Extended release formulations for local anaesthetic agents

• Published in: Anaesthesia Vol. 67; no. 8; pp. 906 - 916
• Main Authors: Weiniger, C. F., Golovanevski, L., Domb, A. J., Ickowicz, D.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01-08-2012; Wiley-Blackwell
• Subjects: Anesthesia; Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy; Anesthetics, Local - administration & dosage; Biological and medical sciences; Chemistry, Pharmaceutical; Clinical Trials as Topic; Delayed-Action Preparations; Drugs; Injections; Lactic Acid - administration & dosage; Liposomes; Medical sciences; Microspheres; Polyglycolic Acid - administration & dosage; Polymers; Local anesthetic; Anesthesia; Formulation
• ISSN: 0003-2409; 1365-2044
• DOI: 10.1111/j.1365-2044.2012.07168.x

Summary
Systemic toxicity through overdose of local anaesthetic agents is a real concern. By encapsulating local anaesthetics in biodegradable carriers to produce a system for prolonged release, their duration of action can be extended. This encapsulation should also improve the safety profile of the local anaesthetic as it is released at a slower rate. Work with naturally occurring local anaestheticss has also shown promise in the area of reducing systemic and neurotoxicity. Extended duration local anaesthetic formulations in current development or clinical use include liposomes, hydrophobic based polymer particles such as Poly(lactic‐co‐glycolic acid) microspheres, pasty injectable and solid polymers like Poly(sebacic‐co‐ricinoleic acid) P(SA:RA) and their combination with synthetic and natural local anaesthetic. Their duration of action, rationale and limitations are reviewed. Direct comparison of the different agents is limited by their chemical properties, the drug doses encapsulated and the details of in vivo models described.