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Int. J. Mol. Sci. 2014, 15(10), 17469-17477; doi:10.3390/ijms151017469

The Pharmacokinetics and Pharmacodynamics of Lidocaine- Loaded Biodegradable Poly(lactic-co-glycolic acid) Microspheres

Department of Anesthesiology, Shanghai Pulmonary Hospital, Tongji University School of Medicine, 507 Zhengmin Road, Yangpu District, Shanghai 200433, China
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Received: 8 July 2014 / Revised: 13 August 2014 / Accepted: 10 September 2014 / Published: 29 September 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

The purpose of this study was to develop novel lidocaine microspheres. Microspheres were prepared by the oil-in-water (o/w) emulsion technique using poly(d,l-lactide-co-glycolide acid) (PLGA) for the controlled delivery of lidocaine. The average diameter of lidocaine PLGA microspheres was 2.34 ± 0.3 μm. The poly disperse index was 0.21 ± 0.03, and the zeta potential was +0.34 ± 0.02 mV. The encapsulation efficiency and drug loading of the prepared microspheres were 90.5% ± 4.3% and 11.2% ± 1.4%. In vitro release indicated that the lidocaine microspheres had a well-sustained release efficacy, and in vivo studies showed that the area under the curve of lidocaine in microspheres was 2.02–2.06-fold that of lidocaine injection (p < 0.05). The pharmacodynamics results showed that lidocaine microspheres showed a significant release effect in rats, that the process to achieve efficacy was calm and lasting and that the analgesic effect had a significant dose-dependency. View Full-Text
Keywords: lidocaine; PLGA; microspheres; pharmacokinetics; pharmacodynamics lidocaine; PLGA; microspheres; pharmacokinetics; pharmacodynamics
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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MDPI and ACS Style

Liu, J.; Lv, X. The Pharmacokinetics and Pharmacodynamics of Lidocaine- Loaded Biodegradable Poly(lactic-co-glycolic acid) Microspheres. Int. J. Mol. Sci. 2014, 15, 17469-17477.

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