Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
1
12
10.35333/jrp.2021.291
872
Preparation and detailed characterization of fusidic acid loaded in situ gel formulations for ophthalmic application
Seda RENÇBER
Ece ÖZCAN BÜLBÜL
Neslihan ÜSTÜNDAĞ OKUR
Zeynep AY ŞENYİĞİT
This study aimed to assess the potential usage of fusidic acid in situ ocular gels for bacterial conjunctivitis treatment. The in situ gelling systems were applied to improve the bioavailability and residence time of fusidic acid in the ocular mucosa. Temperature-triggered in situ ocular gel formulations were prepared by the cold method with Poloxamer 407 and sodium carboxymethyl cellulose. The in situ gels were evaluated for pH, clarity, gelation temperature, rheological properties, mechanical properties, and in vitro drug release. The gelation temperatures of fusidic acid loaded the formulations were between 29–33°C. All prepared in situ gels showed non-Newtonian pseudoplastic flow (shear thinning system) like tear fluid at 32 ± 0.1ºC. The results of in vitro dissolution studies showed that at least 65% of fusidic acid released in 12 hours. As a result of this study, it was concluded that fusidic acid loaded in situ gels might be offered as a promising ocular tool for the treatment of bacterial conjunctivitis.
https://jrespharm.com/abstract.php?id=872
Fusidic acidin situ gelpoloxamerNaCMCocular
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
13
21
10.35333/jrp.2021.284
859
Evaluation of a diltiazem cream preparation for estimation of degradation behavior
Bahar KÖKSEL ÖZGEN
Burcu BULUT
Nagehan SARRAÇOĞLU
Asuman AYBEY DOĞANAY
Onur PINARBAŞLI
Diltiazem cream, which is used in chronic anal fissure (CAF) treatment, is known to be susceptible to hydrolysis and degradation in aqueous solutions. The major pathway of degradation is o-deacetylation which leads to formation of 'desacetyl diltiazem' and this study focuses on this degradation mechanism. In this study, degradation of diltiazem incorporated into an oil-in-water cream base was investigated. It was especially aimed to show the effect of the formulation preparation procedure on impurity formation during the diltiazem cream formulation. In this regard, preliminary studies were performed to optimize the formulation parameters for stability. The outcome of these studies was applied to the preparation procedure; the compositions of excipients were kept constant while the order of addition of excipients to the aqueous phase and the mixing time were varied. To our knowledge, there is no study published regarding the relation between this degradation and the formulation process. Formulations were characterized in terms of formation of the desacetyl diltiazem impurity with a validated stability indicating HPLC method. The cream formulation with the highest stability was obtained through mixing propylene glycol and water first and adding diltiazem active substance in the final step of formation of aqueous phase with a shortened stirring time. This preparation procedure exhibited reduced desacetyl diltiazem impurity formation.
https://jrespharm.com/abstract.php?id=859
Diltiazemcream dosage formformulationdesacetyl diltiazem impurity
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
25
33
10.35333/jrp.2021.289
870
Design and characterisation of colloidal nanocarriers for enhanced skin delivery of etodolac
Güler SARIBEY
Emine KAHRAMAN
Meryem Sedef ERDAL
Sevgi GÜNGÖR
The aim of this work was to develop colloidal nanocarriers for skin delivery of etodolac (ETD), which is a non-steroidal anti-inflammatory drug orally used for the management of acute pain and inflammation, but leads to unfavourable effects on the stomach. The oleic acid and blend of Labrasol/Trancutol P were used as oil phase and surfactant/co-surfactant mixture in the microemulsion formulations, respectively. ETD loaded microemulsions selecting the microemulsion region of pseudo-ternary phase diagrams were prepared, and then the microemulsions were characterised to confirm formation of oil in water microemulsions via optical isotropy, refractive index, droplet size, electrical conductivity, rheological behaviour and morphological analysis. In vitro permeation of ETD through porcine skin was evaluated using Franz diffusion cells for stable ETD loaded microemulsions. ATR-FTIR spectroscopy analysis was performed to elucidate interaction between the microemulsion components and stratum corneum structure on the molecular level. Confocal laser scanning microscopy analysis was further carried out to visualize skin penetration enhancement effect of the microemulsion formulation consisting of a model lipophilic fluorescent marker, Nile Red. The results indicated that the developed microemulsion formulation consisting of oleic acid, Labrasol, Transcutol P and water offer a potential approach to enhance skin delivery of ETD for topical treatment of inflammatory diseases.
https://jrespharm.com/abstract.php?id=870
Microemulsionscolloidal nanocarriersnon-steroidal anti-inflammatory drugsetodolacskin deliverytopical treatment
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
34
41
10.35333/jrp.2021.292
873
Preparation and in vitro evaluation of tacrolimus loaded liposomal vesicles by two methods: a comparative study
Shammy JINDAL
Rajendra AWASTHI
Dhananjay SINGARE
Giriraj T. KULKARNI
Psoriasis is an autoimmune disorder characterized by hyper proliferation of the epidermal layer at the typical body sites, including nails, scalps, cleft and knees. Liposomes are the best carrier for effective delivery of bioactives in the deep skin areas. In the present study, a comparative study of liposomes was carried out using thin film hydration and curvature tuned methods. Liposomes were prepared using cholesterol, soy lecithin and Span 80. The liposomes were evaluated for physical characterization, morphology, surface charge and release properties. Liposomes prepared by the thin film hydration method (formulation TACTL2) had better properties compared to liposomes prepared by the curvature tuned method (formulation TACCT2) in terms of entrapment efficiency (78.5±1.8% vs 53.4±5.6%), particle size (411.8 nm vs 630 nm), surface morphology(round and dispersed particles vs aggregates and lumps), and release profile (70.1% vs 32.87% in 12 h). Based on the results it is concluded that the thin film hydration method is better than a curvature tuned method for the preparation of liposomes.
https://jrespharm.com/abstract.php?id=873
Curvature tuned methodfilm hydration methodliposomesparticle sizepsoriasis
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
42
51
10.35333/jrp.2021.290
871
Thermodynamic protonation constant values of meclizine and buclizine in acetonitrile-water binary mixtures
İkbal Demet NANE
Ebru ÇUBUK DEMİRALAY
In the study, the retention times (tR) values for meclizine (MCZ) and buclizine (BCZ) structurally related benzhydrylpiperazine were determined to modeling the dependence of retention on the acetonitrile concentration in the mobile phase. Reversed-phase liquid chromatography (RPLC) analysis of the MCZ and BCZ was realized with polar embedded amide (15x0.46 cm I.D, 5μm) column. The mobile phase pH range is selected from 5.0-9.0 to determine the structural changes due to protonation that result from a change in pH. The different retention time were attributed to their different hydrophobicities and ionization degree. The thermodynamic protonation constant (
https://jrespharm.com/abstract.php?id=871
Benzhydrylpiperazine compoundsthermodynamic valueextrapolation methodsreversed-phase liquid chromatography
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
52
62
10.35333/jrp.2021.288
869
Electrochemical detection of antioxidant activities of 4-indolyl-5-oxo-6,6 (or 7,7) -dimethyl-1,4,5,6,7,8-hexahydroquinoline derivatives
İncilay SÜSLÜ
Sevilay ERDOĞAN KABLAN
Cihat ŞAFAK
Rahime ŞİMŞEK
Antioxidants used in different medical and industrial fields in order to prevent and delay oxidative stress. They play a crucial role in the protecting biological systems against many diseases. 1,4-dihydropyridines are known as calcium channel modulators. Electrochemical techniques are simple, cheap and fast detection techniques and require small amounts of sample, so they offer advantages over commonly used analytical methods. Voltammetric methods have been applied to investigated the antioxidant activity of compounds in different fields. The proposed work is aimed at examining the electrochemical behavior of the 1,4-dihydropyridines by differential pulse voltammetry and hence the assessment of its antioxidant activity from the cathodic reduction peak of oxygen values. The peak current due to oxygen reduction was found to be proportional to the 1,4-dihydropyridines concentration of 0.1 - 0.5 mg/mL. The coefficient of antioxidant activity of 1,4-dihydropyridine derivatives were calculated and compared each other. Nifedipine used as a reference drug that is known as the calcium channel modulator and it is used to compare the antioxidant activities of 1,4-dihydropyridine-derived compounds.
https://jrespharm.com/abstract.php?id=869
Hexahydroquinoline derivativesnifedipineantioxidant activitydifferential pulse voltammetry
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
63
71
10.35333/jrp.2021.285
866
Morphological and anatomical evaluation of herbal drugs sold under the name of gül (rosa damascena mill.) in turkey
Gülsen KENDİR
Ayşegül KÖROĞLU
Rosa damascena Mill. (Rosaceae) is commonly cultivated all over the world due to its fragrances, aromatic and medicinal properties. The plant has been usually utilized as astringent, analgesic, cardiac, and intestinal tonic in traditional medicine. This plant is cultured in mainly Isparta, Burdur, Afyon and Denizli in Turkey and known as “Isparta gülü, Şam gülü, yağ gülü”. The goal of this study was to determine whether or the samples in different cities of Turkey sold with the name of "gül" carry qualities appropriate for the definition of herbal drug. Roses samples were obtained from 5 different cities in Turkey. Morphological characteristics of all samples were investigated and their purities were checked. The standard sample was obtained from Isparta. The cross and surface sections from the sepals and petals were investigated and determined. Furthermore, the characteristic anatomical structures of the powdered samples (standard sample and purchased samples) were determined. It was observed that the samples sold were usually composed of rosebuds. In anatomical examinations, unicellular non-glandular trichomes were densely observed in the sepal and petal. Calcium oxalate crystals and glandular trichomes with multicellular head and stalk were seen both the sepal and the petal, but glandular trichomes were seen rarely on the petal. Conical papillae and striated cuticle with epidermal cells were observed on the petal. As a result, it was found that the samples examined did not have the necessary properties to be herbal drugs.
https://jrespharm.com/abstract.php?id=866
Rosa damascenaRosaceaemorphologyanatomy
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
72
79
10.35333/jrp.2021.293
874
Bioactivity-guided fractionation of a methanol leaf extract from gnetum africanum with potential anti-diabetic activity: (-)-epicatechin as the active principle
Nkeiruka Emmanuela UDEH
Charles Okeke NNADI
Aruh Otah ANAGA
Isaac Uzoma ASUZU
Dietary constituents of plants such as flavonoids are very important in ameliorating the challenges of
metabolic disorders such as diabetes mellitus. The study evaluated the antidiabetic activities of fractions and a known
flavonoid isolated from Gnetum africanum (Welw) of fasting blood sugar (FBS) in alloxan-induced diabetic albino rats.
Antidiabetic activity-guided isolation by column chromatographic (CC) separation of methanol extract and
purification of the most active CC fractions by semi-preparative high performance liquid chromatograpgy (HPLC)
yielded a known flavonoid (GAF7.4) and four other uncharacterized fractions. The structure of GAF7.4 was
elucidated based on the 1D and 2D NMR and HREIMS spectroscopic analyses. Antidiabetic activity was conducted by
alloxan-induced FBS in diabetic rats model using glibenclamide as standard. The flavonoid (GAF7.4) was identified as
(-)-epicatechin. The CC fraction 7 (50 mg/kg) elicited significant (p < 0.05) reduction in FBS of 42.3 % after 6 h. The
isolated flavonoid (GAF7.4), 10 mg/kg dose caused a significantly higher reduction in FBS of 71.4 % in alloxan
induced diabetic rats compared with 41.2 % reduction in glibenclamide (2 mg/kg) control. This represented the first
report of epicatechin in G. africanum and our findings have contributed new knowledge to antidiabetic constitutents of
the plants.
https://jrespharm.com/abstract.php?id=874
Gnetum africanumalloxanfasting blood sugar(-)-epicatechinantidiabetic
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
80
88
10.35333/jrp.2021.287
868
Hydroalcoholic extract of arum orientale ameliorates myocardial infarction induced by isoproterenol in rats
Asal JAVIDMEHR
Samin ABBASZADEH
Mehdi KIAN
Sanaz HAMEDEYAZDAN
Hamid SORAYA
Arum species have antioxidant, antimicrobial, and anti-cancer effects. However, there is no study on its possible cardioprotective effects. In the present study, the protective effects of hydro-alcoholic extract of Arum orientale (A. orientale) on isoproterenol-induced myocardial infarction (MI) were evaluated. For induction of MI the rats were received isoproterenol (100 mg/kg) for two consecutive days, whereas treated groups received 40, 80 and 160 mg/kg/day of hydroalcoholic extract of A.orientale intraperitoneally (ip) 20 min before each Isoproterenol injection. Isoproterenol-induced MI significantly increased myocardial necrosis and neutrophil infiltration. Histopathological analysis showed that A. orientale at dose of 160 mg/kg significantly reduced necrosis and neutrophil infiltration in the heart tissue (P< 0.046 and P<0.048, respectively). Induction of MI also increased myeloperoxidase (MPO) activity and peripheral neutrophil percent. While A. orientale similarly decreased MPO activity and peripheral neutrophils in blood (P<0.021 p<0.042 respectively) at dose of 160 mg/kg. Administration of the extract markedly decreased serum malondialdehyde level at dose of 80 mg/kg and creatine phosphokinase (CPK) activity with all doses. Our results for the first time reported potential cardioprotective effects of A. orientale that partially can be through suppression of inflammatory responses and reduction of lipid peroxidation following MI. However, any suggestions for potential use in MI needs further studies.
https://jrespharm.com/abstract.php?id=868
ArumMyocardial Infarctionneutrophillipid peroxidationcreatine kinase
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2021
25
1
89
98
10.35333/jrp.2021.286
867
Hepatoprotective activity of ehretia microphylla on paracetamol induced liver toxic rats
Kumarapalayam Ramakrishnan YUVARAJA
Arockiasamy SANTHIAGU
Shabbeer JASEMINE
Kasiramar GOPALASATHEESKUMAR
World wide liver toxicity is the most prevelent healthcare problem. We need to address this with herbal based medicine because herbal products have high efficacy and less side effects. Many of the Ehretia genus (Boraginaceae) have the hepatoprotective property. But Ehretia microphylla (EM) was not reported yet for its hepaptoprotective potential. Therefore the current research was aimed to evaluate the hepatoprotective action of EM. The hepatoprotective activity of EM was assessed against the paracetamol induced liver toxic rats. The chloroform and ethyl acetate extracts of EM were selected for the investigation. The dose was selected by using OECD423 guidelines. The paracetamol intoxicated rats were elevated the liver functional parameters like serum SGOT, SGPT and ALP levels and also triglyceride and total cholesterol. These elevated parameters were significantly lowered in chloroform and ethyl acetate extracts of EM pretreated rats when compared with silymarin. However the antioxidant markers including CAT, SOD, GSH and GPx were significantly increased in EM extract treated rats when compared with paracetamol induced toxic rats. It revealed the plant extracts of EM has significant hepatoprotective activity. Further, this research will useful for the isolation of active principles from EM and determining its molecular mechanisms.
https://jrespharm.com/abstract.php?id=867
LiversilymarinantioxidantBoraginaceaeEhretia