Successful preparation of a biopolymeric nanocarrier enables controlled release of antinociceptive monoterpene for local pain management after transdermal barrier permeation

Abstract

AbstractDeveloping effective and targeted drug delivery systems is crucial in searching for improved pain management strategies. Here, it is shown the preparation of a nanocarrier using chitosan hydrogel, and polymeric nanocapsules loaded with linalool for enhancing transdermal permeation and targeted delivery of this antinociceptive monoterpene for the pain treatment. Extensive characterization was conducted to evaluate the properties of the nanocarrier, and several in vitro studies were performed to investigate the release kinetics of linalool from the nanocarrier and its permeation through the layers of the skin. As results, the prepared polymeric nanocarrier exhibited an average size of 160 ± 9 nm, with a polydispersion index of 0.12 ± 0.01. The kinetic study revealed that the nanocarrier effectively controlled and prolonged the release of linalool, following a pseudo‐second order model (R2 = 0.98). To evaluate the permeation of the nanocarrier through the transdermal barrier, swine ear skin was employed. The nanocarrier efficiently penetrated the transdermal barrier and successfully delivered linalool to the skin layers. Additionally, an in vivo toxicity study indicated no toxicity for the nanocarrier at the tested concentrations (<0.950 μg mL−1). The release kinetics showed a controlled and sustained release of the linalool, suggesting its potential for prolonged therapeutic effects.