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Widening the Therapeutic Perspectives of Clofazimine by Its Loading in Sulfobutylether β-Cyclodextrin Nanocarriers: Nanomolar IC
- Source :
- Molecular pharmaceutics. 15(9)
- Publication Year :
- 2018
-
Abstract
- Clofazimine (CLZ) is an antibiotic with a promising behavior against Gram-positive bacteria; however, the drug is completely insoluble in water and accumulates in fat tissues. We explored nanocarriers, labeled and not labeled with rhodamine, consisting of negatively charged sulfobutylether-β-cyclodextrins for CLZ loading. A new oligomeric carrier was obtained cross-linking βCyD with epichlorohydrin followed by sulfonation in a strongly alkaline aqueous medium. The oligomeric carrier has a MW of 53 kDa and forms small nanoparticles of a few tens of nm. With aqueous solutions containing a 25 mg/mL oligomeric carrier, we loaded up to 0.5 mg/mL of drug. The oligomers exhibited a 10-fold better loading capacity compared to monomers and formed nanoparticles with a size in the 20-60 nm range after drug loading. Circular dichroism confirmed encapsulation of the CLZ in the nanocarriers. All carriers with or without CLZ are not cytotoxic up to 1 μM, while CLZ alone is highly cytotoxic at the same concentration. The drug has IC
Details
- ISSN :
- 15438392
- Volume :
- 15
- Issue :
- 9
- Database :
- OpenAIRE
- Journal :
- Molecular pharmaceutics
- Accession number :
- edsair.pmid..........aa7a309a38c2957979241fd2dae915ee