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Sci. Pharm., Volume 80, Issue 3 (September 2012) – 20 articles , Pages 497-788

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Article
Improvement of the Prediction Power of the CoMFA and CoMSIA Models on Histamine H3 Antagonists by Different Variable Selection Methods
Sci. Pharm. 2012, 80(3), 547-566; https://doi.org/10.3797/scipharm.1204-19 - 24 May 2015
Cited by 17 | Viewed by 900
Abstract
The aim of this study is to enhance the predictivity power of CoMFA and CoMSIA models by means of different variable selection algorithms. The genetic algorithm (GA), successive projection algorithm (SPA), stepwise multiple linear regression (SW-MLR), and the enhanced replacement method (ERM) were [...] Read more.
The aim of this study is to enhance the predictivity power of CoMFA and CoMSIA models by means of different variable selection algorithms. The genetic algorithm (GA), successive projection algorithm (SPA), stepwise multiple linear regression (SW-MLR), and the enhanced replacement method (ERM) were used and tested as variable selection algorithms. Then, the selected variables were used to generate a simple and predictive model by the multilinear regression algorithm. A set of 74 histamine H3 antagonists were split into 40 compounds as a training set, and 17 compounds as a test set, by the Kennard-Stone algorithm. Before splitting the data, 17 compounds were randomly selected from the pool of the whole data set as an evaluation set without any supervision, pretreatment, or visual inspection. Among applied variable selection algorithms, ERM had noticeable improvement on the statistical parameters. The r2 values of training, test, and evaluation sets for the ERM-MLR model using CoMFA fields were 0.9560, 0.8630, and 0.8460 and using the CoMSIA fields were 0.9800, 0.8521, and 0.9080, respectively. In this study, the principles of organization for economic cooperation and development (OECD) for regulatory acceptability of QSARs are considered. Full article
Article
Development and Characterization of Pharmacokinetic Parameters of Fast-Dissolving Films Containing Levocetirizine
Sci. Pharm. 2012, 80(3), 779-788; https://doi.org/10.3797/scipharm.1205-15 - 22 Jul 2012
Cited by 21 | Viewed by 1223
Abstract
A fast-dissolving film containing levocetirizine, a non-sedative antihistamine drug, was developed using pullulan, xanthan gum, propylene glycol, and tween 80 as the base materials. The drug content of the prepared films was within an acceptable limit as prescribed by the USP. The film [...] Read more.
A fast-dissolving film containing levocetirizine, a non-sedative antihistamine drug, was developed using pullulan, xanthan gum, propylene glycol, and tween 80 as the base materials. The drug content of the prepared films was within an acceptable limit as prescribed by the USP. The film exhibited excellent stability for four months when stored at 40 °C and 75% humidity. In vitro dissolution studies suggested a rapid disintegration, in which most of levocetirizine (93.54 ± 3.9%) dissolved within 90 seconds after insertion into the medium. Subse-quently, Sprague–Dawley rats were used to compare the pharmacokinetic properties of the film preparation administered to the oral cavity, to those with oral administration of the pure drug solution. The pharmacokinetic parameters were similar between the two groups in which AUC0–t (ng h/ml), AUC0–∞ (ng h/ml) Cmax (ng/ml), Tmax (min), Kel (h−1), and t1/2 (h) of the reference were 452.033 ± 43.68, 465.78 ± 48.16, 237.16 ± 19.87, 30, 0.453 ± 0.051, and 1.536 ± 0.118, respectively, for the film formulation 447.233 ± 46.24, 458.22 ± 46.74, 233.32 ± 17.19, 30, 0.464 ± 0.060, and 1.496 ± 0.293, respectively. These results suggest that the present levocetirizine containing fast-dissolving film is likely to become one of the choices to treat different allergic conditions. Full article
Article
Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives
Sci. Pharm. 2012, 80(3), 531-546; https://doi.org/10.3797/scipharm.1204-23 - 25 Jun 2012
Cited by 17 | Viewed by 856
Abstract
A new series of pyrazolo[3,4-d]pyrimidines has been synthesized. The new compounds were tested for their antitumor activity on 60 different cell lines, and some of the compounds were found to have potent antitumor activity. In particular, 2-hydroxybenzaldehyde [1-(4-chlorophenyl)-3-methyl-1H-pyrazolo-[3,4-d [...] Read more.
A new series of pyrazolo[3,4-d]pyrimidines has been synthesized. The new compounds were tested for their antitumor activity on 60 different cell lines, and some of the compounds were found to have potent antitumor activity. In particular, 2-hydroxybenzaldehyde [1-(4-chlorophenyl)-3-methyl-1H-pyrazolo-[3,4-d]pyrimidin-4-yl]hydrazone (VIIa) was found to be the most effective among the other derivatives, showing IC50 values of 0.326 to 4.31 μM on 57 different cell lines. Full article
Article
Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
Sci. Pharm. 2012, 80(3), 765-778; https://doi.org/10.3797/scipharm.1201-01 - 18 Jun 2012
Cited by 8 | Viewed by 767
Abstract
This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as [...] Read more.
This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as a volatile cosurfactant. The ME formulations enhanced progesterone transdermal flux compared to the saturated drug solution in 14% aqueous propylene glycol (control). Ethanol-containing ME (EME) was better than the ethanol-free system (EFME). Open application of EFME produced a marginal reduction in flux compared to occlusive application. For EME, open application reduced the flux by 26–28% with the flux remaining significantly higher than that obtained with EFME. The mechanistic studies revealed synergism between ethanol and EFME with EME, producing greater flux than the sum of fluxes obtained from 40% ethanol in water and EFME. Penetration enhancement and supersaturation played a role in enhanced transdermal delivery, but other mechanisms were also possible. This study thus introduced EME as a transdermal delivery system for progesterone with good potential for open application as a spray. Full article
Article
Nanostructured Lipid Carriers (NLC)-Based Gel for the Topical Delivery of Aceclofenac: Preparation, Characterization, and In Vivo Evaluation
Sci. Pharm. 2012, 80(3), 749-764; https://doi.org/10.3797/scipharm.1202-12 - 18 Jun 2012
Cited by 78 | Viewed by 1844
Abstract
The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon [...] Read more.
The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon 90G as the co-surfactant were used. NLCs were prepared by melt-emulsification, low-temperature solidification, and high-speed homogenization methods. Characterization of the NLC dispersion was carried out through particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and an in vitro release study. The anti-inflammatory effect of the NLC gel was assessed by the rat paw edema technique and compared to marketed aceclofenac gel. The NLC dispersions exhibited d90% between 233 nm and 286 nm. All of the NLC showed high entrapment efficiency ranging from 67% to 82%. The particle size of NLC was further confirmed by the SEM study. The result of DSC showed that aceclofenac was dispersed in NLC in an amorphous state. Both the entrapment and release rate were affected by the percentage of oleic acid, but the method of preparation affected only the entrapment efficiency. The nanoparticulate dispersion was suitably gelled and assessed for in vitro permeation. Finally, NLC-based gels were found to possess superior (almost double) the anti-inflammatory activity compared to the marketed product. The anti-inflammatory activity of NLC gel showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel. Full article
Article
Impact of Adjunctive Therapy with Chlorella vulgaris Extract on Antioxidant Status, Pulmonary Function, and Clinical Symptoms of Patients with Obstructive Pulmonary Diseases
Sci. Pharm. 2012, 80(3), 719-730; https://doi.org/10.3797/scipharm.1202-06 - 18 Jun 2012
Cited by 15 | Viewed by 1020
Abstract
This present trial investigated the efficacy of supplementation with Chlorella vulgaris, a bioactive microalga rich in macro- and micronutrients, in the improvement of biochemical and clinical symptoms in patients with obstructive pulmonary disorders. Ninety-seven patients with chronic obstructive pulmonary disease (COPD) or [...] Read more.
This present trial investigated the efficacy of supplementation with Chlorella vulgaris, a bioactive microalga rich in macro- and micronutrients, in the improvement of biochemical and clinical symptoms in patients with obstructive pulmonary disorders. Ninety-seven patients with chronic obstructive pulmonary disease (COPD) or asthma who were under conventional treatment regimens were randomly assigned to C. vulgaris extract (CVE) (n=48; 2700 mg/day) or no adjunctive therapy (n=49) for eight weeks. Serum levels of antioxidants along with spirometric parameters and clinical symptoms were evaluated pre- and post-trial. The magnitude of increases in the concentrations of glutathione, vitamin E, and vitamin C, and activities of glutathione peroxidase, catalase, and superoxide dismutase enzymes were all significantly greater in the CVE vs. control group (p<0.05). In spite of increases, none of the assessed spirometric parameters (FVC, FEV1, FEV1/FVC, and FEF25–75%) did significantly differ by the end of the trial in the study groups, apart from a significant elevation of FEV1 in the control group (p=0.03). The frequency of coughing, shortness of breath, wheezing, and sputum brought up were all significantly reduced in both CVE and control groups (p<0.05). The rate of improvement for sputum brought up and wheezing were significantly greater in the CVE group compared to the control group (p<0.05). Although CVE was found to ameliorate serum antioxidant status, its supplementation was not associated with any broncho-dilatory activity. The results of the present trial do not support any clinical efficacy for CVE in patients with obstructive pulmonary disorders. Full article
Article
The Gastroprotective Role of Acanthus ilicifolius – A Study to Unravel the Underlying Mechanism of Anti-Ulcer Activity
Sci. Pharm. 2012, 80(3), 701-718; https://doi.org/10.3797/scipharm.1108-11 - 18 Jun 2012
Cited by 18 | Viewed by 1027
Abstract
Acanthus ilicifolius (Acanthaceae), a mangrove medicinal plant, is widely used by the local inhabitants of the Sundarbans (India) to treat a variety of diseases. As a part of our continued search for novel bioactive products from mangrove medicinal plants, we were able to [...] Read more.
Acanthus ilicifolius (Acanthaceae), a mangrove medicinal plant, is widely used by the local inhabitants of the Sundarbans (India) to treat a variety of diseases. As a part of our continued search for novel bioactive products from mangrove medicinal plants, we were able to document the anti-inflammatory effects of this plant. In the present study, we have performed a detailed evaluation of the gastroprotective activity of the methanolic extract of Acanthus ilicifolius using different models of gastric ulceration. Unlike the conventional non-steroidal anti-inflammatory drugs, a methanolic extract of Acanthus ilicifolius leaves (MEAL) possessing significant anti-inflammatory properties, as revealed from our previous studies displayed in rats in dosages of 200 mg and 400 mg / kg BW after intraperitoneal administration, showed significant protective activity (anti-ulcer activity) against the gastric lesions induced by aspirin, indomethacin, stress, ethanol, and pylorus ligation. In pylorus-ligated rats, administration of Methanolic extract of Acanthus ilicifolius leaves (MEAL) significantly decreased gastric volume, acidity, and peptic activity. Moreover, pre-treatment with MEAL significantly restored the levels of reduced glutathione (GSH) and the antioxidant enzyme superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPX), along with significant inhibition of both lipid peroxidation and myeloperoxidase (MPO) activity in pylorus-ligated animals. Ulceration induced with ethanol was significantly inhibited with MEAL, and the extract also resulted in the reduction of both lipid peroxidation and myelo-peroxidase activity. Furthermore, in this experimental model, administration of MEAL improved the activities of SOD, CAT, GSH, and GPX. A similar pattern of action was also noticed in cold-restraint stress-induced (CRS) ulceration, where MEAL pre-treatment inhibited CRS-induced ulceration, improved the status of antioxidant enzymes, and also reduced the level of lipid peroxides. These results suggest that extracts of the leaves of Acanthus ilicifolius may exhibit anti-ulcer activities additional to the anti-inflammatory properties. Full article
Article
Simultaneous Determination of Celecoxib, Erlotinib, and its Metabolite Desmethyl-Erlotinib (OSI-420) in Rat Plasma by Liquid chromatography/Tandem Mass Spectrometry with Positive/Negative Ion-Switching Electrospray Ionisation
Sci. Pharm. 2012, 80(3), 633-646; https://doi.org/10.3797/scipharm.1205-09 - 18 Jun 2012
Cited by 19 | Viewed by 916
Abstract
A new method for the simultaneous determination of celecoxib, erlotinib, and its active metabolite desmethyl-erlotinib (OSI-420) in rat plasma, by liquid chromatography/tandem mass spectrometry with positive/negative ion-switching electrospray ionization mode, was developed and validated. Protein precipitation with methanol was selected as the method [...] Read more.
A new method for the simultaneous determination of celecoxib, erlotinib, and its active metabolite desmethyl-erlotinib (OSI-420) in rat plasma, by liquid chromatography/tandem mass spectrometry with positive/negative ion-switching electrospray ionization mode, was developed and validated. Protein precipitation with methanol was selected as the method for preparing the samples. The analytes were separated on a reverse-phase C18 column (50mm×4.6mm i.d., 3μ) using methanol: 2 mM ammonium acetate buffer, and pH 4.0 as the mobile phase at a flow rate 0.8 mL/min. Sitagliptin and Efervirenz were used as the internal standards for quantification. The determination was carried out on a Theremo Finnigan Quantam ultra triple-quadrupole mass spectrometer, operated in selected reaction monitoring (SRM) mode using the following transitions monitored simultaneously: positive m/z 394.5→278.1 for erlotinib, m/z 380.3→278.1 for desmethyl erlotinib (OSI-420), and negative m/z −380.1→−316.3 for celecoxib. The limits of quantification (LOQs) were 1.5 ng/mL for Celecoxib, erlotinib, and OSI-420. Within- and between-day accuracy and precision of the validated method were within the acceptable limits of < 15% at all concentrations. The quantitation method was successfully applied for the simultaneous estimation of celecoxib, erlotinib, and desmethyl erlotinib in a pharmacokinetic study in Wistar rats. Full article
Review
Development of Antimetastatic Drugs by Targeting Tumor Sialic Acids
Sci. Pharm. 2012, 80(3), 497-508; https://doi.org/10.3797/scipharm.1205-01 - 18 Jun 2012
Cited by 17 | Viewed by 802
Abstract
One-third of all cancer categories in clinics have a high incidence of neoplasm metastasis. Neoplasm metastasis is one of the leading causes of cancer deaths. However, the prevailing therapeutic approach to this pathogenic process is presently unsatisfactory. Paradoxically to our efforts and expectations, [...] Read more.
One-third of all cancer categories in clinics have a high incidence of neoplasm metastasis. Neoplasm metastasis is one of the leading causes of cancer deaths. However, the prevailing therapeutic approach to this pathogenic process is presently unsatisfactory. Paradoxically to our efforts and expectations, except for some antibodies, no obvious improvements and therapeutic benefits in currently used drugs have been achieved until now. Therapeutic benefits in late-stage or elderly cancer patients are especially poor and useless. One of the reasons for this, we would guess, is the lack of therapeutic targets specifically related to neoplasm metastasis. In order to enhance the therapeutic efficacy, the development of antimetastatic drugs transcending from current drug-screening pathways is urgently needed. Antimetastatic drugs targeting aberrantly sialylated in tumors have evolved for about a quarter of a century and might be a future therapeutic option other than the currently utilized antimetastatic drugs, such as antivascular and MMP inhibitors. Since neoplasm tissues often manifest high levels of sialic acids and sialyl antigens or glycoligands, some types of sialic acid analogue, such as N-glycolylneuraminic acid (Nau5Gc), occurred in most tumor tissues which is normally absent in most humans. Consequently, more attention is needed to work with new therapeutic approaches to target these changes. This review addresses and discusses the latest six types of therapeutic approaches targeting sialic acids in metastatic tissues. Full article
Communication
Comparative Study of the Cytotoxicity and Genotoxicity of Alpha- and Beta-Asarone
Sci. Pharm. 2012, 80(3), 663-668; https://doi.org/10.3797/scipharm.1204-21 - 31 May 2012
Cited by 29 | Viewed by 1079
Abstract
The cytotoxicity of alpha- and beta-asarone was investigated with the BrdU assay in HepG2-cells. Alpha-asarone was found to be more toxic than beta-asarone after 24 hours of treatment. Investigation of the genotoxicity using the micronucleus assay in the HepG2-cell system showed that only [...] Read more.
The cytotoxicity of alpha- and beta-asarone was investigated with the BrdU assay in HepG2-cells. Alpha-asarone was found to be more toxic than beta-asarone after 24 hours of treatment. Investigation of the genotoxicity using the micronucleus assay in the HepG2-cell system showed that only after metabolic activation by a liver microsomal preparation, beta-asarone was able to induce micronuclei at concentrations higher than 50 μg/mL. Full article
Article
Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Prazosin, Terazosin, and Doxazosin in Pharmaceutical Formulations
Sci. Pharm. 2012, 80(3), 619-632; https://doi.org/10.3797/scipharm.1204-15 - 22 May 2012
Cited by 18 | Viewed by 1191
Abstract
The current study was carried out with an attempt to separate similarly structured title drugs by liquid chromatography. Spectrophotometric techniques were generally insufficient under these conditions because of the spectral overlapping of drugs with similar functional groups. The pharmaceutical drugs prazosin, terazosin, and [...] Read more.
The current study was carried out with an attempt to separate similarly structured title drugs by liquid chromatography. Spectrophotometric techniques were generally insufficient under these conditions because of the spectral overlapping of drugs with similar functional groups. The pharmaceutical drugs prazosin, terazosin, and doxazosin contain the same parent quinazoline nucleus, thus making it especially difficult to separate the former two drugs because of their very similar structures. A simple and sensitive method for the routine determination of these drugs in pharmaceutical formulations was attempted. We found that the mobile phase consisting of A: ACN–diethylamine (0.05 ml), B: methanol, and C: 10 mM Ammonium acetate separated these drugs effectively. Separations were carried out on a new Kromasil C18 column (250 × 4.6 mm, 5.0 μm) at 254 nm wavelength. The calibration curve was found to be linear in the range of 2–500 μg/ml. The stated method was then validated in terms of specificity, linearity, precision, and accuracy. Additionally, the proposed method reduced the duration of the analysis. Full article
Article
Identification and Characterization of Potential Impurities in Raloxifene Hydrochloride
Sci. Pharm. 2012, 80(3), 605-618; https://doi.org/10.3797/scipharm.1204-13 - 22 May 2012
Cited by 1 | Viewed by 1221
Abstract
During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to [...] Read more.
During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxy-phenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy]]benzoate) [Impurity: 6]; HHBA (1-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]ethanone) [Im-purity: 7]; 7-MARLF (7-Acetyl-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-[2-(piperidin-1-yl)ethoxy]phenyl methanone) [Impurity: 8]; of which impurities 5–8 are reported for the first time. Full article
Article
A Rapid, Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Formoterol Fumarate, Tiotropium Bromide, and Ciclesonide in a Pulmonary Drug Product
Sci. Pharm. 2012, 80(3), 591-604; https://doi.org/10.3797/scipharm.1204-06 - 22 May 2012
Cited by 13 | Viewed by 1790
Abstract
A stability-indicating reversed-phase high performance liquid chromatography (RP-HPLC) method was developed for the simultaneous determination of Formoterol fumarate (FOR), Tiotropium bromide (TRI), and Ciclesonide (CLS) in a pulmonary drug product. The desired chromatographic separation was achieved on the Zorbax SB C8, 5 μm [...] Read more.
A stability-indicating reversed-phase high performance liquid chromatography (RP-HPLC) method was developed for the simultaneous determination of Formoterol fumarate (FOR), Tiotropium bromide (TRI), and Ciclesonide (CLS) in a pulmonary drug product. The desired chromatographic separation was achieved on the Zorbax SB C8, 5 μm (150 x 4.6 mm) column, using gradient elution at 230 nm detector wavelength. The optimized mobile phase consisted of a 0.2 % v/v perchloric acid as solvent-A and acetonitrile as solvent-B. The developed method separated FOR, TRI, and CLS in the presence of its five unknown degradation products within 10 minutes. The stability-indicating capability was established by forced degradation experiments and the separation of unknown degradation products. The developed RP-HPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method was applied for the simultaneous estimation of FOR, TRI, and CLS in commercially available Triohale® pMDI (Pressurized Metered-Dose Inhaler) samples. Furthermore, this method can be extended for individual estimation of FOR, TRI, and CLS in various commercially available pulmonary dosage forms. Full article
Article
Formulation and Optimization of Clotrimazole-Loaded Proniosomal Gel Using 32 Factorial Design
Sci. Pharm. 2012, 80(3), 731-748; https://doi.org/10.3797/scipharm.1201-03 - 03 May 2012
Cited by 24 | Viewed by 974
Abstract
The main aim of the study was to develop and statistically optimize the proniosomal gel for enhanced transdermal delivery using 32 factorial designs to investigate the influence of both non-ionic surfactant and cholesterol to maximize the entrapment efficiency and flux. The concentration [...] Read more.
The main aim of the study was to develop and statistically optimize the proniosomal gel for enhanced transdermal delivery using 32 factorial designs to investigate the influence of both non-ionic surfactant and cholesterol to maximize the entrapment efficiency and flux. The concentration of non-ionic surfactant and cholesterol were taken as independent variables, while entrapment efficiency and flux were taken as dependent variables. The study showed that the entrapment efficiency depends on both cholesterol and surfactant, whereas permeation flux depends only on the surfactant. Proniosomal gel showed a significantly enhanced drug permeation through the skin, with an enhancement ratio 3.81±1.85 when compared to the drug solution. Comparative evaluation of permeation studies and the in vitro release study of optimized proniosomal gel (F5) with that of marketed gel and carbopol gel showed that the penetration of the optimized formulation was enhanced 1.75 times in comparison with that of the marketed formulation, and the release was in a controlled manner. Similarly, the anticandidial activity showed a significantly higher activity (p<0.05) than the marketed and carbopol gel. This may be due to the enhanced penetration of noisome-containing drug through the fungal cell wall, inhibiting the ergo sterol synthesis, thereby causing the fungal cell death due to the presence of penetration enhancer. The stability study at two different temperatures (30 ± 2°C and 4 ± 2°C) confirmed that the formulations were stable even at the end of 45 days. Hence, proniosomal gel is an efficient carrier for the delivery of clotrimazole, thereby prolonging the action. Full article
Article
Chronic Inhibition of Central Angiotensin-Converting Enzyme Ameliorates Colchicine-Induced Memory Impairment in Mice
Sci. Pharm. 2012, 80(3), 647-662; https://doi.org/10.3797/scipharm.1203-06 - 03 May 2012
Cited by 12 | Viewed by 766
Abstract
Preclinical and clinical studies indicated involvement of the central renin-angiotensin system (RAS) in memory functions. However, the role of central angiotensin-converting enzyme (ACE) in memory function is still unclear. The present study investigated the involvement of central ACE in colchicine-induced memory impairment in [...] Read more.
Preclinical and clinical studies indicated involvement of the central renin-angiotensin system (RAS) in memory functions. However, the role of central angiotensin-converting enzyme (ACE) in memory function is still unclear. The present study investigated the involvement of central ACE in colchicine-induced memory impairment in the context of cholinergic function and oxidative stress. Memory impairment was induced by intracerebral colchicine administration in mice. The ACE inhibitor, perindopril (0.05 and 0.1 mg/kg/day), was administered orally for 14 days. Memory function was evaluated by the Morris water maze (MWM) test from the 14th day on after colchicine injection. Donepezil was used as a standard. Parameters of oxidative stress and cholinergic function, ACE activity in serum and the brain were estimated after the completion of behavioral studies. Colchicine caused memory impairment as revealed by no significant change in latency to reach a hidden platform in the MWM test. Furthermore, there was a significant increase in MDA, ROS, and nitrite levels with a reduction in GSH level and acetylcholinesterase (AChE) activity in the brain of colchicine-treated mice. Colchicine significantly increased brain ACE activity without affecting serum ACE. Donepezil prevented colchicine-induced memory impairment in mice. The antidementic effect of perindopril may be attributed to reduced oxidative stress and improvement in cholinergic function. Moreover, the elevated brain ACE activity was also inhibited by perindopril. The study showed that central ACE plays an important role in colchicine-induced memory deficit, corroborating a number of studies that show that treatment with ACE inhibitors could be neuroprotective. Full article
Article
Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents
Sci. Pharm. 2012, 80(3), 509-530; https://doi.org/10.3797/scipharm.1204-02 - 03 May 2012
Cited by 31 | Viewed by 994
Abstract
rel-(5aR,11bR)-3,5a,6,11b-tetrahydro-2Н,5Н-chromeno[4',3':4,5]thiopyrano[2,3-d][1,3]thiazol-2-ones formed by the stereoselective Knoevenagel-hetero-Diels-Alder reaction were functionalized at the nitrogen in position 3 via reactions of alkylation, cyanoethylation, and acylation. The synthesized compounds were evaluated for their anticancer [...] Read more.
rel-(5aR,11bR)-3,5a,6,11b-tetrahydro-2Н,5Н-chromeno[4',3':4,5]thiopyrano[2,3-d][1,3]thiazol-2-ones formed by the stereoselective Knoevenagel-hetero-Diels-Alder reaction were functionalized at the nitrogen in position 3 via reactions of alkylation, cyanoethylation, and acylation. The synthesized compounds were evaluated for their anticancer activity in NCI60 cell lines. Among the tested compounds, 3f was found to be the most active candidate with the greatest influence on leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, prostate cancer, and breast cancer subpanel cell lines with GI50 values over a range of 0.37–0.67 μM. Full article
Article
Simultaneous Estimation of Amlodipine Besylate and Indapamide in a Pharmaceutical Formulation by a High Performance Liquid Chromatographic (RP-HPLC) Method
Sci. Pharm. 2012, 80(3), 581-590; https://doi.org/10.3797/scipharm.1203-07 - 30 Apr 2012
Cited by 21 | Viewed by 1304
Abstract
An isocratic reversed-phase liquid chromatograpic assay method was developed for the quantitative determination of amlodipine besylate (AML) and indapamide (IND) in combined dosage form. A Brownlee C-18, 5 μm column with a mobile phase containing 0.02 M potassium dihydrogen phosphate–methanol (30+70, v/v) total [...] Read more.
An isocratic reversed-phase liquid chromatograpic assay method was developed for the quantitative determination of amlodipine besylate (AML) and indapamide (IND) in combined dosage form. A Brownlee C-18, 5 μm column with a mobile phase containing 0.02 M potassium dihydrogen phosphate–methanol (30+70, v/v) total pH-adjusted to 3 using o-phosphoric acid was used. The flow rate was 1.0 mL min−1 and effluents were monitored at 242 nm. The retention times of amlodipine besylate and indapamide were 5.9 min and 3.6 min, respectively. The proposed method was validated with respect to linearity, accuracy, precision, and robustness. The method was successfully applied to the estimation of amlodipine besylate and indapamide in combined tablet dosage forms. Full article
Article
Effects of Calendula Essential Oil-Based Cream on Biochemical Parameters of Skin of Albino Rats against Ultraviolet B Radiation
Sci. Pharm. 2012, 80(3), 669-684; https://doi.org/10.3797/scipharm.1112-18 - 16 Apr 2012
Cited by 16 | Viewed by 1459
Abstract
Reactive oxygen species (ROS) generated from UV-B radiation have the capacity to cause oxidative decomposition which leads to the formation of toxic components as well as lipid peroxidation. Considering this fact, the present study was performed to evaluate the effect of a cream [...] Read more.
Reactive oxygen species (ROS) generated from UV-B radiation have the capacity to cause oxidative decomposition which leads to the formation of toxic components as well as lipid peroxidation. Considering this fact, the present study was performed to evaluate the effect of a cream (O/W) containing the essential oil of Calendula officinalis on biochemical parameters of the skin of albino rats against UV-B radiation. The fingerprint analysis of Calendula essential oil was performed by HPLC with special reference to 1,8-cineole and α-pinene. The results indicated that the treatment with creams containing 4% and 5% of Calendula essential oil caused a significant decrease in the malonyldialdehyde level, whereas the levels of catalase, glutathione, superoxide dismutase, ascorbic acid, and the total protein level were significantly increased after 1 month of daily irradiation and treatment when compared to untreated control groups. The results suggest that the cutaneous application of the essential oil of Calendula prevents UV-B-induced alterations in the level of antioxidants in skin tissue. Full article
Article
Development and Validation of a Stability-Indicating RP-HPLC Method for the Quantitative Analysis of Anagrelide Hydrochloride
Sci. Pharm. 2012, 80(3), 567-580; https://doi.org/10.3797/scipharm.1112-22 - 16 Apr 2012
Cited by 1 | Viewed by 903
Abstract
A simple, rapid, and stability-indicating reverse-phase liquid chromatographic assay method was developed for Anagrelide Hydrochloride (ANG) in the presence of its degradation products generated from forced decomposition studies. The HPLC separation was achieved on a C18 Inertsil column (250 mm x 4.6 mm [...] Read more.
A simple, rapid, and stability-indicating reverse-phase liquid chromatographic assay method was developed for Anagrelide Hydrochloride (ANG) in the presence of its degradation products generated from forced decomposition studies. The HPLC separation was achieved on a C18 Inertsil column (250 mm x 4.6 mm i.d. particle size is 5 μm), using solution A, a mixture of 0.03 M potassium di-hydrogen phosphate pH-adjusted to 3.0 using ortho-phosphoric acid (buffer): methanol: acetonitrile (90:5:5, v/v/v), and solution B, which contains a mixture of buffer: acetonitrile (10:90, v/v). The UV detector was operated at 251 nm while column temperature was maintained at 40°C, and the gradient program had the flow rate of 1.0 mL min−1. The developed method was validated as per ICH guidelines with respect to specificity, linearity, precision, accuracy, robustness, and limit of quantification. The method was found to be simple, specific, precise, accurate, and reproducible. Selectivity was validated by subjecting the stock solution of ANG to acidic, basic, photolysis, oxidative, and thermal degradation. The calibration curve was found to be linear in the concentration range of 0.05–152 μg mL−1 (R2 = 0.9991). The peaks of degradation products did not interfere with that of pure ANG. The utility of the developed method was examined by analyzing the tablets containing ANG. Full article
Article
Anti-Inflammatory and Antinociceptive Activities of a Hydroethanolic Extract of Tamarindus indica Leaves
Sci. Pharm. 2012, 80(3), 685-700; https://doi.org/10.3797/scipharm.1110-09 - 01 Apr 2012
Cited by 26 | Viewed by 1482
Abstract
The present study aimed to investigate the anti-inflammatory and anti-nociceptive potential of a hydroethanolic extract of Tamarindus indica L. leaves (HTI) along with its possible mode of action. The anti-inflammatory activity of HTI was estimated by carrageenan-induced hind paw oedema in male Wistar [...] Read more.
The present study aimed to investigate the anti-inflammatory and anti-nociceptive potential of a hydroethanolic extract of Tamarindus indica L. leaves (HTI) along with its possible mode of action. The anti-inflammatory activity of HTI was estimated by carrageenan-induced hind paw oedema in male Wistar albino rats. Furthermore, HTI was assessed to determine its effects on membrane stabilization. The antinociceptive action was determined by acetic acid-induced writhing, tail-flick, and the hot plate model. Oral administration of HTI at the dose of 500, 750, and 1000 mg/kg body weight produced significant (P < 0.01) anti-inflammatory as well as antinociceptive actions in a dose-dependent manner. Among all tested doses, 1000 mg/kg, p. o. reduced carrageenan-induced rat paw oedema at 1, 2, 3, and 4 h. Moreover, the 1000 mg/kg dose exhibited maximum percentage inhibition of acetic acid-induced writhing (48.9%), whereas standard drug diclofenac (25 mg/kg, p. o.) showed maximum inhibition (50.9%) of writhing. In the hot plate model, HTI (1000 mg/kg, orally) increased mean basal reaction time after 120 min (7.12±0.05 sec). In the tail flick model, HTI increased the maximum percentage of latency (36.06%), whereas the standard drug pethidine (4 mg/kg, intraperitoneally) showed maximum percentage of latency (43.85%) after 60 min. The findings of the present study supported anti-inflammatory and antinociceptive claims of T. indica as were mentioned in Indian traditional and folklore practices. Full article
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