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    Preparation and evaluation of fast-dissolving albendazole sulfoxide and praziquantel-loaded polyvinylpyrrolidone nanofiber films by electrospinning
    (Elsevier, 2024) Gultekin, Yakup; Korkmaz, Cagla; Ozturk, Naile; Filazi, Ayhan; Deniz, Ahmet; Dog, Osman; Pezik, Esra
    Albendazole sulfoxide (ALBSOX) and Praziquantel (PRZ) are broad-spectrum anthelmintic medications used in the treatment of both humans and animals that are challenging to manufacture for geriatric and pediatric populations and have poor oral bioavailability due to their low water solubility and high lipophilicity. To increase the solubility and bioavailability of the drugs, ALBSOX and PRZ-loaded nanofiber films were prepared using polyvinylpyrrolidone K90 (PVP), a non-toxic, inert polymer with high hydrophilic characteristics. SEM analysis of the produced ALBSOX and PRZ-loaded PVP nanofiber films revealed them to be uniform and smooth, with good uniformity and mechanical properties. The PVP nanofiber films of ALBSOX and PRZ disintegrated in phosphate buffer (pH 6.8) in less than 1 s and increased the solubility of ALBSOX and PRZ about five times compared to pure active ingredients. Furthermore, the prepared ALBSOX and PRZ-loaded PVP nanofiber films were found to have no cytotoxic effect in cell viability studies using L929 cells, and increased the protoscolicidal effect of the ALBSOX and PRZ combination approximately 2-fold in studies of Echinococcus granulosus protoscoleces. The findings of the present study reveal that the developed PVP nanofiber films have the potential to improve the dissolution profile and pharmacological efficacy of the ALBSOX and PRZ.
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    Preparation of nanosuspensions of a 1,4-dihydropyridine-based mixed L-/T-type calcium channel blocker by combined precipitation and ultrasonication methods
    (Elsevier, 2023) Pezik, Esra; Gulsun, Tugba; Gunduz, Miyase Gozde; Sahin, Selma; Ozturk, Naile; Vural, Imran
    M3, a condensed 1,4-dihydropyridine (DHP) derivative, targets both L- and T-type calcium channels and therefore, stands as a promising antihypertensive drug candidate. This study aims to improve the poor solubility of M3 using nanocrystal technology (a combination of precipitation and ultrasonication methods) to enhance its oral bioavailability. Pre-formulation studies were performed and M3 nanosuspensions were prepared using different stabilizers (polyvinyl pyrrolidone K30, polyvinyl alcohol, SoluPlus & REG;) and surfactants (poloxamer 188, poloxamer 407, sodium deoxycholate, sodium lauryl sulfate) at different concentrations (0.05, 0.1, 0.5, 1.0, 2.0%, w/v). The optimum nanosuspension formulation was freeze-dried using different cryoprotectants (mannitol, trehalose, glucose, sucrose, dextran) at different ratios (1.25, 2.5, 5.0%, w/v). It was determined that the most suitable cryoprotectant and ratio was 5.0% trehalose, resulting in nanocrystals with a size of 320.2 & PLUSMN; 15.3 nm and a zeta potential of -27.4 & PLUSMN; 0.1 mV. The physicochemical properties of M3, poloxamer 188, physical mixture and freeze-dried nanocrystals were evaluated by XRD, DSC and FT-IR analyses. Characterization studies showed amorphization of M3 in the freeze-dried nanocrystals prepared with poloxamer 188. The result of equilibrium solubility and permeability studies results indicated that M3 could be a BCS class 4 compound. Cell culture studies using Caco-2 cells showed that M3 had no significant toxic effect on the cells and had a Papp value of 2.2 x 10-7 cm/s. Compared to coarse M3 powder freeze-dried M3 nanocrystals showed a 200-fold increase in solubility and a 28.6-fold increase in apparent permeability. The cytotoxic effect of M3 was also reduced by using poloxamers as stabilizers in the formulation. M3 nanosuspensions were found to be a promising candidate for the oral administration of M3 for the potential treatment of hypertension due to the increase in solubility and permeability which could enhance its oral bioavailability.
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    Simultaneous determination of albendazole sulfoxide and praziquantel from PLGA nanoparticles and validation of new HPLC method
    (Marmara Univ, 2022) Gultekin, Yakup; Ozturk, Naile; Filazi, Ayhan; Deniz, Ahmet; Korkmaz, Cagla; Pezik, Esra; Barin, Gozde
    A simple, rapid and reproducible HPLC method has been developed and validated for the quantification of albendazole sulfoxide (ALBSOX) and praziquantel (PRZ), which can coexist in various dosage forms. Chromatographic separation was performed in gradient mode using a mobile phase consisting of an InertSustain (R) C18 column (150 x 4.6 mm, 5 mu m) and acetonitrile: water (v/v) at a flow rate of 1.0 mL/min. The active substance peaks were well separated and detected by a DAD detector at 217 nm. The HPLC method was linear for ALBSOX and PRZ in the concentration range of 0.1-50 mu g/mL. Limit of detection (LOD) was found to be 0.01 mu g/mL for ALBSOX and 0.009 mu g/mL for PRZ. The limit of quantification (LOQ) was found to be 0.03 mu g/mL for ALBSOX and 0.027 mu g/mL for PRZ. The developed HPLC method was validated based on ICH guidelines for specificity, linearity, system suitability, precision and accuracy. The method was applied for simultaneous quantification and characterization studies of ALBSOX and PRA in PLGA nanoparticles.