Search

Lavender oil (LEO) is one of the most well-known essential oils worldwide which, besides its extensive application in aromatherapy, serves as raw material for various fields, including the food, cosmetic, and pharmaceutical industries. Accordingly, several global requirements were established to warrant its quality. Microencapsulation represents an emerging technology widely applied for the preservation of essential oils, simultaneously providing new ways of application. In the current study, lavender oil was obtained from the flowering tops of Lavandula angustifolia Mill. on a semi-industrial-scale steam distillation system. According to the GC-MS investigation, lavender oil obtained in the third year of cultivation met the European Pharmacopoeia standards for linalyl acetate and linalool contents ≈38% and ≈26%, respectively. Microcapsules (MCs) containing the so-obtained essential oil were successfully produced by complex coacervation technology between gum arabic (GA) and three different grades of type-A gelatin (GE). Optical microscopic investigations revealed a significant difference in particle size depending on the gelatin grade used. The variation observed for coacervates was well reflected on the scanning electron micrographs of the freeze-dried form. The highest encapsulation efficiency values were obtained by UV-VIS spectrophotometry for microcapsules produced using gelatin with the medium gel strength. FT-IR spectra confirmed the structural modifications attributed to microencapsulation. According to the GC-MS analysis of the freeze-dried form, the characteristic components of lavender oil were present in the composition of the encapsulated essential oil. [ABSTRACT FROM AUTHOR]

Yarrow (Achillea millefolium L., AM) is a widely used medicinal plant, with its essential oil highly valued in the cosmetic industry. In view of the numerous biological effects, however, microencapsulation, due to its ability to protect sensitive constituents, transform liquids into solid-state material, and provide modification of release kinetics, might open up new possibilities for the biomedical utilization of yarrow essential oil (AMO). In the current work, yarrow plantation was established by its propagation from spontaneous flora. Following the steam distillation of aerial parts, the chemical composition of the essential oil was determined by GC-MS analysis and compared with two commercial samples. This study concludes that Achillea millefolium L. from this region, given the environmental conditions, produces high-azulene-content essential oil. Furthermore, microencapsulation of AMO was successfully performed by complex coacervation into gelatin (GE) and gum arabic (GA) based core–shell microcapsules (MCs). According to the optical microscopic investigation, the particle sizes of the formed polynucleated microcapsules ranged from 14 to 132 µm, with an average of 47 µm. The assessment of morphology by SEM analysis of the freeze-dried form revealed a sponge-like character with embedded circular structures. The microencapsulation was confirmed by FT-IR spectroscopy and differential scanning calorimetry (DSC), while an encapsulation efficiency of 87.6% was determined by UV spectroscopy. GC-MS analysis revealed that microencapsulation preserves the key components of the essential oil. It was concluded that AMO can be effectively processed by complex coacervation followed by freeze-drying into solid-state material for new applications. [ABSTRACT FROM AUTHOR]

A reversed-phase high-performance liquid chromatographic (HPLC) method was developed for the simultaneous determination of the potential impurities of dexketoprofen, including the distomer R-ketoprofen. After screening the separation capability of four polysaccharide columns (Lux Amylose-1, Lux Amylose-2, Lux Cellulose-1 and Lux Cellulose-2) in polar organic and in reversed-phase modes, appropriate enantioseparation was observed only on the Lux Amylose-2 column in an acidified acetonitrile/water mixture. A detailed investigation of the mobile phase composition and temperature for enantio- and chemoselectivity showed many unexpected observations. It was observed that both the resolution and the enantiomer elution order can be fine-tuned by varying the temperature and mobile phase composition. Moreover, hysteresis of the retention times and enantioselectivity was also observed in reversed-phase mode using methanol/water mixtures on amylose-type columns. This could indicate that the three-dimensional structure of the amylose column can change by transitioning from a polar organic to a reversed-phase mode, which affects the enantioseparation process. Temperature-dependent enantiomer elution order and rare enthalpic/entropic controlled enantioseparation in the operative temperature range were also observed in reversed-phase mode. To find the best methodological conditions for the determination of dexketoprofen impurities, a full factorial optimization design was performed. Using the optimized parameters (Lux Amylose-2 column with water/acetonitrile/acetic acid 50/50/0.1 (v/v/v) at a 1 mL/min flow rate at 20 °C), baseline separations were achieved between all compounds within 15 min. Our newly developed HPLC method was validated according to the current guidelines, and its application was tested on commercially available pharmaceutical formulations. According to the authors' knowledge, this is the first study to report hysteretic behavior on polysaccharide columns in reversed-phase mode. [ABSTRACT FROM AUTHOR]

An amorphous fiber-based solid dispersion of chlorzoxazone was prepared for the first time by employing centrifugal spinning, using polyvinylpyrrolidone as the fiber-forming polymer. After optimization of the spinning parameters, the obtained fibers were characterized using a set of analytical techniques, both in a solid- and solution-state. Morphological characterization revealed a slightly aligned, defect-free fibrous structure with an average fiber diameter of d = 3.07 ± 1.32 μm. The differential scanning calorimetric results indicated a crystalline-to-amorphous transition of the active substance during the centrifugal spinning process, while gas chromatographic determinations revealed a residual ethanol content of 0.42 ± 0.04%. UV spectroscopy indicated the incorporation of chlorzoxazone in the fibrous structures, with an average active substance content of 15.91 ± 0.36 w/w%. During small-volume dissolution studies, the prepared fiber mats presented immediate disintegration upon contact with the dissolution media, followed by rapid dissolution of the active substance, with 84.8% dissolved at 1 min and 93.7% at 3 min, outperforming the micronized, pure chlorzoxazone. The obtained results indicate that centrifugal spinning is a low-cost, high-yield, viable alternative to the currently used methods to prepare fiber-based amorphous solid dispersions of poorly soluble drugs. The prepared chlorzoxazone-loaded microfibers could be used as a buccal dosage form for the systematic delivery of chlorzoxazone and could potentially lead to a rapid onset of action and longer efficacy of the muscle relaxant drug. [ABSTRACT FROM AUTHOR]

Vildagliptin (VIL) is a dipeptidyl peptidase-4 inhibitor used in the treatment of type 2 diabetes mellitus; in therapy, it is available as the enantiomerically pure S-VIL, the other enantiomer R-VIL being considered as an enantiomeric impurity. A systematic screening of 16 cyclodextrin (CD) derivatives as chiral selectors was performed at three pH levels using phosphate (pH 2.5, pH 7.0) and acetate (pH 4.5) buffers. Method optimization employed an experimental design approach, systematically investigating the effect of buffer and CD concentration, buffer pH, capillary temperature, and applied voltage on the chiral resolution and analysis time. The method's analytical performance was thoroughly assessed and subsequently employed for determining the enantiomeric purity of VIL in a pharmaceutical formulation. The properties of the inclusion complexes, such as stoichiometry and atomic level intermolecular host–guest interactions were studied by NMR measurements and molecular modeling. Native α-CD at acidic pH has demonstrated its exceptional suitability for the separation of VIL enantiomers with a favorable migration order (R-VIL followed by S-VIL). The optimized analytical conditions (75 mM acetate buffer, pH 4.5, containing 50 mM α-CD, 18 kV applied voltage, and 15 °C capillary temperature) provided a baseline separation of VIL enantiomers within 9 min. The developed method represents a cost-effective alternative to the enantiomeric impurity control of VIL. Symmetry is often a fundamental aspect of molecular structures and interactions, and our detailed analysis of the chiral recognition process contributes to the understanding of symmetry-related aspects in molecular systems. This developed method not only offers a cost-effective alternative for the enantiomeric impurity control of VIL but also provides valuable information regarding the mechanism of the chiral recognition process, aligning with the broader themes of symmetry in molecular sciences. [ABSTRACT FROM AUTHOR]