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Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum

引用

Bioactive Materials 2021年第4期6卷 1163-1174页

作者： Anna Jaromin Silvia Parapini Nicoletta Basilico Magdalena Zaremba-Czogalla Agnieszka Lewi´nska Agnieszka Zag´orska Maria Walczak bozena tyliszczak Aleksandra Grzeszczak MarcinŁukaszewicz Łukasz Kaczmarek Jerzy Gubernator Department of Lipids and Liposomes Faculty of BiotechnologyUniversity of WroclawWroclawPoland Dipartimento di Scienze Biomediche per la Salute Universit`a degli Studi di MilanoMilanItaly Dipartimento di Scienze Biomediche Chirurgiche e OdontoiatricheUniversit`a degli Studi di MilanoMilanItaly Faculty of Chemistry University of WroclawWroclawPoland Department of Medicinal Chemistry Jagiellonian University Medical CollegeCracowPoland Chair and Department of Toxicology Jagiellonian University Medical CollegeFaculty of PharmacyCracowPoland Instytute of Materials Science Cracow University of TechnologyCracowPoland Department of Biotransformation Faculty of BiotechnologyUniversity of WroclawWroclawPoland Pharmaceutical Research Institute WarsawPoland

Alternative therapies are necessary for the treatment of malaria due to emerging drug ***,many promising antimalarial compounds have poor water solubility and suffer from the lack of suitable delivery systems,which seriously limits their *** address this problem,we synthesized a series of azacarbazoles that were evaluated for antimalarial activity against D10(chloroquine-sensitive)and W2(chloroquine-resistant)strains of *** most active compound,9H-3-azacarbazole(3),was encapsulated in a novel o/w nanoemulsion consisting of ethyl esters of polyunsaturated fatty acids n-3 and n-6 obtained from flax oil as the oil phase,Smix(Tween 80 and Transcutol HP)and *** formulation was further analyzed using transmission electron microscopy,dynamic light scattering and in vitro and in vivo *** was shown that droplets of the 3-loaded nanosystem were spherical,with satisfactory stability,without cytotoxicity towards fibroblasts and intestinal cell lines at concentrations corresponding to twice the IC50 for ***,the nanoemulsion with this type of oil phase was internalized by Caco-2 ***,pharmacokinetics demonstrated rapid absorption of compound 3(tmax=5.0 min)after intragastric administration of 3-encapsulated nanoemulsion at a dose of 0.02 mg/kg in mice,with penetration of compound 3 to deep *** 3-encapsulated nanoemulsion was found to be 2.8 and 4.2 times more effective in inhibiting the D10 and W2 strains of the parasite,respectively,compared to non-encapsulated *** findings support a role for novel o/w nanoemulsions as delivery vehicles for antimalarial drugs.

关键词： Azacarbazoles Flax oil n-3 and n-6 polyunsaturated fatty acids ethyl esters Nanoemulsion P.falciparum Malaria

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