A Toolbox for Mimicking Gastrointestinal Conditions in Children: Simulated Paediatric Breakfast Media (SPBM) for Addressing the Variability of Gastric Contents After Typical Paediatric Breakfasts

Freerks, Lisa; Zielke, Carolin; Tarnow, Marie-Josefin; Ariën, Tina; Mackie, Claire; Inghelbrecht, Sabine; Klein, Sandra

doi:10.1016/j.xphs.2021.05.003

Cited by 4 publications

(2 citation statements)

References 38 publications

(40 reference statements)

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“…The extent to which the free pentathiepin dissolves in PBS was determined following the method described by Freerks et al [ 24 ] with modifications. Two milliliters of PBS at 23°C were filled into a 5 mL Schott Fiolax® screw neck vial, then an excess of pentathiepin was added to each vial (ca.…”

Section: Methodsmentioning

confidence: 99%

Liposomal formulation of model pentathiepin improves solubility and stability toward glutathione while preserving anticancer activity

Napierkowski

Janke

Rong

et al. 2023

Archiv der Pharmazie

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The biological properties of pentathiepins have been attracting increased attention in recent years. Experiments have shown a wide range of effects of pentathiepins in vitro, such as induction of apoptosis and alteration of mitochondrial membrane potential in cancer cells, and inhibition of antioxidant enzymes, for example, glutathione peroxidase 1 (GPx1). Biological evaluation is sometimes limited due to low aqueous solubility, high lipophilicity, and poor stability toward thiols, for example, glutathione (GSH). To assess whether liposomes are suitable as drug carriers to overcome these drawbacks, a model pentathiepin was formulated in a liposomal preparation. The success of loading liposomes with pentathiepins was evaluated by using ultraviolet‐visible light (UV‐Vis) spectroscopy, dynamic light scattering (DLS), and high‐performance liquid chromatography (HPLC). Through inclusion into 100‐nm‐sized 1,2‐dioleoyl‐sn‐glycero‐3‐phosphocholine liposomes, the aqueous solubility of a representative pentathiepin could be increased by several orders of magnitude to ca. 400 µM. The stability of the pentathiepin in the presence of GSH was increased fourfold as determined by UV‐Vis spectroscopy. In antiproliferation experiments with two human cancer cell lines, no decrease in potency in the liposomal loaded pentathiepin compared to the free pentathiepin was found. In conclusion, liposomes are a suitable carrier for pentathiepins and improve both solubility and stability in the presence of thiols without compromising anticancer activity.

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Section: Methodsmentioning

confidence: 99%

Liposomal formulation of model pentathiepin improves solubility and stability toward glutathione while preserving anticancer activity

Napierkowski

Janke

Rong

et al. 2023

Archiv der Pharmazie

View full text Add to dashboard Cite

show abstract

“…A major limitation of in-vitro tools to predict a fed effect in paediatrics has been the lack of clinical data against which such methods can be validated. Recent work has generated simulated paediatric breakfast media that may be used in in-vitro risk assessment of fed effects for future paediatric products (Freerks et al, 2021). Additional work has generated biorelevant dissolution testing conditions that include dosing with soft food and drinks (Martir et al, 2020a(Martir et al, , 2020b.…”

Section: Use Of In-vitro Tools To Predict a Food Effectmentioning

confidence: 99%

Practical and operational considerations related to paediatric oral drug formulation: An industry survey

Veken

Brouwers

Budts

et al. 2022

International Journal of Pharmaceutics

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Parameters to consider for successful medication use in older adults - An AGePOP review

Hummler

Sarwinska

Gollasch

et al. 2023

European Journal of Pharmaceutical Sciences

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A Toolbox for Mimicking Gastrointestinal Conditions in Children: Simulated Paediatric Breakfast Media (SPBM) for Addressing the Variability of Gastric Contents After Typical Paediatric Breakfasts

Cited by 4 publications

References 38 publications

Liposomal formulation of model pentathiepin improves solubility and stability toward glutathione while preserving anticancer activity

Liposomal formulation of model pentathiepin improves solubility and stability toward glutathione while preserving anticancer activity

Practical and operational considerations related to paediatric oral drug formulation: An industry survey

Parameters to consider for successful medication use in older adults - An AGePOP review

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