Reduction in the local tissue toxicity of chlorpromazine by beta-cyclodextrin complexation

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