Cytotoxicity and teratogenicity of chlorhexidine diacetate released from hollow nylon fibres

• Published in: Journal of pharmacy and pharmacology Vol. 52; no. 7; p. 779
• Main Authors: Ostad, S N, Gard, P R
• Format: Journal Article
• Language: English
• Published: England 01.07.2000
• Subjects: Animals; Anti-Infective Agents, Local - administration & dosage; Anti-Infective Agents, Local - toxicity; Cell Survival - drug effects; Cells, Cultured; Chlorhexidine - administration & dosage; Chlorhexidine - toxicity; Drug Carriers; Drug Delivery Systems; Endometrium - cytology; Endometrium - drug effects; Female; Guinea Pigs; Nylons; Rats
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1211/0022357001774633

Intra-uterine contraceptive devices are associated with an increased incidence of pelvic infections, possible due to the introduction of vaginal bacteria into the uterus at insertion. One potential means to overcome this problem is the use of a device which releases the antimicrobial agent chlorhexidine although such an approach carries with it the risk of adverse effects on the endometrium and, possibly, teratogenic effects. Cultured monolayers of endometrial cells were used to assess the cytotoxicity of both chlorhexidine and chlorhexidine-releasing devices. The results indicated that the agent is toxic at concentrations of 1 microg mL(-1) and that the devices potentiated the toxicity. When the devices were tested in a guinea-pig model, endometrial damage was seen only at the high dose of chlorhexidine, suggesting that there is greater distribution of chlorhexidine in-vivo. Assessment of the teratogenic effects of chlorhexidine in rat embryonic limb bud tissue cells in-vitro showed that the foetal cells were highly susceptible to the toxic effects of chlorhexidine, but that there was no evidence of teratogenicity. Overall, the findings suggest that chlorhexidine-releasing devices may be a safe means of reducing infections related to intra-uterine devices, but that the chlorhexidine may have a toxic effect on foetal cells.