Exparel for Postoperative Pain Management: a Comprehensive Review

Kaye, Alan D.; Armstead-Williams, Cassandra; Hyatali, Farees; Cox, Katherine S; Kaye, Rachel; Eng, Lauren K.; Anwar, Muhammad; Patel, Perene V; Patil, Shilpa; Cornett, Elyse M.

doi:10.1007/s11916-020-00905-4

Cited by 25 publications

(18 citation statements)

References 48 publications

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“…22 The amide local anesthetic bupivacaine hydrochloride is often used for postoperative analgesia in clinical practice, and the action time of ordinary injection is only 5 to 7 hours, but postoperative pain usually lasts 48 to 72 hours, which is often difficult to meet the clinical needs. 23 Exparel used diethylpyrocarbonate (DEPC), dipalmitoyl phosphatidylglycerol (DPPG), Chol, and trioctyl glyceride to wrap the drug in a honeycomb shape. Bupivacaine is gradually released as each vesicle bursts, wherein the low phase transition temperature of DEPC (∼13°C) can make the drug release easier and take effect more rapidly.…”

Section: Traditional Lipid-based Nanocarriersmentioning

confidence: 99%

Lipid-Based Nanocarrier Systems for Drug Delivery: Advances and Applications

Zhao

Zhou

et al. 2022

Pharmaceutical Fronts

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Lipid-based nanocarriers have been extensively investigated for drug delivery due to their advantages including biodegradability, biocompatibility, nontoxicity, and nonimmunogenicity. However, the shortcomings of traditional lipid-based nanocarriers such as insufficient targeting, capture by the reticuloendothelial system, and fast elimination limit the efficiency of drug delivery and therapeutic efficacy. Therefore, a series of multifunctional lipid-based nanocarriers have been developed to enhance the accumulation of drugs in the lesion site, aiming for improved diagnosis and treatment of various diseases. In this review, we summarized the advances and applications of lipid-based nanocarriers from traditional to novel functional lipid preparations, including liposomes, stimuli-responsive lipid-based nanocarriers, ionizable lipid nanoparticles, lipid hybrid nanocarriers, as well as biomembrane-camouflaged nanoparticles, and further discussed the challenges and prospects of this system. This exploration may give a complete idea viewing the lipid-based nanocarriers as a promising choice for drug delivery system, and fuel the advancement of pharmaceutical products by materials innovation and nanotechnology.

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Section: Traditional Lipid-based Nanocarriersmentioning

confidence: 99%

Lipid-Based Nanocarrier Systems for Drug Delivery: Advances and Applications

Zhao

Zhou

et al. 2022

Pharmaceutical Fronts

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“…Pain treatment is a clinical challenge owing to the short duration of anesthetic effects, associated with the low molecular weight of the drugs, and the potential systemic toxicity provided by current existing treatments . At present, clinical local or regional anesthetic effects rarely last beyond 12 h unless in case of using continuous catheter infusions. , Most common prescriptions are based on antipyretic analgesics and opioids; nevertheless, these medications present severe adverse side effects, such as dizziness, nausea, vomiting, constipation, physical dependence, and respiratory complications. , The development of an effective injectable local anesthetic with prolonged duration of action would enhance the quality of life of patients affected by chronic or postoperative pain …”

Section: Introductionmentioning

confidence: 99%

“…2,3 Most common prescriptions are based on antipyretic analgesics and opioids; nevertheless, these medications present severe adverse side effects, such as dizziness, nausea, vomiting, constipation, physical dependence, and respiratory complications. 4,5 The development of an effective injectable local anesthetic with prolonged duration of action would enhance the quality of life of patients affected by chronic or postoperative pain. 6 Conventional free drugs present several disadvantages that impair their optimal performance, such as short half-life in the organism, high dosages administered, poor selectivity, and associated side effects in healthy tissues.…”

Section: ■ Introductionmentioning

confidence: 99%

Nanogels with High Loading of Anesthetic Nanocrystals for Extended Duration of Sciatic Nerve Block

Alejo

Usón

Landa

et al. 2021

ACS Appl. Mater. Interfaces

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The development of thermoresponsive nanogels loaded with nanocrystals of the local anesthetic bupivacaine nanocrystals (BNCs) for prolonged peripheral nerve pain relief is reported here. BNCs were prepared using the antisolvent precipitation method from the hydrophobic form of bupivacaine (bupivacaine free base). The as-prepared BNCs were used stand-alone or encapsulated in temperature-responsive poly(ethylene glycol) methyl ether methacrylate (OEGMA)-based nanogels, resulting in bupivacaine NC-loaded nanogels (BNC-nanogels) of monodisperse size. The synthesis protocol has rendered high drug loadings (i.e., 93.8 ± 1.5 and 84.8 ± 1.2 wt % for the NC and BNC-nanogels, respectively) and fast drug dissolution kinetics in the resulting composite material. In vivo tests demonstrated the efficacy of the formulation along with an extended duration of sciatic nerve block in murine models of more than 8 h with a formulation containing only 2 mg of the local anesthetic thanks to the thermoresponsive character of the polymer, which, at body temperature, becomes hydrophobic and acts as a diffusion barrier for the encapsulated drug nanocrystals. The hydrophobicity of the encapsulated bupivacaine free base probably facilitates its pass through cell membranes and also binds strongly to their hydrophobic lipid bilayer, thereby protecting molecules from diffusion to extracellular media and to the bloodstream, reducing their clearance. When using BNC-nanogels, the duration of the anesthetic blockage lasted twice as long as compared to the effect of just BNCs or a conventional bupivacaine hydrochloride solution both containing equivalent amounts of the free drug. Results of the in vivo tests showed enough sensory nerve block to potentially relieve pain, but still having mobility in the limb, which enables motor function when required. The BNC-nanogels presented minimal toxicity in the in vivo study due to their sustained drug release and excellent biocompatibility. The encapsulation of nano-sized crystals of bupivacaine provides a prolonged regional anesthesia with reduced toxicity, which could be advantageous in the management of chronic pain.

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“…In the comprehensive review by Kaye et al, authors reviewed the existing literature in which liposomal bupivacaine was used as a component of multimodal analgesia and concluded that when used there was prolonged analgesia, opioid-sparing effect and was better than placebo or conventional bupivacaine infiltration. 1 Researchers have also used liposomal bupivacaine in pediatric patients although…”

mentioning

confidence: 99%

“…comprehensively reviewed the existing literature in which liposomal bupivacaine was used as a component of multimodal analgesia and concluded that when used there was prolonged analgesia, opioid-sparing effect and was better than placebo or conventional bupivacaine infiltration. 1 The success of liposomal bupivacaine encouraged the researchers to develop better liposomal products which can be used in clinical practice. This led to the development of SABER ® -bupivacaine (Durect Corp., Cupertino, California, USA) and HTX-011 (Heron Therapeutics Inc., San Diego, California, USA).…”

mentioning

confidence: 99%