1.Liquid chromatographic methods for determination of the new antiepileptic drugs stiripentol,retigabine,rufinamide and perampanel:A comprehensive and critical review
Meirinho SARA ; Rodrigues MÁRCIO ; Fortuna ANA ; Falc(a)o AMÍLCAR ; Alves GILBERTO
Journal of Pharmaceutical Analysis 2021;11(4):405-421
The new antiepileptic drugs perampanel,retigabine,rufinamide and stiripentol have been recently approved for different epilepsy types.Being them an innovation in the antiepileptics armamentarium,a lot of investigations regarding their pharmacological properties are yet to be performed.Besides,considering their broad anticonvulsant activities,an extension of their therapeutic indications may be worthy of investigation,especially regarding other seizure types as well as other central nervous system disorders.Although different liquid chromatographic (LC) methods coupled with ultraviolet,fluores-cence,mass or tandem-mass spectrometry detection have already been developed for the determination of perampanel,retigabine,rufinamide and stiripentol,new and more cost-effective methods are yet required.Therefore,this review summarizes the main analytical aspects regarding the liquid chro-matographic methods developed for the analysis of perampanel,retigabine (and its main active metabolite),rufinamide and stiripentol in biological samples and pharmaceutical dosage forms.Furthermore,the physicochemical and stability properties of the target compounds will also be addressed.Thus,this review gathers,for the first time,important background information on LC methods that have been developed and applied for the determination of perampanel,retigabine,rufinamide and stiripentol,which should be considered as a starting point if new (bio)analytical techniques are aimed to be imnlemented for these drugs.
2.Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples
Romani F.A. LUCIANA ; Yoshida I. MARIA ; Gomes C.L. ELIONAI ; Machado R. RENES ; Rodrigues F. FELIPE ; Coelho M. MÁRCIO ; Oliveira A. MARCELO ; Freitas-Marques B. MARIA ; Rosane A.S. San Gil ; Mussel N. WAGNER
Journal of Pharmaceutical Analysis 2018;8(2):103-108
Meloxicam (MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies. X-ray diffraction indicated the presence of two crystalline forms in one sample. DSC experiments suggested that crystallization, or a crystal transition, occurred differently be-tween samples. The FTIR and 1H NMR spectra showed characteristic assignments. 13C solid-state NMR spectroscopy indicated the presence of more than one phase in a sample from pharmacy B. The Hirshfeld surface analysis, with electrostatic potential projection, allowed complete assignment of the UV spectra in ethanol solution. The polymorph I of meloxicam was more active than polymorph Ⅲ in an experi-mental model of acute inflammation in mice. Our results highlighted the need for complete crystal-lographic characterization and the separation of freely used raw materials in compounding pharmacies, as a routine procedure, to ensure the desired dose/effect.
3.Miniscrew insertion sites of infrazygomatic crest and mandibular buccal shelf in different vertical craniofacial patterns: A cone-beam computed tomography study
Murilo MATIAS ; Carlos FLORES-MIR ; Márcio Rodrigues de ALMEIDA ; Bruno da SILVA VIEIRA ; Karina Maria Salvatore de FREITAS ; Daniela Calabrese NUNES ; Marcos Cezar FERREIRA ; Weber URSI
The Korean Journal of Orthodontics 2021;51(6):387-396
Objective:
To identify optimal areas for the insertion of extra-alveolar miniscrews into the infrazygomatic crest (IZC) and mandibular buccal shelf (MBS), using cone beam computed tomography (CBCT) imaging in patients with different craniofacial patterns.
Methods:
CBCT reconstructions of untreated individuals were used to evaluate the IZC and MBS areas. The participants were divided into three groups, based on the craniofacial pattern, namely, brachyfacial (n = 15; mean age, 23.3 years), mesofacial (n = 15; mean age, 19.24 years), and dolichofacial (n = 15; mean age, 17.79 years). In the IZC, the evaluated areas were at 11, 13, and 15 mm above the buccal cusp tips of the right and left first molars. In the MBS, the evaluated areas were at the projections of the first molars’ distal roots and second molars’ mesial and distal roots, at a 4- and 8-mm distance from the cementoenamel junction. Intergroup comparisons were performed with analysis of variance and the Tukey test.
Results:
There was no statistically significant difference in the IZC bone thickness among the groups. For MBS bone availability, some comparisons revealed no difference; meanwhile, other comparisons revealed increased MBS bone thickness in the brachyfacial (first molars distal roots) and dolichofacial (second molars mesial and distal roots) patterns.
Conclusions
There was no significant difference in the IZC bone thickness among the groups. The facial skeletal pattern may affect the availability of ideal bone thickness for the insertion of extra-alveolar miniscrews in the MBS region; however, this variability is unlikely to be clinically meaningful.
5.Human Stem Cell-Derived Retinal Pigment Epithelial Cells as a Model for Drug Screening and Pre-Clinical Assays Compared to ARPE-19 Cell Line
Carolina Reis OLIVEIRA ; Mayara Rodrigues Brandão de PAIVA ; Marcela Coelho Silva RIBEIRO ; Gracielle Ferreira ANDRADE ; Juliana Lott CARVALHO ; Dawidson Assis GOMES ; Márcio NEHEMY ; Sílvia Ligório FIALHO ; Armando SILVA-CUNHA ; Alfredo Miranda de GÓES
International Journal of Stem Cells 2021;14(1):74-84
Background and Objectives:
Eye diseases have a high socioeconomic impact on society and may be one of the fields in which most stem cell-related scientific accomplishments have been achieved recently. In this context, human Pluripotent Stem Cell (hPSC) technology arises as an important tool to produce and study human Embryonic Stem cell derived-Retinal Pigmented Epithelial Cells (hES-RPE) for several applications, such as cell therapy, disease modeling, and drug screening. The use of this technology in pre-clinical phases attends to the overall population desire for animal-free product development. Here, we aimed to compare hES-RPE cells with ARPE-19, one of the most commonly used retinal pigmented epithelial immortalized cell lines.
Methods:
and Results: Functional, cellular and molecular data obtained suggest that hES-RPE cells more closely resembles native RPEs compared to ARPE-19. Furthermore, hES-RPE revealed an interesting robustness when cultured on human Bruch’s membrane explants and after exposure to Cyclosporine (CSA), Sirolimus (SRL), Tacrolimus (TAC), Leflunomide (LEF) and Teriflunomide (TER). On these conditions, hES-RPE cells were able to survive at higher drug concentrations, while ARPE-19 cell line was more susceptible to cell death.
Conclusions
Therefore, hES-RPEs seem to have the ability to incur a broader range of RPE functions than ARPE-19 and should be more thoroughly explored for drug screening.