Drug/cyclodextrin complexes self-assemble in aqueous solutions to form nanoparticles or aggregates. The invisible complex aggregates with diameter of less than 250 nm are responsible for many of the physicochemical and biological properties of cyclodextrin complexes. Due to the aggregate formation aqueous drug/cyclodextrin solutions can behave more like dispersed nanoscale systems, such as nano-suspensions and liposomes, rather than true solutions. The drug/cyclodextrin nanoparticles are unstable and dissociate upon media dilution, heating or addition of organic solvent to the aqueous complexation media, a behavior that resembles that of micellar aggregates (i.e. micelles). Although the nanoparticles are unstable their stability can be increased by, for example, including water-soluble polymers in the aqueous complexation media. The drug/cyclodextrin complex nanoparticles can result in enhanced cyclodextrin solubilization of poorly soluble lipophilic drugs; they can serve as building blocks for ternary or higher order complexes; and they can be developed into nanoparticle drug carriers for targeted drug delivery. Several examples will be given of (1) how the aggregation affects analysis of cyclodextrin complexes, (2) how the aggregates affect cyclodextrin solubilization of drugs, (3) excipient-aggregate interactions, and (4) how the larger aggregates enhance topical drug delivery to the eye.

Physicochemical properties of self-assembled cyclodextrin nanoparticles and their application in drug delivery

256th National Meeting (2018)

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