Search Results (1,141)

Vanillin is the compound of great interest to the industry. It is used to augment and enhance the aroma and taste of food preparations and also as a fragrance compound in perfumes and detergents. Currently, majority of the world’s supply consists of chemically synthesized or lignin-derived vanillin. The application of biocatalysis for sustainable manufacturing of food ingredients, pharmaceutical intermediates, and fine chemicals is the key concept of modern industrial biotechnology. The main goal of this research was to conduct optimization procedures aimed at intensifying the microbial hydrolysis process of the lignin-rich plant raw materials and further bioconversion of the released ferulic acid to vanillin. The tests were performed in the solid-state fermentation system with strains selected during the screening stage on agri-food by-products such as brewer’s spent grain. A specially designed single-use bag bioreactor was used to carry out the process on a preparative scale with the most effective strain. The experiment was designed using the RSM, which allowed for an increase in biosynthesis efficiency from 363 mg/kg to 1413 mg/kg (an increase of 389%). The progress of the process was controlled by the use of chromatographic techniques (HPLC) by quantitative determination of vanillin content in the obtained extracts. Full article

Background/Objectives: Smart Formulation is an artificial intelligence-based platform designed to predict the Beyond Use Dates (BUDs) of compounded oral solid dosage forms. The study aims to develop a decision-support tool for pharmacists by integrating molecular, formulation, and environmental parameters to assist in optimizing the stability of extemporaneous preparations. Methods: A tree ensemble regression model was trained using a curated dataset of 55 experimental BUD values collected from the Stabilis database. Each formulation was encoded with molecular descriptors, excipient composition, packaging type, and storage conditions. The model was implemented using the KNIME platform, allowing the integration of cheminformatics and machine learning workflows. After training, the model was used to predict BUDs for 3166 APIs under various formulation and storage scenarios. Results: The analysis revealed a significant impact of excipient type, number, and environmental conditions on API stability. APIs with lower LogP values generally exhibited greater stability, particularly when formulated with a single excipient. Excipients such as cellulose, silica, sucrose, and mannitol were associated with improved stability, whereas HPMC and lactose contributed to faster degradation. The use of two excipients instead of one frequently resulted in reduced BUDs, possibly due to moisture redistribution or phase separation effects. Conclusions: Smart Formulation represents a valuable contribution to computational pharmaceutics, bridging theoretical formulation design with practical compounding needs. The platform offers a scalable, cost-effective alternative to traditional stability testing and is already available for use by healthcare professionals. Its implementation in hospital and community pharmacies may help mitigate drug shortages, support formulation standardization, and improve patient care. Future developments will focus on real-time stability monitoring and adaptive learning for enhanced precision. Full article

The concerning increase in respiratory infections that are resistant to multiple drugs has led to a growing interest in bacteriophage therapy as a potential alternative to conventional antibiotics. Effective phage delivery to the lungs, however, presents several formulation and stability issues, particularly for inhalation-based methods. This review highlights current developments in the creation of dry powder formulations that can be inhaled for pulmonary phage therapy, with a focus on encapsulation methods based on nanoparticles, such as solid lipid nanoparticles (SLNs) and polymer-based nanoparticles. These carriers enhance the aerodynamic characteristics of phages, making them suitable for deep lung deposition, while also protecting them during processing and storage. Several drying methods have been investigated to create powders with optimal morphologies, porosity, and dispersibility, including spray drying and spray freeze drying. The review also emphasizes how the phage morphotype affects stability, especially when nebulization stress is present. Furthermore, the advantages of nanoparticle matrices are confirmed by the reduced viability loss (usually< 0.5 log PFU) of encapsulated phages. Standardizing production processes, scaling up, and ensuring regulatory compliance remain challenging despite encouraging preclinical results. The combination of phage therapy with nanotechnology creates new avenues for the utilization of inhalable delivery methods to treat multidrug-resistant pulmonary infections. To translate these novel formulations from preclinical development to clinical application, sustained multidisciplinary collaboration across pharmaceutical sciences, microbiology, and clinical pharmacology is essential. Full article

Background: Crataegus almaatensis, an endemic hawthorn species from Kazakhstan, is known for its rich content of phenolic compounds and flavonoids with significant pharmacological potential. This study aimed to optimize and compare conventional solid–liquid extraction (SLE) and ultrasound-assisted extraction (UAE) processes for maximizing the extractability of bioactive compounds from hawthorn leaves powder. Methods: The effects of temperature, extraction time, ethanol concentration, and solid-to-liquid ratio (or ultrasound power in the case of UAE) on total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity (FRAP, DPPH, and ABTS assays) were systematically evaluated. Results: The UAE method yielded higher concentrations of TPC and TFC, with up to 16% improvement in TPC and reduced ethanol usage (40% (v/v)) compared to SLE (75% (v/v)), demonstrating its efficiency and sustainability. Optimal extraction conditions were identified as 70 °C, 75% ethanol, 34 min, and an S/L ratio of 0.05 g/mL for SLE, 70 °C, 40% ethanol, 44 min, and 100 W US power for UAE. High-resolution HPLC-DAD and LC-Q/TOF-MS analyses confirmed the presence of key phenolic acids and flavonoid glycosides, including chlorogenic acid and apigenin-8-C-glucoside-2′-rhamnoside as the most abundant compounds identified. Conclusions: These findings validate UAE as an innovative, eco-friendly method for extracting bioactive compounds from hawthorn leaves and highlight its potential for developing natural antioxidants for pharmaceutical and nutraceutical applications. Full article

Cost-effective procedures usually cannot achieve complete removal of priority contaminants present in water at very low concentrations (as pesticides or pharmaceuticals). Advanced oxidation processes (AOPs) represent promising technologies for removing priority contaminants from water at trace concentrations, yet practical implementation remains limited due to technical and economic constraints. This study presents an innovative flow-through photodegradation device designed to overcome current limitations while achieving efficient contaminant removal at industrial scale. The device integrates a UVC 254 nm lamp-equipped flow chamber with automated dosing pumps for hydrogen peroxide and/or solid catalyst suspensions, coupled with a 30 nm porous membrane filtration system for catalyst recirculation. This configuration optimizes light–catalyst–pollutant contact while enabling combined catalytic processes. Performance evaluation using acesulfame (ACE) and iohexol (IHX) as model contaminants demonstrated rapid and effective removal. IHX degradation with UVC and 75 μM H₂O₂ achieved complete removal with t₉₅% = 7.23 ± 1.21 min (pseudo-order 0.25, t₁/₂ = 3.27 ± 0.39 min), while ACE photolysis (with UVC only) required t₉₅% = 14.88 ± 2.02 min (pseudo-order 1.27, t₁/₂ = 2.35 ± 0.84 min). The introduction of t₉₅% as a performance metric provides practical insights for near-complete contaminant removal requirements. Real-world efficacy was confirmed using tertiary wastewater treatment plant effluents containing 14 μg/L IHX, achieving complete removal within 8 min. However, carbamazepine degradation proved slower (t₉₅% > 74 h), highlighting the need for combined catalytic approaches for recalcitrant compounds. Spiking experiments (1000 μg/L) revealed concentration-dependent kinetics and synergistic effects between co-present contaminants. Analysis identified degradation byproducts consistent with previous studies, including tri-deiodinated iohexol (474.17 Da) intermediates. This scalable system, constructed from commercially available components, demonstrates potential for cost-effective industrial implementation. The modular design allows adaptation to various contaminants through adjustable AOP combinations (UV/H₂O₂, photocatalysts, ozone), representing a practical advancement toward addressing the gap between laboratory-scale photocatalytic research and full-scale water treatment applications. Full article

Curcumin is a natural active ingredient with various health benefits but suffers from poor water solubility, chemical instability, and rapid metabolism. This study developed a novel composite gel, blueberry leaf polysaccharide–xanthan gum (BLP-XG), for the protection and delivery of curcumin. The experimental results demonstrate that the formation of stable composite gel networks is predominantly facilitated by hydrogen bonding and electrostatic interactions between BLP and XG components. In comparison with single-component systems, composite gels exhibit superior structural homogeneity and density, as well as higher thermal stability, viscoelasticity, and predominantly elastic solid behavior. The BLP-XG composite gel achieved the highest curcumin encapsulation rate of 84.23% when the BLP concentration was 2.0%. The composite gel system effectively retained curcumin in the gastric juice and released it in the small intestine. Furthermore, the presence of BLP in the composite gel inhibited curcumin degradation under UV irradiation. This study establishes the research foundation for the development of efficient and stable delivery systems to protect and deliver curcumin and extends the use of blueberry leaf polysaccharides in food and pharmaceutical applications. Full article

The consumption of pharmaceuticals during the COVID-19 pandemic increased significantly. As such, over-the-counter drugs such as acetaminophen (ACT), ibuprofen (IBU), metoprolol (MET), and propranolol (PRO) were among the pharmaceuticals that were widely used to contain COVID-19 symptoms. Therefore, this study investigated the occurrence of ACT, IBU, MET, and PRO in wastewater and river water systems, focusing on two provinces in South Africa (Gauteng (GP) and KwaZulu-Natal (KZN)). Generally, WWTP influents had the highest concentrations in both provinces. ACT, MET, and PRO were frequently detected compared to ibuprofen, particularly in KZN, during the second wave of the COVID-19 pandemic. However, a low detection occurred during the fourth wave of the COVID-19 pandemic. The concentrations of ACT, IBU, MET, and PRO in influent wastewater samples ranged from ND-480 µg/L, ND-54.1 µg/L, ND-52.8 µg/L, to ND-13.1 µg/L, respectively. In comparison with influent samples, ACT, IBU, MET, and PRO concentrations of effluent wastewater samples were generally at lower concentration levels: ACT (ND-289 µg/L), IBU (ND-36.1 µg/L), MET (ND-13.9 µg/L), and PRO (ND-5.53 µg/L). The removal efficiencies of the selected pharmaceuticals in KZN WWTPs ranged from 6.1 to 100% and −362.6 to 100% in the GP province. The ecological risk assessment results showed a low to high ecological risk against fish, Daphnia magna, and algae due to the presence of these pharmaceuticals. Full article

This study presents a comprehensive valorization of Juniperus communis L., a plant known for its culinary and therapeutic applications. Juniper berries are rich in antioxidant compounds such as polyphenols and ascorbic acid, while their kernels contain volatile terpenes with notable pharmaceutical properties. We optimized extraction parameters through stirring extraction (1:20 g/mL solid-to-solvent ratio, 55% v/v aqueous ethanol, 80 °C, 30 min) and response surface methodology via a Box–Behnken design. The optimal conditions—55% v/v aqueous ethanol at 80 °C for 30 min—yielded a high polyphenol content of 55.11 ± 1.54 mg GAE/g of defatted dry weight. Antioxidant capacity was confirmed through ferric-reducing and radical-scavenging assays, and 11 individual polyphenols (totaling 5.41 ± 0.27 mg/g) were quantified using a validated HPLC-DAD method. Additionally, this study identified several bioactive compounds in juniper berry raw kernel oil, which exhibited a high oleic acid content (58.75 ± 2.76%)—a nutritionally valuable fatty acid contributing to the oil’s strong radical-scavenging activity (399.83 ± 34.18 µmol Trolox equivalents/kg oil). GC–MS analysis revealed 58 volatile compounds, underscoring the terpene-rich profile of the oil and its influence on antioxidant potential and aroma. These findings underscore the dual valorization of juniper berry fruit and kernel for both medicinal and food industries. The aromatic kernel oil and polyphenol-rich extracts offer natural alternatives to synthetic antioxidants, with added benefits of flavor enhancement and promotion of health. Full article

Objectives: Transforming poorly soluble crystalline drugs into their amorphous form is a well-established strategy in pharmaceutical science to enhance their solubility and improve their clinical efficacy. However, developing amorphous forms of organic drugs for pharmaceutical applications presents significant technical hurdles due to the lack of suitable analytical tools for the amorphization process. Carbamazepine is a crystalline BCS class II drug commonly used for epilepsy and trigeminal neuralgia, whose clinical efficacy is compromised by its low solubility and slow dissolution. Therefore, this study focuses on investigating the amorphization of carbamazepine to enhance its solubility by using a micro-droplet precipitation system. Methods: These micro-droplets serve as individual reactors, enabling homogeneous nucleation for precipitation of carbamazepine. During crystallization, carbamazepine undergoes an intermediate liquid–liquid phase transition characteristic of two-step nucleation. By varying the solvent’s composition (methanol/water), we characterized the kinetics and stability of the intermediate liquid phase under various conditions. Results: Our results indicate that carbamazepine can undergo either a one-step liquid-to-amorphous-solid phase transition or a two-step liquid-to-crystalline-solid phase transition. Notably, both transitions pass through a liquid-to-dense-liquid phase separation process starting from the supersaturated solution, where the generated intermediate phases exhibit different sizes and numbers that are influenced by the solvent and its concentration. Conclusions: Our findings not only elucidate the mechanism underlying the carbamazepine phase transition but also propose a novel method for studying the amorphous process, which could be broadly applicable to other poorly soluble pharmaceutical compounds and may be helpful to amorphous formulations production, potentially offering significant improvements in drug efficacy and patient compliance. Full article

Cutibacterium acnes is linked to the prevalent inflammatory skin disorder known as Acne Vulgaris (AV). Some topical agents exhibit unfavorable side effects like dryness and skin inflammation, and antimicrobial resistance (AMR) poses an increasing risk to effective AV management. This study develops and characterizes stable topical essential oil (EO)-loaded microemulgels with in vitro validated antimicrobial activities against C. acnes ATCC 6919, providing a solid scientific basis for their effectiveness. These microemulgels, with their potential to serve as an alternative to AMR-prone synthetic agents, could revolutionize the field of acne treatment. The MICs of the EOs (citronella, tea tree, and lemongrass) against C. acnes were determined. EO-loaded microemulgels were developed using a blend of microemulsion and carbopol/hyaluronic acid gel in a ratio of 1:1 and characterized, and their stability was observed over three months. The MICs of citronella, tea tree, and lemongrass EOs were 0.08, 0.16, and 0.62% v/v, respectively. The microemulgels were whitish and smooth, with characteristic EO odors. They demonstrated pH values ranging between 4.81 ± 0.20 and 5.00 ± 0.03, good homogeneity, a spreadability of 9.79 ± 0.6 and 12.76 ± 0.8 cm², a viscosity of 29,500 and 31,130 cP, and retained stability at 4, 25, and 40 °C. EO-loaded microemulgels were developed with the potential of C. acnes management. The formulation shows adequate potential for further pharmaceutical development towards translational adoption in acne management. Full article

Concern over the presence of pharmaceutical waste in the environment has prompted research into the management of emerging organic micropollutants (EOMs). In response, sustainable technologies have been applied as alternatives to reduce the effects of these contaminants. This study investigated the capacity of filamentous fungi isolated from iron mine soil in the Amazon region to biodegrade the drug chloroquine diphosphate. An initial screening assessed the growth of four fungal strains on solid media containing chloroquine diphosphate: Trichoderma pseudoasperelloides CBMAI 2752, Penicillium rolfsii CBMAI 2753, Talaromyces verruculosus CBMAI 2754, and Penicillium sp. cf. guaibinense CBMAI 2758. Among them, Penicillium sp. cf. guaibinense CBMAI 2758 was selected for further testing in liquid media. A Box–Behnken factorial design was applied with three variables, pH (5, 7, and 9), incubation time (5, 10, and 15 days), and chloroquine diphosphate concentration (50, 75, and 100 mg·L⁻¹), totaling 15 experiments. The samples were analyzed by gas chromatography–mass spectrometry (GC-MS). The most effective conditions for chloroquine biodegradation were pH 7, 100 mg·L⁻¹ concentration, and 10 days of incubation. Four metabolites were identified: one resulting from N-deethylation M1 (N4-(7-chloroquinolin-4-yl)-N1-ethylpentane-1,4-diamine), two from carbon–carbon bond cleavage M2 (7-chloro-N-ethylquinolin-4-amine) and M3 (N1,N1-diethylpentane-1,4-diamine), and one from aromatic deamination M4 (N1-ethylbutane-1,4-diamine) by enzymatic reactions. The toxicity analysis showed that the products obtained from the biodegradation of chloroquine were less toxic than the commercial formulation of this compound. These findings highlight the biotechnological potential of Amazonian fungi for drug biodegradation and decontamination. Full article

Background: Precision medicine refers to the formulation of personalized drug regimens according to the individual characteristics of patients to achieve optimal efficacy and minimize adverse reactions. Additive manufacturing (AM), also known as three-dimensional (3D) printing, has emerged as an optimal solution for precision drug delivery, enabling customizable and the fabrication of multifunctional structures with precise control over morphology and release behavior in pharmaceutics. However, the influence of 3D printing parameters on the printed tablets, especially regarding in vitro and in vivo performance, remains poorly understood, limiting the optimization of manufacturing processes for controlled-release profiles. Objective: To establish the fabrication process of 3D-printed controlled-release tablets via comprehensively understanding the printing parameters using fused deposition modeling (FDM) combined with hot-melt extrusion (HME) technologies. HPMC-AS/HPC-EF was used as the drug delivery matrix and carbamazepine (CBZ) was used as a model drug to investigate the in vitro drug delivery performance of the printed tablets. Methodology: Thermogravimetric analysis (TGA) was employed to assess the thermal compatibility of CBZ with HPMC-AS/HPC-EF excipients up to 230 °C, surpassing typical processing temperatures (160–200 °C). The formation of stable amorphous solid dispersions (ASDs) was validated using differential scanning calorimetry (DSC), hot-stage polarized light microscopy (PLM), and powder X-ray diffraction (PXRD). A 15-group full factorial design was then used to evaluate the effects of the fan speed (20–100%), platform temperature (40–80 °C), and printing speed (20–100 mm/s) on the tablet properties. Response surface modeling (RSM) with inverse square-root transformation was applied to analyze the dissolution kinetics, specifically t_50% (time for 50% drug release) and Q_4h (drug released at 4 h). Results: TGA confirmed the thermal compatibility of CBZ with HPMC-AS/HPC-EF, enabling stable ASD formation validated by DSC, PLM, and PXRD. The full factorial design revealed that printing speed was the dominant parameter governing dissolution behavior, with high speeds accelerating release and low speeds prolonging release through porosity-modulated diffusion control. RSM quadratic models showed optimal fits for t_50% (R² = 0.9936) and Q_4h (R² = 0.9019), highlighting the predictability of release kinetics via process parameter tuning. This work demonstrates the adaptability of polymer composite AM for tailoring drug release profiles, balancing mechanical integrity, release kinetics, and manufacturing scalability to advance multifunctional 3D-printed drug delivery devices in pharmaceutics. Full article

In the preceding and early stages of cancer progression, local drug delivery to pre-cancerous and cancerous skin lesions may be applied as an alternative or supplementary therapy. At present, 5-Fluorouracil, imiquimod, and tirbanibulin creams and ointments have established their place in practice, while several other active pharmaceutical ingredients (APIs) (e.g., calcipotriol, tretinoin, diclofenac) have been repurposed, used off-label, or are currently being investigated in mono- or combined chemotherapies of skin cancers. Apart from them, dozens to hundreds of therapeutics of natural and synthetic origin are proven to possess anti-tumor activity against melanoma, squamous cell carcinoma (SCC), and other skin cancer types in in vitro studies. Their clinical introduction is most often limited by low skin permeability, challenged targeted drug delivery, insufficient chemical stability, non-selective cytotoxicity, or insufficient safety data. A variety of prodrug and nanotechnological approaches, including vesicular systems, micro- and nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanoparticles, and others, offer versatile solutions for overcoming the biophysical barrier function of the skin and the undesirable physicochemical nature of some drug molecules. This review aims to present the most significant aspects and latest achievements on the subject. Full article

The article presents the first method based on high-performance liquid chromatography and ultraviolet detection (HPLC-UV) for the determination of timonacic (thioproline, 1,3-thiazolidine-4-carboxylic acid, tPro) in pharmaceutical tablets and face care products (creams, sera, foundations, suncreams). Sample preparation primarily involves solid-liquid extraction (SLE) of tPro with 0.2 mol/L phosphate buffer pH 6, derivatization with 0.25 mol/L 2-chloro-1-methylquinolinium tetrafluoroborate (CMQT), followed by polytetrafluoroethylene (PTFE) membrane filtration. The chromatographic separation of the stable UV-absorbing 2-S-quinolinium derivative is achieved within 14 min at 25 °C on a Zorbax SB-C18 (150 × 4.6 mm, 5 µm) column using gradient elution. The eluent consists of 0.1 mol/L trichloroacetic acid (TCA), pH 1.7, in a mixture with acetonitrile (ACN) delivered at a flow rate of 1 mL/min. The analyte is quantified by monitoring at 348 nm. The assay linearity was observed within 0.5–125 μmol/L. The limit of quantification (LOQ) was found to be 0.5 μmol/L. The accuracy ranged from 93.22% to 104.31% and 97.38% to 103.48%, while precision varied from 0.30% to 11.23% and 1.13% to 9.64% for intra- and inter-assay measurements, respectively. The method was successfully applied to commercially available on the Polish market pharmaceutical and cosmetic products. Full article

Poor aqueous solubility still disqualifies many promising drug candidates at late stages of development. Amorphous solid dispersion (ASD) technology solves this limitation by trapping the active pharmaceutical ingredient (API) in a high-energy, non-crystalline form, yet most marketed ASDs rely on synthetic carriers such as polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC), which raise concerns about long-term biocompatibility, residual solvent load, and sustainability. This study summarizes the emergence of natural polymer-based ASDs (NP-ASDs), along with the bond mechanism reactions through which these natural polymers enhance drug performance. As a result, NP-ASDs exhibit improved physical stability and significantly enhance the dissolution rate of poorly soluble drugs. The structural features of natural polymers play a critical role in stabilizing the amorphous state and modulating drug release profiles. These findings support the growing potential of NP-ASDs as sustainable and biocompatible alternatives to synthetic carriers in pharmaceutical development. Full article