.075% capsaicin) with a sustained release effect can provide higher effectiveness for severe chronic pain [7], but application may be associated with a burning sensation, leading to severe skin irritation and poor patient compliance [1,8]. These unwanted side effects are due to the rapid uptake of capsaicin in the epidermis and poor penetration into the dermis layer [9], resulting in capsaicin accumulation on the skin surface and in the epidermis. External stimuli and transient receptor potential vanilloid subfamily, member 1 (TRPV1) pain receptors located in the epidermis [1,10] become flooded with capsaicin, resulting in a severe skin irritation cascade [1]
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