REDUCTION IN THE LOCAL TISSUE TOXICITY OF CHLORPROMAZINE BY β-CYCLODEXTRIN COMPLEXATION

Effect of β-cyclodextrin (β-CyD) on the local tissue toxicity of chlorpromazine (CPZ) was investigated following the intramuscular injection to rabbits. From the gross and histological examinations, β-CyD was found to alleviate the muscular tissue damage produced by CPZ on M. vastus lateralis in rabbits. The protective effect of β-CyD may be ascribed to the decrease in affinity of CPZ to the tissue membrane through inclusion complexation. The present data suggest that β-CyD complexation is particularly useful to reduce the local toxicity of phenothiazine neuroleptics without altering the pharmacological efficacy.