%0 Journal Article
%T Formulation of Bioerodible Ketamine Microparticles as an Analgesic Adjuvant Treatment Produced by Supercritical Fluid Polymer Encapsulation
%A Andrew K. Whittaker
%A Andrew Naylor
%A Anjumn Shabir-Ahmed
%A Cheng Zhang
%A Felicity Y. Han
%A Maree T. Smith
%A Steven M. Howdle
%J Archive of "Pharmaceutics".
%D 2018
%R 10.3390/pharmaceutics10040264
%X Pain is inadequately relieved by escalating doses of a strong opioid analgesic such as morphine in up to 25% of patients with cancer-related severe pain complicated by a neuropathic (nerve damage) component. Hence, there is an unmet medical need for research on novel painkiller strategies. In the present work, we used supercritical fluid polymer encapsulation to develop sustained-release poly(lactic-co-glycolic acid) (PLGA) biodegradable microparticles containing the analgesic adjuvant drug ketamine, for injection by the intrathecal route. Using this approach with a range of PLGA co-polymers, drug loading was in the range 10¨C60%, with encapsulation efficiency (EE) of 60¨C100%. Particles were mainly in the size range 20¨C45 ¦Ìm and were produced in the absence of organic solvents and surfactants/emulsifiers. Investigation of the ketamine release profiles from these PLGA-based microparticles in vitro showed that release took place over varying periods in the range 0.5¨C4.0 weeks. Of the polymers assessed, the ester end-capped PLGA5050DLG-1.5E gave the best-controlled release profile with drug loading at 10%
%K analgesic adjuvant
%K ketamine
%K cancer pain
%K drug delivery
%K poly(lactic-co-glycolic acid) (PLGA)
%K sustained release
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321204/