Polymeric Nanocapsules Loaded with Lidocaine: A Promising Formulation for Topical Dental Anesthesia.

Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate whether an approximate 50% encapsulation of lidocaine in poly(ε-caprolactone) nanocapsules (LDC-Nano) would be able to increase its permeation and analgesic efficacy and reduce cytotoxicity.

Resistivity Technique for the Evaluation of the Integrity of Buccal and Esophageal Epithelium Mucosa for In Vitro Permeation Studies: Swine Buccal and Esophageal Mucosa Barrier Models.

Permeation assays are important for the development of topical formulations applied on buccal mucosa. Swine buccal and esophageal epithelia are usually used as barriers for these assays, while frozen epithelia have been used to optimize the experimental setup. However, there is no consensus on these methods.

Promising potential of articaine-loaded poly(epsilon-caprolactone) nanocapules for intraoral topical anesthesia.

To determine whether the permeation capacity and analgesic efficacy of articaine (ATC) could be increased and cytotoxicity decreased by encapsulation in poly(ɛ-caprolactone) nanocapsules (ATCnano), aiming at local or topical anesthesia in dentistry. Cellular viability was evaluated (using the MTT test and fluorescence microscopy) after 1 h and 24 h exposure of HaCaT cells to ATC, ATCnano, ATC with epinephrine (ATCepi), and ATC in nanocapsules with epinephrine (ATCnanoepi). The profiles of permeation of 2% ATC and 2% ATCnano across swine esophageal epithelium were determined using Franz-type vertical diffusion cells.

A crossover clinical study to evaluate pain intensity from microneedle insertion in different parts of the oral cavity.

The objective of the present study was to evaluate discomfort and safety of microneedle (MN) insertion in several intraoral regions. A device was developed to standardize MN insertions. MNs were inserted in the following regions of the oral cavity: gingiva, palatine alveolar process, buccal mucosa, dorsum of the tongue and inner portion of the lower lip.

Effects of 2-Hydroxypropil-Β-Cyclodextrin-Lidocaine on Tumor Growth and Inflammatory Response.

Background: Antiproliferative and cytotoxic effects of lidocaine have been reported in tumor cells. However, the use of these drugs is restricted due to their short action with rapid dispersion from the injected site. The complexation of local anesthetics in 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) is able to improve pharmacological features.

Physicochemical characterization and cytotoxicity of articaine-2-hydroxypropyl-β-cyclodextrin inclusion complex.

Articaine (ATC) is one of the most widely used local anesthetics in dentistry. Despite its safety, local toxicity has been reported. This study aimed to develop an ATC-2- hydroxypropyl-β-cyclodextrin inclusion complex (ATC HPβCD) and to assess its toxicity in vitro.

Hybrid Hydrogel Composed of Polymeric Nanocapsules Co-Loading Lidocaine and Prilocaine for Topical Intraoral Anesthesia.

This study reports the development of nanostructured hydrogels for the sustained release of the eutectic mixture of lidocaine and prilocaine (both at 2.5%) for intraoral topical use. The local anesthetics, free or encapsulated in poly(ε-caprolactone) nanocapsules, were incorporated into CARBOPOL hydrogel.

Full-Thickness Intraoral Mucosa Barrier Models for In Vitro Drug-Permeation Studies Using Microneedles.

The use of permeation enhancers such as microneedles (MNs) to increase drug penetration across intraoral mucosa has increased in recent years. Permeation studies, commonly performed using vertical diffusion cells, are a well-established way to preview formulations and enhance their performance during the development stage. However, to our knowledge, the existing intraoral mucosa barrier models do not permit permeation using MN-pretreated mucosa due to their insufficient thickness.

The effect of two drug delivery systems in ropivacaine cytotoxicity and cytokine release by human keratinocytes and fibroblasts.

Objectives: Modified drug delivery systems have been developed to improve pharmacological properties of local anaesthetics. However, the inflammatory potential of these formulations was not investigated. This study compared the in-vitro effects of ropivacaine (ropi) in plain, liposomal (MLV) or 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) formulations on cell viability, apoptosis and cytokine (IL-1α, TNF-α, IL-6 and IL-10) release.

Recent advances and perspectives in topical oral anesthesia.

Topical anesthesia is widely used in dentistry to reduce pain caused by needle insertion and injection of the anesthetic. However, successful anesthesia is not always achieved using the formulations that are currently commercially available. As a result, local anesthesia is still one of the procedures that is most feared by dental patients.

Influence of salivary washout on drug delivery to the oral cavity using coated microneedles: An in vitro evaluation.

The objective of this study was to determine whether in buccal tissues, after insertion and removal of coated microneedles, the presence of saliva over the insertion site can lead to loss of the deposited drug, and if saliva can influence in vitro permeation of the drug across the tissue. Microneedles were coated with sulforhodamine (SRD), which was used as a model drug, and inserted in to porcine buccal mucosa in vitro. Fluorescence microscopy was used to study microneedle coating quality and the diffusion of SRD through the mucosa.

Comparison of liposomal and 2-hydroxypropyl-β-cyclodextrin-lidocaine on cell viability and inflammatory response in human keratinocytes and gingival fibroblasts.

Objectives: The aim of this study was to observe the effect multilamellar liposomes (MLV) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) in the in-vitro effects of lidocaine in cell viability, pro-inflammatory cytokines and prostaglandin E2 release of both human keratinocytes (HaCaT) and gingival fibroblasts (HGF) cells.

Methods: HaCaT and HGF cells were exposed to lidocaine 100-1 μm in plain, MLV and HP-β-CD formulations for 6 h or 24 h. The formulation effects in cell viability were measured by XTT assay and by fluorescent labelling.

Anaesthetic efficacy of unilamellar and multilamellar liposomal formulations of articaine in inflamed and uninflamed tissue.

We compared the efficacy of articaine encapsulated in multilamellar and unilamellar liposomes with that of articaine with epinephrine, after infiltration into inflamed and uninflamed tissue in rats. We encapsulated 4% articaine in multilamellar (articaine:multi) and unilamellar (articaine:uni) liposomes and compared them with 4% articaine with 1:100 000 epinephrine (articaine:epinephrine), in inflamed (plantar incision into the hind paw) and uninflamed (infraorbital nerve block) tissue in rats. Anaesthetic formulations (0.

Evaluation of different pig oral mucosa sites as permeability barrier models for drug permeation studies.

The objective of the present study was to investigate the influence of preparation and storage conditions on the histology and permeability of different parts of porcine oral mucosa used for in vitro studies of transbuccal formulations. Fresh and frozen (-20°C and -80°C, with or without cryoprotectant) epithelia of porcine palatal, gingival, dorsum of the tongue, and buccal mucosa were submitted for histological analyses to determine the effects of storage conditions on barrier integrity. Permeation of lidocaine hydrochloride (used as a hydrophilic model drug) across fresh and previously frozen oral epithelium was measured in order to evaluate the barrier function.

Liposomal lidocaine gel for topical use at the oral mucosa: characterization, in vitro assays and in vivo anesthetic efficacy in humans.

Objective: To characterize liposomal-lidocaine formulations for topical use on oral mucosa and to compare their in vitro permeation and in vivo anesthetic efficacy with commercially available lidocaine formulations.

Materials And Methods: Large unilamellar liposomes (400 nm) containing lidocaine were prepared using phosphatidylcholine, cholesterol, and α-tocoferol (4:3:0.07, w:w:w) and were characterized in terms of membrane/water partition coefficient, encapsulation efficiency, size, polydispersity, zeta potential, and in vitro release.

Methylparaben concentration in commercial Brazilian local anesthetics solutions.

Objective: To detect the presence and concentration of methylparaben in cartridges of commercial Brazilian local anesthetics.

Material And Methods: Twelve commercial brands (4 in glass and 8 in plastic cartridges) of local anesthetic solutions for use in dentistry were purchased from the Brazilian market and analyzed. Different lots of the commercial brands were obtained in different Brazilian cities (Piracicaba, Campinas and São Paulo).

Effect of articaine on mental nerve anterior portion: histological analysis in rats.

Objectives: The aim of this study was to evaluate the possible toxic effects of articaine and lidocaine on mental nerve, due to the increasing number of paresthesia cases after nerve blocks.

Materials And Methods: The drugs were injected in the anterior portion of mental nerve of 24 rats, divided into three groups: G1--4% articaine with 1:100,000 epinephrine; G2--2% lidocaine with 1:100,000 epinephrine and G3--plain 1:100,000 epinephrine solution. These solutions were injected in the right side of the rat's mandible and the left side was used as control (0.

The influence of local anesthetic solutions storage on tissue inflammatory reaction.

Objective: This study aimed to analyze the influence of storage conditions of local anesthetic solutions in the inflammatory reaction after injection in rats.

Study Design: Twenty-four rats received in their oral mucosa the injection of 2% lidocaine with epinephrine 1:100.000 solutions (LA) submitted to the following storage conditions during a twelve-month period: G1--inside the original packaging, in refrigerator (5±1°C); G2--inside the original box, under light shelter, at room temperature; G3--outside the original box at room temperature (exposed to artificial light for 12 hours/day) and G4--brand new solution.

Anesthetic efficacy of liposomal prilocaine in maxillary infiltration anesthesia.

Animal studies have shown that liposome encapsulation increases prilocaine anesthetic efficacy. This randomized, blind, crossover, three-period study evaluated the anesthetic efficacy of liposome-encapsulated 3% prilocaine, compared to 3% plain prilocaine and 3% prilocaine with 0.03IU/mL felypressin, after a 1.

Anesthetic efficacy of articaine and lidocaine for incisive/mental nerve block.

Introduction: The incisive/mental nerve block (IMNB) could be an alternative to the inferior alveolar nerve block in the mandibular anterior teeth. The effectiveness of articaine has not been tested in IMNB.

Methods: This prospective randomized double-blind crossover study compared the anesthetic efficacy of 0.

Pharmacokinetic and local toxicity studies of liposome-encapsulated and plain mepivacaine solutions in rats.

The pharmacokinetics and the local toxicity of commercial and liposome-encapsulated mepivacaine formulations injected intra-orally in rats were studied. Animals were divided in groups (n = 4-6) and treated with 0.1 mL of the formulations: 2% mepivacaine with 1:100,000 epinephrine (MVC(2%EPI)), 3% mepivacaine (MVC(3%)), and 2% liposome-encapsulated mepivacaine (MVC(LUV)).

Cariogenic potential of cows', human and infant formula milks and effect of fluoride supplementation.

The aim of the present study was to evaluate the cariogenicity of cows', human and infant formula milks, supplemented or not with fluoride, in rats. Sixty female Wistar rats were desalivated and infected with Streptococcus sobrinus 6715.Animals were divided into six groups: group 1, sterilised deionised distilled water (SDW; negative control); group 2, 5 % sucrose added to SDW (positive control); group 3, human milk; group 4, cows' milk; group 5, Ninho(R) formula reconstituted with SDW; group 6, Ninho(R) formula reconstituted with 10 parts per million F and SDW.

Anesthetic efficacy of 3 volumes of lidocaine with epinephrine in maxillary infiltration anesthesia.

The objective of this randomized double-blind investigation was to compare the anesthetic efficacy and injection discomfort of 3 volumes of 2% lidocaine with 1:100,000 epinephrine for maxillary infiltration anesthesia. A total of 25 subjects received 0.6, 0.

Efficacy of 1% ropivacaine gel for topical anesthesia of human oral mucosa.

Objective: To evaluate the efficacy of 1% ropivacaine for topical anesthesia in dentistry.

Method And Materials: Thirty healthy volunteers randomly (blind crossover) received the following treatments: 20 mg of 1% ropivacaine gel (ropivacaine-20), 60 mg of 1% ropivacaine gel (ropivacaine-60), 20 mg of the eutectic mixture of local anesthetics 2.5% lidocaine and 2.

Anesthetic efficacy and pain induced by dental anesthesia: the influence of gender and menstrual cycle.

Objective: To assess the influence of the menstrual cycle and oral contraceptives on pain sensitivity and local anesthetic effectiveness.

Study Design: Thirty volunteers were designated into 3 groups (n = 10): group 1, women using contraceptives; group 2, women not using contraceptives; and group 3, men. Groups 1 and 2 had a buccal infiltration of 2% lidocaine with 1:100,000 epinephrine at the upper-right canine during each one of the 5 phases of the menstrual cycle and group 3 at a randomly selected day.