Prolonged Local Anesthetic Action Through Slow Release from Poly(Lactic Acid Co Castor Oil)

Sokolsky-Papkov, Marina; Golovanevski, Ludmila; Domb, Abraham J.; Weiniger, Carolyn F.

doi:10.1007/s11095-008-9699-8

Cited by 33 publications

(41 citation statements)

References 11 publications

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“…On the contrary, incorporation of bupivacaine into polymer carrier is easy and reliable and offers high loading potential. Previously, we demonstrated that poly(lactic acid co castor oil 3:7) loaded with 10% bupivacaine and 15% bupivacaine formulation prolonged in vivo efficacy of bupivacaine up to 48 (12) and 96 (13) hours, respectively. However, these formulations were viscous (about 10,000 cP) at room temperature, which hindered their injectability.…”

Section: Introductionmentioning

confidence: 95%

“…Bupivacaine free base was prepared from bupivacaine hydrochloride by alkaline precipitation and filtration as previously described (12). Two additives: ricinoleic acid (RA) or castor oil (CO) were selected as potential liquefying agents, and their effect on previously reported polymerbupivacaine formulations was examined in vitro and in vivo.…”

Section: Preparation Of Formulation and In Vitro Drug Releasementioning

confidence: 99%

“…Bupivacaine delivered directly in massive doses in non-encapsulated form would be lethal. Several delivery systems were evaluated (liposomes, liquid injectable polymers, lipospheres, lipidprotein-sugar particles, PLGA micro and nanospheres) (5)(6)(7)(8)(9); however, only liposomes and injectable liquid polymers met the desired criteria in terms of formulation administration, degradation rates of the carrier, and in vivo efficacy (10)(11)(12)(13)(14). Clinical application of a bupivacainepolymer formulation has potential advantages over liposomes.…”

Section: Introductionmentioning

confidence: 99%

“…In addition, increasing carrier hydrophobicity by increasing hydrophobic drug loads reduces bupivacaine release rates and doubles in vivo efficacy (12)(13)(14)16). It was previously demonstrated that the bupivacaine release rates have been reduced using oil depot formulations (17).…”

Section: Introductionmentioning

confidence: 99%

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Long-Acting Poly(DL:Lactic Acid-Castor Oil) 3:7-Bupivacaine Formulation: Effect of Hydrophobic Additives

et al. 2011

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Section: Introductionmentioning

confidence: 95%

Section: Preparation Of Formulation and In Vitro Drug Releasementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Long-Acting Poly(DL:Lactic Acid-Castor Oil) 3:7-Bupivacaine Formulation: Effect of Hydrophobic Additives

et al. 2011

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“…Previous data shows that single injection of bupivacaine in poly(d,l:lactic acid-co-castor oil) 3:7 caused sensory block in mice that lasted 48 hours. 17,18 In our previous study, the PELA copolymers were well developed and their released characterization was ~1 week in vitro. 19 However, little information is available about the Rop-loaded nanoparticle (Rop-PELA) and its effects for sciatic nerve block on postoperative pain in vivo.…”

Section: Introductionmentioning

confidence: 99%

Long-term effect of ropivacaine nanoparticles for sciatic nerve block on postoperative pain in rats

Wang

Huang

Yang

et al. 2016

IJN

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Purpose The analgesic effect of ropivacaine (Rop) for nerve block lasts only ~3–6 hours for single use. The aim of this study was to develop long-acting regional anesthetic Rop nanoparticles and investigate the effects of sciatic nerve block on postoperative pain in rats. Materials and methods Rop nanoparticles were developed using polyethylene glycol-co-polylactic acid (PELA). One hundred and twenty adult male Wistar rats were randomly divided into four groups (n=30, each): Con (control group; 0.9% saline, 200 µL), PELA (PELA group; 10 mg), Rop (Rop group; 0.5%, 200 µL), and Rop-PELA (Rop-PELA group; 10%, 10 mg). Another 12 rats were used for the detection of Rop concentration in plasma. The mechanical withdrawal threshold and thermal withdrawal latency were measured at 2 hours, 4 hours, 8 hours, 1 day, 2 days, 3 days, 5 days, and 7 days after incision. The expression of c-FOS was determined by immunohistochemistry at 2 hours, 8 hours, 48 hours, and 7 days. Nerve and organ toxicities were also evaluated at 7 days. Results The duration of Rop absorption in the plasma of the Rop-PELA group was longer (>8 hours) than that of the Rop group (4 hours). Mechanical withdrawal threshold and thermal withdrawal latency in the Rop-PELA group were higher than that in other groups (4 hours–3 days). c-FOS expression in the Rop-PELA group was lower than that in the control group at 2 hours, 8 hours, and 48 hours and lower than that in the Rop group at 8 hours and 48 hours after paw incision. Slight foreign body reactions were observed surrounding the sciatic nerve at 7 days. No obvious pathophysiological change was found in the major organs after Rop-PELA administration at 7 days. Conclusion Rop-PELA provides an effective analgesia for nerve block over 3 days after single administration, and the analgesic mechanism might be mediated by the regulation of spinal c-FOS expression. However, its potential long-term tissue toxicity needs to be further investigated.

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Biodegradable Hydrophobic Injectable Polymers for Drug Delivery and Regenerative Medicine

Arun

Ghosh

Domb

2021

Adv Funct Materials

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Biodegradable, hydrophobic, and injectable liquid polymers are capable of achieving the minimally invasive, sustained, and local release of drugs. These hydrophobic injectable polymers also have potential in the area of regenerative medicine where the biomaterial should be stable for a certain period and then degrade to allow the growth of cells/tissues. This review presents exclusive coverage of biocompatible hydrophobic injectable pasty or liquid polymers that can be injected without the use of any solvent for drug delivery, tissue augmentation, and regenerative medicine application. The synthesis methodologies of several major types of hydrophobic pasty polymers used in the biomedical fields and their properties with the foremost criteria to serve as injectable biomaterial for localized drug delivery and regenerative medicine is described. The hydrophobic biodegradable injectable polymers discussed are aliphatic polyesters, polycarbonates and polyanhydrides, prepared from: lactic acid, glycolic acid, caprolactone, aliphatic diols and diacids, hydroxy fatty acids, and triglycerides such as castor oil.

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Prolonged Local Anesthetic Action Through Slow Release from Poly(Lactic Acid Co Castor Oil)

Abstract: Previously we developed a ricinoleic acid based polymer with incorporated bupivacaine which prolonged anesthesia to 30 h. The new polymer poly(lactic acid co castor oil) 3:7 provides slow release of effective doses of the incorporated local anesthetic agent and prolongs anesthesia to 48 h.

Cited by 33 publications

References 11 publications

Long-Acting Poly(DL:Lactic Acid-Castor Oil) 3:7-Bupivacaine Formulation: Effect of Hydrophobic Additives

Long-Acting Poly(DL:Lactic Acid-Castor Oil) 3:7-Bupivacaine Formulation: Effect of Hydrophobic Additives

Long-term effect of ropivacaine nanoparticles for sciatic nerve block on postoperative pain in rats

Biodegradable Hydrophobic Injectable Polymers for Drug Delivery and Regenerative Medicine

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