کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5550083 1557283 2017 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Efficient loading of ethionamide in cyclodextrin-based carriers offers enhanced solubility and inhibition of drug crystallization
ترجمه فارسی عنوان
بارگذاری کارآمد از اتونامید در حامل های مبتنی بر سیکلوکود کسترین باعث افزایش حلالیت و مهار کریستال شدن دارو می شود
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

Ethionamide (ETH) is a second line antitubercular drug suffering from poor solubility in water and strong tendency to crystallize. These drawbacks were addressed by loading ETH in β-cyclodextrin (βCyD)-based carriers. The drug was incorporated in a molecular state avoiding crystallization even for long-term storage and obtaining a tenfold increased solubility up to 25 mM. The binding of ETH to polymeric βCyD nanoparticles (pβCyD NPs) was investigated in neutral aqueous medium by means of solubility phase diagrams, circular dichroism (CD) and UV-vis absorption and compared with the corresponding βCyD monomer. The binding constants and the absolute CD spectra of the drug complexes were determined by global analysis of multiwavelength data from spectroscopic titrations. The spectroscopic and photophysical properties of the complexes evidenced an alcohol-like environment for ETH included in the cavity. Additionally, ETH was found to be located not only in βCyD cavities, but also in confined microdomains inside the crosslinked NPs. This double modality of complexation together with a slightly higher binding constant makes the utilization of pβCyD NPs preferable over the monomeric βCyDs. In order to pave the way to future in vitro experiments, fluorescein labeled pβCyDs were synthesized. Interestingly the FITC labeling did not hamper the encapsulation of ETH and the drug improved the fluorescent signal of FITC molecules. The βCyD-based carriers appeared as versatile “green” systems for efficient incorporation and future delivery of ETH.

Α βCyD-epichlorohydrin crosslinked polymer organised in nanoparticles of ca. 15 nm size is able to solubilize the anti-tuberculosis drug Ethionamide up to 25 mM in water.266

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 531, Issue 2, 15 October 2017, Pages 568-576
نویسندگان
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