Antimalarial Activity of Orally Administered Curcumin Incorporated in Eudragit®-Containing Liposomes

Abstract

Curcumin is an antimalarial compound easy to obtain and inexpensive, having shown little toxicity across a diverse population. However, the clinical use of this interesting polyphenol has been hampered by its poor oral absorption, extremely low aqueous solubility and rapid metabolism. In this study, we have used the anionic copolymer Eudragit® S100 to assemble liposomes incorporating curcumin and containing either hyaluronan (Eudragit-hyaluronan liposomes) or the water-soluble dextrin Nutriose® FM06 (Eudragit-nutriosomes). Upon oral administration of the rehydrated freeze-dried nanosystems administered at 25/75 mg curcumin·kg−1·day−1, only Eudragit-nutriosomes improved the in vivo antimalarial activity of curcumin in a dose-dependent manner, by enhancing the survival of all Plasmodium yoelii-infected mice up to 11/11 days, as compared to 6/7 days upon administration of an equal dose of the free compound. On the other hand, animals treated with curcumin incorporated in Eudragit-hyaluronan liposomes did not live longer than the controls, a result consistent with the lower stability of this formulation after reconstitution. Polymer-lipid nanovesicles hold promise for their development into systems for the oral delivery of curcumin-based antimalarial therapies.

Polymeric nanoparticles loaded with Baccharis dracunculifolia DC essential oil: Preparation, characterization, and antibacterial activity in milk

“…The positive control used in the test was 0.1% Triton X-100, which caused extensive erythrocyte lysis. The results are in agreement with previous studies that indicate low hemolysis by Eudragit nanoparticles (Coma-Cros et al, 2018) and some essential oils at concentrations above 1 mg/ml (Fabri et al, 2019;Sobrinho et al, 2016).…”

Promising nanomaterials in the fight against malaria

“…Eudragitnutriosomes presented better performance than Eudragithyaluronan liposomes due to the greater stability of the former, as shown by the vesicle behavior in gastrointestinal fluids. 64 Several studies have tried to target liposomes encapsulating PQ to the liver stage of malaria. 65 In P. berghei infections in mice, liposomes could decrease the toxicity of parenteral PQ delivery, which allowed for the administration of higher doses and resulted in the cure of the animals following a single intravenous injection.…”

Determination and pharmacokinetic study of isothiouronium-modified pyrimidine-substituted curcumin analog (1G), a novel antitumor agent, in rat plasma by liquid chromatography–tandem mass spectrometry

“…Curcumin (1,7-bis (4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3, 5-dione; also called diferuloylmethane, Figure 1) is a polyphenolic phytochemical extracted from the root of Curcuma longa, commonly called turmeric. Numerous studies have shown the antioxidant [1,2], anti-inflammatory [3,4], antimalarial [5,6] and neuroprotective properties [7,8] of curcumin. Moreover, cell culture experiments have shown the antitumor activity of curcumin in various human cancer cell lines, such as leukemia [9], esophageal cancer [10], gastric cancer [11], liver cancer [12], lung cancer [13] and cervical cancer [14].…”