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The human ether-a’-go-go related gene (hERG) Kplus channel blockade by the investigative selective-serotonin reuptake inhibitor CONA-437: limited dependence on S6 aromatic residues

100%

Alexandrou A. J., Milnes J. T., Sun S. Z., Fermini B., Kim S. C., Jenkinson S., Leishman D. J., Witchel H. J., Hancox J. C., Leaney J.

Journal of Physiology and Pharmacology

2014

tom 65

nr 4

Cellular uptake of coumarin-6 as a model drug loaded in solid lipid nanoparticles

58%

Rivolta I., Panariti A., Lettiero B., Sesana S., Gasco P., Gasco M. R., Masserini M., Miserocchi G.

Journal of Physiology and Pharmacology

2011

tom 62

nr 1

The aim of present work was to elucidate the interaction of solid lipid nanoparticles (SLNs) with cellular plasma-membrane to gain insight of intracellular drug delivery. To this aim we followed the uptake of coumarin-6 (a drug model) either free in the extracellular medium or loaded on SLN (c-SLN). Alveolar epithelial cells were exposed to a biocompatible concentration of c-SLN (0.01 mg/ml of tripalmitin) prepared by warm microemulsion whose lipid matrix was constituted by low melting point molecules (fatty acids, triglycerides). Intracellular fluorescence and preferential accumulation in the perinuclear region were increased by 54.8% on comparing c-SLN to the same amount of free coumarin-6 in the medium. Lowering temperature from 37° to 4°C decreased the intracellular signal intensity by about 48% equally for the free as well as for loaded drug, thus suggesting the inhibition of a similar non-endocytotic entrance pathway. No specific co-localization of the fluorescence with intracellular organelles was found. The c-SLN calorimetric profile obtained with differential scanning calorimetry (DSC), revealing transition within the range 58-62°C, altered remarkably upon incubation with cells, suggesting a change in SLN structure after association with cells membranes. We propose that the uptake of the model drug loaded on SLN is only partly related to the endocytotic pathway; it occurs despite the loss of integrity of the original SLN structure and it appears to be more efficient when the drug is vehicled rather than being free in the culture medium.

Ograniczanie wyników

2 Journal of Physiology and Pharmacology

1 Alexandrou A. J.

1 Fermini B.

1 Gasco M. R.

1 Gasco P.

1 Hancox J. C.

1 Jenkinson S.

1 Kim S. C.

1 Leaney J.

1 Leishman D. J.

1 Lettiero B.

1 Masserini M.

1 Milnes J. T.

1 Miserocchi G.

1 Panariti A.

1 Rivolta I.

1 Sesana S.

1 Sun S. Z.

1 Witchel H. J.

1 2014

1 2011

Wyniki wyszukiwania

The human ether-a’-go-go related gene (hERG) Kplus channel blockade by the investigative selective-serotonin reuptake inhibitor CONA-437: limited dependence on S6 aromatic residues

Cellular uptake of coumarin-6 as a model drug loaded in solid lipid nanoparticles