Evaluation of the cytotoxicity of cyclodextrins and hydroxypropylated derivatives

The haemolytic effect toward human erythrocytes and the cytotoxicity toward P388 cells of the three natural cyclodextrins and their hydroxypropylated derivatives have been compared. The cytotoxicity of the six cyclodextrins toward these two cell types follows a similar pattern, and the curve paramet...

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Published inInternational journal of pharmaceutics Vol. 101; no. 1; pp. 97 - 103
Main Authors Leroy-Lechat, Frédérique, Wouessidjewe, Denis, Andreux, Jean-Paul, Puisieux, F., Duchêne, Dominique
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier B.V 1994
Elsevier
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Abstract The haemolytic effect toward human erythrocytes and the cytotoxicity toward P388 cells of the three natural cyclodextrins and their hydroxypropylated derivatives have been compared. The cytotoxicity of the six cyclodextrins toward these two cell types follows a similar pattern, and the curve parameters are generally of the same order of magnitude for both cell types in spite of the biological differences. The in vitro cytotoxic effect decreases in the order βCD > αCD > γCD and HPβCD > HPγCD > = HPαCD. These results showed that phenomena involved in cyclodextrin cytotoxicity are not specific to the cell type, and bore out the hypothesis of destruction of membranes by the removal of basic membrane components. Moreover, they demonstrated the influence of parameters other than CD concentration, i.e., the presence of serum components, or the density of the cells, which can dramatically influence the cytotoxic effect of CDs. In fact, the cytotoxicity of a cyclodextrin is determined by the relative proportion of cellular and extracellular molecules likely to be included and cyclodextrins.
AbstractList The haemolytic effect toward human erythrocytes and the cytotoxicity toward P388 cells of the three natural cyclodextrins and their hydroxypropylated derivatives have been compared. The cytotoxicity of the six cyclodextrins toward these two cell types follows a similar pattern, and the curve parameters are generally of the same order of magnitude for both cell types in spite of the biological differences. The in vitro cytotoxic effect decreases in the order βCD > αCD > γCD and HPβCD > HPγCD > = HPαCD. These results showed that phenomena involved in cyclodextrin cytotoxicity are not specific to the cell type, and bore out the hypothesis of destruction of membranes by the removal of basic membrane components. Moreover, they demonstrated the influence of parameters other than CD concentration, i.e., the presence of serum components, or the density of the cells, which can dramatically influence the cytotoxic effect of CDs. In fact, the cytotoxicity of a cyclodextrin is determined by the relative proportion of cellular and extracellular molecules likely to be included and cyclodextrins.
Author Andreux, Jean-Paul
Duchêne, Dominique
Leroy-Lechat, Frédérique
Puisieux, F.
Wouessidjewe, Denis
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Issue 1
Keywords Cyclodextrin
P388 cell
Cytotoxicity
Serum
Inclusion ability
Hydroxypropylated cyclodextrin
In vitro hemolysis
Cell density
Human
Hemolysis
Toxicity
Oligosaccharide
P388-Leukemia
Red blood cell
In vitro
Blood
Inclusion compound
Tumor cell
Language English
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Snippet The haemolytic effect toward human erythrocytes and the cytotoxicity toward P388 cells of the three natural cyclodextrins and their hydroxypropylated...
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elsevier
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StartPage 97
SubjectTerms Biological and medical sciences
Cell density
Cyclodextrin
Cytotoxicity
Drug toxicity and drugs side effects treatment
Hydroxypropylated cyclodextrin
In vitro hemolysis
Inclusion ability
Medical sciences
P388 cell
Pharmacology. Drug treatments
Serum
Toxicity: blood
Title Evaluation of the cytotoxicity of cyclodextrins and hydroxypropylated derivatives
URI https://dx.doi.org/10.1016/0378-5173(94)90080-9
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