Article ID Journal Published Year Pages File Type
5521516 European Journal of Pharmaceutics and Biopharmaceutics 2017 6 Pages PDF
Abstract

•Cochleates are phospholipid-based, calcium-stabilized drug delivery vehicles.•They tend to self-aggregate during production and storage.•Transient addition of citric acid effectively disperses cochleate aggregates.•Citric acid removes calcium ions from the cochleate surface.•Dispersity and structure of the particles are stable for long time.

Cochleates, calcium-stabilized membrane rolls of nanoscale diameter, promise a unique and efficient way of delivering lipid-soluble drugs, proteins or nucleic acids into biological systems because they protect the encapsulated material against enzymatic or chemical degradation. Self-aggregation, which typically arises during production and storage is a major obstacle that has so far precluded the development of an efficient cochleate-based drug-delivery system. Here we show that citric acid, added transiently in a narrow concentration range, effectively disperses cochleate aggregates, stabilizes the disperse state for long-term storage and preserves the canonical ultrastructure and topological characteristics of cochleate nanoparticles.

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