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Öğe Determination of Antioxidant, Antidiabetic, Anticholinergic, Antiglaucoma Properties and Comprehensive Phytochemical Content by LC-MS/MS of Bingöl Honeybee Pollen(Wiley, 2025) İzol, Ebubekir; Turhan, Münire; Yılmaz, Mustafa Abdullah; Çağlayan, Cüneyt; Gülçin, İlhamiHoneybee pollen is the most important food and protein source for bees. It is a highly nutritious natural product for humans due to its content. Pollen shows different phytochemical content and variable biological activity according to different geography and vegetation. Therefore, in this study, the comprehensive phytochemical content by LC-MS/MS, and its antioxidant properties by different assays, with enzyme inhibition potential; antidiabetic, anticholinergic, and antiglaucoma properties, were determined from a pollen sample from Bingö l province, one of the significant beekeeping centers in Tü rkiye. As a result of LC-MS/MS, 15 metabolites were determined, and the highest concentration of quinic acid (1.531 mg analyte/g extract) was found. Antioxidant results: total phenolic content 113.14 mg GAE/g, total flavonoid content 64.11 mg QE/g, Fe3+ reduction 0.43 mu g/mL, CUPRAC 0.511 mu g/mL, FRAP 0.976 mu g/mL, DPPH IC50: 1.06 mu g/mL, ABTS IC50: 0.933 mu g/mL, and DMPD IC50: 0.598 mu g/mL. In addition, pollen showed antiglaucoma, anticholinergic, and antidiabetic properties by inhibiting carbonic anhydrase isoenzyme II (hCA II), acetylcholinesterase (AChE), and alpha- amylase enzymes, respectively. In this study, it was determined that Bingö l pollen has a comprehensive phytochemical content and antioxidant properties and, for the first time, inhibits hCA II, AChE, and alpha-amylase enzymes.Öğe Quality by Design approach for development and characterization of gabapentin-loaded solid lipid nanoparticles for intranasal delivery: In vitro, ex vivo, and histopathological evaluation(Mashhad University of Medical Sciences, 2024) Toksoy, Mahmut Ozan; Aşır, Fırat; Güzel, Mert CanObjective(s): ”Quality by Design” (QbD) is a novel approach to product development that involves understanding the product and process, as well as the relationship between critical quality attributes (CQA) and critical process parameters (CPP). This study aimed to optimize the gabapentin-loaded solid lipid nanoparticle formulation (GP-SLN) using a QbD approach and evaluate in vitro and ex vivo performance. Materials and Methods: The GP-SLN formulation was created using the microemulsion method by combining Gelucire 48/16, Tween 80, and Plurol Oleique CC 497. The Box-Behnken experimental design was adopted to investigate the effects of independent factors on dependent factors. The GP-SLN formulation was assessed based on particle size and distribution, zeta potential, morphology, entrapment efficiency, release kinetics, permeation parameters, stability, and nasal toxicity. Results:The nanoparticles had a cubical shape with a particle size of 185.3±45.6 nm, a zeta potential of -24±3.53 mV, and an entrapment efficiency of 82.57±4.02%. The particle size and zeta potential of the GP-SLNs remained consistent for 3 months and followed Weibull kinetics with a significantly higher ex vivo permeability (1.7 fold) than a gabapentin solution (GP-SOL). Histopathology studies showed that intranasal administration of the GP-SLN formulation had no harmful effects. Conclusion: The current study reports the successful development of a GP-SLN formulation using QbD. A sustained release of GP was achieved and its nasal permeability was increased. Solid lipid nanoparticles with optimum particle size and high entrapment efficiency may offer a promising approach for the intranasal delivery of drugs.Öğe Nanoemulsions a new topical drug delivery system for the treatment of acne(Marmara University Faculty of Pharmacy, 2023) Samancı, Bülent; Yener, Fatma Gülgün; Değim, İsmail TuncerThe main aim of this review is to investigate published research that related nanoemulsions formulations as the for improving of acne and to evaluate the recent developments and future of nanoemulsions for acne care. Nanoemulsion, skin penetration, acne vulgaris, topical drug delivery using as keywords were sequentially searched three databases (PubMed, ScienceDirect, Google Scholar). Following the removal of duplications and irrelevant results, research articles and reviews were included in the final literature overview. Systemic therapy includes anti-inflammatory and antibiotics drugs that can bring on undesirable adverse. On the other hand, the low solubility in water of the drug and insufficient penetration through the skin limits the drugs’ topical administration. Innovative topical nanoemulsion systems can be very impactful to decrease the side effects of drugs and provide tremendous drug penetration through the skin. They provide advantage over traditional topical medications by enhancing bioavailability of drugs, and the persistency of drugs in the skin layers. Furthermore, nanoemulsions have significant potential to overcome the drawbacks of the conventional dosage forms contains natural molecules and essential oils for acne therapy. Additionally, some comparative studies showed that nanoemulsions increase the permeability of the drug molecule through the skin more than other nanocarriers (SLN, NLC).Öğe QbD application for a fixed-dose combination with biowaiver potential: Evaluations of In vitro and In vivo applications(Springer, 2022) Yaşın, Diren Sarısaltık; Uslu, Abdullah; Uyar, Emre; Erdinç, Meral; Teksin, Zeynep ŞafakPurpose The purpose of this study was to use the quality by design (QbD) approach to design a directly compressed fixed-dose combination (FDC) tablet comprising amlodipine besylate and enalapril maleate with biowaiver potential in alignment with the Biopharmaceutical Classification System (BCS). Methods As a result of the risk assessment, the amounts of the formulation components such as disintegrant, binder, and lubricant were selected as critical material attributes, and the processes of blending and lubrication were accepted as critical process parameters in a screening design of Plackett-Burman. These factors were evaluated based on the statistical significance of their impact on the drug product's content uniformity, assay, friability, disintegration, and dissolution. The most significant factors determined with the use of Pareto charts and half-normal graphs were the amount of lubricant and disintegrant and blending time, all of which were subsequently optimized using Box-Behnken Design. The optimum formulation was evaluated with in vitro quality tests and in vivo blood pressure-lowering efficacy tests, the results of which were compared to the individual references in rats. Results As a result of the optimization process, a design space was established for the critical factors. FDC product showed quality and dissolution profiles similar to those of the references. Combination therapy was superior to individual drugs in rats (p < 0.05). Conclusion It was concluded that an FDC product eligible for BCS-based biowaiver can be developed systematically by using the QbD concept. It was demonstrated that using scanning designs prior to optimization can reduce the number of unnecessary experiments and yield more reliable results in less time.Öğe Development and validation of an HPLC method using an experimental design for analysis of amlodipine besylate and enalapril maleate in a fixed-dose combination(Galenos Publication, 2021) Yaşın, Diren Sarısaltık; Bingül, Alev Arslantürk; Karaküçük, Alptuğ; Teksin, Zeynep ŞafakObjectives: The aim of this study was to develop and optimize a simple, cost-effective, and robust high-performance liquid chromatography (HPLC) method by taking an experimental design approach to the assay and dissolution analysis of amlodipine besylate and enalapril maleate from a fixed-dose combination tablet. Materials and Methods: The chromatographic analysis was performed on a C18 column (4.6x250 mm id., particle size of 5 mu m). The injection volume was 5 mu L, and the detection wavelength was 215 nm. A Box-Behnken design was used to test the robustness of the method. The flow rate (1, 1.2, and 1.4 mL/min), column temperature (25 degrees C, 30 degrees C, and 35 degrees C), methanol ratio of the mobile phase (5, 10, and 15%), and pH of the mobile phase (2.8, 3, and 3.2) were selected as independent variables. The method was validated according to International Conference on Harmonization guidelines. Dissolution of the tablets was performed by using USP apparatus 2 and analyzed using the optimized HPLC method. Multivariate linear regression analysis and ANOVA were used in the statistical evaluation. Results: Linear models were fitted for all variables. The flow rate was the most significant factor affecting the APIs' concentrations. The optimized method included the following parameters: Column temperature of 25 degrees C, 10% methanol as the mobile phase, pH of 2.95, and flow rate of 1.205 mL/min. Retention times were 3.8 min and 7.9 min for enalapril and amlodipine, respectively. The method was found to be linear in the range of 0.8-24 mu g/mL (R-2 >0.999) and 1.6-48 mu g/mL (R-2 >0.999) for amlodipine and enalapril, respectively. Both APIs were dissolved more than 85% within 10 min. Conclusion: The experimental design was proved as a useful tool for the determination and separation of enalapril maleate and amlodipine besylate in dosage forms. The optimized method can be used for in vitro performance and quality control tests of fixed-dose tablet combinations containing enalapril maleate and amlodipine besylate.Öğe Enhancing skin penetration: The role of microneedles(Farmasötik Bilimler Ankara Derneği, 2021) Samancı, Bülent; Yener, Fatma Gülgün; Değim, İsmail TuncerSince transdermal delivery systems provide some important advantages over oral delivery systems and parenteral delivery systems, they have attracted the attention of researchers. Degradation of the drug in the gastrointestinal (GI) system, irritation of the GI system tract, and the first-pass effect of the drug are some of the disadvantages of oral administration, while the need for medical staff to administer it and creating phobia in the patient are among the disadvantages of parenteral administration. To overcome these drawbacks, researchers have developed formulations for the transdermal delivery of drugs. The most important handicap of transdermal drug administration is the Stratum Corneum layer (St. Corneum), which forms the enormous barrier layer of the skin. Some techniques have been developed to overcome this serious barrier problem of the skin. Microneedles are one of the physical methods to increase the penetration of therapeutic agents through the skin. Microneedles consist of needle arrays long enough to deliver the drug to the dermis layer and micron-sized enough to not reach the nerve cells and not cause pain. Microneedles can be classified into five different types as solid microneedles, dissolving microneedles, hollow microneedles, coated microneedles, and hydrogel microneedles according to the properties of the materials used in the fabrication and the mechanisms of release of the therapeutic agent. Microneedles can be used in the application of vaccines, proteins, nucleotides, drug delivery systems, cosmetic, and for diagnostic purposes. Although important technological developments have been experienced for microneedle in many areas such as drug delivery systems, disease diagnosis, and cosmetics in the last two decades, there are many working areas that need to be developed. Especially in longterm treatments, studies should be done to develop them as smart devices.Öğe Katı lipit nanopartiküller ve beyne özgü ilaç taşıyıcı sistem olarak uygulamaları(Ankara Üniversitesi Eczacılık Fakültesi, 2021) Toksoy, Mahmut Ozan; Tırnaksız, Fahriye FigenAmaç: Son 20 yılda nanoteknolojik gelişmeler ile birlikte ilaç moleküllerinin beyne hedeflenmesine yönelik çalışmalarda artış gözlenmektedir. Beyin, kan dolaşımından kendine özgü bir bariyer ile ayrılmıştır. Kan-beyin bariyeri olarak adlandırılan bu yapı astrosit, perisit, endotel hücreleri ve bunlar arasında bulunan sıkı bağlantılardan oluşmaktadır. Moleküllerin beyne geçişini engelleyen enzimatik aktivitenin yanında, beynin sistemik dolaşımdan kan-beyin bariyeri ile ayrılması, terapötik moleküllerinin beyne geçişini olumsuz etkilemektedir. Bu yüzden merkezi sinir sistemi rahatsızlıklarında tedavi zorlaşmakta, terapötik etki azalmakta veya gözlenememektedir. Bu durumu anlamak ve olası sorunları giderebilmek için beynin ve kan-beyin bariyerinin yapısı bilinmeli, ilaç moleküllerinin geçiş mekanizmaları aydınlatılmalıdır. Beyne hedeflemede ilaç taşıyıcı sistemlerin önemi günden güne artmaktadır. Üretilen sistemler arasında katı lipit nanopartiküllerin kolay üretimi, biyo-uyumluluğu, biyo-bozunabilirliği açısından diğer sistemlere göre avantajları bulunmaktadır. Bu derlemede, kan beyin bariyerinden bahsedilmesi, beyne ilaç hedefleme yöntemlerinin açıklanması ve beyne ilaç moleküllerinin hedeflenmesinde katı lipit nanopartiküllerle yapılan çalışmalardan söz edilmesi amaçlanmıştır. Sonuç ve Tartışma: İlaç moleküllerinin beyne hedeflenmesinde kan-beyin bariyeri en büyük engeldir. Bu engeli aşabilmek amacıyla geliştirilen sistemlerden biri de katı lipit nanopartiküller olmuş, sayısız çalışmalarla etkinliği kanıtlanmıştır. Hedefleme ile merkezi sinir sistemi rahatsızlıklarında ilaçların etkinliğinin arttırılabileceği görülmüştür.Öğe Determination of enzyme inhibition potential and anticancer effects of pistacia khinjuk stocks raised in in vitro and in vivo conditions(MDPI, 2021) Tilkat, Emine Ayaz; Batıbay, Hayri; Yener, İsmail; Yılmaz, Pelin Köseoğlu; Akdeniz, Mehmet; Kaplan, Alevcan; Ercişli, Sezai; Ertas, Abdulselam; Holubec, VojtechIn this study, antihypertensive, anticholinesterase, antiurease, antityrosinase and antielastase enzyme inhibition and anticancer activities of in vivo (male and female) and in vitro samples (root, stem and leaf parts) of the Pistacia khinjuk Stocks were investigated comparatively. In this context, in vitro shoot cultures were obtained from germinated mature seeds. Then, the juvenile shoots were proliferated in Murashige and Skoog (MS) medium supplemented with 1 mg/L 6-Benzylaminopurine (BAP). In terms of anticancer activity, the whole of the samples studied was found to have apoptotic effects against MCF-7 (breast cancer) and HT-29 (colon cancer) cell lines. The extracts obtained from in vivo female root parts showed better cytotoxicity than all the other tested extracts on MCF-7 (IC50: 31.86 +/- 1.40 mu g/mL) and HT-29 cell series (IC50: 59.60 +/- 0.69 mu g/mL). Even though all the samples showed a strong butyrylcholinesterase enzyme inhibition (BChE) activity, it was detected that none of the samples had shown acetylcholinesterase enzyme inhibition (AChE). It was also determined that in vivo leaf samples of female trees had the highest BChE activity (Inhibition%: 75.20 +/- 1.50). All the samples showed a low-moderate level of urease and tyrosinase enzyme activity, while in vivo samples showed a significant level of the elastase enzyme activities (Inhibition%: 58.72 for female root extracts; 58.25 for female leaf extracts, at 50 mu g/mL concentration), and they were more active than the standard oleanolic acid (Inhibition%: 39.46 +/- 0.52). The antihypertensive activities as the inhibition of angiotensin I-converting enzyme (ACE) of in vivo samples (Inhibition%: 95.88 for female stem extracts; 95.18 for female root extracts) were detected as close to the standard (Inhibition%: 96.64 +/- 1.85) used. In general, it can be stated that in vivo samples had higher biological activities compared to in vitro ones. Consequently, according to our results, it was concluded that in vitro stem parts of khinjuk pistachio could also be evaluated as an alternative new antihypertensive, antielastase and anticancer agent source.Öğe Phytochemical analysis and antioxidant and anticholinesterase activities of Pulicaria dysenterica from Turkey(Dicle Üniversitesi Fen Bilimleri Estitüsü, 2014) Boğa, Mehmet; Ertaş, Abdulselam; Yeşil, Yeter; Haşimi, Nesrin; Yılmaz, Mustafa Abdullah; Özaslan, Cumali[Özet Yok]
