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Comparative Evaluation of Solubilization Strategies for an ABCG2 Transporter Inhibitor
Views:137Poor 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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Formulation and investigation of Lactobacillus rhamnosus cek-R1 filled alginate microspheres with different excipients
Views:308Microspheres 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.
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Comparison and evaluation of the efficacy of topical drug formulations containing diclofenac
Views:23The 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.
