Bulletin of Faculty of Pharmacy, Cairo University最新文献

{"title":"Sapium ellipticum (Hochst) Pax leaf extract: Antioxidant potential in CCl4-induced oxidative stress model","authors":"Osasenaga Macdonald Ighodaro ,&nbsp;Oluseyi Adeboye Akinloye","doi":"10.1016/j.bfopcu.2017.11.001","DOIUrl":"10.1016/j.bfopcu.2017.11.001","url":null,"abstract":"<div><h3>Objective</h3><p>The antioxidant potential of <em>Sapium ellipticum</em> (SE) extract was examined against CCl₄-generated reactive species in experimental rats, using Butylated hydroxytoluene (BHT) and L-Ascorbic acid (L-AA) as reference antioxidants.</p></div><div><h3>Methods</h3><p>Animals were assigned to six experimental groups (n = 6): Control, CCl₄-treated, CCl₄  +  SE (400 mg dosage) treated, CCl₄  +  SE (800 mg dosage) treated, CCl₄  +  L-AA (100 mg dosage) treated and CCl₄  +  BHT (100 mg dosage) treated. Single intraperitoneal injection of CCl₄ was used to induce oxidative stress whereas treatments with SE, LAA and BHT were done orally (p.o) for 28 days.</p></div><div><h3>Results</h3><p>SE elicited notable antioxidant capacity both in the liver and kidney, mainly through anti-peroxidation and promotion of superoxide dismutase (SOD) and catalase (CAT) activities. The extract at the two doses did not differ significantly in its antioxidant activities. Relative to CCl₄-untreated group, SE particularly at 800 mg dose significantly (p &lt; .05) lowered the degree of peroxidation (69.74% and 47.75%) and improved the activities of SOD (45.12 and 51.2%) and CAT (30, 21 and 28.49%) in the liver and kidney respectively. The extract also increased reduced glutathione (GSH) level in the kidney but the change was not significant when compared with the CCl₄-untreated group.</p></div><div><h3>Conclusion</h3><p>SE extract appears to have the phyto-proficiency to protect against membrane peroxidation and improve the activities of some first line antioxidant enzymes such a SOD and CAT <em>in vivo</em>. This is probably due to its array of bioactive compounds (α-tocopherol, amentoflavone and lupeol) which we have previously identified and reported.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"56 1","pages":"Pages 54-59"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.11.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77049480","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Spectrophotometric analysis of two eye preparations, vial and drops, containing ketorolac tromethamine and phenylephrine hydrochloride binary mixture and their ternary mixture with chlorphenirmaine maleate","authors":"Marwa A.A. Ragab ,&nbsp;Fawzy A. El Yazbi ,&nbsp;Ekram M. Hassan ,&nbsp;Essam F. Khamis ,&nbsp;Mohamed M.A. Hamdy","doi":"10.1016/j.bfopcu.2018.03.004","DOIUrl":"10.1016/j.bfopcu.2018.03.004","url":null,"abstract":"<div><p>Ketorolac tromethamine, KTC and phenylephrine hydrochloride, PHE binary mixture is co-formulated as eye vial, while their ternary mixture with chlorpheniramine maleate is co-formulated as eye drops. The existing work utilizes different spectrophotometric methods which are considered to be simple and rapid for the determination of both mixtures. These methods include: zero-order (D⁰), first derivative (D¹), derivative (DR) or difference ratio (R.D), delta absorbance (ΔA) and finally convolution of derivative data using discrete Fourier functions (FFD). In the binary mixture, KTC is assayed using D⁰, D¹ and ΔA methods with no interference from PHE, while PHE needed some spectroscopic treatments for its analysis due to the spectral overlap of KTC with its maximum wavelength (λ_max) at 273 nm. Such treatments involve D¹ R.D, D²R, FFD² and ΔA methods. In the ternary mixture, KTC is assayed using D⁰ and D¹ with no interference from both PHE and CPM, while R.D, D¹R and FFD² are used to assay both PHE and CPM to resolve the overlap in their spectra. Linear regression lines were obtained over the concentration ranges 1–18 and 6–48 μg.mL⁻¹ for KTC and PHE (binary mixture), respectively and 2–9, 1–18 and 2–9 μg.mL⁻¹ for CPM, KTC and PHE (ternary mixture), respectively yielding high correlation coefficients values (higher than 0.999). The lowest LOQ value for KTC (0.46 μg.mL⁻¹) was obtained upon using the D¹ method in the binary mixture while the R.D method yielded the lowest LOQ values for both PHE (0.34 μg.mL⁻¹) and CPM (0.97 μg.mL⁻¹) in the ternary mixture.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"56 1","pages":"Pages 91-100"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2018.03.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85495671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Identification of possible Ser/Thr/Tyr phosphorylation sites in the fungal histidine kinase CaNik1p by peptide array technique","authors":"Mohammed El-Mowafy,&nbsp;Ursula Bilitewski","doi":"10.1016/j.bfopcu.2018.03.007","DOIUrl":"10.1016/j.bfopcu.2018.03.007","url":null,"abstract":"<div><p>CaNik1p is a histidine kinase (HK) that is present in <em>Candida albicans</em>. It was found to be a target for antifungal activities on the hyperosmotic glycerol pathway. The protein has two well-known phosphorylation sites (P-sites); His510 and Asp924, that were found to be crucial for maintaining the fungicidal sensitivity. Our previous work showed that the double mutated protein, in H510 and D924, was still possessing kinase activity. In this study, we aimed to identify additional possible P-sites in this HK. Therefore, we constructed a peptide array that covers the full length protein. Incubation of the purified His-tagged CaNik1p with the peptide array in the presence of radioactive ATP [γ-³²P] revealed the possible P-sites in each peptide. We classified the peptides according to their intensities. Peptides bearing His510 and D924 showed either null or very weak intensities. The highest intensity was corresponding to the peptide containing the amino acid T994, while lower intensities were related mainly to serine and threonine residues and to lower extent to tyrosine amino acid. We could show for the first time the detection of additional P-sites in CaNik1p that might contribute in the signalling pathways of <em>C. albicans</em>. Moreover, the protocol used in this study allows for direct focusing and prediction of the possible Ser, Thr, and Tyr phosphoaccepting residues in the newly discovered kinases.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"56 1","pages":"Pages 68-72"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2018.03.007","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85260216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antihyperglycemic activity of Caralluma quadrangula in streptozotocin-induced diabetic rats","authors":"Essam Abdel-Sattar ,&nbsp;Shohda A. EL-Maraghy ,&nbsp;Riham Salah El-Dine ,&nbsp;Sherine M. Rizk","doi":"10.1016/j.bfopcu.2017.07.002","DOIUrl":"10.1016/j.bfopcu.2017.07.002","url":null,"abstract":"<div><p>Diabetes of type 2 is a worldwide epidemic disease of global prevalence. <em>Caralluma quadrangula</em> is wild Saudi plant used by traditional healers as antidiabetic, in case of hunger, and many other diseases. Nothing was reported to justify the use of the plant in case of diabetes. The plant material was extracted with water and with methanol, the methanol fraction was further fractionated into chloroform, <em>n</em>-butanol, in addition to the remaining mother liquor. The water and methanolic extracts as well as different methanolic fractions were evaluated in STZ-induced diabetic rats for their antihyperglycaemic activity. The results showed a significant decrease in fasting blood glucose levels in diabetic treated rats after the administration of most of the extracts and fractions of <em>C. quadrangula</em> and glibenclamide. The most potent activity was shown by administration of the methanolic extract (200<!--> <!-->mg/kg), chloroform, <em>n</em>-butanol fraction at dose of 100<!--> <!-->mg/kg, as well as the major pregnane glycoside russelioside B isolated from <em>C. quadrangula.</em> In conclusion, this study proved the traditional use of <em>C. quadrangula</em> in diabetes mellitus.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 269-272"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.07.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86995720","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Influence of surface charge on the in vitro protein adsorption and cell cytotoxicity of paclitaxel loaded poly(ε-caprolactone) nanoparticles","authors":"Sathyamoorthy Nandhakumar ,&nbsp;Magharla Dasaratha Dhanaraju ,&nbsp;Vankayalu Devendran Sundar ,&nbsp;Battu Heera","doi":"10.1016/j.bfopcu.2017.06.003","DOIUrl":"10.1016/j.bfopcu.2017.06.003","url":null,"abstract":"<div><p>The biokinetic fate of polymeric nanoparticles in the physiological milieu is strongly influenced by its properties such as size, surface charge and surface affinity. The electrostatic properties of the polymeric nanoparticles and, thereby, the reliant properties such as cellular interactions, reactivity and toxicity, can be tailored by modulating the surface charge. Therefore, the present study aimed at studying the influence of surface charge on the physicochemical properties, <em>in vitro</em> protein adsorption and cell cytotoxicity of poly(ε-caprolactone) (PCL) nanoparticles (NPs). Paclitaxel loaded PCL nanoparticles were obtained by emulsion solvent evaporation extraction technique and differently charged using ionic surfactants. The NPs were characterized for size, zeta potential, morphology, entrapment and release. <em>In vitro</em> protein adsorption and cytotoxicity of NPs with different surface charge was investigated. The prepared NPs were rounded with a smooth surface and had a particle size less than 250<!--> <!-->nm with narrow distribution and high entrapment efficiency (&gt;80%). The zeta potential of the particles varied between −22<!--> <!-->mV and +16<!--> <!-->mV depending on its composition. The <em>in vitro</em> protein adsorption studies revealed that positively charged NPs adsorbed more proteins than other formulations. The cytotoxicity studies on MCF-7 cells exhibited that positively charged NPs engender the highest cell inhibition due to preferential uptake based on electrostatic interactions with cell membranes. The results suggest that surface charge could be undeniably significant in determining the protein adsorption and cellular interactions and must be intently considered during the design of colloidal particles to impart better performance in the physiological system.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 249-258"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.06.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85639146","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Multivariate optimization for simultaneous determination of aspirin and simvastatin by reverse phase liquid chromatographic method using AQbD approach","authors":"Kalpana G. Patel ,&nbsp;Apeksha T. Patel ,&nbsp;Purvi A. Shah ,&nbsp;Tejal R. Gandhi","doi":"10.1016/j.bfopcu.2017.08.003","DOIUrl":"10.1016/j.bfopcu.2017.08.003","url":null,"abstract":"<div><p>The present study describes the development of a robust method for the separation of aspirin and simvastatin using reverse phase high performance liquid chromatographic method on Kintex reverse phase C₁₈ column (5<!--> <!-->μm, 250<!--> <!-->mm<!--> <!-->×<!--> <!-->4.6<!--> <!-->mm) with UV detection at 234<!--> <!-->nm. Box-Behnken design was applied for multivariate optimization of the experimental conditions of RP-HPLC for obtaining desired chromatographic resolution with limited number of experiments. Risk assessment was performed to identify the critical method parameters. Three independent parameters; volume of acetonitrile, molarity of buffer and flow rate were used to design mathematical models and study the in depth effects of these independent factors on various responses. The optimized and predicted condition consisted of acetonitrile and potassium dihydrogen orthophosphate buffer pH 2.9 adjusted with orthophosphoric acid (83.89:16.11,<!--> <!-->v/v) as mobile phase at a flow rate of 0.93<!--> <!-->ml/min. Using these optimum conditions, baseline separation of both drugs with good resolution and a run time of less than 6<!--> <!-->min was achieved. Perturbation plot revealed that the most important factor affecting the selected responses was volume of acetonitrile. Percent recoveries in terms of accuracy for both drugs at all three levels was found in the range of 99.15–101.86%. The pooled % relative standard deviation values for repeatability and intermediate precision studies was found to be less than 2% for both drugs. Hence, a robust, simple, accurate and reproducible high performance liquid chromatographic method was developed and validated and could be applied for routine quality control testing.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 293-301"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.08.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78063730","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"TLC-densitometric and first derivative spectrophotometric methods for determination of cefoxitin-sodium in presence of its alkali-induced degradation product","authors":"Khalid Abdel-Salam M. Attia ,&nbsp;Omar Abdel-Aziz ,&nbsp;Nancy Magdy ,&nbsp;Ghada F. Mohamed","doi":"10.1016/j.bfopcu.2017.09.004","DOIUrl":"10.1016/j.bfopcu.2017.09.004","url":null,"abstract":"<div><p>Two simple and accurate methods were developed for quantitative estimation of cefoxitin sodium in presence of its open ring alkali-induced degradation product. The first method was based on TLC separation of the drug from its alkali-induced degradation product followed by densitometric measurement of the intact drug at 254<!--> <!-->nm. The proposed method obeys Beer’s law in range (1–20<!--> <!-->µg/band). The second method was first derivative (¹D) spectrophotometric method; was based on measurement of amplitude of first order spectra of cefoxitin sodium (in the range of 4–36<!--> <!-->µg<!--> <!-->mL⁻¹) at 282<!--> <!-->nm which showed zero crossing point of its degradation product. The two methods were validated according to ICH guideline for accuracy, precision and were successfully applied for the determination of the drug in pure form and pharmaceutical preparation in presence of its alkali-induced degradation product.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 281-286"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.09.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79987844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chromatographic methods for the simultaneous determination of binary mixture of Saxagliptin HCl and Metformin HCl","authors":"Hanan A. Merey,&nbsp;Nesrin K. Ramadan,&nbsp;Sherine S. Diab,&nbsp;Azza A. Moustafa","doi":"10.1016/j.bfopcu.2017.04.002","DOIUrl":"10.1016/j.bfopcu.2017.04.002","url":null,"abstract":"<div><p>Two chromatographic methods were suggested for the simultaneous determination of a binary mixture containing Saxagliptin HCl (SAG) and Metformin HCl (MET). First method was RP-HPLC method. Chromatographic separation was done on Kinetex™ column–C₁₈ (4.6<!--> <!-->×<!--> <!-->150<!--> <!-->mm, 2.6<!--> <!-->µm) using mobile phase consisted of acetonitrile:phosphate buffer pH<!--> <!-->=<!--> <!-->4.5 ±<!--> <!-->0.1 adjusted with orthophosphoric acid (13:87, v/v). Isocratic elution at a flow rate 1.5<!--> <!-->mL/min and UV detection at 220.0<!--> <!-->nm was performed. Second method was spectro-densitometric method. Chromatographic separation was done on precoated silica gel aluminium plates 60 F₂₅₄ as a stationary phase and developing system consisting of chloroform:methanol:formic acid (80:20:0.3, by volume). The density of the separated bands was measured by UV detector at 210.0<!--> <!-->nm. The proposed methods were validated as per the ICH guidelines parameters like Linearity, precision, accuracy, selectivity, limit of detection and limit of quantitation. Statistical comparison was done between the obtained results and those obtained by the reported methods, showing no significant difference with respect to accuracy and precision.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 311-317"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.04.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85750923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Acute and subchronic toxicity evaluation of methanol stem-bark extract of Ximenia americana Linn (Olacaceae) in Wistar rats","authors":"Isaac A. Agyigra,&nbsp;Jane I. Ejiofor,&nbsp;Mohammed G. Magaji","doi":"10.1016/j.bfopcu.2017.08.004","DOIUrl":"10.1016/j.bfopcu.2017.08.004","url":null,"abstract":"<div><p><em>Ximenia americana</em> is used in African ethno-medicine for spasmodic bowel diseases with stem bark particularly used for ulcers. This study evaluated the toxicity-profile of methanol stem-bark extract. Extract doses were selected from estimated oral median lethal dose (LD₅₀) of acute toxicity test. Ten male Wistar rats in 4-groups, weekly weighed and daily treated orally per body-weight for 28<!--> <!-->days with normal-saline and extract-doses (250, 500, 1000<!--> <!-->mg/kg) respectively were euthanized. Blood for biochemical and haematological analyses were collected into plain and anticoagulated (EDTA) sample-bottles respectively from each group. Vital-organs were isolated, weighed and fixed in buffered-formalin fixatives for histo-analyses. Mean<!--> <!-->±<!--> <!-->standard-error of mean and statistical-significance at (<em>p</em> <!-->≤<!--> <!-->0.05) of obtained-data were evaluated. The extract at up to 5000<!--> <!-->mg/kg caused no mortality or behavioural toxic-signs and thus, oral LD₅₀ was estimated to be greater than 5000<!--> <!-->mg/kg. No changes in organ-sizes, body-weights or anatomy of brain, heart, liver and stomach occurred, but at 1000<!--> <!-->mg/kg, kidney showed vascular-congestion with polymorphonuclear cells, lungs had consolidated areas of polymorphs infiltration, while spleen had distorted germinal-centres. Liver enzymes and urea levels were not altered significantly, but a dose dependent significant increase in total-protein only at 1000<!--> <!-->mg/kg; and significant reduction in albumin level at 500 and 1000<!--> <!-->mg/kg were observed. The observed dose-dependent reduction in creatinine was not significant. Total-calcium and chloride ion concentrations increased significantly only at 250<!--> <!-->mg/kg. In conclusion, acute oral administration of methanol stem-bark extract of <em>Ximenia americana</em> was relatively non-toxic in mice, but minimal anatomical changes in kidney, lungs and spleen occurred when used for few weeks in rats.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 263-267"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.08.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91249638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancement of antibacterial activity of ciprofloxacin hydrochloride by complexation with sodium cholate","authors":"Uduma E. Osonwa ,&nbsp;Jane I. Ugochukwu ,&nbsp;Eze E. Ajaegbu ,&nbsp;Kingsley I. Chukwu ,&nbsp;Ricardo B. Azevedo ,&nbsp;Charles O. Esimone","doi":"10.1016/j.bfopcu.2017.09.006","DOIUrl":"10.1016/j.bfopcu.2017.09.006","url":null,"abstract":"<div><p>Ciprofloxacin is a broad spectrum bactericidal anti-infective agent of the fluoroquinolones class used in treatment of many bacterial infections. In recent times, there has been increasing resistance to the antibiotic. In this work, we investigated the effect of making an ion- pair complex of Ciprofloxacin – hydrochloride with Sodium cholate on bacterial activity. The optimal ratio of the reactants and pH were determined using UV spectrometry. The complex was characterized by octanol-water partitioning, melting point, and IR spectrometry. The antibacterial activity of the complex was determined against <em>Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae,</em> and <em>Streptococcu</em>s <em>pneumoniae</em> by the agar-well diffusion method. The complex was whitish to off-white in color and crystalline, with a melting point of 238 °C. The stoichiometry of the complex shows a molar ratio of 1:1 of sodium cholate to ciprofloxacin. The best pH for complexation was pH 9. The complex partitioned 3.38 times into octanol than in water. The FTIR revealed interaction between the 4-nitrogen atom in the 7-piperazinyl group of ciprofloxacin and the carbonyl of the cholate. The drug in complex form gave double the antibacterial activity of the uncomplexed drug. This study showed that development of hydrophobic ion pair complex enhances antibacterial activity of ciprofloxacin hydrochloride.</p></div>","PeriodicalId":9369,"journal":{"name":"Bulletin of Faculty of Pharmacy, Cairo University","volume":"55 2","pages":"Pages 233-237"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bfopcu.2017.09.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88544379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}