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Application of Extended-release Local Anesthetics Based on Composite Polymer Materials in an Animal Model of Chronic Pain
Medical Journal of Peking Union Medical College Hospital 2022, 13(3): 433-439
Published: 30 May 2022
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Objective

To evaluate the release characteristics and analgesic effect of extended-release composite polymers of local anesthetics.

Methods

Polymer extended-release film containing bupivacaine hydrochloride was prepared via electrospinning (nanomembrane, group M), and was furthermore loaded intoPLGA-PEG-PLGA thermo-sensitive gel forming composite extended-release carrier (group G). The in vitro release profile, analgesic effect and safety in vivo were evaluated.

Results

In vitro, the cumulative release of bupivacaine hydrochloride reached more than 5 d in the group M and 10 d in the group G. In vivo, the analgesic effect in the model of chronic compression injury of sciatic nerve lasted for 14 d in the group M and group G. There was no significant difference between the two groups (P > 0.05). The peak plasma concentration of bupivacaine hydrochloride in the group M was (0.294±0.029)μg/L one day after drug administration, while (0.192±0.064)μg/L in the group G three days after drug administration, which were far below the toxic plasma level of bupivacaine chloride. Meanwhile, there were no significant pathological changes in the heart, liver, spleen, lung and kidney of the two groups.

Conclusions

In this study, the composite extended-release drug delivery prepared by bupivacaine hydrochloride electrospinning film as the basis and PLGA-PEG-PLGA thermo-sensitive gel can further prolong the release time of bupivacaine chloride and exhibit long-term analgesic effect without toxicity.

Issue
Development and Translation of Super Long-acting Analgesics
Medical Journal of Peking Union Medical College Hospital 2024, 15(2): 251-257
Published: 20 February 2024
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Pain management, listed as the fifth vital sign, has gained increasing attention from clinicians. Conventional analgesics have limited duration, leading to intense monitor and frequent dosing during the early phase in order to prevent the progression of chronic pain. Thus, prolonging the duration of analgesics has become one focus of the pain research. Several strategies, such as adding adjuvants, producing derivatives, and applying extended-release carriers, make it possible for super long-acting analgesics to come into reality. This review briefly introduces the strategies and development of the super long-acting analgesics, including the successful translation and commercialization of the present products of super long-acting analgesics. It also summarizes the application and translation of extended-release drug carriers, providing invaluable reference for the future research on the field of super long-acting analgesics.

Issue
Transdermal Technology of Local Anesthetics in Plastic and Cosmetic Surgery
Medical Journal of Peking Union Medical College Hospital 2022, 13(3): 358-362
Published: 25 April 2022
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Intraoperative anesthesia can be divided into general anesthesia and local anesthesia according to the distribution of anesthetic drugs, and local anesthesia has broad applications in plastic surgery. The short acting time and poor lipid solubility of local anesthetics on conventional dosage limit their application in transdermal delivery. In recent years, there has been rapid developments in the topical analgesic transdermal delivery system, through which a drug penetrates the cuticle of the skin and enters the dermis to block the introduction of nerve terminal pain, so as to achieve the analgesic effect. In addition, transdermal administration can significantly increase safety and patient comfort compared to injectable administration. In this review, the commonly used methods of promoting transdermal absorption and topical analgesics on the market were overviewed, and the application and future direction of anesthetics in plastic and cosmetic surgery were prospected based on the research progress.

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