Development, Characterization, and In Vitro and In Vivo Evaluation of Benzocaine- and Lidocaine-Loaded Nanostructrured Lipid Carriers

Application of quality by design principles in the development and evaluation of semisolid drug carrier systems for the transdermal delivery of lidocaine

“…The components of the NLC formulation have similar lipophilicity as the skin, so they have good miscibility with the skin lipids, and this can cause greater penetration [37]. Our results are in good agreement with other studies, which revealed that lipid nanocarriers can improve penetration and effectiveness of encapsulated lidocaine [2,5,38,39]. The high penetration rate of LID through the epidermis predicts the fast accumulation of the drug in the dermis, which is the site of action for local anesthetics.…”

“…Surprisingly, through the epidermis, the NLC formulation exhibited the most complete penetration (19.44 %±5.05), whereas in vitro it was the lowest. This finding could be explained by the special structure of the NLC, which allows the high bioavailability of this formulation [2]. The components of the NLC formulation have similar lipophilicity as the skin, so they have good miscibility with the skin lipids, and this can cause greater penetration [37].…”

“…However, most of the marketed topical formulations have moderate skin penetration properties, rapid but short effect, thus the development of local topical anesthetics with a release in a prolonged fashion at the site of action is desperately desired [2]. Therefore, this work was undertaken to develop and compare a new formulation of lidocaine (LID), proposed to improve its clinical effectiveness in topical anesthesia in terms of both enhanced anesthesia and a prolonged duration of action.…”

Delivery of drugs applied topically to the skin

“…Vaccines, 5-fluorouracil, IL-2 and IFN-α [149][150][151] SECosomes or nanosomes Mixture of surfactant, ethanol and cholesterol siRNA [121] SLNs Produced with one single solid lipid and surfactants, with perfect crystalline lattice CoQ-10, glucocorticoids, minoxidil and oxybenzone [152][153][154][155] NLCs Produced with solid and liquid lipids and surfactants, with distorted crystalline lattice Targeted tumor delivery, phospholipase A2 inhibitors, benzocaine, lidocaine and psoriasis treatment [156][157][158][159] Polymeric nanoparticles Consist of micro-and nano-spheres or capsules developed to control the release of the entrapped drug Chlorhexidine, indomethacin, melatonin and poorly soluble drugs [160][161][162][163] ALA: Aminolevulinic acid; NLC: Nanostructured lipid carrier; SECosome: Surfactant-ethanol-cholesterol-osome; SLN: Solid lipid nanoparticle.…”

Local anesthetic lidocaine delivery system: chitosan and hyaluronic acid-modified layer-by-layer lipid nanoparticles

“…It has been known that when these lipophilic drugs are encapsulated in lipid-based nanoparticles such as liposomes, solid lipid nanoparticles (SLNs), and nanostructured lipid nanoparticles (NLCs), their permeation through the skin is enhanced (Pathak & Nagarsenker, 2009;Shim et al, 2010;Puglia et al, 2011;de Araújo et al, 2013). NLCs are formed from a combination of solid and liquid lipids, which is still solid at body temperature (Müller et al, 2011).…”