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1.
Braz Oral Res ; 38: e036, 2024.
Article in English | MEDLINE | ID: mdl-38747823

ABSTRACT

This study aimed to evaluate in vitro the effect protocols and anticaries agents containing casein amorphous calcium fluoride phosphopeptide-phosphate (CPP-ACPF, MI Paste Plus), sodium trimetaphosphate (TMP) and fluoride (F), in remineralization of caries lesions. Bovine enamel blocks with initial caries lesions were divided into groups (n = 12): 1) Toothpaste without F-TMP-MI Plus (Placebo); 2) Toothpaste 1100 ppm F (1100F), 3) 1100F + MI Paste Plus (1100F-MI Paste Plus), 4) Toothpaste with 1100F + Neutral gel with 4,500 ppm F + 5%TMP (1100F + Gel TMP) and 5) Toothpaste with 1100F + Neutral gel with 9,000 ppm F (1100F + Gel F). For the 4 and 5 groups the gel was applied only once for 1 minute, initially to the study. For the 3 group, after treatment with 1100F, MI Paste Plus was applied 2x/day for 3 minute. After pH cycling, the percentage of surface hardness recovery (%SHR); integrated loss of subsurface hardness (ΔKHN); profile and depth of the subsuperficial lesion (PLM); concentrations of F, calcium (Ca) and phosphorus (P) in enamel was determined. The data were analyzed by ANOVA (1-criterion) and Student-Newman-Keuls test (p < 0.001). Treatment with 1100F alone led to ~ 28% higher remineralization when compared to treatment with 1100F associated with MI Paste Plus (p < 0.001). The 1100F and 1100F + Gel F groups showed similar values for %SHR (p = 0.150). 1100F + Gel TMP treatment also remineralized the enamel surface by ~ 30% and 20% when compared to the 1100F + Gel F and 1100F groups (p < 0.001). The lower lesion depth (ΔKHN) was observed for the 1100F + Gel TMP group (p < 0.001), where it was 54% and 44% lower in comparison to the 1100F and 1100F + Gel F groups (p < 0.001). Polarized light microscopy photomicrographs showed subsurface lesions in all groups, but these lesions were present to a lower extent in the 1100F + Gel TMP group (p < 0.001). Treatment with 1100F + Gel TMP promoted an increase in the concentration of Ca in the enamel by ~ 57% and ~ 26% when compared to the 1100F and 1100F + MI Paste Plus groups (p < 0.001), respectively. There were no significant differences between the 1100F, 1100F + MI Paste Plus and 1100F + Gel F groups (p > 0.001). Similar values of P in the enamel were observed in the 1100F, 1100F + MI Paste Plus and 1100F + Gel F groups (p > 0.001), except for the 1100F + Gel TMP group, which presented a high concentration (p < 0.001). We conclude that the 1100F+TMP gel treatment/protocol led to a significant increased remineralization when compared to the other treatments/protocols and may be a promising strategy for patients with early caries lesions.


Subject(s)
Cariostatic Agents , Caseins , Dental Enamel , Fluorides , Tooth Remineralization , Caseins/pharmacology , Caseins/therapeutic use , Tooth Remineralization/methods , Cattle , Animals , Dental Enamel/drug effects , Cariostatic Agents/pharmacology , Fluorides/pharmacology , Time Factors , Toothpastes/chemistry , Dental Caries/drug therapy , Analysis of Variance , Reproducibility of Results , Polyphosphates/pharmacology , Polyphosphates/chemistry , Polyphosphates/therapeutic use , Hardness Tests , Hydrogen-Ion Concentration , Surface Properties/drug effects , Materials Testing , Treatment Outcome , Reference Values , Hardness/drug effects , Phosphates
2.
Acta Odontol Scand ; 83: 264-272, 2024 May 06.
Article in English | MEDLINE | ID: mdl-38709122

ABSTRACT

PURPOSE: The purpose of the present in vitro study is to investigate and compare the remineralising potential of Moringa Oleifera extract, eggshell, and sodium fluoride varnish on microhardness of artificially demineralised enamel of primary teeth with biomimetic minimally invasive approach following the world paradigm shift towards natural products in paediatric dentistry. MATERIAL AND METHODS: Sample size included 44 primary molars. The mineral content and surface microhardness of all specimens were initially assessed using energy dispersive x-ray examination (EDX) and Vickers microhardness. The specimens were artificially demineralised for 96 h at a temperature of 37°C and then reassessed directly after demineralisation. The demineralised enamel specimens were randomly divided into four groups according to the remineralisation regimen utilised. Group 1: Artificial saliva (control); Group 2: Sodium fluoride varnish; Group 3: Eggshell hydrogel; and Group 4: Moringa Oleifera hydrogel. The specimens were stored for 8 days and then subsequently evaluated using EDX and microhardness assessment by Vickers microhardness test and scanning electron microscope (SEM).  Results: Regarding the microhardness test, there was a significant difference between the Moringa Oleifera group and Eggshell group compared to fluoride varnish (p < 0.05). Regarding EDX analysis, there was a statistically significant difference (p < 0.05) between Moringa Oleifera group and Eggshell group compared to fluoride varnish as the highest values were for Moringa Oleifera and Eggshell. On the other hand, there was no statistically significant difference (p > 0.05) between Moringa Oleifera and Eggshell in both the measurements. CONCLUSION: Moringa Oleifera and Eggshell might be considered as a biomimetic natural material capable of guiding enamel tissue remineralisation in early carious lesion of primary teeth. CLINICAL RELEVANCE: This research demonstrated the capability for early enamel caries to be remineralised using novel materials with a naturally counterpart implicated in biomineralisation as proved to be more effective than traditionally used fluoride varnish in primary teeth.


Subject(s)
Egg Shell , Hydrogels , Moringa oleifera , Sodium Fluoride , Tooth, Deciduous , Sodium Fluoride/administration & dosage , Tooth, Deciduous/drug effects , Egg Shell/chemistry , Humans , Moringa oleifera/chemistry , Tooth Remineralization/methods , Animals , In Vitro Techniques , Fluorides, Topical/administration & dosage , Microscopy, Electron, Scanning , Dental Enamel/drug effects , Hardness/drug effects , Spectrometry, X-Ray Emission , Tooth Demineralization/prevention & control , Tooth Demineralization/drug therapy
3.
Int J Mol Sci ; 22(16)2021 Aug 23.
Article in English | MEDLINE | ID: mdl-34445798

ABSTRACT

The bacterium Legionella pneumophila is still one of the probable causes of waterborne diseases, causing serious respiratory illnesses. In the aquatic systems, L. pneumophila exists inside free-living amoebae or can form biofilms. Currently developed disinfection methods are not sufficient for complete eradication of L. pneumophila biofilms in water systems of interest. Photodynamic inactivation (PDI) is a method that results in an antimicrobial effect by using a combination of light and a photosensitizer (PS). In this work, the effect of PDI in waters of natural origin and of different hardness, as a treatment against L. pneumophila biofilm, was investigated. Three cationic tripyridylporphyrins, which were previously described as efficient agents against L. pneumophila alone, were used as PSs. We studied how differences in water hardness affect the PSs' stability, the production of singlet oxygen, and the PDI activity on L. pneumophila adhesion and biofilm formation and in biofilm destruction. Amphiphilic porphyrin showed a stronger tendency for aggregation in hard and soft water, but its production of singlet oxygen was higher in comparison to tri- and tetracationic hydrophilic porphyrins that were stable in all water samples. All three studied porphyrins were shown to be effective as PDI agents against the adhesion of the L. pneumophila to polystyrene, against biofilm formation, and in the destruction of the formed biofilm, in their micromolar concentrations. However, a higher number of dissolved ions, i.e., water hardness, generally reduced somewhat the PDI activity of all the porphyrins at all tested biofilm growth stages.


Subject(s)
Biofilms/drug effects , Cations/pharmacology , Hardness/drug effects , Legionella pneumophila/drug effects , Photosensitizing Agents/pharmacology , Porphyrins/pharmacology , Water/chemistry , Amoeba/microbiology , Singlet Oxygen/pharmacology , Water Microbiology
4.
PLoS One ; 15(12): e0231606, 2020.
Article in English | MEDLINE | ID: mdl-33382707

ABSTRACT

Keratin intermediate filaments are the principal structural element of epithelial cells. Their importance in providing bulk cellular stiffness is well recognized, but their role in the mechanics of cell cortex is less understood. In this study, we therefore compared the cortical stiffness of three keratinocyte lines: primary wild type cells (NHEK2), immortalized wild type cells (NEB1) and immortalized mutant cells (KEB7). The cortical stiffness was measured by lateral indentation of cells with AOD-steered optical tweezers without employing any moving mechanical elements. The method was validated on fixed cells and Cytochalasin-D treated cells to ensure that the observed variations in stiffness within a single cell line were not a consequence of low measurement precision. The measurements of the cortical stiffness showed that primary wild type cells were significantly stiffer than immortalized wild type cells, which was also detected in previous studies of bulk elasticity. In addition, a small difference between the mutant and the wild type cells was detected, showing that mutation of keratin impacts also the cell cortex. Thus, our results indicate that the role of keratins in cortical stiffness is not negligible and call for further investigation of the mechanical interactions between keratins and elements of the cell cortex.


Subject(s)
Actin Cytoskeleton/metabolism , Intermediate Filaments/metabolism , Keratinocytes/metabolism , Keratins/metabolism , Microtubules/metabolism , Actin Cytoskeleton/ultrastructure , Cell Line , Cytochalasin D/pharmacology , Elasticity/drug effects , Gene Expression , Hardness/drug effects , Humans , Intermediate Filaments/ultrastructure , Keratinocytes/drug effects , Keratinocytes/ultrastructure , Keratins/genetics , Microtubules/ultrastructure , Optical Tweezers , Organ Specificity
5.
J Mater Sci Mater Med ; 31(12): 127, 2020 Nov 28.
Article in English | MEDLINE | ID: mdl-33247779

ABSTRACT

The aim of the present study was to characterize nanohybrid and nanofilled composites in terms of degree of conversion (DC), rate of cure (RC), microhardness (Vickers hardness number; VHN), depth of cure, and contraction stress (CS). Ceram.X® universal- A3, duo enamel E2, and duo dentin D3 composites were compared to Tetric EvoCeram® and FiltekTMSupreme XTE composites of equivalent dentin and enamel shades under a 40 s photopolymerization protocol. DC was measured by infrared spectroscopy, calculating RC from the kinetic curve. Top and bottom VHN were determined using a Vickers indenter, and bottom/top surface ratio (Vickers hardness ratio; VHR) calculated. CS vs. time was assessed by a universal testing machine and normalized for the specimen bonding area. All materials showed DC < 60%, Ceram.X® composites reaching higher values than the other composites of corresponding shades. RC at 5 s of photopolymerization was always higher than that at 10 s. All the Ceram.X® composites and the lighter-shaded Tetric EvoCeram® and FiltekTMSupreme XTE composites reached the RC plateau after 25 s, the remaining materials showed a slower kinetic trend. Tetric EvoCeram® and FiltekTMSupreme XTE composites displayed the softest and the hardest surfaces, respectively. Differently from darker-shaded materials, the universal and the three enamel-shaded composites resulted optimally cured (VHR > 80%). The tested composites differed in CS both during and after light cure, Tetric EvoCeram® and FiltekTMSupreme XTE composites displaying the highest and the lowest CS, respectively. Only the Ceram.X® universal-A3 reached a CS plateau value. The tested composites exhibited material-dependent chemo-mechanical properties. Increasing the curing time and/or reducing the composite layer thickness for dentin-shaded composites appears advisable.


Subject(s)
Curing Lights, Dental , Dental Restoration, Permanent , Hardness/drug effects , Compressive Strength/radiation effects , Hardness/radiation effects , Kinetics , Light , Materials Testing , Microspheres , Nanocomposites/chemistry , Nanocomposites/radiation effects , Polymerization/radiation effects , Stress, Mechanical , Surface Properties/radiation effects
6.
Sci Rep ; 10(1): 8127, 2020 05 15.
Article in English | MEDLINE | ID: mdl-32415190

ABSTRACT

The present study aimed to evaluate the efficiency, effectiveness, and biocompatibility of two agents used for the chemomechanical removal of carious dentin. Sixty extracted carious human teeth were treated with a conventional bur (CBG) or chemomechanical agents - Papacarie Duo (PG) and Brix 3000 (BG). Treatment efficiency and effectiveness were assessed by the working time for carious dentin removal and Knoop microhardness values, respectively. Human pulp fibroblasts (FP6) were used to evaluate cytotoxicity by incorporating MTT dye, and genotoxicity was evaluated with the micronuclei test. The carious tissue was removed in a shorter time with CBG (median = 54.0 seconds) than the time required for chemomechanical agents (p = 0.0001). However, the time was shorter for Brix 3000 (BG) than that for Papacarie Duo (PG), showing mean values of 85.0 and 110.5 seconds, respectively. Regarding microhardness testing, all approaches tested were effective (p < 0.05). The final mean microhardness values were 48.54 ± 16.31 KHN, 43.23 ± 13.26 KHN, and 47.63 ± 22.40 KHN for PG, BG, and CBG, respectively. PG decreased cell viability compared to that of BG, but it presented no genotoxicity. Brix 3000 may be a good option for chemomechanical dentin caries removal due to its reduced removal time and lower cytotoxicity compared to the other treatment options.


Subject(s)
Dental Caries/therapy , Dental Cavity Preparation/methods , Dentin/chemistry , Fibroblasts/drug effects , Hardness/drug effects , Papain/pharmacology , Sodium Hypochlorite/pharmacology , Cell Proliferation , Cells, Cultured , Dentin/drug effects , Fibroblasts/pathology , Humans , In Vitro Techniques , Stress, Mechanical
7.
Drug Dev Ind Pharm ; 46(2): 309-317, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31944867

ABSTRACT

Objective: Develop a child-friendly Fixed Dose Combination (FDC) water-dispersible tablet for Tuberculosis (TB) treatment, with 50, 150, and 75 mg of isoniazid, pyrazinamide and rifampicin respectively. This new formulation must contain the lowest number of excipients accepted for pediatrics and fulfill all the pharmacopeia requirements.Significance: At present, there is no adequate market dosage form available for children. There is, however, one in a prequalification phase by the World Health Organization but its composition contains excipients which may not be suitable for pediatrics. Therefore, this new formulation would cover this therapeutic gap.Methods: A factorial design, based on three quantitative factors (compression force and concentration of AcDiSol® and Explosol®) at three levels each, was performed to elucidate their influence over disintegration time and friability. In addition, the influence of the press speed on disintegration time, friability, tensile strength, fineness of dispersion and content uniformity over the target tablet was tested. A stability test was done following ICH guideline for accelerated conditions.Results: Tablets developed with 9% w/w of Explosol® and a compression force of 16 kN disintegrated in less than 3 min and showed a friability below 1% when 15-mm punches were used. The tableting process could be done up to 25 and 50 cycles/minute ensuring good quality attributes when 15 and 12-mm punches were used, respectively. All APIs remained inside the limit of ± 5% of drug content till 6 months of storage.Conclusion: A high-quality child-friendly FDC water-dispersible tablet was developed improving the treatment of TB in pediatric.


Subject(s)
Antitubercular Agents/administration & dosage , Antitubercular Agents/chemistry , Isoniazid/chemistry , Pyrazinamide/chemistry , Rifampin/chemistry , Tablets/chemistry , Tuberculosis/drug therapy , Chemistry, Pharmaceutical/methods , Child , Drug Compounding/methods , Excipients/chemistry , Hardness/drug effects , Humans , Isoniazid/administration & dosage , Pediatrics/methods , Pyrazinamide/administration & dosage , Rifampin/administration & dosage , Solubility/drug effects , Tablets/administration & dosage , Tensile Strength
8.
Int J Pharm ; 574: 118902, 2020 Jan 25.
Article in English | MEDLINE | ID: mdl-31794786

ABSTRACT

Tablet quality can be affected by material, configuration and design of the tooling which comprise punches and dies. Much research attention had centred around punches, with very little reported on the dies. Dies with modified bore lining materials or inserts are available for special applications. However, the influence of such die types on tablet properties and the compaction process has not been well studied. Often, the reason for selecting dies with harder lining material is for improved wear resistance. In this study, flat-faced and convex-faced tablets were produced from paracetamol granules using dies with different bore inserts. Tablet properties and response parameters of the compaction process were evaluated to understand the impact of die mechanical and surface properties on the compacts formed. Compaction pressure was found to have the greatest impact on tablet elastic recovery (r ≥ 0.96, p < 0.01 in all bivariate correlations) and thus affecting the tensile strength. Choice of die inserts could impact the mechanical properties of convex-faced paracetamol tablets, particularly at high compaction pressures.


Subject(s)
Acetaminophen/chemistry , Tablets/chemistry , Drug Compounding/methods , Excipients/chemistry , Hardness/drug effects , Pressure , Surface Properties/drug effects , Tensile Strength/drug effects
9.
Biomed Mater Eng ; 30(5-6): 487-496, 2020.
Article in English | MEDLINE | ID: mdl-31594192

ABSTRACT

BACKGROUND: Many novel biomaterials have been incorporated in toothpastes to promote remineralization of tooth structure. OBJECTIVES: This study was carried out to compare the discrepancies between declared and actual total fluoride (TF) or total soluble fluoride (TSF) concentration of two modern toothpastes containing bioactive glasses; these were also assessed for their remineralization potential. MATERIALS AND METHODS: The TF and TSF concentration were assessed using a fluoride ion selective electrode. Enamel remineralization was evaluated through micro-hardness analysis. Eighteen enamel blocks were divided into three groups: 1 (n = 6; control), 2 (n = 6; Novamin® toothpaste), and 3 (n = 6; BiominF® toothpaste). The specimens were demineralized by 6 wt% citric acid (pH = 2.2). Subsequently, the specimens in group 1 were kept in artificial saliva (AS), while the specimens in groups 2 and 3 were stored in AS + Novamin® and AS + Biomin®, respectively. RESULTS: Both Novamin® or BiominF® showed less TF concentration than their label claims. BiominF® had more TF and TSF compared to Novamin® (p < 0.05). The BiominF® toothpaste presented higher micro-hardness values on remineralization. CONCLUSION: BiominF® toothpaste demonstrated more fluoride content and greater potential to promote remineralization of demineralized human enamel compared to Novamin®.


Subject(s)
Ceramics/pharmacology , Dental Enamel/drug effects , Fluorides/analysis , Tooth Remineralization/methods , Toothpastes/pharmacology , Ceramics/chemistry , Dental Enamel/physiology , Hardness/drug effects , Humans , In Vitro Techniques , Materials Testing , Molar, Third , Particle Size , Surface Properties/drug effects , Toothpastes/chemistry
10.
Braz Oral Res ; 33: e037, 2019.
Article in English | MEDLINE | ID: mdl-31508726

ABSTRACT

Iontophoresis is a noninvasive technique, based on the application of a constant low-intensity electric current to facilitate the release of a variety of drugs, whether ionized or not, through biological membranes. The objective of this research was to evaluate the effect of iontophoresis using different electric current intensities on the uptake of fluoride in dental enamel with artificial caries lesions. In this in vitro operator-blind experiment, bovine enamel blocks (n = 10/group) with caries-like lesions and predetermined surface hardness were randomized into 6 groups: placebo gel without fluoride applied with a current of 0.8 mA (negative control), 2% NaF gel without application of any current, and 2% NaF gel applied with currents of 0.1, 0.2, 0.4 and 0.8 mA. Cathodic iontophoresis was applied for 4 min. The concentration of loosely bound fluoride (calcium fluoride) and firmly bound fluoride (fluorapatite) was determined. The results were analyzed by the nonparametric Kruskal-Wallis and Dunn tests. Iontophoresis at 0.8 mA, combined with the application of fluoridated gel (2% NaF), increased fluoride uptake in enamel with caries-like lesions, as either calcium fluoride or fluorapatite.


Subject(s)
Cariostatic Agents/pharmacology , Dental Caries , Dental Enamel/drug effects , Fluorides/pharmacology , Iontophoresis/methods , Animals , Apatites/analysis , Calcium Fluoride/analysis , Cattle , Disease Models, Animal , Electricity , Hardness/drug effects , Random Allocation , Surface Properties/drug effects , Treatment Outcome
11.
J Pharm Sci ; 108(12): 3859-3869, 2019 12.
Article in English | MEDLINE | ID: mdl-31542437

ABSTRACT

Hydroxypropyl methylcellulose acetate succinate (HPMCAS) has gained popularity as a carrier for amorphous solid dispersion because of its ability to maintain drugs in supersaturated state after dissolution in aqueous media. In part I and II of this series of articles, we have demonstrated that amorphous solid dispersions containing HPMCAS may be prepared using surfactants as plasticizers to reduce processing temperature (Solanki et al., J Pharm Sci. 2019; 108:1453-65), where surfactants also increase dissolution rate and degree of supersaturation (Solanki et al., J Pharm Sci. 2019; 108: 3063-73). The present investigation was undertaken to develop melt extrudates of itraconazole-HPMCAS and itraconazole-surfactant-HPMCAS mixtures into tablets having tensile strength ≥2 MPa, where poloxamer 407 and d-α-tocopherol polyethylene glycol 1000 succinate were used as surfactants. Milled filaments were sieved to collect <212-µm particles, which were then compressed into tablets with different excipients (silicified microcrystalline cellulose [MCC], Avicel PH-102, dicalcium phosphate, lactose, and Starch 1500). Initial screening of various diluents showed that only silicified MCC and Avicel PH-102 could provide the target tensile strength of ≥2 MPa. Tabletability (tensile strength vs. compaction pressure), compressibility (porosity vs. compaction pressure), and compactibility (tensile strength vs. porosity) were then studied for tablet formulations. The desired tensile strength could be obtained at the diluent level of 50%-70%, where silicified MCC provided better hardness than Avicel PH-102. Tablets disintegrated in <2 min, and drug release from tablets was comparable to that of milled filaments.


Subject(s)
Itraconazole/chemistry , Methylcellulose/analogs & derivatives , Surface-Active Agents/chemistry , Tablets/chemistry , Cellulose/chemistry , Chemistry, Pharmaceutical/methods , Drug Compounding/methods , Drug Liberation/drug effects , Excipients/chemistry , Hardness/drug effects , Hot Melt Extrusion Technology/methods , Lactose/chemistry , Methylcellulose/chemistry , Polyethylene Glycols/chemistry , Solubility/drug effects , Temperature , Tensile Strength/drug effects
12.
Drug Dev Ind Pharm ; 45(10): 1617-1623, 2019 Oct.
Article in English | MEDLINE | ID: mdl-31353966

ABSTRACT

Context: AS FDSTs will provide an accessible alternative for AS autoinjector (ATROPEN®), and a noninvasive first-aid antidote for the treatment of organophosphate (OP) poisoning and reduce the number of fatalities due to nerve gas attacks or OP pesticide poisoning. Objective: The effects of changing the filler grade on the characteristics of atropine sulfate (AS) fast disintegrating sublingual tablets (FDSTs) and AS sublingual permeability were investigated in order to optimize the formulation of AS FDSTs and, therefore, AS sublingual permeability. Methods: Two batches of AS FDSTs containing AS 8 mg were formulated and manufactured using two different filler grades: microcrystalline cellulose (MCC) UF-702 (formulation A) and MCC PH-301 (formulation B). Several United States Pharmacopeia (USP) and non-USP physical tests were performed to evaluate the AS FDSTs' characteristics. The AS permeability from the two AS FDST batches were evaluated using Franz cells through excised porcine sublingual membranes. Results were statistically compared at p < .05. Results: Both batches passed the content uniformity and friability tests. Formulation A tablets were significantly different from formulation A tablets and resulted in better powder flowability, higher breaking force, faster disintegration, faster dissolution rate, higher water uptake, and higher AS permeability. Conclusion: The selection of the filler grade to be used in the formulation of AS FDSTs can significantly impact their characteristics and significantly affect AS sublingual permeability, which can be used to improve the sublingual delivery of AS and the potential of using AS FDSTs as an alternative dosage form for the first-aid treatment of OP poisoning.


Subject(s)
Atropine/chemistry , Tablets/chemistry , Administration, Sublingual , Cellulose/chemistry , Chemistry, Pharmaceutical/methods , Drug Compounding/methods , Excipients/chemistry , Hardness/drug effects , Permeability/drug effects , Powders/chemistry , Solubility/drug effects
13.
J Pharm Sci ; 108(10): 3240-3251, 2019 10.
Article in English | MEDLINE | ID: mdl-31216450

ABSTRACT

This work aimed at establishing a framework to screen and understand the product variability deeming from factors that affect the quality features of cream formulations. As per Quality by Design - based approach, cream quality target profile and critical quality attributes were identified, and a risk assessment analysis was conducted to qualitatively detect the most critical variables for cream design and development. A Plackett-Burman design was used to screen out unimportant factors, avoiding collecting large amounts of data. Accordingly, 2 designs of experiments (DoE-1 and DoE-2) were performed, and the effects of independent variables on the cream formulations responses were estimated. At different factor combinations, significant variability was observed in droplet size, consistency, hardness, compressibility, and adhesiveness with values ranging from 2.6 ± 0.9 to 10 ± 6 µm, 7.93 ± 0.05 to 13.53 ± 0.14 mm, 27.6 ± 0.3 to 58.4 ± 1.1 g, 38 ± 6 to 447 ± 37 g.s, and 25.7 ± 2.1 to 286 ± 33 g.s, respectively. The statistical analysis allowed determining the most influent factors. This study revealed the potential of Quality by Design methodology in understanding product variability, recognizing the most critical independent variables for the final product quality. This systematic approach in the pharmaceutical field will yield more robust products and processes, provisioning time and cost effective developments.


Subject(s)
Ointments/chemistry , Chemistry, Pharmaceutical/methods , Drug Compounding/methods , Hardness/drug effects , Particle Size , Quality Control
14.
PLoS One ; 14(4): e0215370, 2019.
Article in English | MEDLINE | ID: mdl-30978248

ABSTRACT

Alterations in the structure and mechanical properties of teeth in adult Wistar rats exposed to cadmium were investigated. Analyses were conducted on two sets of incisors from female and male specimens, that were intoxicated with cadmium (n = 12) or belonged to the control (n = 12). The cadmium group was administered with CdCl2 dissolved in drinking water with a dose of 4mg/kgbw for 10 weeks. The oral intake of cadmium by adult rats led to the range of structural changes in enamel morphology and its mechanical features. A significant increase of cadmium levels in the teeth in comparison to the control, a slight shift in the colour and reduction of pigmented enamel length, higher surface irregularity, a decrease of hydroxyapatite crystals size in the c-axis and simultaneous increase in pigmented enamel hardness were observed. The extent of these changes was sex-dependent and was more pronounced in males.


Subject(s)
Cadmium/toxicity , Incisor/drug effects , Animals , Biomechanical Phenomena , Cadmium/administration & dosage , Cadmium/pharmacokinetics , Crystallization , Dental Enamel/drug effects , Dental Enamel/pathology , Dental Enamel/physiopathology , Durapatite/chemistry , Durapatite/metabolism , Female , Hardness/drug effects , Incisor/pathology , Incisor/physiopathology , Male , Microscopy, Atomic Force , Microscopy, Electron, Scanning , Minerals/metabolism , Rats , Rats, Wistar , X-Ray Diffraction
15.
PLoS One ; 14(4): e0214948, 2019.
Article in English | MEDLINE | ID: mdl-30951549

ABSTRACT

This work aimed to evaluate the roughness, microhardness, ultrastructure, chemical composition and crystalline structure in submitted teeth to a prolonged home bleaching regimen with 10% carbamide peroxide (10% PC) for different periods. The specimens were divided into the following groups: G1: negative control (application of water-soluble gel); G2: tooth whitening group (positive control), under application time recommended by the manufacturer (4h/14 days); G3: prolonged whitening 50%, under prolonged time recommended by the manufacturer in 50% (4h/21 days); G4: excessive whitening 100%, under exceeded manufacturer recommended time by 100% (4h/ 28 days). The results were evaluated descriptively and analytically. There were no changes in the roughness in any of the evaluated groups. However, the microhardness decreased in the G4 group. Scanning electron microscopy showed changes in the enamel surface of groups G2, G3 and G4. Dispersive X-ray spectroscopy identified changes in the concentration of chemical elements O, Mg, P, K in all groups. Thus, this study showed that prolonged home bleaching could cause changes in the ultrastructure, chemical composition and microhardness of the enamel.


Subject(s)
Carbamide Peroxide/pharmacology , Dental Enamel , Hardness/drug effects , Tooth Bleaching , Animals , Cattle , Dental Enamel/metabolism , Dental Enamel/ultrastructure , Microscopy, Electron, Scanning , Surface Properties/drug effects
16.
Int J Pharm ; 559: 210-219, 2019 Mar 25.
Article in English | MEDLINE | ID: mdl-30682448

ABSTRACT

This paper compares batch and continuous technologies in terms of product quality and process performance in pharmaceutical tablet manufacturing using ethenzamide as the active pharmaceutical ingredient. Batch and continuous processes using wet granulation were investigated by performing experiments on the scale of 5 and up to 100 kg/lot, using the same raw materials. Three technologies were tested and compared: (i) batch technology using fluidized bed granulation, (ii) batch technology using high shear granulation, (iii) continuous technology using high shear granulation. In the full-scale experiment, in all three technologies including continuous technology, the quality of the tablets fulfilled the target values regarding hardness, active pharmaceutical ingredient content, and dissolution. The granules produced by different technologies, however, presented varying attributes regarding granule size distribution, loose bulk density, or scanning electron microscope images. The process performance, more specifically the yield, was slightly better for batch technologies than for the continuous technology, mainly due to losses in the start-up operation. Notably, this study has shown that continuous technology, which is generally believed to not entail scale-up procedures, could in fact, require parameter adjustment for prolonged operation. The results provided suggestions for improvements to implement large-scale continuous technologies in the pharmaceutical industry.


Subject(s)
Salicylamides/chemistry , Tablets/chemistry , Chemistry, Pharmaceutical/methods , Excipients/chemistry , Hardness/drug effects , Particle Size , Solubility/drug effects , Technology, Pharmaceutical/methods
17.
Caries Res ; 53(1): 33-40, 2019.
Article in English | MEDLINE | ID: mdl-29879720

ABSTRACT

The aim of this in vitro study was to investigate the impact of saliva on the abrasion of eroded enamel using two measuring methods. A total of 80 bovine enamel specimens from 20 bovine incisors were allocated to four experimental groups (n = 20 specimens per group). After baseline surface microhardness (SMH) measurements and profilometry all specimens were subjected to erosion (2 min, 1% citric acid, pH: 3.6, 37°C). SMH was determined again, and the depths of the Knoop indentations were calculated. Thereafter, specimens were incubated in human saliva (group 1 - no incubation/control, group 2 - 0.5 h, group 3 - 1 h, group 4 - 2 h) before toothbrush abrasion was performed. After final SMH measurements and profilometry, indentations were remeasured, and surface loss was calculated. SMH did not return to baseline values regardless of the length of saliva incubation. Further, an irreversible substance loss was observed for all specimens. With the indentation method, significantly (p < 0.05) more substance loss was found for controls (least square means ± standard error of 198 ± 19 nm) than for groups 2-4 (110 ± 10, 114 ± 11, and 105 ± 14 nm). Profilometric assessment showed significantly more substance loss for controls (122 ± 8 nm) than for group 4 (106 ± 5 nm). Intraclass correlation for interrater reliability between measurement methods was low (0.21, CI: 0.1-0.3), indicating poor agreement. Exposure of eroded enamel to saliva for up to 2 h could not re-establish the original SMH. The amount of measured substance loss depended on the measurement method applied.


Subject(s)
Dental Enamel/physiopathology , Hardness/drug effects , Saliva/chemistry , Tooth Abrasion/chemically induced , Tooth Erosion/chemically induced , Animals , Cattle , Citric Acid/adverse effects , Hardness/physiology , Humans , Reproducibility of Results , Surface Properties/drug effects , Tooth Remineralization , Toothbrushing
18.
Pak J Pharm Sci ; 32(6(Supplementary)): 2811-2816, 2019 Nov.
Article in English | MEDLINE | ID: mdl-32024618

ABSTRACT

Sugar free chewable tablets are considered to be desired medication for diabetic population having acid reflex problems. The main objective of this study is to develop a patient complaint tablet dosage form which is sugar free, chewable and easy to use. The formulation is designed for hyperglycemic and dysphasic patients along acidity or stomach ulcer. For manufacturing Aluminum Hydroxide (Kyowa Japan), Magnesium Hydroxide (Taurus chemicals India) Simethicone, Povidone (JRS pharma) Sorbitol powder, Magnesium stearate, Dilcalcium phosphate anhydrous, SSG (JRS pharma) and Aspartame were used. The granules formed by wet granulation method and tablets are compressed by rotary compression machine. The pre-formulation studies of granules (Angle of repose, Bulk/Tapped density, Carr's compressibility index and Hausner's ratio), uniformity of content (assay), acid neutralizing capacity, Identification by FTIR spectroscopy all are found within the limits as per USP specifications. All three formulation batches are stable under accelerated and ambient stability conditions for 6 months and 24 months respectively. The formulation development of sugar free oral chewable antacid tablet is pharmaceutically stable and can further analyze for safety and efficacy studies.


Subject(s)
Antacids/chemistry , Antacids/pharmacology , Anti-Ulcer Agents/chemistry , Diabetes Mellitus/physiopathology , Heartburn/drug therapy , Sugars/chemistry , Tablets/chemistry , Anti-Ulcer Agents/pharmacology , Chemistry, Pharmaceutical/methods , Diabetes Complications/drug therapy , Drug Compounding/methods , Excipients/chemistry , Hardness/drug effects , Heartburn/etiology , Humans , Povidone/chemistry , Powders/chemistry , Powders/pharmacology , Solubility/drug effects , Sorbitol/chemistry , Tablets/pharmacology
19.
J Mech Behav Biomed Mater ; 90: 460-471, 2019 02.
Article in English | MEDLINE | ID: mdl-30448560

ABSTRACT

Titanium alloys (Ti-6Al-4V) are promising materials as bone implants in clinical surgeries owing to their excellent performances. However, wear debris caused by the tribological behavior of the cortical bone and titanium alloy interface were found to be paramount for implant stability. The contact environment between the cortical bone and Ti-6Al-4V in vivo has been considered to affect the tribological behavior. Currently, the tribological behaviors of bone and Ti-6Al-4V in different biolubricants remain elusive. Therefore, in this work, the tribological behaviors of Ti-6Al-4V plates sliding against bovine cortical bone were investigated in dry sliding and in biolubricants of physiological saline (PS), simulated body fluids (SBF), and fetal bovine serum (FBS). Results show that the friction coefficient and wear rate of the bovine cortical bone and Ti-6Al-4V interface exhibit the same sequence as follows: FBS > SBF > PS > dry sliding. These results are attributed to bone hardness variation and corrosion of different biolubricants. Meanwhile, the effects of normal load and velocity on the tribological behavior of bone and Ti-6Al-4V interface were also investigated in dry sliding and three different biolubricants. Results show that as the normal load is increased and the sliding velocity is decreased, the friction coefficient decreases in dry condition, adhering to the Hertz contact theory. However, according to the boundary lubrication theory, the friction coefficient in three biolubricants correlates positively to the normal load and negatively to the sliding velocity. Moreover, the wear rates of the bone samples increase with the increase in normal load and sliding velocity under dry and biolubrication conditions. Finally, the characterization results indicate that the wear mechanisms of the cortical bone and Ti-6Al-4V interface in dry friction are primarily adhesive and abrasive wear. Further, corrosive wear occurs in biolubrications, apart from adhesive and abrasive wear.


Subject(s)
Biocompatible Materials/pharmacology , Cortical Bone/drug effects , Lubricants/pharmacology , Titanium/pharmacology , Alloys , Animals , Biocompatible Materials/chemistry , Cattle , Corrosion , Electrochemistry , Friction , Hardness/drug effects , Lubricants/chemistry , Mechanical Phenomena , Surface Properties , Titanium/chemistry
20.
Int J Biol Macromol ; 123: 10-19, 2019 Feb 15.
Article in English | MEDLINE | ID: mdl-30408455

ABSTRACT

Assembling between polyphenols and proteins has been freshly spotlighted. We studied the antiglycation and anti-hardening effects of microencapsulated mulberry polyphenols (MMPs) in a high-protein-sugar ball (HPSB) model during storage using multi-dimensional approaches, including UPLC-ESI-MS/MS, SDS-PAGE, MALDI-TOF-MS, FTIR, and a molecular docking study. It was found that MMPs significantly relegated the browning development, AGEs, and/or CML levels of HPSB after 45 d of storage at 45 °C. MMPs also downgraded the protein insolubility, aggregation, oligomerization, and glycoxidation during late-storage. A molecular docking scrutiny proved that cyanidin 3-O-rutinoside and quercetin 3-O-rutinoside interacted with whey proteins subunits via H-bonding and π-π interactions. This binding blocked some glycation residues of whey proteins especially lysyl residues, namely Lys5, 16, 60, 69, 93, 94, and 122. Our data disclosed that MMPs could be valorized as promising antiglycative ingredients to mitigate AGEs-generation and other subsequent unwanted changes in protein-rich food matrices.


Subject(s)
Glycosylation/drug effects , Hardness/drug effects , Morus/chemistry , Polyphenols/pharmacology , Sugars/metabolism , Whey Proteins/metabolism , Anthocyanins/pharmacology , Fruit/chemistry , Glucosides/pharmacology , Molecular Docking Simulation/methods , Plant Extracts/pharmacology , Quercetin/analogs & derivatives , Quercetin/pharmacology , Tandem Mass Spectrometry/methods
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