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Pharmaceutics 2018, 10(4), 264; https://doi.org/10.3390/pharmaceutics10040264

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

1
School of Biomedical Sciences, Faculty of Medicine, The University of Queensland, Brisbane QLD 4072, Australia
2
Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, Brisbane QLD 4072, Australia
3
ARC Centre of Excellence in Convergent Bio Nano Science and Technology, The University of Queensland, Brisbane QLD 4072, Australia
4
School of Chemistry, University of Nottingham, Nottingham NG7 2RD, UK
5
Critical Pharmaceuticals Ltd., BioCity Nottingham, Nottingham NG1 1GF, UK
6
Upperton Limited, Biocity Nottingham, Nottingham NG7 2TN, UK
7
School of Pharmacy, Faculty of Health and Behavioural Sciences, The University of Queensland, Brisbane QLD 4072, Australia
*
Author to whom correspondence should be addressed.
Received: 7 November 2018 / Revised: 28 November 2018 / Accepted: 4 December 2018 / Published: 6 December 2018
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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%. View Full-Text
Keywords: analgesic adjuvant; ketamine; cancer pain; drug delivery; poly(lactic-co-glycolic acid) (PLGA); sustained release analgesic adjuvant; ketamine; cancer pain; drug delivery; poly(lactic-co-glycolic acid) (PLGA); sustained release
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Han, F.Y.; Whittaker, A.K.; Howdle, S.M.; Naylor, A.; Shabir-Ahmed, A.; Zhang, C.; Smith, M.T. Formulation of Bioerodible Ketamine Microparticles as an Analgesic Adjuvant Treatment Produced by Supercritical Fluid Polymer Encapsulation. Pharmaceutics 2018, 10, 264.

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