Search Results (459)

The study focuses on the development of an in situ gelling dexamethasone (DEX) oromucosal formulation designed for the treatment of aphthous stomatitis. Three series of formulations were prepared; a first series containing DEX suspended, a second series containing DEX and, in addition, mint essential oil (EO), and a third series containing EO and DEX solubilized in propylene glycol (PG). In the composition, polymers in the role of mucoadhesive agent were interchanged (hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), hydroxyethyl cellulose (HEC), methyl cellulose (MC), carboxymethyl cellulose (CMC), and sodium carboxymethyl cellulose (NaCMC). Specifically, DEX was incorporated at a concentration of 0.1% (w/w) in each formulation. The influence of mint EO and DEX solubilization on the physical properties (pH measurements, rheological analysis, swelling ability, and texture analysis) and in vitro drug release was studied. Key findings revealed that HPMC-based formulation containing mint EO and PG exhibited best swelling properties (700 ± 46% after 5 h), adequate adhesiveness and in vitro drug release (34.7 ± 5.9%). Furthermore, the irritation potential assessed via the hen’s egg test on the chorioallantoic membrane (HET-CAM) demonstrated low irritancy risk. Finally, Fourier-transform infrared spectroscopy (FT-IR) showed no incompatibility between DEX and excipients. Overall, the research highlights the potential of mucoadhesive systems in improving the therapeutic efficacy of oromucosal drug delivery for managing painful oral lesions. Full article

Background/Objectives: This study aimed to evaluate the safety and efficacy of chitosan-based bioadhesive films for facilitating the topical delivery of curcumin in skin cancer treatment, addressing the pharmacokinetic limitations associated with oral administration. Methods: The films, which incorporated curcumin, were formulated using varying proportions of chitosan, polyvinyl alcohol, Poloxamer^® 407, and propylene glycol. These films were assessed for stability, drug release, in vitro skin permeation, cell viability (with and without radiotherapy), and skin irritation. Results: The films demonstrated physical stability and preserved curcumin content at room temperature for 90 days. Drug release was effectively controlled during the first 8 h, with release rates ranging from 51.6 ± 4.8% to 65.6 ± 13.0%. The films also enhanced drug penetration into the skin compared to a curcumin solution used as a control (stratum corneum: 1.3 ± 0.1 to 1.9 ± 0.8 µg/cm²; deeper skin layers: 1.7 ± 0.1 to 2.7 ± 0.2 µg/cm²). A cytotoxicity test on metastatic melanoma cells showed that curcumin at topical doses exerted activity similar to that delivered via the skin. Furthermore, curcumin alone was more effective in inhibiting tumor cells than radiotherapy alone (p < 0.01), with no additional benefit observed when curcumin was combined with radiotherapy. Finally, irritation tests confirmed that the films were safe for topical application. Conclusion: The developed chitosan-based bioadhesive films represent a promising alternative for the topical treatment of skin tumors using curcumin. Full article

The objective of this study is to investigate the potential mutagenic effects of the exposure of mice to aerosols produced from the component liquids of an electronic nicotine delivery system (ENDS). The use of electronic cigarettes (e-cigs) and ENDSs has increased tremendously over the past two decades. From what we know to date, ENDSs contain much lower levels of known carcinogens than tobacco smoke. While conventional tobacco smoke is a well-established mutagen, little is known about the mutagenicity of ENDS aerosols. Here, we report the mutagenic effects of a 3-month whole body exposure of C57 lacI mice (BigBlue^TM) to filtered air (AIR) or ENDS aerosols in several tissues. Aerosols were generated from a 50/50 vegetable glycerin (VG)/propylene glycol (PG) mixture with and without nicotine. The results revealed that in the lung, bladder urothelial tissue, and tongue, mutagenesis was significantly greater in the VG/PG/nicotine group than in the AIR group. In all organs except the bladder, mutagenesis in the VG/PG only group was similar to those exposed to AIR. In the bladder, mutagenesis in the VG/PG group was elevated compared to that in the AIR group. In the liver, mutagenesis was modestly elevated in the VG/PG/nicotine group, but the elevation failed to reach statistical significance. Overall, there were no consistent differences in mutagenesis between the sexes. The results of this study suggest that exposure to e-cig aerosols containing nicotine represents a risk factor for carcinogenesis in several organ systems, and exposure to VG/PG alone may be a risk factor for bladder cancer. Full article

Background/Objectives: Nowadays, sustainability efforts focus on extracting natural cosmeceutical ingredients, such as polyphenols, from agri-food waste, for example, black bentonite (BB). The aims of this work were to validate an antioxidant cosmetic ingredient obtained from the waste BB and embed it into an ad hoc designed oromucosal spray intended for oral cavity wellness. Methods: Focusing on sustainability, the study tested PEG200, propylene glycol, and their mixtures as unconventional and green extraction solvents, aligned with a waste-to-market approach. The extracts obtained by maceration were characterized through HPLC-DAD and HPLC-MS analyses, DPPH, Bradford, and Folin–Ciocalteu assays. The best P extract was further subjected to OECD-compliant in vitro validation as novel cosmetic raw material and used to prepare a thermosensitive buccal spray for oral daily care. Results: PEG200 enabled the obtainment of a cost-effective polyphenol-rich extract, which was validated as a safe, high value-added cosmetic secondary raw material. The extract was incorporated into a liquid thermosensitive buccal formulation, able to gel once at body temperature and enhance polyphenol accumulation into the oral mucosae even with short contact times. Conclusions: BB is confirmed as a valuable source of polyphenols, and PEG200 represents an effective extraction solvent leading to a novel functional liquid excipient characterized by an OECD-compliant variegate pool of phenols. The buccal spray then proposed represents a valuable, friendly solution for daily oral care, as it is simple to use, as well as the in vitro and ex vivo tests carried out suggested its effectiveness. Full article

This study successfully developed edible films with excellent mechanical strength and notable water resistance, utilizing curdlan (CL) as the primary matrix and incorporating various plasticizers, including glycerol (GLY), ethylene glycol (EG), propylene glycol (PRO), xylitol (XY), sorbitol (SOR), and polyethylene glycol (PEG). A comprehensive suite of analytical techniques, including Fourier transform infrared spectroscopy (FTIR), wide-angle X-ray diffraction (XRD), scanning electron microscopy (SEM), dynamic mechanical analysis (DMA), and tensile testing, were employed to evaluate the films’ structural and mechanical properties. After incorporating PEG, the water sensitivity increased slightly, with a contact angle (CA) of 97.6°, and a water solubility (WS) of 18.75%. The inclusion of plasticizers altered the crystalline structure of the CL matrix, smoothing and flattening the film surface while reducing hydrogen-bonding interactions. These structural changes led to a more uniform distribution of amorphous chain segments and a decrease in glass transition temperatures. Among the tested plasticizers, GLY exhibited the highest compatibility with CL, resulting in the smoothest surface morphology and delivering the most effective plasticizing effect. The CL-GLY film showed a dramatic improvement in flexibility, with an elongation at break that was 5.2 times higher than that of the unplasticized film (increasing from 5.39% to 33.14%), indicating significant enhancement in extensibility. Overall, these findings highlight the potential of CL-GLY films as sustainable and effective materials for food packaging applications. Full article

Background: Hypertension affects 32% of adults worldwide, leading to a significant global consumption of cardiovascular medications. Atenolol, a β-adrenergic receptor blocker, is widely prescribed for cardiovascular diseases such as hypertension, angina pectoris, and myocardial infarction. According to the Biopharmaceutics Classification System (BCS), atenolol belongs to Class III, characterized by high solubility but low permeability. Currently, atenolol is commercially available in oral formulations. Increasing attention is being directed towards developing cost-effective transdermal delivery systems, due to their ease of use and better patient compliance. Eutectogels represent next-generation systems that are attracting great interest in the scientific community. Typically obtained from deep eutectic solvents (DESs) combined with gelling agents, these systems exhibit unique properties due to the intrinsic characteristics of DESs. Methods: In this study, a DES based on choline chloride as a hydrogen bond acceptor (HBA) and propylene glycol as a hydrogen bond donor (HBD) was explored to enhance the topical delivery of atenolol. The solubility of atenolol in the DES was evaluated using spectroscopic and thermodynamic measurements which confirmed the formation of hydrogen bonds between the drug and DES components. Additionally, the safety of the DES was assessed in a cell viability assay. Subsequently, we formulated eutectogels with different concentrations using animal gelatin and Tego Carbomer 140, and characterized these formulations through rheological measurements, swelling percentage, and permeation studies with Franz cells. Results: These novel eutectogels exhibit superior performance over conventional hydrogels, with a release rate of approximately 86% and 51% for Carbomer- and gelatin-based eutectogels, respectively. In contrast, comparable hydrogels released only about 27% and 35%. Conclusions: These findings underscore the promising potential of eutectogels for the transdermal delivery of atenolol. Full article

Background: Ketamine HCl, an FDA-approved therapeutic, is administered through various routes, including intranasal delivery. Administering an adequate therapeutic dose of intranasal ketamine HCl is challenging due to the limited volume that can be delivered intranasally given the current commercially available concentrations. Objectives: This study investigates solubilizing strategies to enhance the aqueous solubility of ketamine HCl for intranasal administration. Methods: We assessed the solubility profile of ketamine HCl by evaluating factors such as pH, co-solvents, and surfactants. Additionally, we developed and validated a UV-Vis spectroscopy method for ketamine HCl analysis. Results: Our solubility screening in various organic co-solvents revealed the following order of effectiveness in enhancing solubility: methanol > water > propylene glycol > ethanol > dimethyl sulfoxide (DMSO) > N-methyl-2-pyrrolidone (NMP). Despite methanol’s superior solubility, its potential toxicity, coupled with the relatively lower effectiveness of other solvents compared to water, suggests that a co-solvency approach is not advantageous for ketamine HCl. We found that ketamine HCl solubility increased with medium acidity, with pH 3.5 being the optimal for further formulation studies. The impact of pharmaceutical surfactants on ketamine HCl solubility at an acidic pH was also evaluated. Surfactants tested included SDS, PEG 400, PVP, Tween 20, poloxamer 188, and lecithin. Notably, PEG 400 and PVP reduced solubility due to a salting-out effect, whereas Tween 80, lecithin, and poloxamer 188 slightly improved solubility through micelle formation. Among the surfactants tested, 1% SDS emerged as the most effective in enhancing ketamine HCl solubility. Conclusions: These outcomes highlight the potential of these solubilization strategies to address the solubility limitations of ketamine HCl, enabling the preparation of highly concentrated ketamine HCl formulations for intranasal delivery. Full article

This study aimed to develop a supersaturated liquid formulation (SSLF) to enhance the solubility and dissolution of pazopanib hydrochloride (PZH). SSLFs were prepared by a simple stirring method in a heated silicon oil bath (70 °C). PZH showed highly pH-dependent solubility (pH 1.2 > water >> pH 4.0 and pH 6.8) at 37 °C. The SSLF containing glycerol and polyvinylpyrrolidone K30 (PVP K30) increased PZH dispersion solubility (273.66 ± 48.91 μg/mL) at pH 6.8 by more than 50-fold compared with that of glycerol alone (<5 μg/mL), and the PZH precipitate particle size was considerably small (<100 nm). Moreover, the dispersion solubility of PZH from SSLF containing additional propylene glycol (PG) increased to 364.41 ± 2.47 μg/mL. The optimized SSLF10 (PZH/glycerol/PG/PVP K30 = 10/50/20/20, w/w) exhibited a high dissolution rate at pH 4.0 (>90%) and 6.8 (>55%) until 360 min, whereas PZH powder and PZH glycerol solution showed pH-dependent, low dissolution rates (<10%) under similar conditions. The supersaturation ratio of SSLF10 was very high at 29.88 and 18.36 at pH 6.8 and 4.0, respectively, indicating a stable PZH supersaturation solution. In the transmission electron microscopy analysis, PVP K30 and PG in SSLF10 synergistically suppressed PZH precipitation and recrystallization with small amorphous particles (<200 nm). Therefore, SSLF10 would be a promising formulation with enhanced solubility and dissolution rates regardless of medium pH. Full article

Thermoresponsive self-nanoemulsifying drug delivery systems (T-SNEDDS) offer a promising solution to the limitations of conventional SNEDDS formulations. Liquid SNEDDS are expected to enhance drug solubility; however, they are susceptible to leakage during storage. Even though solid SNEDDS offers a solution to this storage instability, they introduce new challenges, namely increased total dosage and potential for drug trapping within the formulation. The invented T-SNEDDS was used to overcome these limitations and improve the dissolution of glibenclamide (GBC). Solubility and transmittance studies were performed to select a suitable oil and surfactant. Design of Experiments (DoE) software was used to study the impact of propylene glycol and Poloxamer 188 concentrations on measured responses (liquefying temperature, liquefying time, and GBC solubility). The optimized formulation was subjected to an in vitro dissolution study. The optimized T-SNEDDS consisted of Kolliphor EL and Imwitor 308 as surfactants and oil. The optimized propylene glycol and Poloxamer 188 concentrations were 13.7 and 7.9% w/w, respectively. It exhibited a liquefying temperature of 35.0 °C, a liquefying time of 119 s, and a GBC solubility of 5.51 mg/g. In vitro dissolution study showed that optimized T-SNEDDS exhibited 98.8% dissolution efficiency compared with 2.5% for raw drugs. This study presents a promising approach to enhance pharmaceutical applicability by resolving the limitations of traditional SNEDDS. Full article

Enhancing the thermal conductivity of fluids by using nanoparticles with outstanding thermophysical properties has acquired significant attention for heat-transfer applications. Nanofluids have the potential to optimize energy systems by improving heat-transfer efficiency. In this study, cobalt ferrite nanoparticles clusters with controlled mean sizes ranging from 97 to 192 nm were synthesized using a solvothermal method to develop novel nanofluids with enhanced thermal conductivity. These clusters were comprehensively characterized using transmission electron microscopy, X-ray diffraction, Raman spectroscopy, vibrating-sample magnetometry, and nitrogen physisorption. The CoFe₂O₄ cluster nanofluids were prepared using the two-step method with various base fluids (water, propylene glycol, and a mixture of both). Dynamic light scattering analyses of the average Z-size of the dispersed nanoadditives over time revealed that the stability of the dispersions is influenced by cluster size and the proportion of glycol in the base fluid. The thermal conductivity of the base fluid and nine different 0.5 wt% CoFe₂O₄ cluster nanofluids was measured using the transient hot wire method at temperatures of 293.15, 303.15, and 313.15 K, showing different temperature dependencies. The study also explores the relationships between the thermal conductivity, cluster size, and specific surface area of the nanoadditives. A maximum thermal conductivity enhancement of 4.2% was reported for the 0.5 wt% nanofluid based on propylene glycol containing 97 nm CoFe₂O₄ clusters. The findings suggest that the specific surface area of nanostructures is a more relevant parameter than size for describing improvements in thermal conductivity. Full article

Objectives: Hydrogels produced using the freeze–thaw method have demonstrated significant potential for wound management applications. However, their production requires precise control over critical factors including freezing temperature and the choice of matrix-forming excipients, for which no consensus on the optimal conditions currently exists. This study aimed to address this gap by evaluating the effects of the above-mentioned variables on cryogel performance. Methods: Mechanical properties, absorption capacity, and microstructure were assessed alongside advanced analyses using differential scanning calorimetry (DSC) and low-field nuclear magnetic resonance relaxometry (LF TD NMR). Results: The results demonstrated that fully hydrolyzed polyvinyl alcohol (PVA) with a molecular weight above 61,000 g/mol is essential for producing high-performance cryogels. Among the tested formulations, an 8% (w/w) PVA_56–98 solution (Mw~195,000; DH = 98.0–98.8%) with 10% (w/w) propylene glycol (PG) provided the best balance of stretchability, durability, and low adhesion. Notably, while −25 °C is often used for cryogel preparation, freezing the gel precursor at −80 °C yielded superior results, producing materials with more open, interconnected structures and enhanced mechanical strength and elasticity—deviating from conventional practices. Conclusions: The designed cryogel prototypes exhibited functional properties comparable to or even surpassing commercial wound dressings, except for absorption capacity, which remained lower. Despite this, the cryogel prototypes demonstrated potential as wound dressings, particularly for use in dry or minimally exuding wounds. All in all, this study provides a comprehensive analysis of the physicochemical and functional properties of PVA cryogels, establishing a strong foundation for the development of advanced wound dressing systems. Full article

The permeation of cryoprotectants into insect embryos is critical for successful cryopreservation. However, the permeability of silkworm embryos to cryoprotectants and the effects of cryopreservation remain poorly studied. In this study, we evaluated the permeability and toxicity of four cryoprotective agents (CPAs) as well as the vitrification effect on the viability of silkworm embryos. Among the four CPAs, propylene glycol (PG) showed the best permeability. Ethylene glycol (EG) and PG were the least toxic CPAs, but glycerol (GLY) and dimethyl sulfoxide (DMSO) were more toxic. Moreover, we examined several factors including the kind and the concentration of CPAs, exposure time, embryonic stage, and silkworm strains. Embryos at the earlier phases of stage 25 were more tolerant to vitrification using EG. We found that over 21% of embryos treated with EG at the early 2 phase of stage 25: 163 h after egg laying (AEL) developed and progressed to serosa ingestion after vitrification and rewarming. The result was the same in other strains as well. Our results are valuable for the development of new cryopreservation protocols of silkworm embryos. Full article

The extractive distillation process using propylene glycol (IUPAC name: 1,2 propanediol) as an extractive agent for the separation of the isopropanol–water system was investigated in this work. A systematic procedure was set out to obtain the optimal design and process conditions for extractive distillation and solvent recovery columns using the PRO/II process simulator. Four thermally integrated flowsheets were proposed, implying the recovery of the sensible heat and latent heat from the hot streams in the process. To establish the economic feasibility of the proposed process, we calculated the total annual cost for all the simulated versions, and the proposed fully thermally integrated flowsheets could save up to 43.13% in terms of the utility costs and up to 15.57% in terms of the TAC compared to the conventional design. Thus, propylene glycol (PG) is found to be suitable as a new solvent for isopropanol dehydration, being comparable with other classical solvents used for the dehydration of alcohols. Full article

Background/Objectives: Wound healing relies on a coordinated process with the participation of different mediators. Natural products are a source of active compounds with healing potential. Isoorientin is a natural flavone recognized as having several pharmacological properties, such as anti-inflammatory effects, making it a potential treatment for wounds. We investigated the effect of isoorientin on the healing of excisional skin wounds. Methods: Male Swiss mice were subjected to the induction of excisional skin wounds (6 mm diameter) and treated with a vehicle (2% dimethyl sulfoxide in propylene glycol) or 2.5% isoorientin applied topically once a day for 14 days. The wound area was measured on days 0, 3, 7, and 14. Histopathological analyses were performed on the cicatricial tissue after 14 days. The myeloperoxidase activity and the interleukin-1β, tumoral necrosis factor (TNF)-α, and interleukin-6 concentrations were determined on the third day. Results: We observed that 3 days after the topical application of isoorientin, the lesion area was significantly smaller when compared to those of the vehicle (p < 0.01) and control (p < 0.05) groups. No difference was observed after 7 and 14 days of induction. Despite this, on day 14, histological analysis of cicatricial tissue from the animals treated with isoorientin showed reduced epidermal thickness (p < 0.001) and increased collagen deposition (p < 0.001). These effects were accompanied by decreased myeloperoxidase activity and interleukin-1β concentration on the third day of induction, without alteration in TNF-α and interleukin-6. Conclusions: The treatment with isoorientin promoted better tissue repair in excisional wounds in mice, which may be linked to the modulation of the early inflammatory response. Full article

Background: Effective wound dressing is the key solution to combating the increased death rate and prolonged hospital stay common to patients with wounds. Methods: Sodium alginate-based single- and double-layer membranes incorporated with Capparis sepiaria root extract were designed using the solvent-casting method from a combination of polyvinyl alcohol (PVA), Pluronic F127 (PF127), and gum acacia. Results: The successful preparation of the membranes and loading of the extract were confirmed using Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD). The prepared membranes were biodegradable and non-toxic to human skin cells (HaCaT), with high biocompatibility of 92 to 112% cell viability and good hemocompatibility with absorbance ranging from 0.17 to 0.30. The membrane’s highest water vapor transmission rate was 1654.7333 ± 0.736 g/m²/day and the highest % porosity was 76%. The membranes supported cellular adhesion and migration, with the highest closure being 68% after 4 days compared with the commercial wound dressings. This membrane exhibited enhanced antimicrobial activity against the pathogens responsible for wound infections. Conclusions: The distinct features of the membranes make them promising wound dressings for treating infected wounds. Full article