4.4 Article

Loading, release profile and accelerated stability assessment of monoterpenes-loaded solid lipid nanoparticles (SLN)

Journal

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
Volume 25, Issue 7, Pages 832-844

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/10837450.2020.1744008

Keywords

Monoterpenes; Alpha-pinene; citral; geraniol; limonene; SLN; LUMiSizer

Funding

  1. Portuguese Science and Technology Foundation (FCT/MCT)
  2. European Funds (PRODER/COMPETE) [UIDB/04469/2020, M-ERA-NET/0004/2015-PAIRED]
  3. FEDER under Partnership Agreement [PT2020]

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Glycerol monostearate solid lipid nanoparticles (SLN) were produced by hot high-pressure homogenization technique to load alpha-pinene, citral, geraniol or limonene. SLN were composed of 1 wt.% monoterpene, 4 wt.% of Imwitor(R) 900K as a solid lipid and 2.5 wt.% of Poloxamer188 as a surfactant. Empty SLN consisted of 5 wt.% of Imwitor (R) 900K and 2.5 wt.% of Poloxamer188. The mean particles size (Z-Ave) and polydispersity index (PDI) of SLN were analyzed by dynamic light scattering (DLS), while the zeta potential (ZP) of each formulation were measured by electrophoretic light scattering. LUMiSizer(R) was applied to calculate the velocity distribution in the centrifugal field and instability index. Drug release profile from SLN was analyzed using Franz cell diffusion cells assayed by UV-Vis spectrophotometry, whereas the gas chromatography technique was applied to determine the encapsulation parameters of volatile monoterpenes. The matrix state, polymorphism and phase behavior of SLN were studied by X-ray diffraction (XRD, low and wide angles) and differential scanning calorimetry (DSC). Selected monoterpenes were successfully loaded in glycerol monostearate SLN. A burst release profile within the first 15 min was observed for all formulations, being the modified release profile dependent on the type of monoterpene and on the encapsulation efficiency.

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