Prolonged Sciatic Nerve Blockade Using Sustained Release of Bupivacaine From a Biodegradable Polymer Matrix

Masteis, D. B.; Berde, Charles B.; Dutta, Swarup; Langer, Robert

doi:10.1097/00000542-199109001-00764

Cited by 9 publications

(4 citation statements)

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“…Bioerodible and biodegradable polymer-local anesthetic matrix implants formed by impregnating polyanhydride copolymers with dibucaine and bupivacaine may produce sciatic nerve blocks for 3–5 days in rats [3–5]. Although these solid implants can become useful therapeutic candidates, their use is so far limited to surgical procedures.…”

Section: Introductionmentioning

confidence: 99%

Experimental research A novel ropivacaine-loaded in situ forming implant prolongs the effect of local analgesia in rats

Lü¹,

Zhang²,

Wu³

et al. 2013

aoms

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IntroductionProlonged postoperative analgesia cannot be achieved by a single injection of local anesthetic solution. The objective of this study was to optimize the formulation of a ropivacaine hydrochloride (Ropi-HCl) loaded in situ forming implant (ISI) by addition of different co-solvents, and evaluate the in vitro release of Ropi-HCl, and the analgesic effect and toxicity of the optimized formulation in rats.Material and methodsTriacetin (TA), benzyl benzoate (BB) and polyethylene glycol 400 (PEG 400) were used as additives and added to the solvent of N-methyl-2-pyrrolidone (NMP). Drug release to the surface and inner structural properties of the formed implant were evaluated by scanning electron microscopy (SEM). The analgesic effect was determined by injection near the rat sciatic nerve.ResultsThe solvent system added with TA or BB significantly decreased the burst release, whereas PEG 400 increased the Ropi-HCl burst release from the formulation. Over 70% of the incorporated Ropi-HCl was released from all formulations in 14 days in the in vitro assay. The SEM showed that the surface of NMP-BB formulation was less porous and more homogeneous, compared with the other formulations. Compared with Ropi-HCl injection, the optimized formulation (NMP-BB) significantly prolonged the analgesic effect in 48 h (p < 0.05), with a mild degree of motor block from 3 h to 12 h. Histological evaluation of the injection site revealed only mild inflammatory infiltration without obvious pathological nerve alterations.ConclusionsThe biodegradable Ropi-HCl-loaded ISI system with NMP-BB may prove to be an attractive and safe alternative for the delivery of parenteral local anesthetics to prolong pain relief.

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Section: Introductionmentioning

confidence: 99%

Experimental research A novel ropivacaine-loaded in situ forming implant prolongs the effect of local analgesia in rats

Lü¹,

Zhang²,

Wu³

et al. 2013

aoms

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“…observed, with observations comparable to those of 70% release required approx. 14 14). microcrystals wererapidly dissociated, indicating alack Microscopic Observations °f f°V fo f * e c colla g en ^^ ™* microcrystals were 60 predominantly 2-5 urn.…”

Section: Lecithin-otc-collagen Matrix and Otc-collagenmentioning

confidence: 99%

“…(6) Prolonged release of bupivacaine has been achieved by surgical implantation of pellets composed of bupivacaine and biodegradable polyanhydride polymers to provide sciatic nerve blockade in rats. (14) It is theorized that this system allows sustained release of the local anesthetic agent via enzyme-catalyzed cleavages of the polymeric system. (15) Prolonged release has also been achieved with lipid encapsulation of various local anesthetics to include lidocaine, etidocaine, bupivacaine and tetracaine.…”

Section: Introductionmentioning

confidence: 99%

Development of Ultra Long Duration Local Anesthetic Agents in a Rat Model.

Kline¹

1994

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“…However, adding a vasoconstrictor to a long‐acting local anaesthetic such as bupivacaine has been shown to have little effect (Walters and others 1970). Slow‐delivery systems have been used successfully to prolong the duration of different nerve blocks produced by bupivacaine or lidocaine (Langerman and others 1991, Masters and others 1991, Mashimo and others 1992, Boogaerts and others 1993). Oilin‐water emulsions are good formulations for use as vehicles in slow‐release systems (Longer and Robinson 1987).…”

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confidence: 99%

Prolongation of epidural anaesthesia in dogs with bupivacaine in a lipid emulsion

Franquelo¹,

Toledo

Manubens³

et al. 2000

Veterinary Record

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An aqueous solution and a lipid emulsion of bupivacaine were administered epidurally in doses of 1.8 mg/kg to six beagle dogs following a randomised two-phase crossover design. The aqueous solution was absorbed rapidly and the mean (sd) peak venous plasma concentration of bupivacaine, 1.4 (0.4) microg/ml, was detected after five minutes. After administration of the lipid emulsion, the peak plasma concentration of bupivacaine, 0.6 (0.2) microg/ml, was detected after 30 minutes. The mean (sd) t1/2beta of the aqueous preparation was 149.1 (32.6) minutes, and of the lipid emulsion 119.2 (34.0) minutes. Both preparations had a similar bioavailability. The mean time to the onset of motor block after the administration of the aqueous solution, 2.3 (2.2) minutes, was significantly shorter (P=0.028) than after the administration of the lipid emulsion, 9.4 (1.9) minutes, and the duration of the motor block induced by the lipid emulsion, 217.6 (26.2) minutes, was significantly longer (P=0.043) than for the aqueous solution, 158 (48.8) minutes. During anaesthesia, the plasma concentrations of bupivacaine ranged between 1.3 and 0.2 microg/ml. Non-significant changes in systolic blood pressure and heart rate were observed which coincided with the peak plasma concentrations of bupivacaine.

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Prolonged Sciatic Nerve Blockade Using Sustained Release of Bupivacaine From a Biodegradable Polymer Matrix

Cited by 9 publications

References 0 publications

Experimental research A novel ropivacaine-loaded in situ forming implant prolongs the effect of local analgesia in rats

Experimental research A novel ropivacaine-loaded in situ forming implant prolongs the effect of local analgesia in rats

Development of Ultra Long Duration Local Anesthetic Agents in a Rat Model.

Prolongation of epidural anaesthesia in dogs with bupivacaine in a lipid emulsion

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