In this study, we had developed Naringenin-loaded liquid crystalline nanoparticles (LCNs) and investigated the anti-inflammatory and anticancer activities of Naringenin-LCNs against human airway epithelium-derived basal cells (BCi-NS1.1) and human lung epithelial carcinoma (A549) cell lines, respectively. The anti-inflammatory potential of Naringenin-LCNs evaluated by qPCR revealed a decreased expression of IL-6, IL-8, IL-1β, and TNF-α in lipopolysaccharide-induced BCi-NS1.1 cells. The activity of LCNs was comparable to the positive control drug Fluticasone propionate (10 nM). The anticancer activity was studied by evaluating the antiproliferative (MTT and trypan blue assays), antimigratory (scratch wound healing assay, modified Boyden chamber assay, and immunoblot), and anticolony formation activity in A549 cells. Naringenin LCNs showed promising antiproliferative, antimigratory, and anticolony formation activities in A549 cells, in vitro. Therefore, based on our observations and results, we conclude that Naringenin-LCNs may be employed as a potential therapy-based intervention to ameliorate airway inflammation and to inhibit the progression of lung cancer. Practical applications Naringenin was encapsulated into liquid crystalline nanoparticles, thus, attributing to their sustained-release nature. In addition, Naringenin-loaded LCNs efficiently reduced the levels of pro-inflammatory markers, namely, IL-1β, IL-6, TNF-α, and IL-8. In addition, the Naringenin-loaded LCNs also possess potent anticancer activity, when tested in the A549 cell line, as revealed by the inhibition of proliferation and migration of cells. They also attenuated colony formation and induced apoptosis in the A549 cells. The findings from our study could form the basis for future research that may be translated into an in vivo model to validate the possible therapeutic alternative for lung cancer using Naringenin-loaded LCNs. In addition, the applications of
The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol ® ATO 5 (glyceryl palmitostearate) and Labrasol ® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol ® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol ® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, −21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 μg/cm 2 /h) as compared with plain 5-FU gel (2.85±1.12 μg/cm 2 /h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 μg/cm 2 ) as compared with that from the 5-FU plain gel (12.23±3.86 μg/cm 2 ) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations.
Caulerpa racemosa (Forsskal) J. Agardh is a green seaweed used as food and folk medicine since ancient times in the Indo-Pacific region, particularly in southeast Asia. In this study, the proximate nutrient composition, phytochemical, anti-oxidant and anti-diabetic properties of sea grape C. racemosa collected from culture fishponds in Johor, Malaysia were analysed. The contents (dry weight basis) of carbohydrate, crude protein, crude lipids, ash and caloric value obtained were 33.42 ± 1.34%, 20.27 ± 0.14%, 4.20 ± 0.32%, 28.25 ± 0.27% and 2544.67 ± 7.04 cal g−1, respectively. The amino acid score (AAs) and biological protein value (213.43 mg g−1) indicated that C. racemosa presented a better protein quality. The most abundant fatty acids were C16:0 (palmitic acid: 63.27%), followed by C18:1 (oleic acid: 5.80%), and C18:2 ῳ6 (linoleic acid: 5.33%). The analysis of the ash content indicated that essential minerals and trace elements, such as Ca, Fe, and Mn, were present in the seaweed. The total phenolic content (TPC) and total flavonoid content (TFC) observed in the ethyl acetate extract were 17.88 ± 0.78 mg GAE g−1 and 59.43 ± 2.45 mg QE g−1, respectively. The ethyl acetate extract of C. racemosa demonstrated notable anti-diabetic activity in diabetic induced rats. The low (100 mg kg−1) and high (200 mg kg−1) doses of cultivated C. racemosa extract exhibited a significant decrease (p < 0.05) in blood glucose levels while preventing weight loss, reducing plasma AST, ALT levels as a sign of hepatoprotective effect and recording albumin levels similar to positive control in diabetic induced rats. The results support the usefulness of cultivated C. racemosa as a potential functional food.
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