title: Amorphous nanodrugs prepared by complexation with polysaccharides: carrageenan versus dextran sulfate.
abstract: 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.
authors.affiliation: School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore 637459, Singapore.
authors.forename: Wean Sin
authors.initials: WS
authors.lastname: Cheow
authors.affiliation: School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore 637459, Singapore.
authors.forename: Tie Yi
authors.initials: TY
authors.lastname: Kiew
authors.affiliation: School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore 637459, Singapore. Electronic address: kunnong@ntu.edu.sg.
authors.forename: Kunn
authors.initials: K
authors.lastname: Hadinoto
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002939:Ciprofloxacin / Q000737:chemistry / Q000494:pharmacology*; D016264:Dextran Sulfate / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004926:Escherichia coli / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D053769:Nanocapsules / Q000737:chemistry; D010316:Particle Size; D011134:Polysaccharides / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013499:Surface Properties
chemical_list: D000900:Anti-Bacterial Agents; D053769:Nanocapsules; D011134:Polysaccharides; D002939:Ciprofloxacin; D002351:Carrageenan; D016264:Dextran Sulfate
keywords: Colloidal polysaccharides; Drug-polysaccharide complex; Nanomedicine; Polysaccharide nanoparticles; Supersaturated drug delivery system