The aim in this study was to develop and evaluate a nanofluconazole (FLZ) formulation with increased solubility and permeation rate using nanosuspensions. The FLZ nanosuspensions were stabilized using a variety of stabilizing agents and surfactants in various concentrations. The FLZ nanosuspension was characterized in vitro using particle size, zeta potential, X-ray powder diffraction (XRPD), and solubility. In addition, the ex vivo ocular permeation of FLZ through a goat cornea was analyzed. The results showed that the particle size of all nanosuspension formulations was in the nanometer range from 174.5 ± 1.9 to 720.2 ± 4.77 nm; that of the untreated drug was 18.34 μm. The zeta potential values were acceptable, which indicated suitable stability for formulations. The solubility of the nanosuspensions was up to 5.7-fold higher compared with that of the untreated drug. The results of the ex vivo ocular diffusion of the FLZ nanosuspensions showed the percentage of FLZ penetrating via the goat cornea increased after using Kollicoat to stabilize the nanosuspension formulation. Consequently, when using a nanosuspension formulation of Kollicoat, the antifungal activity of the drug strengthens.

Solvent evaporation within an adhesive layer is a crucial step during a bonding process. The aim of this current research was to test whether the use of different air temperatures (20 °C, 40 °C, and 60 °C) for solvent evaporation improves the performance of four adhesive systems to dentin. Sixty non-carious human molar teeth were randomly prepared for micro-tensile bond strength (μTBS) tests. Four different adhesive systems, Prime&Bond Universal (PBU), OptiBond Universal (OBU), OptiBond FL (OBFL), and Clearfil SE (CSE), were applied following the manufacturer\'s instructions. Three groups based on the air-drying temperature were used: solvent evaporation was performed with either of warm (40 °C), (60 °C), and cold air as control group (20 °C) for 10 s at a distance of 5 cm. In all bonded surfaces, three resin composite (Reflectys, Itena Clinical, Paris, France) layers of 2 mm thickness were built up. The resin-dentin samples were kept in distilled water at 37 °C for 24 h and 6 months, respectively, before μTBS testing. Failure analysis, scanning electron microscopy of resin-dentin bonded interface, and solvent evaporation rate were tested as secondary variables. All analyses were conducted using a significance level of α = 0.05. Bond strength (BS) values were similar among all the adhesive systems used (p > 0.05). Also, the aging factor did not affect the BS (p > 0.05). Only the factor of temperature used for solvent evaporation resulted in a statistically significant effect (p < 0.05), with the temperature of 60 °C being the highest value (p < 0.05). A failure mode evaluation revealed mostly adhesive or mixed modes of failures in all the different temperatures of air used for the solvent evaporation of each adhesive system. The thickness of the adhesive layer and the creation of resin tags varied amongst the temperatures evaluated. For all adhesive systems tested, the use of 40 °C or 60 °C air for solvent evaporation led to an increased mass loss. Warmer temperatures for solvent evaporation contributed positively to bonding performance, enhancing both the quality of the adhesive layer and its interaction with the dentin tissue. Optimizing solvent evaporation with warmer air temperatures (40 °C and 60 °C) significantly improved µTBS, offering a practical means to enhance the quality and longevity of adhesive restorations in esthetic dentistry.

OBJECTIVE: To prepare aloe-emodin solid dispersion (AE-SD) and determine the metabolic process of AE and AE-SD in vivo.
METHODS: AE-SD was prepared viasolvent evaporation or solvent melting using PEG-6000 and PVP-K30 as carriers. Thermogravimetric analysis, X-ray diffraction spectroscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy and scanning electron microscopy were used to identify the physical state of AE-SD. Optimal prescriptions were screened viathe dissolution degree determination method. Using Phoenix software, AE suspension and AE-SD were subjected to a pharmacokinetic comparison study analyzing the alteration of behavior in vivo after AE was prepared as a solid dispersion. Acute toxicity was assessed in mice, and the physiological toxicity was used as the determination criterion for toxicity.
RESULTS: AE-SD showed that AE existed in the carrier in an amorphous state. Compared with polyethylene glycol, polyvinylpyrrolidone (PVP) inhibited AE crystallization, causing the drug to transform from a dense crystalline state to an amorphous form and increasing the degree of drug dispersion. Therefore, it was more suitable as a carrier material for AE-SD. The addition of poloxamer (POL) was more beneficial to the stability of solid dispersions and could reduce the amount of PVP. The dissolution test confirmed that the optimal ratio of AE to the composite vector AE-PVP-POL was 1：2：2, and its dissolution effect was also optimal. Based on the pharmacokinetic comparison, the drug absorption was faster and quickly reached the peak of blood drug concentration in AE-SD compared to AE, the Cmax of AE-SD was greater than that of AE, and t1/2 and mean residence time of AE-SD were less than AE. The results showed that the drug metabolism in AE-SD was better, and the residence time was shorter. The toxicology study showed that both AE and AE-SD had no toxicity.
CONCLUSIONS: This paper established that the solubility of the drug could be increased after preparing a solid dispersion, as demonstrated by in vitro dissolution experiments. In vivo pharmacokinetics studies confirmed that AE-SD could improve the bioavailability of AE in vivo, providing a new concept for the research and development of AE preparations.

Euglena gracilis (EG) is a unicellular freshwater alga known for its high β-1,3-glucan (BG) content with well-known biological properties and immune response. The high molecular weight structure of BG traditionally poses a challenge in terms of its size and absorption. Therefore, the aim of this study was to develop a novel drug delivery mechanism of BG and EG to nanophytosomes (NPs) by converting the heavy molecular weight of BG and EG into lipid phosphatidylcholine (PC), which plays an important role in improving their bioavailability and entrapment in captivity. The BG and EG NPs were developed by the solvent evaporation method while varying time and temperature to optimize their drug delivery ability. The size of BG-PC and EG-PC obtained by the Dynamic Light Scattering (DLS) method was 134.62 and 158.38 nm, respectively. Chemical (Fourier Transform Infra-Red) and structural (X-Ray Diffraction) characterization of NPs improved the binding capacity and the amorphous nature of both NPs. The shape of the NPs by Scanning electron microscopy (SEM) and Transmission electron microscopy (TEM) revealed their spherical, vesicular nature. The encapsulation efficiency of BG-PC and EG-PC was 82 ± 1.62 % and 87 ± 3.22 %, respectively, which improves the bioavailability. The developed methodology has thus proven effective in synthesizing BG-PC and EG-PC, which may be useful as NP drug delivery carriers. Future research could demonstrate the safety and effectiveness of long-term storage conditions for medical and pharmaceutical applications.•Nanophytosomes are tailored in size, shape and composition to optimize the delivery of phytochemicals/phytocompounds through nanoscale size and surface modification for better physiological absorption.•Nanophytosomes increase the stability of phytochemicals/phytocompounds and protect them from degradation due to heat or chemical reactions, leading to longer shelf life and improved therapeutic efficacy.•In this method, optimal conditions were created for the formation of β-1,3-glucan and Euglena gracilis extract nanophytosomes for successful development of drug delivery system that can effectively deliver bioactive compounds.

Porous polymer microspheres are employed in biotherapeutics, tissue engineering, and regenerative medicine. Porosity dictates cargo carriage and release that are aligned with the polymer physicochemical properties. These include material tuning, biodegradation, and cargo encapsulation. How uniformity of pore size affects therapeutic delivery remains an area of active investigation. Herein, we characterize six branched aliphatic hydrocarbon-based porogen(s) produced to create pores in single and multilayered microspheres. The porogens are composed of biocompatible polycaprolactone, poly(lactic-co-glycolic acid), and polylactic acid polymers within porous multilayered microspheres. These serve as controlled effective drug and vaccine delivery platforms.

Since its first use as a drug delivery system, mesoporous silica has proven to be a surprisingly efficient vehicle due to its porous structure. Unfortunately, most synthesis methods are based on using large amounts of surfactants, which are then removed by solvent extraction or heat treatment, leading to an undesired environmental impact because of the generated by-products. Hence, in the present study, we followed the synthesis of a silica material with a wormhole-like pore arrangement, using two FDA-approved substances as templates, namely Tween-20 and starch. As far as we know, it is the first study using the Tween-20/starch combo as a template for mesoporous silica synthesis. Furthermore, we investigated whether the obtained material using this novel synthesis had any potential in using it as a DDS. The material was further analyzed by XRD, TEM, FT-IR, N2 adsorption/desorption, and DLS to investigate its physicochemical features. Vancomycin was selected as the active molecule based on the extensive research engaged towards improving its bioavailability for oral delivery. The drug was loaded onto the material by using three different approaches, assuming its full retention in the final system. Thermal analysis confirmed the successful loading of vancomycin by all means, and pore volume significantly decreased upon loading, especially in the case of the vacuum-assisted method. All methods showed a slower release rate compared to the same amount of the pure drug. Loadings by physical mixing and solvent evaporation released the whole amount of the drug in 140 min, and the material loaded by the vacuum-assisted method released only 68.2% over the same period of time, leading us to conclude that vancomycin was adsorbed deeper inside the pores. The kinetic release of the three systems followed the Higuchi model for the samples loaded by physical mixing and vacuum-assisted procedures, while the solvent evaporation loading method was in compliance with the first-order model.

Amorphous solid dispersions (ASDs) are popular for enhancing the solubility and bioavailability of poorly water-soluble drugs. Various approaches have been employed to produce ASDs and novel techniques are emerging. This review provides an updated overview of manufacturing techniques for preparing ASDs. As physical stability is a critical quality attribute for ASD, the impact of formulation, equipment, and process variables, together with the downstream processing on physical stability of ASDs have been discussed. Selection strategies are proposed to identify suitable manufacturing methods, which may aid in the development of ASDs with satisfactory physical stability.

Thermal treatment conditions of solid polymer polymer electrolyte (SPE) were studied with respect to their impact on the surface morphology, phase composition and chemical composition of an imidazolium ionic-liquid-based SPE, namely PVDF/NMP/[EMIM][TFSI] electrolyte. These investigations were done using scanning electron microscopy, Raman spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry as well as X-ray photoelectron spectroscopy and time-of-flight secondary ion mass spectroscopy. A thoroughly mixed blend of polymer matrix, ionic liquid and solvent was deposited on a ceramic substrate and was kept at a certain temperature for a specific time in order to achieve varying crystallinity. The morphology of all the electrolytes consists of spherulites whose average diameter increases with solvent evaporation rate. Raman mapping shows that these spherulites have a semicrystalline structure and the area between them is an amorphous region. Analysis of FTIR spectra as well as Raman spectroscopy showed that the β-phase becomes dominant over other phases, while DSC technique indicated decrease of crystallinity as the solvent evaporation rate increases. XPS and ToF-SIMS indicated that the chemical composition of the surface of the SPE samples with the highest solvent evaporation rate approaches the composition of the ionic liquid.

The objective of this work was to investigate the effect of microfluidics on the quality attributes of metformin hydrochloride-loaded poly lactic-co-glycolic acid polymeric particles (MFH-PLGA PPs) when compared to a traditional double emulsion batch method. The relationship of encapsulation and loading efficiencies, yield %, particle size, surface morphology, and release profile with process and formulation variables were determined using design of experiments (DoE). The effects of the dispersal method of the primary (sonication vs. vortex) or secondary emulsion (microfluidics vs. batch), polyvinyl alcohol concentration (PVA), and drug to polymer ratio were investigated. The PPs\' size was impacted by both the PVA concentration and the type of primary and secondary emulsion dispersion methods. Microfluidics significantly increased the PPs\' yield %, particle size, encapsulation, and loading efficiencies. The higher loaded microfluidic-based PPs had more burst release, following first-order release kinetics when compared to the lower loaded batch-based particles, which followed the Korsmeyer-Peppas model for release kinetics. Microfluidic-based PPs exhibited a smooth, porous, more uniform, and larger particle size with hollow structure than the batch-based PPs with a matrix-like structure. In conclusion, we have elucidated the effect of microfluidics on the quality attributes of MFH-PLGA PPs and their comparison to the traditional batch technique.

The choice of carrier and drug ratio are critical factors as far as the type of solid dispersion is concerned. Amorphous solid dispersion has been cited as the most desirable type among the different types of solid dispersion due to the benefit of amorphicity in increasing the drug solubility of a poorly soluble drug. Recent reports delineated that a partially crystalline solid dispersion system may perform better due to the inherent issue of solution mediated recrystallisation of a completely amorphous system. In oppose to the conventional choice of using amorphous polymer, this study aimed to investigate the use of a crystalline carrier, polyethylene glycol (PEG) for dissolution enhancement of a model poorly soluble drug, Flurbiprofen (FBP), a BCS Class II candidate. Solid dispersions of different FBP to PEG 6000 molar ratios via solvent evaporation were prepared. Physical characterisation of preparations was performed using differential scanning calorimetry (DSC), attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and optical microscope. DSC and ATR-FTIR analyses suggest the obtained solid dispersion exhibits crystalline FBP. This is then supported by the optical microscope analysis as the birefringence of crystals was noted. Further increasing the drug-carrier molar ratio to one-to-three and one-to-six showed that there was an amorphous FBP constituent in the system. DSC analysis revealed the melting point depression of FBP by the carrier which signifies interaction between the drug and polymer. Dissolution study showed the solid dispersion of FBP improves the drug solubility and drug release compared to the pure drug. A higher carrier ratio in the formulation results in a higher drug release.