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Development and pharmaceutical evaluation of the anticancer Anthrafuran/Cavitron complex, a prototypic parenteral drug formulation.

Abstract
To improve the water solubility of the anticancer drug candidate LCTA-2034 (A1), we investigated the formation of complexes of this anthrax[2,3-b]furan congener with the solubilizing 2-hydroxypropyl derivative of β-cyclodextrin HP-βCD (Cavitron®). The interaction of A1 with HP-βCD resulted in the inclusion complex A1/HP-βCD in 1:1 stoichiometry. The A1/HP-βCD complex was used to develop a prototype of a lyophilised drug formulation with enhanced (>10-fold) aqueous solubility than A1 and a long-term stability. The use of HP-βCD decreased the acute toxicity of A1 by >30%. The A1/HP-βCD drug formulation as well as A1 in equal doses (5×30mg/kg) to increase the lifespan by up to 140% for mice with i.p. transplanted P388 leukaemia. Furthermore, the A1/HP-βCD formulation demonstrated a significant and reliable antitumor efficacy in a Р388/ADR drug resistant leukaemia and B16/F10 melanoma, proving a perspective of investigations of toxicology, biodistribution and pharmacokinetics.
AuthorsHelen M Treshalina, Vladimir I Romanenko, Dmitry N Kaluzhny, Michael I Treshalin, Aleksey A Nikitin, Alexander S Tikhomirov, Andrey E Shchekotikhin
JournalEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences (Eur J Pharm Sci) Vol. 109 Pg. 631-637 (Nov 15 2017) ISSN: 1879-0720 [Electronic] Netherlands
PMID28927751 (Publication Type: Journal Article)
CopyrightCopyright © 2017 Elsevier B.V. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Furans
  • LCTA-2034
  • 2-Hydroxypropyl-beta-cyclodextrin
Topics
  • 2-Hydroxypropyl-beta-cyclodextrin (chemistry, pharmacology, therapeutic use, toxicity)
  • Animals
  • Antineoplastic Agents (chemistry, pharmacology, therapeutic use, toxicity)
  • Cell Survival (drug effects)
  • Drug Resistance, Neoplasm
  • Female
  • Furans (chemistry, pharmacology, therapeutic use, toxicity)
  • HCT116 Cells
  • Humans
  • Lethal Dose 50
  • Leukemia (drug therapy)
  • Melanoma, Experimental (drug therapy)
  • Mice, Inbred C57BL
  • Mice, Inbred DBA

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