Articles

• Comparative Evaluation of Solubilization Strategies for an ABCG2 Transporter Inhibitor

  Pálma Fehér

  Kata Kárándi

  Gergő Kis

  Christelle Marminon

  Marc Le Borgne

  Liza Józsa

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  137

  Poor aqueous solubility remains one of the major challenges in the development of orally administered drugs, particularly for lipophilic molecules such as ABCG2 transporter inhibitors. These compounds possess high molecular weight, significant lipophilicity, and limited water solubility, which restrict their bioavailability and therapeutic application. This study aimed to enhance the solubility of a model ABCG2 inhibitor using different solubilization techniques, including co-grinding with hydroxypropyl-β-cyclodextrin (HP-β-CD) or polyvinylpyrrolidone (PVP) and micellar solubilization using nonionic surfactants. Each formulation was optimized and characterized for drug loading, equilibrium solubility and dissolution behavior under simulated gastrointestinal conditions. The micellar formulation exhibited the highest solubilization efficiency, The HP-β-CD complex and PVP co-grinding dispersions also resulted in notable enhancement compared to the pure drug. These findings highlight the potential of simple formulation strategies to overcome solubility limitations of ABCG2 inhibitors and improve their oral bioavailability.

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• Comparison and evaluation of the efficacy of topical drug formulations containing diclofenac

  Krisztina Bodnár

  Gergő Kis

  Liza Józsa

  Views:

  21

  The choice of dermal dosage form is critical for therapeutic success, as it directly influences drug absorption, bioavailability, and overall efficacy. The skin possesses distinct physiological and anatomical characteristics that determine the performance of topical formulations. In addition to efficacy, the selected dosage form affects patient comfort, treatment adherence, and overall therapeutic outcomes. Therefore, optimizing dermal formulations is essential. This study aimed to compare different diclofenac sodium-containing dermal dosage forms in terms of drug release, bioavailability, cytotoxicity, and anti-inflammatory activity. Three formulations were evaluated: cream, foam and gel. Texture analysis was performed to predict bioavailability. Drug release and membrane penetration were assessed using a Franz diffusion cell combined with UV–VIS spectrophotometry. Biocompatibility was determined by MTT assay on HaCaT human keratinocyte cells. The in vitro anti-inflammatory effect was evaluated by measuring TNF-α and IL-1β levels using ELISA. Franz diffusion studies demonstrated that the foam formulation exhibited the most favorable penetration profile, followed by the cream and gel. MTT results confirmed acceptable biocompatibility for all formulations; however, cream and gel showed a greater reduction in cell viability, likely due to excipients. The foam achieved the greatest reduction in inflammatory markers, while no significant difference was observed between cream and gel. Based on the results, it can be concluded that the foam formulation containing diclofenac sodium is the most advantageous in terms of drug release, bioavailability, toxicity, and anti-inflammatory effect.

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• New anticancer medicines approved by the EMA in 2025

  Miklós Bege

  Anikó Borbás

  Views:

  17

  Despite the serious progress in the antitumor therapy, cancer did not cease to be one of the leading causes of death in the developed world. Hence still there is high interest for new anticancer agents. In 2025, the EMA approved 104 new medicines, 37 of them containing new active substances. 18 new anticancer medicines were approved (14 new active substances).  In this review, we aim to shortly summarize the mechanism of action and use of the new drugs approved by the EMA in the year 2025.

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• Estimation of Renal Function for Antibiotic Dosing Decision

  Adina Fésüs

  Zsanett Szilágyi

  Ghazal Mohammadi Khabbaz

  Attila Vaskó

  Views:

  24

  Background: Accurate renal function assessment is essential for appropriate antibiotic dosing in critically ill patients. However, different estimation equations may yield discrepant results, potentially leading to dosing errors and suboptimal clinical outcomes.

  Objectives: To compare antibiotic dosing appropriateness based on renal function estimated using Cockcroft–Gault (CG), MDRD, and CKD-EPI equations, and to evaluate associated clinical outcomes in ICU patients with pneumonia-associated sepsis.

  Methods: In this single-center retrospective observational study, 229 adult ICU patients were included. Renal function was estimated using CG, MDRD, and CKD-EPI equations. Antibiotic dosing was classified as appropriate or inappropriate according to SPC and local guidelines. Clinical outcomes, including 30-day mortality/survival, and length of stay (LOS) were analyzed.

  Results: Based on CKD-EPI and MDRD, 57.2% and 55.5% of patients received appropriate dosing, respectively. However, 7.4% of patients considered appropriately dosed by these equations were reclassified as inappropriately dosed using CG. While mean renal function values were similar across equations (~67 mL/min), median values differed by approximately 20 mL/min (CG: 74 mL/min vs. CKD-EPI/MDRD: 52 and 50 mL/min), leading to clinically relevant reclassification. Inappropriate dosing was associated with older age and higher comorbidity burden. Piperacillin/tazobactam was most frequently underdosed, whereas clarithromycin, cefepime, and amikacin were commonly overdosed. Patients with inappropriate dosing had longer hospital LOS (median 14 vs. 11 days) and ICU-LOS (9 vs. 6 days), and showed worse survival, although 30-day mortality differences were not significant.

  Conclusions: The choice of renal function equation significantly impacts antibiotic dosing decisions. CG-based assessment may better identify dosing inaccuracies, and inappropriate dosing is associated with worse clinical outcomes. Optimized, individualized dosing strategies are warranted in critically ill patients.

   

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