Hybrid nanofilms as topical anesthetics for pain-free procedures in dentistry

Abstract

Topical anesthetics are widely applied in order to relieve the discomfort and anxiety caused by needle insertion and other painful superficial interventions at the oral cavity. So far, there are no commercially available effective topical anesthetic formulations for that purpose, and the most of developments are related to hydrophilic and low mucoadhesive forms. Therefore, we have prepared different hybrid nanofilms composed of biopolymer matrices (chitosan, pectin, and chitosan-pectin) blended with nanostructured lipid carriers (NLC) loading the eutectic mixture of 5% lidocaineprilocaine (LDC-PLC), in order to fulfill this gap in the market. These dual systems were processed as hybrid nanofilms by the solvent/casting method, and its mucoadhesive, structural and mechanical properties were detailed. The most appropriate hybrid nanofilm combined the advantages of both pectin (PCT) and NLC components. The resultant material presented sustained LDC-PLC release profile for more than 8 h; permeation across porcine buccal mucosa almost twice higher than control and non-cytotoxicity against 3T3 and HACAT cell lines. Then, the in vivo efficacy of PCT/ NLC formulation was compared to biopolymer film and commercial drug, exhibiting the longestlasting anesthetic effect (> 7 h), assessed by tail flick test in mice. These pectin-based hybrid nanofilms open perspectives for clinical trials and applications beyond Dentistry.

Hybrid Pectin-Liposome Formulation against Multi-Resistant Bacterial Strains

“…In addition, the acidic liposomes containing PCT in their inner aqueous phase (PCT@LIP/NOR) have driven a different release kinetic profile (first order) of NOR in comparison to LIP/NOR and PCT-LIP/NOR (Korsmeyer-Peppas), corroborating its more complex supramolecular structure. Considering that NOR release profile from PCT@LIP/NOR was best described by the first-order model, it means that the kinetics was governed by two phases, an initial given by the erosion of biopolymer matrix containing NOR (outside the vesicles), followed by the sustained drug diffusion from the liposomes, where the drug had to overcome two physical barriers to be released: the lipid bilayer and polysaccharide network, as also described for carboxymethyl-chitosan coated liposomes, xanthan-lipid nanoparticles hydrogels and pectin-lipid nanofilms [20,38,39].…”

Current progress and challenges of nanoparticle-based therapeutics in pain management

“…Ribeiro et al [77] optimized a process for the synthesis of NLCs based on cetyl palmitate and capric/caprylic triglycerides for delivery of the local anesthetics lidocaine and prilocaine applied in dentistry. The optimal formulation, which was physicochemically stable during 14 months in storage at room temperature, presented desirable structure-dependent properties, high encapsulation efficiency of the eutectic mixture of both local anesthetics and satisfactory sustained release profile, confirming the potential of this formulation for use during and after the dental procedures.…”

Functional Hybrid Nanoemulsions for Sumatriptan Intranasal Delivery

“…Biopolymers are natural materials that have been used in biomedical applications as DDS and biosensors, and in tissue engineering and diagnoses for at least 75 years (George et al, 2020;Qureshi et al, 2020). Due to their available carboxyl groups, hydrophilic biopolymers such as dextran, pectin (PCT), alginate (ALG), pullulan and xanthan (XAN) provide systems with mucoadhesive properties, favoring the permeation of drugs across the mucous tissue (Ribeiro et al, 2018b(Ribeiro et al, , 2020. Polymerlipid DDS is one of the best combinations of pharmaceutical excipients, resulting in several optimized properties (Siepmann et al, 2019).…”