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Improved efficacy of doxycycline in liposomes against Plasmodium falciparum in culture and Plasmodium berghei infection in mice

The rate at which Plasmodium falciparum is developing resistance to clinically used antimalarial drugs is alarming. Therefore, there is a compelling need to develop an efficient drug delivery system to improve the efficacy of existing antimalarial agents and circumvent drug resistance. Here, we repo... Full description

Journal Title: Canadian journal of physiology and pharmacology November 2018, Vol.96(11), pp.1145-1152
Main Author: Rajendran, Vinoth
Other Authors: Singh, Chanchal , Ghosh, Prahlad C
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: E-ISSN: 1205-7541 ; PMID: 30075085 Version:1 ; DOI: 10.1139/cjpp-2018-0067
Link: http://pubmed.gov/30075085
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recordid: medline30075085
title: Improved efficacy of doxycycline in liposomes against Plasmodium falciparum in culture and Plasmodium berghei infection in mice
format: Article
creator:
  • Rajendran, Vinoth
  • Singh, Chanchal
  • Ghosh, Prahlad C
subjects:
  • Peg-Liposomes
  • Plasmodium
  • Antimalarials
  • Antimalariaux
  • Doxycycline
  • Liposomes
  • Antimalarials -- Administration & Dosage
  • Doxycycline -- Administration & Dosage
  • Drug Carriers -- Chemistry
  • Malaria -- Drug Therapy
  • Plasmodium Berghei -- Pathogenicity
  • Plasmodium Falciparum -- Drug Effects
ispartof: Canadian journal of physiology and pharmacology, November 2018, Vol.96(11), pp.1145-1152
description: The rate at which Plasmodium falciparum is developing resistance to clinically used antimalarial drugs is alarming. Therefore, there is a compelling need to develop an efficient drug delivery system to improve the efficacy of existing antimalarial agents and circumvent drug resistance. Here, we report the antibacterial drug doxycycline (DOXY) in liposomal formulations exhibits enhanced antiplasmodial activity against blood stage forms of P. falciparum (3D7) in culture and established Plasmodium berghei NK-65 infection in murine model. Parasite killing on blood stage forms in culture was determined by a radiolabeled [H] hypoxanthine incorporation assay and infected erythrocytes stained with Giemsa were counted using microscopy in vivo. The 50% inhibitory concentration (IC) of DOXY-stearylamine liposome (IC 0.36 μM) and DOXY-SPC:Chol-liposome (IC 0.85 μM) exhibited marked growth inhibition of parasites compared with free DOXY (IC 14 μM), with minimal toxicity to normal erythrocytes. Administration...
language: eng
source:
identifier: E-ISSN: 1205-7541 ; PMID: 30075085 Version:1 ; DOI: 10.1139/cjpp-2018-0067
fulltext: fulltext
issn:
  • 12057541
  • 1205-7541
url: Link


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titleImproved efficacy of doxycycline in liposomes against Plasmodium falciparum in culture and Plasmodium berghei infection in mice
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subjectPeg-Liposomes ; Plasmodium ; Antimalarials ; Antimalariaux ; Doxycycline ; Liposomes ; Antimalarials -- Administration & Dosage ; Doxycycline -- Administration & Dosage ; Drug Carriers -- Chemistry ; Malaria -- Drug Therapy ; Plasmodium Berghei -- Pathogenicity ; Plasmodium Falciparum -- Drug Effects
descriptionThe rate at which Plasmodium falciparum is developing resistance to clinically used antimalarial drugs is alarming. Therefore, there is a compelling need to develop an efficient drug delivery system to improve the efficacy of existing antimalarial agents and circumvent drug resistance. Here, we report the antibacterial drug doxycycline (DOXY) in liposomal formulations exhibits enhanced antiplasmodial activity against blood stage forms of P. falciparum (3D7) in culture and established Plasmodium berghei NK-65 infection in murine model. Parasite killing on blood stage forms in culture was determined by a radiolabeled [H] hypoxanthine incorporation assay and infected erythrocytes stained with Giemsa were counted using microscopy in vivo. The 50% inhibitory concentration (IC) of DOXY-stearylamine liposome (IC 0.36 μM) and DOXY-SPC:Chol-liposome (IC 0.85 μM) exhibited marked growth inhibition of parasites compared with free DOXY (IC 14 μM), with minimal toxicity to normal erythrocytes. Administration...
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descriptionThe rate at which Plasmodium falciparum is developing resistance to clinically used antimalarial drugs is alarming. Therefore, there is a compelling need to develop an efficient drug delivery system to improve the efficacy of existing antimalarial agents and circumvent drug resistance. Here, we report the antibacterial drug doxycycline (DOXY) in liposomal formulations exhibits enhanced antiplasmodial activity against blood stage forms of P. falciparum (3D7) in culture and established Plasmodium berghei NK-65 infection in murine model. Parasite killing on blood stage forms in culture was determined by a radiolabeled [H] hypoxanthine incorporation assay and infected erythrocytes stained with Giemsa were counted using microscopy in vivo. The 50% inhibitory concentration (IC) of DOXY-stearylamine liposome (IC 0.36 μM) and DOXY-SPC:Chol-liposome (IC 0.85 μM) exhibited marked growth inhibition of parasites compared with free DOXY (IC 14 μM), with minimal toxicity to normal erythrocytes. Administration...
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abstractThe rate at which Plasmodium falciparum is developing resistance to clinically used antimalarial drugs is alarming. Therefore, there is a compelling need to develop an efficient drug delivery system to improve the efficacy of existing antimalarial agents and circumvent drug resistance. Here, we report the antibacterial drug doxycycline (DOXY) in liposomal formulations exhibits enhanced antiplasmodial activity against blood stage forms of P. falciparum (3D7) in culture and established Plasmodium berghei NK-65 infection in murine model. Parasite killing on blood stage forms in culture was determined by a radiolabeled [H] hypoxanthine incorporation assay and infected erythrocytes stained with Giemsa were counted using microscopy in vivo. The 50% inhibitory concentration (IC) of DOXY-stearylamine liposome (IC 0.36 μM) and DOXY-SPC:Chol-liposome (IC 0.85 μM) exhibited marked growth inhibition of parasites compared with free DOXY (IC 14 μM), with minimal toxicity to normal erythrocytes. Administration...
doi10.1139/cjpp-2018-0067
pmid30075085
date2018-11