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Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity. / Berezin, Alexander S.; Skorik, Yury A.

In: Carbohydrate Polymers, Vol. 127, 2015.

Research output: Contribution to journal › Article

Harvard

Berezin, AS & Skorik, YA 2015, 'Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity', Carbohydrate Polymers, vol. 127. https://doi.org/10.1016/j.carbpol.2015.03.060

APA

Berezin, A. S., & Skorik, Y. A. (2015). Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity. Carbohydrate Polymers, 127. https://doi.org/10.1016/j.carbpol.2015.03.060

Vancouver

Berezin AS, Skorik YA. Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity. Carbohydrate Polymers. 2015;127. https://doi.org/10.1016/j.carbpol.2015.03.060

Author

Berezin, Alexander S. ; Skorik, Yury A. / Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity. In: Carbohydrate Polymers. 2015 ; Vol. 127.

BibTeX

@article{87435cac24e245579483150d99980397,
title = "Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity",
abstract = "tNovel water-soluble chitosan-isoniazid conjugates were synthesized by two methods: (1) the carbodi-imide method using isoniazid (INH) and N-(2-carboxyethyl)chitosan (CEC), and (2) the reaction betweenINH and N-(3-chloro-2-hydroxypropyl)chitosan (CHPC). The solubility of the conjugates under physi-ological conditions was enhanced by phosphorylation. Method (1) is preferable in terms of obtainingconjugates with a high content of active substance; depending on reaction conditions, the degree ofsubstitution in the INH-CEC conjugates varies from 0.08 tо 0.39. Ultrasound treatment increased thereaction rate by a factor of 1.3–1.5, but caused partial degradation of the polymer. Consecutive modifi-cation led to a considerable decrease in polymer biodegradability in the following order: chitosan > CECor CHPC > conjugate. In vitro screening of the antimicrobial activity against Mycobacterium tuberculosisH37Rv demonstrated a comparable or slightly higher minimum inhibitory concentration for conjugatesthan for INH itsel",
keywords = "Chitosan Isoniazid Conjugate Carbodiimide activation Activated ester method Drug delivery Toxicity Limax flavus",
author = "Berezin, {Alexander S.} and Skorik, {Yury A.}",
year = "2015",
doi = "10.1016/j.carbpol.2015.03.060",
language = "English",
volume = "127",
journal = "Carbohydrate Polymers",
issn = "0144-8617",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Chitosan-isoniazid conjugates: Synthesis, evaluation of tuberculostatic activity, biodegradability and toxicity

AU - Berezin, Alexander S.

AU - Skorik, Yury A.

PY - 2015

Y1 - 2015

N2 - tNovel water-soluble chitosan-isoniazid conjugates were synthesized by two methods: (1) the carbodi-imide method using isoniazid (INH) and N-(2-carboxyethyl)chitosan (CEC), and (2) the reaction betweenINH and N-(3-chloro-2-hydroxypropyl)chitosan (CHPC). The solubility of the conjugates under physi-ological conditions was enhanced by phosphorylation. Method (1) is preferable in terms of obtainingconjugates with a high content of active substance; depending on reaction conditions, the degree ofsubstitution in the INH-CEC conjugates varies from 0.08 tо 0.39. Ultrasound treatment increased thereaction rate by a factor of 1.3–1.5, but caused partial degradation of the polymer. Consecutive modifi-cation led to a considerable decrease in polymer biodegradability in the following order: chitosan > CECor CHPC > conjugate. In vitro screening of the antimicrobial activity against Mycobacterium tuberculosisH37Rv demonstrated a comparable or slightly higher minimum inhibitory concentration for conjugatesthan for INH itsel

AB - tNovel water-soluble chitosan-isoniazid conjugates were synthesized by two methods: (1) the carbodi-imide method using isoniazid (INH) and N-(2-carboxyethyl)chitosan (CEC), and (2) the reaction betweenINH and N-(3-chloro-2-hydroxypropyl)chitosan (CHPC). The solubility of the conjugates under physi-ological conditions was enhanced by phosphorylation. Method (1) is preferable in terms of obtainingconjugates with a high content of active substance; depending on reaction conditions, the degree ofsubstitution in the INH-CEC conjugates varies from 0.08 tо 0.39. Ultrasound treatment increased thereaction rate by a factor of 1.3–1.5, but caused partial degradation of the polymer. Consecutive modifi-cation led to a considerable decrease in polymer biodegradability in the following order: chitosan > CECor CHPC > conjugate. In vitro screening of the antimicrobial activity against Mycobacterium tuberculosisH37Rv demonstrated a comparable or slightly higher minimum inhibitory concentration for conjugatesthan for INH itsel

KW - Chitosan Isoniazid Conjugate Carbodiimide activation Activated ester method Drug delivery Toxicity Limax flavus

U2 - 10.1016/j.carbpol.2015.03.060

DO - 10.1016/j.carbpol.2015.03.060

M3 - Article

VL - 127

JO - Carbohydrate Polymers

JF - Carbohydrate Polymers

SN - 0144-8617

ER -

ID: 3979382