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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Table of Contents

Sci. Pharm., Volume 78, Issue 1 (March 2010), Pages 1-132

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Open AccessArticle Antiproliferative Activity of Plant Extracts Used Against Cancer in Traditional Medicine
Sci. Pharm. 2010, 78(1), 33-46; https://doi.org/10.3797/scipharm.0912-11 (registering DOI)
Received: 10 December 2009 / Accepted: 12 February 2010 / Published: 13 February 2010
Cited by 40 | PDF Full-text (735 KB)
Abstract
Forty four extracts from sixteen plants used traditionally as anticancer agents were evaluated in vitro for their antiproliferative activity against Hep-2, MCF-7, and Vero cell lines. Plants were fractionated using ethanol, methanol, chloroform, n-hexane, distilled water, and butanol. The antiproliferative activity was
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Forty four extracts from sixteen plants used traditionally as anticancer agents were evaluated in vitro for their antiproliferative activity against Hep-2, MCF-7, and Vero cell lines. Plants were fractionated using ethanol, methanol, chloroform, n-hexane, distilled water, and butanol. The antiproliferative activity was measured by MTT assay. TLC was used to identify active fractions. The apoptotic activity of active fractions was determined using TUNEL colorimetric assay. 20 of these extracts demonstrated significant antiproliferative activity against one or more of the cell lines. These extracts were prepared from Ononis hirta, Inula viscosa, Salvia pinardi, Verbascum sinaiticum and Ononis sicula. Methanol fractions of Ononis hirta (aerial parts) and Inula viscosa (flowers) were the most active fractions against MCF-7 cells with IC50 of 27.96 and 15.78 μg/ml respectively and they were less toxic against other cell lines. Other extracts showed lower activity against cancer cell lines. TLC analysis showed the presence of flavonoids and terpenoids in active plants while alkaloids were detected in Ononis hirta (aerial parts) extracts. Ononis hirta (aerial parts) and Inula viscosa (flowers) extracts exerted their antiproliferative activity by inducing apoptosis in cancer cell lines. Further studies are necessary for detailed chemical characterization and more extensive biological evaluation of the most active ingredients. Full article
Open AccessEditorial Scientia Pharmaceutica, Autorenhinweise 2010
Sci. Pharm. 2010, 78(1), 119-132; https://doi.org/10.3797/scipharm.aut-10-01 (registering DOI)
Received: 18 January 2010 / Accepted: 18 January 2010 / Published: 18 January 2010
Cited by 11 | PDF Full-text (188 KB)
Abstract
Die Zeitschrift Scientia Pharmaceutica (www.scipharm.at) erscheint vierteljährlich jeweils am Quartalsende und ist ein Medium zur Publikation von Originalarbeiten, Kurzmitteilungen und ausgewählten Übersichtsarbeiten aus allen wissenschaftlichen Disziplinen der Pharmazie und angrenzenden Gebieten sowie der pharmazeutischen Praxis. [...]
Full article
Open AccessEditorial Retraction
Sci. Pharm. 2010, 78(1), 118; https://doi.org/10.3797/scipharm.ed-10-02 (registering DOI)
Received: 18 January 2010 / Accepted: 18 January 2010 / Published: 18 January 2010
PDF Full-text (112 KB)
Abstract
On May 22nd 2009 we received an article by Jignesh P. Raval, Anil J. Malaviya, Nilesh H. Patel, Hemul V. Patel and Pradip S. [...] Full article
Open AccessEditorial Zum 90. Geburtstag von Frau Univ.-Prof. Dr. Maria Kuhnert-Brandstätter
Sci. Pharm. 2010, 78(1), 117; https://doi.org/10.3797/scipharm.ed-10-01 (registering DOI)
Received: 18 January 2010 / Accepted: 18 January 2010 / Published: 18 January 2010
Cited by 11 | PDF Full-text (80 KB)
Abstract
Frau Prof. Kuhnert-Brandstätter wurde 1919 in Lamprechtshausen bei Salzburg geboren. [...] Full article
Open AccessArticle In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation
Sci. Pharm. 2010, 78(1), 103-116; https://doi.org/10.3797/scipharm.0909-08 (registering DOI)
Received: 17 September 2009 / Accepted: 18 January 2010 / Published: 18 January 2010
Cited by 7 | PDF Full-text (264 KB)
Abstract
The aim of present investigation was 1) to evaluate the in vivo bioavailability of an Etodolac (ETD)-β-cyclodextrin (β-CD) inclusion complex system prepared by kneading and spray drying techniques in rats, 2) to study the pharmacodynamic parameters in various animal models for analyzing the
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The aim of present investigation was 1) to evaluate the in vivo bioavailability of an Etodolac (ETD)-β-cyclodextrin (β-CD) inclusion complex system prepared by kneading and spray drying techniques in rats, 2) to study the pharmacodynamic parameters in various animal models for analyzing the therapeutic response and, 3) to evaluate the pharmacokinetic profile of the drug administered. Inclusion complexation with β-CD enhanced the solubility of the drug, improved bioavailability and reduced ulcerogenicity of ETD in rats. Pharmacodynamic studies were carried out in normal LACA mice and pharmacokinetic evaluation was done in male Wistar rats. Pharmacokinetic parameters evaluated for the inclusion complexes revealed good correlation. The minimum dose necessary to produce analgesic or anti-arthritic activity was also decreased, indicating that the host-guest strategy that uses β-CD and ETD was very effective and could be successfully employed in the preparation of pharmaceutical formulations of anti-arthritics and analgesics. Full article
Open AccessArticle Different Spontaneous Pulmonary Metastasis Inhibitions against Lewis Lung Carcinoma in Mice by Bisdioxopiperazine Compounds of Different Treatment Schedules
Sci. Pharm. 2010, 78(1), 13-20; https://doi.org/10.3797/scipharm.0910-16 (registering DOI)
Received: 25 October 2009 / Accepted: 28 December 2009 / Published: 29 December 2009
Cited by 3 | PDF Full-text (140 KB)
Abstract
Spontaneous neoplasm metastasis, a fatalist pathological feature of cancer, is a long-evolving, multi-steps process that can now only be treated or controlled by drugs or immuno-modulators. As we have previously hypothesized, each drug or immuno-modulator might act differently within various stages of a
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Spontaneous neoplasm metastasis, a fatalist pathological feature of cancer, is a long-evolving, multi-steps process that can now only be treated or controlled by drugs or immuno-modulators. As we have previously hypothesized, each drug or immuno-modulator might act differently within various stages of a metastasis. Therefore any researches helping to determine these differences will be beneficial for updating therapeutics for metastasis. In this work, we have testified this hypothesis by using a series of well-known anti-metastatic agents – Bisdioxopiperazine compounds. Full article
Open AccessArticle Release Kinetic Studies of Aspirin Microcapsules from Ethyl Cellulose, Cellulose Acetate Phthalate and their Mixtures by Emulsion Solvent Evaporation Method
Sci. Pharm. 2010, 78(1), 93-102; https://doi.org/10.3797/scipharm.0908-09 (registering DOI)
Received: 15 August 2009 / Accepted: 17 December 2009 / Published: 19 December 2009
Cited by 14 | PDF Full-text (242 KB)
Abstract
The present study was oriented towards microencapsulation of aspirin and the study of its release kinetics. The desired encapsulation was achieved by emulsion solvent evaporation method using ethyl cellulose (EC), cellulose acetate phthalate (CAP) and their mixture (1:1) of polymeric constituents. Characterization of
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The present study was oriented towards microencapsulation of aspirin and the study of its release kinetics. The desired encapsulation was achieved by emulsion solvent evaporation method using ethyl cellulose (EC), cellulose acetate phthalate (CAP) and their mixture (1:1) of polymeric constituents. Characterization of the formulations was performed by size, shape, drug loading efficiency and in-vitro drug release analysis. The in-vitro release profiles from different polymeric microcapsules were applied on different kinetic models. The prepared microcapsules were found free flowing and almost spherical in shape with particle sizes ranging from 300–700μm, having a loading efficiency of 75– 85%. The best fit model with the highest correlation coefficient was observed in Higuchi model, indicating diffusion controlled principle. The n value obtained from Korsemeyer-Peppas model varied between 0.5–0.7, confirming that the mechanism of drug release was diffusion controlled. Comparative studies revealed that the release of aspirin from EC microcapsules was slower as compared to that of CAP and their binary mixture. Full article
Open AccessArticle Evaluation of Ketorolac Tromethamine Microspheres by Chitosan/Gelatin B Complex Coacervation
Sci. Pharm. 2010, 78(1), 79-92; https://doi.org/10.3797/scipharm.0903-16 (registering DOI)
Received: 28 March 2009 / Accepted: 17 December 2009 / Published: 19 December 2009
Cited by 12 | PDF Full-text (563 KB)
Abstract
Microspheres (MS) of Ketorolac Tromethamine (KT) for oral delivery were prepared by complex coacervation (method-1) and simple coacervation (method-2) methods without the use of chemical cross–linking agent (glutaraldehyde) to avoid the toxic reactions and other undesirable effects of the chemical cross-linking agents. Alternatively,
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Microspheres (MS) of Ketorolac Tromethamine (KT) for oral delivery were prepared by complex coacervation (method-1) and simple coacervation (method-2) methods without the use of chemical cross–linking agent (glutaraldehyde) to avoid the toxic reactions and other undesirable effects of the chemical cross-linking agents. Alternatively, ionotropic gelation was employed by using sodium-tripolyphosphate (Na-TPP) as cross linking agent. Chitosan and gelatin B were used as polymer and copolymer respectively. All the prepared microspheres were subjected to various physico-chemical studies, such as drug-polymer compatibility by Thin Layer Chromatography (TLC) and Fourier Transform Infra Red Spectroscopy (FTIR), surface morphology by Scanning Electron Microscopy (SEM), frequency distribution, encapsulation efficiency, in-vitro drug release characteristics and release kinetics. The physical state of drug in the microspheres was determined by Differential Scanning Calorimetry (DSC) and X-ray powder Diffractometry (XRD). TLC and FTIR studies indicated no drug-polymer incompatibility. All the MS showed release of drug by a fickian diffusion mechanism. DSC and XRD analysis indicated that the KT trapped in the microspheres existed in an amorphous or disordered-crystalline status in the polymer matrix. It is possible to design a controlled drug delivery system for the prolonged release of KT, improving therapy by possible reduction of time intervals between administrations. Full article
Open AccessArticle Studies on the Reactivity of (9-Methyl-5,6-dihydronaphtho[1',2':4,5]- thieno[2,3-d]pyrimidin-11-yl)hydrazine Towards Some Reagents for Biological Evaluation
Sci. Pharm. 2010, 78(1), 1-12; https://doi.org/10.3797/scipharm.0910-11 (registering DOI)
Received: 20 October 2009 / Accepted: 27 November 2009 / Published: 11 December 2009
Cited by 8 | PDF Full-text (205 KB) | Supplementary Files
Abstract
(9-Methyl-5,6-dihydronaphtho[1',2':4,5]thieno[2,3-d]pyrimidin-11-yl)hydrazine (1) was used as a precursor for preparation of some novel 1-(9-methyl-5,6- dihydronaphtho[1',2':4,5]thieno[2,3-d]pyrimidin-11-yl)-1H-pyrazoles 27, -1H-isoindole- 1,3(2H)-dione 8, and -pyridazin-3(2H)-one 9. Moreover, the acyclic
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(9-Methyl-5,6-dihydronaphtho[1',2':4,5]thieno[2,3-d]pyrimidin-11-yl)hydrazine (1) was used as a precursor for preparation of some novel 1-(9-methyl-5,6- dihydronaphtho[1',2':4,5]thieno[2,3-d]pyrimidin-11-yl)-1H-pyrazoles 27, -1H-isoindole- 1,3(2H)-dione 8, and -pyridazin-3(2H)-one 9. Moreover, the acyclic C-nucleosides 10 and 11 were prepared by treating compound 1 with D-glucose. The in vitro antimicrobial activity of the tested compounds was evaluated by measuring the zone diameters and some of the prepared products showed potent antimicrobial activity in compared with those of well known drugs (standard). In general, the non-acetylated sugar hydrazone derivative 10 showed the highest antibacterial and antifungal potency among the tested compounds and standard with IZ = 22, 21 and 22 mm and MIC = 62.5 and 31.25 μg/ml, respectively. Full article
Open AccessArticle Antioxidant and Immunomodulatory Activity of the Alkaloidal Fraction of Cissampelos pareira Linn.
Sci. Pharm. 2010, 78(1), 21-32; https://doi.org/10.3797/scipharm.0904-16 (registering DOI)
Received: 20 April 2009 / Accepted: 4 December 2009 / Published: 6 December 2009
Cited by 13 | PDF Full-text (189 KB)
Abstract
The alkaloidal fraction (AFCP) of roots of Cissampelos pareira Linn. was screened for in-vitro antioxidant activity and immunomodulatory activity in mice. The HPTLC finger print profile was also established for the identification of AFCP which was found to contain 0.176 % of berberine.
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The alkaloidal fraction (AFCP) of roots of Cissampelos pareira Linn. was screened for in-vitro antioxidant activity and immunomodulatory activity in mice. The HPTLC finger print profile was also established for the identification of AFCP which was found to contain 0.176 % of berberine. AFCP possess strong antioxidant activity which was revealed by its ability to scavenge the stable free radical DPPH, superoxide ion and to inhibit lipid peroxidation in rat liver homogenate induced by iron/ADP/Ascorbate complex. AFCP was found to have significant immunosuppressive activity at lower doses (25 and 50 mg/kg) while no activity was observed at higher doses (75 and 100 mg/kg). Humoral antibody titre was significantly (p<0.01) lowered by AFCP at the doses of 25 and 50 mg/kg. Delayed type hypersensitivity response was also significantly (p<0.01) suppressed by the AFCP at the dose of 75 mg/kg. Thus the present study revealed the immunosuppressive and antioxidant activities of the alkaloidal fraction of C. pareira roots. Full article
Open AccessArticle Chitosan-Carboxymethyl Tamarind Kernel Powder Interpolymer Complexation: Investigations for Colon Drug Delivery
Sci. Pharm. 2010, 78(1), 57-78; https://doi.org/10.3797/scipharm.0908-10 (registering DOI)
Received: 25 August 2009 / Accepted: 2 December 2009 / Published: 3 December 2009
Cited by 18 | PDF Full-text (583 KB)
Abstract
The present study was aimed at evaluating the possible use of inter polymer complexed (IPC) films of chitosan (CH) and carboxymethyl tamarind kernel powder (CMTKP) for colon release of budesonide. Viscosity analysis of the supernatant liquid obtained after reacting CH and CMTKP in
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The present study was aimed at evaluating the possible use of inter polymer complexed (IPC) films of chitosan (CH) and carboxymethyl tamarind kernel powder (CMTKP) for colon release of budesonide. Viscosity analysis of the supernatant liquid obtained after reacting CH and CMTKP in different proportions revealed 40:60 to be the optimum stoichiometric ratio. The FTIR spectra of IPC films formed from 50:50 or 40:60 ratio of CH:CMTKP did not reveal any reduction in the peaks at 1560cm−1 and 1407cm−1 after exposure to pH 1.2, suggesting resistance of the interaction between –COO groups of CMTKP and –NH3+ groups of CH to gastric pH. Tablets containing Avicel pH 102 as diluent and coated to a weight gain of 10%, w/w with aqueous solutions of 40:60 or 50:50 ratio of CH:CMTKP did not release budesonide in pH 1.2 buffer. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBSinduced ulcerative colitis as compared to that after administration of uncoated tablets. The Cmax of budesonide achieved after oral administration of these IPC film coated tablets was comparable to that observed after administration of uncoated tablets. The results strongly indicate versatility of CH-CMTKP IPC films to deliver budesonide in the colon. Full article
Open AccessArticle Preparation and In Vivo Evaluation of Indomethacin Loaded True Nanoemulsions
Sci. Pharm. 2010, 78(1), 47-56; https://doi.org/10.3797/scipharm.0911-04 (registering DOI)
Received: 7 November 2009 / Accepted: 23 November 2009 / Published: 23 November 2009
Cited by 12 | PDF Full-text (447 KB)
Abstract
Indomethacin, a potent nonsteroidal anti-inflammatory drug, has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of indomethacin produces serious gastrointestinal adverse effects. Therefore the aim of the present investigation was to evaluate the antiinflammatory effects,
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Indomethacin, a potent nonsteroidal anti-inflammatory drug, has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of indomethacin produces serious gastrointestinal adverse effects. Therefore the aim of the present investigation was to evaluate the antiinflammatory effects, skin irritation, activation energy and histopathology of indomethacin from transdermally applied true nanoemulsion. The antiinflammatory effects of true nanoemulsions were compared with marketed Indobene® gel on carrageenan-induced paw edema in rats. Skin irritation tests were performed on Wistar rats for 14 days. The % inhibition value after 12 h application was significant for optimized formulation F6 (83) as compared to marketed Indobene® gel (P<0.01). Results of skin irritation test indicated that developed true nanoemulsion is safe for human use. The significant decrease in activation energy (1.396 kcal/mol) for indomethacin across rat skin indicated that the stratum corneum lipid bilayers were significantly disrupted (P<0.05). From these results it was concluded that the developed nanoemulsion have great potential for transdermal application of indomethacin. Full article
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