Aescin nanoparticles prepared using SEDS: Composition stability and dissolution enhancement

- Nanoparticle of aescin, a mixture, is firstly prepared using SEDS.
- Composition is controlled by analyzing supersaturation-related parameters.
- Aescin dissolution is enhanced close to salt form but with moderate initial burst.

Aescin nanoparticles (ANPs) were prepared using solution-enhanced dispersion by supercritical fluids (SEDS) in order to improve the dissolution properties of aescin and avoid complicated salt-forming procedures. Because aescin is a mixture, the effects of the operating conditions on the composition of the ANPs were first investigated. The compositional ratio of the four dominant active components in aescin changed with the pressure at low solution concentrations (5 mg/mL), but remained constant at higher concentrations (>10 mg/mL). Spherical ANPs with an average diameter below 50 nm was obtained at 12 MPa with solution concentration between 10 to 15 mg/mL. The morphology of ANPs was primarily influenced by the concentration and pressure but not affected by the nozzle diameter. The dissolution of aescin was increased by near 5.5 times from raw aescin to ANPs. Compared with the sodium aescinate, the ANPs exhibited the similar dissolution, but had a moderate initial dissolution burst.

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