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Int. J. Mol. Sci. 2014, 15(10), 17469-17477;

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
Author to whom correspondence should be addressed.
Received: 8 July 2014 / Revised: 13 August 2014 / Accepted: 10 September 2014 / Published: 29 September 2014
(This article belongs to the Section Biochemistry)
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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

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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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