Bupivacaine-Loaded PLGA Nanoparticles for Long-Term Management of Chronic Neuropathic Pain.
4 affiliations
- 1Department of Human Anatomy, Histology and Embryology, State Key Laboratory of Common Mechanism Research for Major Diseases, Neuroscience Center, Joint Laboratory of Anesthesia and Pain, Institute of Basic Medical Sciences Chinese Academy of Medical Sciences, School of Basic Medicine Peking, Union Medical College, Beijing 100005, China.
- 2Department of Dermatology, State Key Laboratory of Complex Severe and Rare Diseases, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, National Clinical Research Center for Dermatologic and Immunologic Diseases, Beijing 100730, China.
- 3National Human Brain Bank for Development and Function, Beijing 100005, China.
- 4Chinese Institute for Brain Research, Beijing 102206, China.
Abstract
Background/Objectives: Chronic neuropathic pain imposes a substantial burden on patients and society, and opioids are unsuitable for long-term use due to their addictive potential. To overcome this limitation, we encapsulated bupivacaine in PLGA nanoparticles to achieve sustained-release analgesia with reduced systemic toxicity. Methods: The analgesic efficacy was evaluated in rat models of chronic compression of the dorsal root ganglion (CCD) and chronic constriction injury (CCI). Nanoparticles were characterized using scanning electron microscopy (SEM) for morphology and size, and X-ray diffraction (XRD) for dispersion. In vivo electrophysiological recordings, including action potentials from DRG neuronal somata and compound action potentials in the sciatic nerve, were performed to investigate peripheral analgesic mechanisms, while plasma bupivacaine concentrations were measured by high-performance liquid chromatography (HPLC). Results: Bupivacaine nanoparticles significantly alleviated mechanical pain in both CCD and CCI rats, but had no effect on thermal pain. They selectively inhibited C-fiber conduction without affecting A-fibers. Importantly, plasma bupivacaine levels remained well below the corresponding toxic thresholds, indicating a favorable safety profile. Conclusions: These findings suggest that bupivacaine-loaded PLGA nanoparticles represent a promising long-term therapeutic option for chronic neuropathic pain management.
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BibTeX
@article{wang2026bupivacaineloaded,
title = {{Bupivacaine-Loaded PLGA Nanoparticles for Long-Term Management of Chronic Neuropathic Pain.}},
author = {Tao Wang and Keyun Tang and Fengrun Sun and Yujia Ma and Yehong Fang and Ning Yu and Fan Liu and Chao Ma},
journal = {Pharmaceutics},
year = {2026},
month = sep,
doi = {10.3390/pharmaceutics18101226},
url = {https://europepmc.org/article/MED/42942757},
note = {CC BY},
}
RIS
TY - JOUR
TI - Bupivacaine-Loaded PLGA Nanoparticles for Long-Term Management of Chronic Neuropathic Pain.
AU - Tao Wang
AU - Keyun Tang
AU - Fengrun Sun
AU - Yujia Ma
AU - Yehong Fang
AU - Ning Yu
AU - Fan Liu
AU - Chao Ma
PY - 2026
DA - 2026/09/27
JO - Pharmaceutics
DO - 10.3390/pharmaceutics18101226
UR - https://europepmc.org/article/MED/42942757
AB - Background/Objectives: Chronic neuropathic pain imposes a substantial burden on patients and society, and opioids are unsuitable for long-term use due to their addictive potential. To overcome this limitation, we encapsulated bupivacaine in PLGA nanoparticles to achieve sustained-release analgesia with reduced systemic toxicity. Methods: The analgesic efficacy was evaluated in rat models of chronic compression of the dorsal root ganglion (CCD) and chronic constriction injury (CCI). Nanoparticles were characterized using scanning electron microscopy (SEM) for morphology and size, and X-ray diffraction (XRD) for dispersion. In vivo electrophysiological recordings, including action potentials from DRG neuronal somata and compound action potentials in the sciatic nerve, were performed to investigate peripheral analgesic mechanisms, while plasma bupivacaine concentrations were measured by high-performance liquid chromatography (HPLC). Results: Bupivacaine nanoparticles significantly alleviated mechanical pain in both CCD and CCI rats, but had no effect on thermal pain. They selectively inhibited C-fiber conduction without affecting A-fibers. Importantly, plasma bupivacaine levels remained well below the corresponding toxic thresholds, indicating a favorable safety profile. Conclusions: These findings suggest that bupivacaine-loaded PLGA nanoparticles represent a promising long-term therapeutic option for chronic neuropathic pain management.
SN - 1999-4923
ER -