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Formulation of Bioerodible Ketamine Microparticles as an Analgesic Adjuvant Treatment Produced by Supercritical Fluid Polymer Encapsulation

Han, Felicity; Whittaker, Andrew; Howdle, Steven; Naylor, Andrew; Shabir-Ahmed, Anjumn; Zhang, Cheng; Smith, Maree

Formulation of Bioerodible Ketamine Microparticles as an Analgesic Adjuvant Treatment Produced by Supercritical Fluid Polymer Encapsulation Thumbnail


Authors

Felicity Han

Andrew Whittaker

Steven Howdle

Andrew Naylor

Anjumn Shabir-Ahmed

Cheng Zhang

Maree Smith



Abstract

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 10–60%, with encapsulation efficiency (EE) of 60–100%. Particles were mainly in the size range 20–45 µm 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 0.5–4.0 weeks. Of the polymers assessed, the ester end-capped PLGA5050DLG-1.5E gave the best-controlled release profile with drug loading at 10%.

Citation

Han, F., Whittaker, A., Howdle, S., Naylor, A., Shabir-Ahmed, A., Zhang, C., & Smith, M. (2018). Formulation of Bioerodible Ketamine Microparticles as an Analgesic Adjuvant Treatment Produced by Supercritical Fluid Polymer Encapsulation. Pharmaceutics, 10(4), Article 264. https://doi.org/10.3390/pharmaceutics10040264

Journal Article Type Article
Acceptance Date Dec 4, 2018
Online Publication Date Dec 6, 2018
Publication Date Dec 6, 2018
Deposit Date Mar 4, 2019
Publicly Available Date Mar 4, 2019
Journal Pharmaceutics
Electronic ISSN 1999-4923
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 10
Issue 4
Article Number 264
DOI https://doi.org/10.3390/pharmaceutics10040264
Keywords analgesic adjuvant; ketamine; cancer pain; drug delivery; poly(lactic-co-glycolic acid) (PLGA); sustained release
Public URL https://nottingham-repository.worktribe.com/output/1603001
Publisher URL https://www.mdpi.com/1999-4923/10/4/264
Contract Date Mar 4, 2019

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