Effect of the Carrier on the Coprecipitation of Curcumin through Supercritical-Assisted Atomization

In this paper, composite systems containing curcumin (CUR) were prepared through supercritical-assisted atomization (SAA), using different carriers. Curcumin is particularly interesting in the pharmaceutical and nutraceutical fields for its antioxidant, antitumoral, and anti-inflammatory properties. However, its therapeutic effect on human health is restricted by its poor water solubility and low dissolution rate, limiting its absorption after its oral administration. To increase the dissolution rate and then the bioavailability of the active compound, CUR was coprecipitated with polymeric, i.e., polyvinylpyrrolidone (PVP) and dextran (DXT), and not polymeric, i.e., hydroxypropyl-β-cyclodextrin (HP-β-CD), carriers. The effects of some operating parameters, namely the concentration of solutes in solution and the active compound/carrier ratio, on the morphology and the particle size distribution of the powders were investigated. Submicrometric particles were produced with all the carriers. Under the best operating conditions, the mean diameters ± standard deviation were equal to 0.69 ± 0.20 μm, 0.40 ± 0.13 μm, and 0.81 ± 0.25 μm for PVP/CUR, DXT/CUR, and HP-β-CD/CUR, respectively. CUR dissolution rates from coprecipitated particles were significantly increased in the case of all the carriers. Therefore, the results are exciting from a pharmaceutical and nutraceutical point of view, to produce supplements containing curcumin, but assuring a high dissolution rate and bioavailability and, consequently, a more effective therapeutic effect.

Bio-Functionalization of a Novel Biocompatible High Entropy Alloy Used For Bone Implants

In this paper, a novel biocompatible alloy defined as FeMoTaTiZr was obtained and functionalized by hydroxyapatite-based coatings (HAP) in order to increase their biocompatibility, bioactivity, and resistance to corrosion for to be used as bone implants. To obtain the surface with antibacterial properties, the HAP coatings were doped with small amount of Zn. The alloy was prepared using the VAR (Vacuum Arc Remelting) equipment, while the coatings by RF magnetron sputtering method. The EDS analysis confirmed the presence of Ca and P in the case of all developed coatings, having Ca/P or Ca/(P+Zn) ratio of about 1.70 and 1.66, respectively. The XRD and ATR-FTIR investigations confirmed the presence of calcium phosphate phases. The roughness of uncoated substrates increased after coating with HAP, and it was considerably increased by the Zn addition. The electrochemical tests showed that the un-doped HAP exhibited good corrosion behavior, while Zn doped HAP coatings have a high dissolution rate in fetal bovine serum, being more proper as a biodegradable material.

Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs

This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.

Solubility, Permeability, and Dissolution Rate of Naftidrofuryl Oxalate Based on BCS Criteria

The Biopharmaceutics Classification System (BCS) was conceived to classify drug substances by their in vitro aqueous solubility and permeability properties. The essential activity of naftidrofuryl oxalate (NF) has been described as the inhibition of the serotonin receptors (5-HT2), resulting in vasodilation and decreasing blood pressure. Since the early 1980s, NF has been used to treat several venous and cerebral diseases. There is no data available on the BCS classification of NF. However, based on its physical-chemical properties, NF might be considered to belong to the 1st or the 3rd BCS class. The present study aimed to provide data concerning the solubility and permeability of NF through Caco-2 monolayers and propose its preliminary classification into BCS. We showed that NF is a highly soluble and permeable drug substance; thus, it might be suggested to belong to BCS class I. Additionally, a high dissolution rate of the encapsulated NF based on Praxilene® 100 mg formulation was revealed. Hence, it might be considered as an immediate-release (IR).

Improving solubility and storage stability of rifaximin via solid-state solvation with Transcutol®

Crystallization of rifaximin from Transcutol® affords the new anhydrous τ-form, which combines a high dissolution rate with a high storage stability, as it is not affected by exposure to humidity.

Synthesis and evaluation of factors affecting the in vitro bioactivity and antibacterial activity of bioactive glass ceramics

In the present study, two novel silicate glass-ceramics having chemical composition 38SiO2–41CaO–6P2O5–([Formula: see text])Na2O–[Formula: see text]CaF2 ([Formula: see text], 0.43 mol%) were synthesized. These glass derivatives were subjected to stimulated body fluid for 24 days in SBF under static condition at [Formula: see text]C in order to evaluate the bioactive properties of specimens. The antibacterial activity of glass ceramics against three pathogenic bacteria was determined using the modified Kirby Bauer method. It was found that the antibacterial activity primarily depends on the dissolution rate; faster release of ions caused rapid increase in the pH of the solution. Antibacterial properties were found to be strongly affected by changes in the pH of supernatant. The in vitro bioactivity assays showed that both glass derivatives were capable of bonding with bone and secondly effectively inhibit bacteria. However, the glass ceramic without CaF2 (B2) showed high dissolution rate, better bioactive ability and stronger antibacterial efficacy.

Long-Term Cytotoxicity, pH and Dissolution Rate of AH Plus and MTA Fillapex

The aim of the present study was to verify the long-term cytotoxic effects of the MTA Fillapex and to compare them with AH Plus. Dissolution rate and pH were also evaluated. Human osteoblast cells were incubated with elutes of fresh specimens from AH Plus and MTA Fillapex, and with elutes of the same specimens for 4 successive weeks. Elute's pH was evaluated at each time point. A multiparametric cell viability assay was performed. For dissolution rate, ISO methodology was used. The results were analyzed by one-way analysis of variance, complemented with the Tukey post-test (p<0.05). No significant difference was found among the materials when fresh mixed (p>0.05). After 1 week, AH Plus became non-cytotoxic on all three evaluated parameters. Conversely, MTA Fillapex remained severely and mildly cytotoxic over the entire experimental period (p<0.05). The dissolution rate of AH Plus was significantly lower than MTA Fillapex at all time points (p>0.05). The pH of AH Plus was significantly lower than MTA Fillapex at the second and third week (p<0.05). In the other tested time points no statistical difference was observed. In conclusion, MTA Fillapex remained cytotoxic after 4 weeks and its cytotoxicity may be related to the high dissolution rate of this material.

Nucleation, Growth and Evolution of Hydroxyapatite Films on Calcite

ABSTRACTMarble, a non-porous stone composed of calcite, is subject to acid rain dissolution due to its relatively high dissolution rate. With the goal of preventing such damage, we have investigated the deposition of films of relatively insoluble hydroxyapatite (HAP) on marble. This paper investigates the factors that affect the nucleation and growth kinetics of HAP on marble. A mild, wet chemical synthesis route, in which diammonium hydrogen phosphate (DAP) salt was reacted with marble, alone and with cationic and anionic precursors under different reaction conditions, was used to produce inorganic HAP films on the mineral surface. Film nucleation, growth and metastable phase evolution were studied, using techniques such as scanning electron microscopy (SEM) and grazing incidence X-ray diffraction (GID). The onset of nucleation, and the growth rate of the film, increased with cationic (calcium) and anionic (carbonate) precursor additions. The calcium and phosphate precursors also influenced metastable phase formation, introducing a new phase.

Experimental Study on Reactivity of Limestone in FGD System

The limestone collected from the Ji county of Tianjin was investigated in this study. The characterization of the limestone dissolution in wet FGD system is carried out by sulfuric acid titration. The results indicate that A lower PH value is benefit for the limestone dissolution, which causes high dissolution rate within short time. Smaller particle size results in higher dissolution rate. The addition of inorganic salt and organic acid significantly affect the limestone dissolution. The limestone dissolution rate increases with the increase of organic acid concentration. In all the inorganic salt, it is obvious that Na+ has an positive effect while CI- plays a negative role on the limestone dissolution. However, the addition of composite additive of adipic acid plus MgO to the limestone slurry is greatly better than using the adipic acid or MgO only.