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A dietary supplement potentially employed for the treatment and/or prevention of hyperlipidemia was developed. The proposed product is composed of a combination of natural macromolecules as chitosan (CH), α-cyclodextrin (α-CD), and lupin proteins (LP). First, the anti-hyperlipidemic effect of the α-CD and LP binary mixture was assessed and compared to that of the extensively utilized anti-hyperlipidemic CH, using a hyperlipidemic rat model. The anti-hyperlipidemic effect of their combination was also demonstrated. Additionally, ligand–target and protein–protein docking studies were performed. The in vivo results displayed that on intergroup comparison, blending CH, α-CD, and LP promised a superior therapeutic effect over α-CD and LP mixture, CH, and the marketed atorvastatin, potentiating a considerable reduction of serum lipid profile and the calculated atherogenic risk predictor indices. Molecular docking study revealed a weak hydrophobic cholesterol–CH and cholesterol–α-CD interactions, while protein–protein docking study showed a good lipase–LP interaction, involving eight hydrogen bonds. Then, on the base of the in vivo and docking study results, a tablet formulation was produced aimed to overcome the negative technological effects of the anti-hyperlipidemic macromolecules: long disintegration time and tablets mechanical resistance. The optimized tablet formulation has a disintegration time shorter than 15 min and a weight loss from friability test lower than 1%, which are in line with the regulatory specifications for uncoated tablets. Overall, this anti-hyperlipidemic formulation is attractive for the dietary and nutraceutical market, despite further clinical studies are required to assess the efficacy, possible side effects, and product compliance. [ABSTRACT FROM AUTHOR]

Carlina acaulis root essential oil (EO) is one of the most potent mosquito larvicides (LC50 < 2 ppm). This EO is mainly composed of carlina oxide (> 90%). Poor water solubility and rapid degradation from UV light and oxygen in the environment limit the real-world use of this EO. Herein, we developed nanocarrier-based formulations, namely micro- and nanoemulsions (ME and NE, respectively) containing C. acaulis EO or carlina oxide (both at 0.5%) as active ingredients (a.i.). The larvicidal activity of ME and NE was evaluated against Culex quinquefasciatus. The highest larvicidal activity was achieved by the ME containing 0.5% of the EO (M1); its LC50(90) was 579.1 (791.3) µL L−1. Sublethal effects of this ME and its a.i. were assessed testing both at the LC16, LC30, LC50 and LC90 on mosquito larvae exposed to each product for 1–7 h, and then monitoring mortality for 18 days. At variance with the EO, ME application, even at LC16, led to 100% mortality at 18 days. The EO and its encapsulated form were scarcely toxic to human keratinocytes (HaCaT) and human fibroblast (NHF A12) cell lines. The acute toxicity of C. acaulis EO and its ME (M1) was also evaluated in Wistar rats through oral administration; EO LD50 was 1098 mg kg−1 bw, whereas its ME, even at 5000 mg kg−1 bw (considered the upper testing limit to establish safety to mammals), was not toxic. This study highlights the outstanding efficacy of C. acaulis EO ME for developing long-lasting and safe larvicides against Cx. quinquefasciatus. [ABSTRACT FROM AUTHOR]

Isofuranodiene is a bioactive furanosesquiterpene occurring as the major volatile compound in the essential oil from Smyrnium olusatrum (Apiaceae). It has a notable potentiality to be used as a botanical insecticide. However, its low solubility together with susceptibility to oxidation and thermal degradation limits its application on a wide scale. To face these challenges, isofuranodiene was encapsulated in stable microemulsions (MEs) at two concentrations (ME 750: 0.75%, ME 375: 0.375%). We assessed the larvicidal activity in the short term and after several days of exposure of pure isofuranodiene and its MEs against the filariasis vector Culex quinquefasciatus. The impact of ME-based larvicide at sublethal concentrations on adult emergence was evaluated. Finally, to shed light on potential ecotoxicology risks for nontarget invertebrates, MEs were tested on the aquatic microcrustacean Daphnia magna and on the earthworm Eisenia fetida. Pure isofuranodiene and S. olusatrum leaf essential oil, used as controls, showed their potential as mosquito larvicidal agents (LC50 of 29.2 and 18.6 μL L−1, respectively). Isofuranodiene formulated in ME 750 was effective against C. quinquefasciatus larvae, leading to significant larval mortality over time and a marked decrease in adult emergence. Both isofuranodiene MEs showed little impact on the nontarget aquatic microcrustacean Daphnia magna (ME 750 and ME 375: mortality < 19% after 48 h of exposure at 32 mL L−1 and 20 mL L−1, respectively) as well as on earthworms (ME 750 and ME 375: no mortality and mortality < 7% after 14 days of exposure to 1000 mg kg−1, respectively), outlining their potential employ in vector control operations. [ABSTRACT FROM AUTHOR]