Assessing the Use of 50% Enantiomeric Excess Bupivacaine-Loaded Microspheres after Sciatic Nerve Block in Rats

Oliveira, Rohnelt Machado de; Tanaka, Pedro Paulo; Tenório, Sérgio Bernardo

doi:10.1016/s0034-7094(11)70083-6

Cited by 5 publications

(3 citation statements)

References 22 publications

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“…Bupivacaine and ropivacaine have demonstrated to produce longer peripheral neural blockade (4.5–12 h) than lidocaine (1–2 h) as such bupivacaine is commonly used for long-acting anesthetic effects; however, it is also linked with compelling cardiotoxicity and neurotoxicity [ 11 ]. The toxicity of bupivacaine has been overcome by ropivacaine, the propyl analog of bupivacaine while still maintaining the same duration of action [ 12 ]. Additionally, ropivacaine shows a lower lipid solubility and vasodilation when compared with bupivacaine resulting in their increased circulation time within the delivered local environment [ 13 ].…”

Section: Reviewmentioning

confidence: 99%

New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles

2016

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Lipid nanoparticles (liposomes) were first described in 1965, and several work have led to development of important technical advances like triggered release liposomes and drug-loaded liposomes. These advances have led to numerous clinical trials in such diverse areas such as the delivery of anti-cancer, antifungal, and antibiotic drugs; the delivery of gene medicines; and most importantly the delivery of anesthesia drugs. Quite a number of liposomes are on the market, and many more are still in developmental stage. Lipid nanoparticles are the first nano-medicine delivery system to be advanced from laboratory concept to clinical application with high considerable clinical acceptance. Drug delivery systems for local anesthetics (LAs) have caught the interest of many researchers because there are many biomedical advantages connected to their application. There have been several formulation techniques to systemically deliver LA that include encapsulation in liposomes and complexation in cyclodextrins, nanoparticles, and to a little extent gold nanoparticles. The proposed formulations help to decrease the LA concentration utilized, increase its permeability, and most importantly increase the localization of the LA for a long period of time thereby leading to increase in the duration of the LA effect and finally to reduce any local and systemic toxicity. In this review, we will highlight on new updates pertaining to drug delivery of local anesthetics in particular bupivacaine using lipid nanoparticles.

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Section: Reviewmentioning

confidence: 99%

New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles

2016

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“…To prevent mice from disturbing the wound stitches by themselves or others, absorbable suture was used to sew muscle and skin. 23 , 24 …”

Section: Methodsmentioning

confidence: 99%

Preparation of novel biodegradable ropivacaine microspheres and evaluation of their efficacy in sciatic nerve block in mice

Chen

Tong

et al. 2016

DDDT

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In this study, ropivacaine chitosan-loaded microspheres for subcutaneous administration were developed. The systems were characterized in terms of surface morphology, particle size, encapsulation efficiency, and in vitro release behavior. Results showed that the microspheres had drug loading rate of 7.3% and encapsulation efficiency of 91.2%, and their average diameter was 2.62±0.76 µm. The morphology study revealed that the microspheres are uniform monodispersed spheres and did not form aggregates in aqueous solution. It was clearly observed that the release profile of ropivacaine microspheres exhibited a biphasic pattern: the initial burst release within the first 2 hours and a following slower and sustained release over a long time. In vivo, a greater area under the plasma concentration–time curve from 0 to t (AUC0–t) was obtained from the microspheres (4.27-fold), than from the injection group, which indicated that there was a significantly improved systemic exposure to ropivacaine. Pharmacodynamics result showed that preparing ropivacaine as microsphere preparation could not only extend the drug effect time but also decrease the administration dosage.

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“…The administration of bupivacaine clinically has been reported to be related with systemic toxicity [13], as such several researchers have applied nanotechnology formulated biomaterials like lipospheres, microspheres [14], cyclodextrin matrices, lipid-protein-sugar nanoparticles, microcrystals to decrease the toxicity associated with bupivacaine and liposomal bupivacaine [15][16][17] has been the most reported of them (Table 1). bupivacaine in form of DepoFoam bupivacaine, Exparel€ a, on healthy volunteers in order to achieve long-lasting pain relief in a single dose [16]. In their in vitro study, they compared the Exparel€ a complex with bupivacaine hydrochloride 0.5 and 1.31%, respectively, and established that the Exparel€ a complex was more efficient.…”

Section: Nano-technology Application To Local Anaesthesia (La)mentioning

confidence: 99%

Nanotechnology application to local anaesthesia (LA)

Moradkhani

Karimi

Negahdari

2017

Artificial Cells, Nanomedicine, and Biotechnology

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Several advancements have been made on the exact release of local anaesthetics formulation and its efficiency at inducing motor and sensory block for an extended time has been harnessed in clinical practice. The use of sustained release formulations delivers analgesia for a lengthier period of time with one administration, thereby reducing complications that usually arise with administration of conventional analgesia. In addition, controlled release of an anaesthetic drug is said to prevent overdosing, reduced side effects, especially cardiotoxicity, neurotoxicity and tissue lesions. The use of nanotechnology knowledge via liposomal formulation has recorded high successful results in pain control and quick patient recovery.

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Assessing the Use of 50% Enantiomeric Excess Bupivacaine-Loaded Microspheres after Sciatic Nerve Block in Rats

Abstract: Controlled-release of 50% enantiomeric excess bupivacaine-loaded microspheres showed similar results regarding analgesia and less motor blockade when compared to other anesthetic formulations.

Cited by 5 publications

References 22 publications

New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles

New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles

Preparation of novel biodegradable ropivacaine microspheres and evaluation of their efficacy in sciatic nerve block in mice

Nanotechnology application to local anaesthesia (LA)

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