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• Comparative Evaluation of Solubilization Strategies for an ABCG2 Transporter Inhibitor

  Pálma Fehér

  Kata Kárándi

  Gergő Kis

  Christelle Marminon

  Marc Le Borgne

  Liza Józsa

  Views:

  71

  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.

• Formulation and investigation of Lactobacillus rhamnosus cek-R1 filled alginate microspheres with different excipients

  Pálma Fehér

  Boglárka Papp

  Liza Józsa

  Dávid Sinka

  Eszter Fidrus

  Fruzsina Nacsa

  Ildikó Bácskay

  Gábor Kardos

  Views:

  268

  Microspheres are spherical particles containing the active substance, in our case bacterial probiotic strain Lactobacillus rhamnosus (L. rhamnosus), in an individually coated form. L. rhamnosus is a natural constituent of the human intestinal flora and is known to improve immune function, enhance healing of the intestinal mucosa, reduce inflammation, bloating and diarrhoea.  

  The aim of our experimental work was to formulate sodium alginate microspheres containing L. rhamnosus bacterial strain as active ingredient and prebiotic (galactooligosaccharide, pectin, inulin). The microspheres were formulated using Büchi Encapsulator equipment, after which the entrapment efficiency was measured. The lyophilized product was filled into hydroxypropylmethylcellulose (HPMC) capsules and was subjected to a dissolution assay using Erweka equipment. The number of viable L. rhamnosus was determined from samples of the dissolution fluid.  The microspheres are lyophilised to improve shelf-life and facilitate filling into traditional capsules. The number of viable bacteria in the lyophilizate was determined by inoculation on medium and standard microdilution test. Microspheres containing different compositions of pro- and prebiotics were formulated, and their antioxidant capacity was detected by 2,2-diphenyl-l-1-picrylhydrazyl (DPPH). We tested the anti-inflammatory effect of the microspheres using human IL-4 ELISA Kit on colon adenocarcinoma (CaCo-2) cell line.