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Sustained Release of Lidocaine from Solvent-Free Biodegradable Poly[(d,l)-Lactide-co-Glycolide] (PLGA): In Vitro and In Vivo Study

1
Department of Anesthesiology, Chang Gung Memorial Hospital, Tao-Yuan 333, Taiwan
2
Graduate Institute of Medical Mechatronics, Chang Gung University, Tao-Yuan 333, Taiwan
3
Department of Mechanical Engineering, Chang Gung University, Tao-Yuan 333, Taiwan
*
Author to whom correspondence should be addressed.
Materials 2014, 7(9), 6660-6676; https://doi.org/10.3390/ma7096660
Received: 24 July 2014 / Revised: 19 August 2014 / Accepted: 9 September 2014 / Published: 16 September 2014
(This article belongs to the Section Biomaterials)
Local anesthetics are commonly used for pain relief by regional nerve blocking. In this study, we fabricated solvent-free biodegradable pellets to extend the duration of lidocaine release without any significant local or systemic toxicity levels. To manufacture the pellets, poly[(d,l)-lactide-co-glycolide] (PLGA) was first pre-mixed with lidocaine powder into different ratios. The powder mixture was then compressed with a mold (diameter of 1, 5, 8 or 10 mm) and sintered at 65 °C to form pellets. The in vitro release study showed that the lidocaine/PLGA pellets exhibited a tri-phase release behavior (a burst, a diffusion-controlled release and a degradation-dominated release) and reached completion around day 28. Scanning electron microscope (SEM) photos show that small channels could be found on the surfaces of the pellets on day 2. Furthermore, the polymer matrix swelled and fell apart on day 7, while the pellets became viscous after 10 days of in vitro elution. Perineural administration of the lidocaine/PLGA pellets produced anti-hypersensitivity effects lasting for at least 24 h in rats, significant when compared to the control group (a pure PLGA was pellet administered). In addition, no inflammation was detected within the nerve and in the neighboring muscle by histopathology. View Full-Text
Keywords: poly[(d,l)-lactide-co-glycolide] (PLGA); lidocaine; sustained release; biodegradable pellets poly[(d,l)-lactide-co-glycolide] (PLGA); lidocaine; sustained release; biodegradable pellets
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Kau, Y.-C.; Liao, C.-C.; Chen, Y.-C.; Liu, S.-J. Sustained Release of Lidocaine from Solvent-Free Biodegradable Poly[(d,l)-Lactide-co-Glycolide] (PLGA): In Vitro and In Vivo Study. Materials 2014, 7, 6660-6676.

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