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Article Publish Status: FREE
Abstract Title:

Berberine-Loaded Liposomes for the Treatment of-Infected BALB/c Mice.

Abstract Source:

Pharmaceutics. 2020 Sep 9 ;12(9). Epub 2020 Sep 9. PMID: 32916948

Abstract Author(s):

Alba Calvo, Esther Moreno, Esther Larrea, Carmen Sanmartín, Juan Manuel Irache, Socorro Espuelas

Article Affiliation:

Alba Calvo

Abstract:

Berberine (BER)-an anti-inflammatory quaternary isoquinoline alkaloid extracted from plants-has been reported to have a variety of biologic properties, including antileishmanial activity. This work addresses the preparation of BER-loaded liposomes with the aim to prevent its rapid liver metabolism and improve the drug selective delivery to the infected organs in visceral leishmaniasis (VL). BER liposomes (LP-BER) displayed a mean size of 120 nm, negative Z-potential of -38 mV and loaded 6 nmol/μmol lipid. In vitro, the loading of BER in liposomes enhanced its selectivity index more than 7-fold by decreasing its cytotoxicity to macrophages. In mice, LP-BER enhanced drug accumulation in the liver and the spleen. Consequently, the liposomal delivery of the drug reduced parasite burden in the liver and spleen by three and one logarithms (99.2 and 93.5%), whereas the free drug only decreased the infection in the liver by 1-log. The organ drug concentrations-far from ICvalues- indicate that BER immunomodulatory activity or drug metabolites also contribute to the efficacy. Although LP-BER decreased 10-fold-an extremely rapid clearance of the free drug in mice-the value remains very high. Moreover, LP-BER reduced plasma triglycerides levels.

Study Type : Animal Study
Additional Links
Pharmacological Actions : Leishmanicidal : CK(118) : AC(79)

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