Search

Lycopene is a carotenoid with high antioxidant activity. Numerous studies show its positive effects in the prevention and amelioration of many diseases. However, due to its lack of water solubility, its use is very limited. Developing a formulation with lycopene with favorable therapeutic parameters will allow for a more effective use of this ingredient. The aim of this study was therefore to use supercritical phase extraction to obtain lycopene-containing preparations, and to obtain complexes of the extract with cyclodextrins to improve its solubility and increase its antioxidant potential. Lycopene-containing extracts were obtained by ultrasound-assisted acetone extraction and supercritical phase extraction. The supercritical extract was combined with g-cyclodextrin, b-cyclodextrin and 2-hydroxypropyl-b-cyclodextrin. Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) and X-ray diffraction (XRD) analyses were performed for the obtained systems and extracts. A paddle apparatus was used to evaluate the in vitro dissolution, and the samples collected were analysed by HPLC. The antioxidant activity was assessed using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical method. The results show that cyclodextrins increase the dissolution of lycopene into an acidic environment and enhance the antioxidant potential of the compound. We conclude that the development of a formulation containing a combination of lycopene obtained by supercritical extraction and cyclodextrin will allow for a wider and more effective use of this ingredient.

Curcumin, a compound known for its antioxidant and neuroprotective properties, faces challenges due to its low water solubility, which can limit its effectiveness. One effective method to address this issue is through amorphization. Incorporating curcumin into a polymeric matrix to form amorphous solid dispersions is a common approach. Another strategy involves co-amorphous systems, where low-molecular-weight components act as co-formers. A recent innovative approach combines these strategies. This study used tryptophan as a co-former and prepared systems using supercritical fluid technology. The amorphous nature of two systems was confirmed through X-ray powder diffraction: one with 10% curcumin and a polymer, and another with 10% curcumin, a polymer, and tryptophan. Fourier-transform infrared analysis demonstrated molecular interactions among all components in the systems. Scanning electron microscopy revealed that the amorphization process significantly modified the morphology of the powder particles. The ternary system with tryptophan notably increased curcumin solubility by over 300-fold. The amorphous form of curcumin in both systems exhibited significantly higher dissolution rates compared to its crystalline form. The system with tryptophan showed more than a threefold improvement in permeability according to the PAMPA test. The enhanced solubility led to over a sixfold increase in antioxidant activity and a 25-fold improvement in the inhibition of the enzyme butyrylcholinesterase. [ABSTRACT FROM AUTHOR]

Apigenin (APG), a bioactive flavonoid with promising therapeutic potential, suffers from poor water solubility, which limits its bioavailability. To address this, solid dispersions of APG were prepared using ball milling with sodium alginate (SA), Pluronic® F-68 (PLU68), Pluronic® F-127 (PLU127), PVP K30, and PVP VA64 as polymeric excipients. These dispersions were screened for apparent solubility in water and buffers with pH 1.2, 5.5, and 6.8. Based on improved solubility after 60 min, APG–PLU68 and APG–PLU127 dispersions were selected for further study. DSC and FT-IR analysis confirmed molecular interactions between APG and the polymer matrices, contributing to enhanced solubility and dissolution rates. Dissolution rate studies showed that APG–PLU127 achieved 100% solubility at pH 6.8, suggesting its potential use in environments such as the small intestine. Additionally, APG–PLU127 exhibited 84.3% solubility at pH 1.2, indicating potential for solid oral dosage forms, where APG could be absorbed in the acidic conditions of the stomach. The stability study confirmed that storage for one year under ambient conditions does not cause chemical degradation but affects the physical state and solubility of the dispersion. Antioxidant activity was assessed using the ABTS assay. Freshly obtained APG–PLU127 showed 68.1% ± 1.94% activity, whereas APG–PLU127 stored for one year under ambient conditions exhibited 66.2% ± 1.62% (significant difference, p < 0.05). The difference was related to a slight decrease in the solubility of APG in the solid dispersion (T0 = 252 ± 1 μg∙mL−1, T1 = 246 ± 1 μg∙mL−1). The findings demonstrate the superior performance of PLU127 as a carrier for enhancing the solubility, release, and antioxidant activity of APG. [ABSTRACT FROM AUTHOR]

Evernia prunastri is a lichen widely distributed in the Northern Hemisphere. Its biological properties still need to be discovered. Therefore, our paper focuses on studies of E. prunastri extracts, including its main metabolites evernic acid (EA) or atranorin (ATR). Phytochemical profiles using chromatographic analysis were confirmed. The antioxidant activity was evaluated using in vitro chemical tests and in vitro enzymatic cells-free tests, namely superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), and catalase (CAT). The anti-inflammatory potential using cyclooxygenase-2 (COX-2) and hyaluronidase were determined. The neuroprotective potential using acetylcholinesterase, (AChE), butyrylcholinesterase (BChE), and tyrosinase (Tyr) was estimated. The hypoglycemic activity was also confirmed (α-glucosidase). Principal component analysis was performed to determine the relationship between the biological activity of extracts. The inhibitory effect of EA and ATR on COX-2 AChE, BChE, Tyr, and α-glucosidase was evaluated using molecular docking techniques and confirmed for EA and ATR (besides α-glucosidase). The penetration of EA and ATR from extracts through the blood–brain barrier was confirmed using the parallel artificial membrane permeability assay blood–brain barrier test. In conclusion, depending on chemical surroundings and the concentration, the E. prunastri extracts, EA or ATR, showed attractive pleiotropic properties, which should be further investigated. [ABSTRACT FROM AUTHOR]

Fisetin (FIS), a senolytic flavonoid, mitigates age-related neuroprotective changes. An amorphous FIS dispersion with a co-carrier was prepared using supercritical fluid extraction with carbon dioxide (scCO2). Characterisation, including powder X-ray diffraction and Fourier-transform infrared spectroscopy, confirmed amorphization and assessed intermolecular interactions. The amorphous FIS dispersion exhibited enhanced solubility, dissolution profiles, and bioavailability compared to the crystalline form. In vitro, the amorphous FIS dispersion demonstrated antioxidant activity (the ABTS, CUPRAC, DDPH, FRAP assays) and neuroprotective effects by inhibiting acetylcholinesterase and butyrylcholinesterase. FIS modulated gut microbiota, reducing potentially pathogenic gram-negative bacteria without affecting probiotic microflora. These improvements in solubility, antioxidant and neuroprotective activities, and gut microbiome modulation suggest the potential for optimising FIS delivery systems to leverage its health-promoting properties while addressing oral functionality limitations. [ABSTRACT FROM AUTHOR]

The study compares the active substance, alverine citrate, from three commercial sources in order to demonstrate polymorphic forms using the XRPD, SEM, and ATR-FTIR techniques. Based on the solubility tests of alverine citrate, a hard capsule was prepared with the highest possible dose of the active substance. Alverine citrate release profiles and stability were also investigated. XRPD and ATRFTIR analysis showed that all alverine citrate samples (despite differences in the synthesis process) were in the same polymorphic Form I. Scanning electron micrographs of alverine citrate from each manufacturer showed differences in the morphology (texture). Solubility studies confirmed complete solubility of the highest dose of alverine citrate in media with a pH of 1.2-6.8. Release studies showed that the release of the active substance, regardless of the manufacturer type, meets the immediate release requirement. Accelerated stability studies confirmed the stability of alverine citrate from selected manufacturers. As a result, the manufacturer of the final medicinal product may allow for their interchangeability during production without compromising the safety or efficacy of the medicinal product. [ABSTRACT FROM AUTHOR]

The influence of ionizing radiation on the physicochemical properties of panipenem in the solid-state was studied. In the first part of our studies, we evaluated the possibility of applying radiosterilization to obtain sterile panipenem. Spectroscopic (FT-IR, Raman), chromatography (HPLC and HPLC-MS) and X-ray powder diffraction (XRPD) studies have shown that irradiation of panipenem with the 25 kGy, the dose required to achieve sterility, does not change the physicochemical properties of the studied compound. The antimicrobial activity of panipenem irradiated with the dose of 25 kGy was reduced for three species. It was confirmed that the decrease in antimicrobial activity might be related to the isomerization of panipenem. [ABSTRACT FROM AUTHOR]

Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives. [ABSTRACT FROM AUTHOR]