Development of New Dosage forms of Niclosamide with Increased Solubility and Cytotoxic Activity

The work was devoted to increasing the solubility of the anthelmintic agent niclosamide (NS). Methods for increasing the solubility of NS were described. Alternative methods to obtaining drugs with NS solubility increased 2 – 12 times were proposed. The cytotoxic effect of the various forms of NS wa...

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Bibliographic Details
Published inPharmaceutical chemistry journal Vol. 55; no. 11; pp. 1229 - 1233
Main Authors Khalikov, S. S., Il’in, M. M., Lokshin, B. V., Kabanov, D. S., Fedotcheva, T. A., Shimanovsky, N. L.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.02.2022
Springer
Subjects
Antiparasitic agents
Drug Synthesis Methods and Manufacturing Technology
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Povidone
solubility
niclosamide
dosage forms
cytotoxicity
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Summary:The work was devoted to increasing the solubility of the anthelmintic agent niclosamide (NS). Methods for increasing the solubility of NS were described. Alternative methods to obtaining drugs with NS solubility increased 2 – 12 times were proposed. The cytotoxic effect of the various forms of NS was tested on HeLa tumor cells. It was found that a nanosuspension containing 6.6% NS showed the highest cytotoxic activity. The initial NS substance exhibited the minimum cytotoxic effect on HeLa cells as compared to a microemulsion, microcapsules, a solid dispersion, and a mixed NS:PVP solid dispersion (1:10 ratio). The cytotoxic effect of all dosage forms grew and did not depend on the NS concentration in the studied dosage forms if the incubation period of the tumor cells increased from 24 to 48 h.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02562-w