Impact of Storage on In Vitro Permeation and Mucoadhesion Setup Experiments Using Swine Nasal Mucosa.

Intranasal topical administration offers a promising route for local and systemic drug delivery, with in vitro permeation and mucoadhesion studies often using porcine models. However, the impact of storage on mucosal integrity after the procedure remains unaddressed. This study aimed to standardize the preparation process and evaluated whether storage of porcine nasal mucosa impairs its integrity and permeability for experimental comparisons.

Transdermal delivery of bisphosphonates using dissolving and hydrogel-forming microarray patches: Potential for enhanced treatment of osteoporosis.

As of 2023, more than 200 million people worldwide are living with osteoporosis. Oral bisphosphonates (BPs) are the primary treatment but can cause gastrointestinal (GI) side effects, reducing patient compliance. Microarray (MAP) technology has the potential to overcome GI irritation by facilitating the transdermal delivery of BPs.

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.

Analysis of Key Factors for Evaluating Mucosal Adhesion Using Swine Buccal Tissue.

The assessment of the mucoadhesive properties peak mucoadhesive force (F) and work of mucoadhesion (W) with texture analyzers is a common in vitro method for analyzing formulation capabilities. Challenges arise in selecting and standardizing experimental conditions due to various variables influencing mucoadhesion. This complexity hampers direct product performance comparisons.

Microneedles for oral mucosal delivery - Current trends and perspective on future directions.

Introduction: Oral cavity drug and vaccine delivery has the potential for local targeting, dose reduction, minimization of systemic side effects, and generation of mucosal immunity. To overcome current limitations of delivery into the oral cavity mucosa, microneedles (MNs) have emerged as a promising technology.

Areas Covered: We reviewed the literature on MN application in the oral cavity, including in vitro studies, in vivo animal studies, and human clinical trials.

Polymeric Biomaterials for Topical Drug Delivery in the Oral Cavity: Advances on Devices and Manufacturing Technologies.

There are several routes of drug administration, and each one has advantages and limitations. In the case of the topical application in the oral cavity, comprising the buccal, sublingual, palatal, and gingival regions, the advantage is that it is painless, non-invasive, allows easy application of the formulation, and it is capable of avoiding the need of drug swallowing by the patient, a matter of relevance for children and the elderly. Another advantage is the high permeability of the oral mucosa, which may deliver very high amounts of medication rapidly to the bloodstream without significant damage to the stomach.

Altered physical-chemical properties of home bleaching gels after an accelerated stability study and their effects on tooth enamel.

Objectives: To investigate the physical-chemical properties of home bleaching gels based on Carbamide Peroxide (CP) and Hydrogen Peroxide (HP) after accelerated stability (AS) and its effects on enamel.

Materials And Methods: A total of 360 bovine teeth blocks were divided (n = 12): Control, CP10%-Whiteness Perfect, CP10%-Pola Night, HP7.5%-Pola Day, and HP7.

Effect of accelerated stability on the physical, chemical, and mechanical properties of experimental bleaching gels containing different bioadhesive polymers.

Objective: To evaluate the physical-chemical (weight, pH, quantification of hydrogen peroxide) and mechanical (texture profile and rheology tests) properties of the experimental bleaching gel based on the bioadhesive polymer Aristoflex® AVC, after accelerated stability testing.

Materials And Methods: A total of 300 syringes of bleaching gels were divided into 5 groups (n = 60): Whiteness Perfect® 10%-FGM (WP); carbamide peroxide 10% with aristoflex (CPa); carbamide peroxide 10% with Carbopol (CPc); aristoflex thickener (A); and Carbopol thickener (C). According to the following requirements and time, the accelerated stability test was performed: in an incubator at 40 °C and 75% humidity per 1, 3, and 6 months, and baseline (refrigerator at 5 °C and 25% humidity).

Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia.

Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTC) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity.

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.

Innovative Mucoadhesive Precursor of Liquid Crystalline System Loading Anti-Gellatinolytic Peptide for Topical Treatment of Oral Cancer.

Current researches report an actual benefit of a treatment for oral cancer via inhibition of proteolytic matrix metallopro-teinases (MPP) with a peptide drug, called CTT1. However, peptides present poor oral bioavailability. Topical administration on oral mucosa avoids its passage through the gastrointestinal tract and the first-pass liver metabolism, but the barrier function of the oral mucosa can impair the permeation and retention of CTT1.

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.

Capsaicin-Cyclodextrin Complex Enhances Mepivacaine Targeting and Improves Local Anesthesia in Inflamed Tissues.

Acidic environments, such as in inflamed tissues, favor the charged form of local anesthetics (LA). Hence, these drugs show less cell permeation and diminished potency. Since the analgesic capsaicin (CAP) triggers opening of the TRPV1 receptor pore, its combination with LAs could result in better uptake and improved anesthesia.

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

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% lidocaine-prilocaine (LDC-PLC), in order to fulfill this gap in the market.

Palatal needle-free anesthesia for upper molars extraction. A randomized clinical trial.

Background: The aim of this study was to compare the ability of liposomal and non-liposomal lidocaine and prilocaine in hydrogel formulations to promote topical anesthesia in palatal mucosa during upper molar extractions.

Methods: In this randomized, cross over, triple-blinded clinical trial, a liposomal and a non-liposomal formulation of the eutectic mixture of local anesthetics, 2.5% lidocaine and 2.

Effects of academic stress on the levels of oral volatile sulfur compounds, halitosis-related bacteria and stress biomarkers of healthy female undergraduate students.

To investigate whether academic stress changes the salivary microbiota and its relationship with salivary parameters, evaluating the effects on the production of volatile sulfur compounds (VSCs) in healthy women. Fifty-five women who were enrolled in a four-year Dentistry course were assessed for academic stress by the questionnaire Maslach Burnout Inventory-Student Survey and were then classified into 'Not Stressed' and 'Stressed' groups. Cortisol and alpha-amylase (AA) were measured as physiological stress biomarkers.

Anaesthetic benefits of a ternary drug delivery system (Ropivacaine-in-Cyclodextrin-in-Liposomes): in-vitro and in-vivo evaluation.

Objectives: To evaluate whether a ternary system composed of hydroxypropyl-β-cyclodextrin (HP-βCD) further encapsulated into egg phosphatidylcholine liposomes (LUV) could prolong the action and reduce the toxicity of ropivacaine (RVC).

Methods: Dynamic light scattering and NMR were used to characterize the inclusion complex (RVC : HP-βCD), liposomal (RVC : LUV) and ternary (LUV : RVC : HP-βCD) systems containing 0.25% RVC.

Fusogenic Liposomes Increase the Antimicrobial Activity of Vancomycin Against Biofilm.

The aim of the present study was to encapsulate vancomycin in different liposomal formulations and compare the antimicrobial activity against biofilms. Large unilamellar vesicles of conventional (LUV VAN), fusogenic (LUV VAN), and cationic (LUV VAN) liposomes encapsulating VAN were characterized in terms of size, polydispersity index, zeta potential, morphology, encapsulation efficiency (%EE) and release kinetics. The formulations were tested for their Minimum Inhibitory Concentration (MIC) and inhibitory activity on biofilm formation and viability, using methicillin-susceptible ATCC 29213 and methicillin-resistant ATCC 43300 strains.

Comparison of antinociceptive effects of plain lidocaine versus lidocaine complexed with hydroxypropyl-β-cyclodextrin in animal models of acute and persistent orofacial pain.

Herein, it was investigated whether a complex of lidocaine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) would present a better antinociceptive profile in vivo when compared with plain lidocaine in models of orofacial pain. Plain lidocaine (LDC) and complexed lidocaine (LDC:HP-β-CD) were initially evaluated in vitro to determine the release rate of the two formulations. Subsequently, the effect of both formulations was evaluated in independent groups of rats submitted to the orofacial formalin test, induction of facial heat hyperalgesia by capsaicin and carrageenan, and induction of facial heat and mechanical hyperalgesia by constriction of the infraorbital nerve.

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.

Nanohybrid hydrogels designed for transbuccal anesthesia.

Background: Local anesthesia in dentistry is by far the most terrifying procedure for patients, causing treatment interruption. None of the commercially available topical formulations is effective in eliminating the pain and phobia associated to the needle insertion and injection.

Materials And Methods: In this work we prepared a nanostructured lipid-biopolymer hydrogel for the sustained delivery of lidocaine-prilocaine (LDC-PLC) for transbuccal pre-anesthesia.

Stress-related salivary proteins affect the production of volatile sulfur compounds by oral bacteria.

Objective: To determine whether stress-related substances and sex hormones influence the growth and in vitro production of volatile sulfur compounds (VSCs) by Solobacterium moorei and Fusobacterium nucleatum.

Materials And Methods: Bacteria growth and VSCs production were evaluated in the presence of alpha-amylase, beta-defensin-2, mucin, estradiol, and progesterone. Growth was evaluated by colony counting, and the production of the VSCs hydrogen sulfide (H S) and methyl mercaptan (CH SH) was measured using the Oral Chroma™ instrument.

Bupivacaine in alginate and chitosan nanoparticles: an in vivo evaluation of efficacy, pharmacokinetics, and local toxicity.

Objective: This study reports a preclinical evaluation of an alginate/chitosan nanoparticle formulation containing NovaBupi®, a racemic bupivacaine (BVC) containing 25% dextrobupivacaine and 75% levobupivacaine.

Methods: New Zealand White rabbits (n=6) received intraoral or intrathecal injections of BVC 0.5% or BVC 0.