Amorphous nanodrugs prepared by complexation with polysaccharides: carrageenan versus dextran sulfate.
Amorphous nanodrugs prepared by electrostatic complexation of drug molecules with oppositely charged polysaccharides represent a promising bioavailability enhancement strategy for poorly-soluble drugs owed to their high supersaturation generation capability and simple preparation. Using ciprofloxacin (CIP) as the model drug, we investigated the effects of using dextran sulfate (DXT) or carrageenan (CGN) on the (1) preparation efficiency, (2) physical characteristics, (3) supersaturation generation, (4) antimicrobial activity, and (5) cytotoxicity of the amorphous drug-polysaccharide nanoparticle complex (nanoplex) produced. Owing to the higher charge density and chain flexibility of DXT, coupled with the greater hydrophobicity of CGN, the CIP-DXT nanoplex exhibited superior preparation efficiency and larger size than the CIP-CGN nanoplex. Whereas the low solubility and high gelation tendency of CGN resulted in superior supersaturation generation capability for the CIP-DXT nanoplex. The non-cytotoxicity, antimicrobial activity, colloidal, and amorphous state stability were established for both nanoplexes, making them an ideal supersaturated drug delivery system.
['Cheow|Wean Sin|WS|', 'Kiew|Tie Yi|TY|', 'Hadinoto|Kunn|K|']
D000900:Anti-Bacterial Agents D002351:Carrageenan D045744:Cell Line, Tumor D002939:Ciprofloxacin D016264:Dextran Sulfate D004305:Dose-Response Relationship, Drug D004926:Escherichia coli D006801:Humans D008826:Microbial Sensitivity Tests D015394:Molecular Structure D053769:Nanocapsules D010316:Particle Size D011134:Polysaccharides D013329:Structure-Activity Relationship D013499:Surface Properties
Supersaturated drug delivery system Colloidal polysaccharides Drug-polysaccharide complex Nanomedicine Polysaccharide nanoparticles