Evaluation of the Efficacy, Biocompatibility, and Permeation of Bupivacaine-Loaded Poly(epsilon-caprolactone) Nano-Capsules as an Anesthetic

Abstract

In this study bupivacaine (BVC) was encapsulated in Nano-capsules of poly-ε-caprolactone (PCL) and its cytotoxicity in HaCaT (MTT) cells, its permeability in the oesophageal epithelium of pigs, as well as its anesthetic effect in the incision model of rat’s hind paw (electronic von Frey anesthesiometer) were evaluated. BVC and epinephrine-associated bupivacaine (BVC-Epi) have been compared to BVC-Nano and it was demonstrated that BVC-Nano had high physicochemical properties and remained stable for 120 days; also, encapsulation of bupivacaine did not affect its toxicity to HaCaT cells, but epinephrine reduced its toxicity. Although both methods of combination with epinephrine and encapsulation in nanocapsules resulted in an extended time of anesthesia, the efficacy of epinephrine was more favorable. The permeation evaluation indicated that encapsulation increased both the permeability coefficient and the steady-state flux of bupivacaine across the esophageal epithelium. BVC permeation was enhanced by encapsulation into Nano-capsules, as a new novel therapeutic strategy, facilitating future research as a topical anesthetic.

Buccal Permeation of Polysaccharide High Molecular Weight Compounds: Effect of Chemical Permeation Enhancers

“…The model membrane used for this kind of experiment should be, however, very well characterized. In the literature, there is some evidence indicating that the porcine esophageal mucosa is a relevant model of the buccal epithelium [ 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 ]. However, most of these studies have been performed with low MW compounds, and these results cannot be directly extrapolated to hydrophilic macromolecules, probably characterized by different penetration pathways [ 37 ].…”

Novel CO2-encapsulated Pluronic F127 hydrogel for the treatment of Achilles tendon injury

“…Bupivacaine can be administered via various routes, including intravenous, epidural, and local infiltration 51 – 53 . Currently, bupivacaine is applied using an encapsulated technique to the polymers to guarantee the long-action analgesic effect 37 , 54 , 55 . In this study, bupivacaine was co-encapsulated with CO 2 into the hydrogel with progressive elution to enhance tendon healing under a continuous analgesic condition.…”

Advances in the use of local anesthetic extended-release systems in pain management

“…embedded bupivacaine in PCL nancapsules, which exhibited high physicochemical stability and remained stable for up to 120 days. Compared to free bupivacaine, its anesthetic duration was up to two times more effective, and no significant cytotoxicity was observed (Zhao W et al., 2022 ).…”