Licochalcone A-Loaded Solid Lipid Nanoparticles Improve Antischistosomal Activity In Vitro and In Vivo

Abstract

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

“…In addition, ZP of the obtained peptide targeted NPs showed a surface charge modification from negative to highly positive. This has been previously described by other authors using CPP [8]. Furthermore, this positive charge will ensure better interaction with corneal tissues due to their negative charge [57].…”

“…Moreover, Lico-A exhibits a carrageenan-induced anti-inflammatory effect in a murine model [6]. Despite the suitable properties of Lico-A against ocular inflammation, its solubility in water is extremely low, making its topical administration as conventional eye-drops difficult [7,8]. Moreover, it has also been reported that less than 5% of conventional ocular formulations are able reach inner ocular tissues [9].…”

Prenylated Flavonoids in Topical Infections and Wound Healing

“…Licochalcone A is at the forefront of scientific interest as a lead agent against various diseases, but unfavourable biopharmaceutical properties limit its therapeutic use. Fortunately, its poor solubility and potential haemolytic and cytotoxic effects were overcome in a study by Silva et al [ 266 ], in which licochalcone A was incorporated into solid lipid nanoparticles. The penetration of licochalcone A into the epidermis can be increased with micellar vehicles coloaded with glycyrrhizic acid [ 267 ].…”

Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity

“…The discovery of new antischistosomal compounds is crucial in terms of public health, since schistosomiasis remains as the second most important human parasitic disease [ 1 , 4 , 41 ]. Due to the imperative need to identify new drugs, several natural compounds have been recently studied against S. mansoni [ 1 , 6 ]. Additionally, our previous studies have shown that cardamonin has in vitro and in vivo antischistosomal activity against S. mansoni , also being effective in inhibiting both potato apyrase and SmNTPDases [ 13 ].…”

“…Schistosomiasis, caused by helminth parasites of the genus Schistosoma , is a neglected tropical disease with an estimated global prevalence of 240 million infected people in 78 countries and significant mortality and social and economic consequences [ 1 , 2 , 3 ]. Praziquantel (PZQ) is the only drug currently available for the treatment of all Schistosoma species [ 2 , 3 , 4 , 5 ], including Schistosoma mansoni , which is the species prevalent in South America, the Middle East, and Africa [ 1 , 3 , 6 ]. However, despite its effectiveness, PZQ has no efficacy against juvenile worms, which is a limit to schistosomiasis control and elimination [ 1 , 4 , 5 ].…”