Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect

Abstract

The aim of the present work is the development and evaluation of solid lipid nanoparticles (SLNs) as carrier system for topical delivery of benzocaine (BZC) improving its local anesthesia aiming to produce a fast acting and long lasting topical formulation. BZC loaded SLNs were prepared using a full factorial design to study the influence of the type of polyoxyethylene sorbitan ester surfactants as well as their concentration as independent variables on the particle size, entrapment efficacy and zeta potential selected as dependent variables. Design of experiment (DOE) and the analysis of variance (ANOVA) were conducted to assess the optimization of the developed formulations. The results indicated that the fatty acid chain length of tested surfactants and their concentration had a significant effect on the studied responses. The optimized formulations were spherical in shape of mean particle diameters<350 nm with negatively charged surface <-20mV. Particles were characterized using differential scanning calorimetry and X-ray powder diffraction confirming the amorphous nature and the uniformity of drug inclusion in the lipid matrix. Optimized BZC-SLNs were incorporated into hydrogels characterized by a pseudoplastic non-Newtonian behavior. In vitro release study revealed an apparently biphasic release process with sustained release profile following Higuchi kinetics. BZC loaded SLNs hydrogels showed more potent anesthetic effect compared to BZC hydrogel evaluated using tail-flick analgesimeter, confirming significant improvement in both the intensity and duration of anesthetic effect. The above results proved that SLNs represent good candidates to encapsulate BZC improving its therapeutic efficacy for the topical treatment of pain.

Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

“…Lipid-based delivery systems can be utilized for skin delivery in topical anesthesia. 35 SLNs and NLCs are the most suitable ones because of their high adhesion to the skin, thus bringing about a pleasant esthetic character and skin feel, and controlled release of the drug leading to persistent anesthetic effect. In this study, LID and PRI were co-encapsulated in SLNs as well as NLCs.…”

Optimization and antimicrobial efficacy of curcumin loaded solid lipid nanoparticles against foodborne bacteria in hamburger patty

“…The effect of Tween 80 on the interface between particle and water as well as electric double layer can cause more steric stabilization of particles. Furthermore, the differential adsorption of the hydroxyl and hydrated oxonium ions at neutral pH by the non‐ionic surfactants induce to generate negative charge at the interface (Basha et al., 2015). Thus, Tween 80, as a non‐ionic surfactant, is preferred due to its nontoxicity (Choi et al., 2014).…”

Colon Available Bioactive Compounds Exhibits Anticancer Effect onIn-VitroModel of Colorectal Cancer

“…Average particle size and zeta potential of the CS nanoparticles were determined by Particle Size Analyzer (Zetasizer Ver System; Malvern Instruments Ltd., Malvern, UK). To analyze particle size, nanosuspension was diluted with filtered (0.22 lm) ultra pure water [43][44][45].…”