bluuebunny/crossref_metadata_2025_split huggingface dataset:
Cardioprotective actions of two bioflavonoids, quercetin and rutin, in experimental myocardial infarction in both normal and streptozotocin-induced type I diabetic rats
Authors: Annapurna Akula , Reddy Challa S , Akondi Raju B , Rao Sangana R C 
Published: October 2010

Abstract

Objectives
Revascularization therapy is the mainstay of treatment in the management of myocardial infarction in normal and diabetic patients. We attempted to evaluate the cardioprotective actions of quercetin and rutin in ischaemia-reperfusion-induced myocardial infarction in both normal and diabetic rats.

Methods
Myocardial infarct size was measured using the staining agent 2,3,5-triphenyltetrazoliumchloride. Serum and tissue malondialdehyde levels and superoxide dismutase and catalase in heart tissue were estimated spectrophotometrically. A lead II electrocardiogram was monitored at various intervals throughout the experiment.

Key findings
Results demonstrated the larger infarct size, enhanced lipid peroxidation, partial depletion of antioxidant enzymes and drastic drop in heart rate in diabetic hearts subjected to in-vivo ischaemia-reperfusion in comparison to normal rats subjected to ischaemia-reperfusion. Furthermore, quercetin and rutin significantly limit the infarct size in both normal and diabetic animals in a similar fashion. However, rutin offered complete cardioprotection at a dose of 10 mg/kg in terms of limiting infarct size. Both flavonoids could partially but significantly attenuate the lipid peroxidation. In addition, treatment has shown moderate improvement in heart rate in both normal and diabetic rats.

Conclusions
Our data suggest the possible cardioprotective effects of quercetin and rutin in ischaemia-reperfusion injury in both normal and diabetic rats, and that protection might be in part due to the attenuation of oxidative stress and moderate increment in antioxidant reserves.
Potential beneficial effect of naringenin on lipid peroxidation and antioxidant status in rats with ethanol-induced hepatotoxicity
Authors: Jayaraman Jayachitra , Veerappan Muniappan , Namasivayam Nalini 
Published: October 2010

Abstract

Objectives
The aim was to study the effect of naringenin, a biologically active compound, on tissue antioxidant status and lipid peroxidation in ethanol-induced hepatotoxicity in rats.

Methods
Rats were divided into four groups: Groups 1 and 2 received isocaloric glucose and 0.5% carboxymethyl cellulose; groups 3 and 4 received 20% ethanol equivalent to 6 g/kg daily for 60 days. In addition, groups 2 and 4 were given naringenin (50 mg/kg) daily for the last 30 days of the experiment.

Key findings
The results showed significantly elevated levels of serum aspartate and alanine transaminases, γ-glutamyl transpeptidase, tissue thiobarbituric acid reactive substances, conjugated dienes, lipid hydroperoxides and protein carbonyl content, and significantly lowered activities/levels of antioxidants such as superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glutathione-S-transferase, reduced glutathione and vitamins C and E in ethanol-treated rats compared with control rats. Administration of naringenin to rats with ethanol-induced liver injury significantly decreased the levels of serum aspartate and alanine transaminases, γ-glutamyl transpeptidase, tissue thiobarbituric acid reactive substances, conjugated dienes, lipid hydroperoxides and protein carbonyl content and significantly elevated the activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase and glutathione-S-transferase, and the levels of reduced glutathione and vitamins C and E in the tissues compared with unsupplemented ethanol-treated rats. Histological changes observed in the liver correlated with the biochemical findings.

Conclusions
Taken together these findings suggest that naringenin has a therapeutic potential in the abatement of ethanol-induced hepatotoxicity.
Modelling of diclofenac sodium diffusion from swellable and water-soluble polyethylene oxide matrices
Authors: Petrović Jelena , Jocković Jelena , Ibrić Svetlana , Ɖurić Zorica 
Published: October 2010

Abstract

Objectives
The main objective of this study was to develop a mathematical model for the characterization of diclofenac sodium diffusion from polyethylene oxide (PEO) matrices. A model was developed on the basis of the diffusion theory accounting for the characteristics of the polymer: swelling with subsequent dissolution in water. The concentration-dependent diffusion of drug and water was taken into account. Experimental data were analysed using a computer software program as an aid for solving partial differential equations.

Methods
Six formulations of matrix tablets with different drug-excipient ratios were prepared using low-molecular-weight PEO as a matrix-forming material. For obtaining drug release data, dissolution studies were performed and water uptake by pure PEO matrices was studied as well.

Key findings
A good agreement of the developed model with experimental results was demonstrated. Some anomalies in drug diffusion were observed and their origin was questioned. Changes in the parameters characterizing the process of diffusion are attributed to glassy-rubbery polymer transitions. Additional interpretation of this phenomenon on the basis of percolation theory is also provided.

Conclusions
The obtained model has the ability to predict the required characteristics of matrices for desired drug release. The composition of batches with undesirable release properties can be predetermined and avoided in manufacturing.
Effective vaginal DNA delivery with high transfection efficiency is a good system for induction of higher local vaginal immune responses
Authors: Kanazawa Takanori , Takashima Yuuki , Shibata Yasunori , Tsuchiya Miki , Tamura Toshiaki , Okada Hiroaki 
Published: October 2010

Abstract

Objectives
To investigate the local vaginal and systemic immune responses of effective vaginal DNA delivery with high transfection efficiency, we determined the effects on Th1-dependent cytokine (interferon-γ) production in spleen and inguinal lymph node cells and antibody responses of vaginal pDNA immunization with a cell-penetrating peptide, and compared our vaginal immunization with intradermal and intranasal immunizations.

Methods
Mice were immunized by vaginal, nasal or dermal administration of pCMV-OVA with or without peptide carriers, and serum, vaginal fluids, spleen and inguinal cells were harvested. The serum immunoglobulin (Ig)G2a and vaginal IgA antibody responses were determined by sandwich enzyme-linked immunosorbent assay (ELISA). The interferon-γ production from spleen cells or inguinal lymph node cells was determined by an ELISA kit.

Key findings
The direct vaginal immunization strongly induced IgA in the vaginal fluids and interferon-γ production in the local lymph node draining from the vagina. In addition, co-vaccination with the peptide carriers elevated these immune responses compared with vaccination with pCMV-OVA alone. Vaginal immunization with high transfection efficiency promoted vaginal IgA production to a significantly greater extent than intradermal or nasal immunization.

Conclusions
These results suggested that direct vaginal DNA vaccines under high transfection conditions induced higher local vaginal antibody than that by intranasal or intradermal administration, and peptide carriers effectively elevated mucosal immune responses. Therefore, this vaginal DNA vaccination method may be expected to be useful in the prevention and treatment methods for vaginal infectious diseases such as HIV infection.
Evaluation of molecular pharmaceutical and in-vivo properties of spray-dried isolated andrographolide—PVP
Authors: Bothiraja C , Shinde Mukesh B , Rajalakshmi S , Pawar Atmaram P 
Published: October 2010

Abstract

Objectives
Andrographolide, a natural lipophilic molecule, has a wide range of pharmacological actions. However, due to low aqueous solubility, it has low oral bioavailability. The purpose of the study was to increase the solubility and dissolution rate of isolated andrographolide by formulating its solid dispersion.

Method
Solid dispersions were obtained by a spray-drying technique using different ratios of drug to polyvinylpyrrolidine (PVP K-30). Solid dispersions in compression with isolated drug and corresponding physical mixtures were characterized for various molecular pharmaceutical properties and subjected to stability study for up to 3 months.

Key findings
A five-fold increase in saturation solubility of andrographolide with higher values of Q5min (cumulative percentage release in 5 min) and lower values of t75% (time required for 75% w/w drug release) for solid dispersion was observed in different dissolution mediums. This was attributed to the formation of amorphous nature and intermolecular hydrogen bonding between drug and PVP K-30. The stability study showed there to be no significant change in molecular pharmaceutical properties and dissolution profile over the period of 3 months. Moreover, the in-vivo study in Wistar albino rats also justified improvement in the therapeutic efficacy of andrographolide after solid dispersion.

Conclusions
This study demonstrates the utility of solid dispersion to improve primary and secondary pharmaceutical properties of andrographolide using PVP K-30 as a carrier.
Preparation and pharmacokinetics of docetaxel based on nanostructured lipid carriers
Authors: Li Xiang , Wang Dongkai , Zhang Jing , Pan Weisan 
Published: October 2010

AbstractObjectivesThis study describes the preparation and pharmacokinetics of docetaxel based on freeze-dried nanostructured lipid carriers (NLCs).MethodsThe docetaxel-incorporated NLCs were developed using hot high-pressure homogenisation, and lyophilised to obtain freeze-dried docetaxel NLCs. The influences of different concentrations of lipid matrices, ratio of drug to lipid, and different cryoprotectants on the characteristics of the NLCs were investigated.Key findingsFreeze-dried docetaxel NLCs were spherical, with 5% (w/w) docetaxel loading efficiency and were stable for at least 6 months at 25°C. X-ray powder diffraction and differential scanning calorimetry analysis suggested that docetaxel was distributed in a molecular or amorphous status. In-vitro release studies showed sustained drug release, with the cumulated release rate of 13% within 24 h without burst release. The freeze-dried docetaxel NLCs also showed sustained-release properties after intravenous injection into rats. The area under the plasma–concentration time curve and mean residence time were increased 4.90 and 2.82 times compared with docetaxel solution. The concentration of docetaxel in the lungs was significantly higher in rats treated with the NLCs than in those given docetaxel solution.ConclusionsDocetaxel NLCs have an organ-targeting effect and prolonged mean retention time and have potential for the treatment of lung cancer.
Involvement of adipokines in rimonabant-mediated insulin sensitivity in ob/ob mice
Authors: Mohapatra Jogeswar , Sharma Manoranjan , Singh Satinder , Pandya Gaurav , Chatterjee Abhijit , Balaraman Ramachandran , Patel Pankaj R , Jain Mukul R 
Published: October 2010

Abstract

Objectives
It has been recently reported that blockade of type 1 cannabinoid (CB1) receptors by specific antagonists or genetic manipulation alleviates dyslipidaemia, hyperglycaemia and insulin resistance in animal models of obesity and type 2 diabetes. However, the precise role of adipokines in the insulin-sensitising effects of the CB1 antagonist rimonabant is not clear.

Methods
ob/ob mice were treated with different doses of rimonabant and then subjected to an oral glucose tolerance test. The expression of different adipokines in white adipose tissue was analysed by quantitative real-time PCR.

Key findings
Rimonabant (30 mg/kg) significantly inhibited body weight and fat pad weight gain (P &lt; 0.05) and improved glucose tolerance. Gene expression analysis indicated that tumour necrosis factor-α, visfatin and retinol binding protein-4 were downregulated in the adipose tissue of ob/ob mice treated with rimonabant compared with controls, whereas adiponectin was significantly upregulated.

Conclusions
Rimonabant-mediated alteration of adipokines in white adipose tissues may play a role in improving insulin sensitivity in obese animals.
Nootropic activity of lipid-based extract of Bacopa monniera Linn. compared with traditional preparation and extracts
Authors: Lohidasan Sathiyanarayanan , Paradkar Anant R , Mahadik Kakasaheb R 
Published: October 2010

Abstract

Objectives
The aim was to design an alternative solvent-free extraction method using the hydrophilic lipid Gelucire (polyethylene glycol glycerides) for herbal extraction and to confirm the efficacy of extraction using biological screening.

Methods
Bacopa monniera Linn. (BM) was selected for the study. Conventional methanolic extract (MEBM), Ayurvedic ghrita (AGBM) and lipid extracts (LEBM) were prepared and standardised by high-performance thin-layer chromatography (HPTLC). Nootropic activity in rats was evaluated using the two-trial Y-maze test and the anterograde amnesia induced by scopolamine (1 mg/kg i.p.) determined by the conditioned avoidance response. The extracts were administered daily at doses of 100, 200 and 400 mg/kg orally. At the end of the conditioned avoidance response test, brain monoamine levels were estimated by HPLC.

Key findings
The LEBM, MEBM and AGBM contained 3.56%, 4.10% and 0.005% bacoside A, respectively. Significantly greater spatial recognition was observed with LEBM (P &lt; 0.001 at 400 and 200 mg/kg) and MEBM (P &lt; 0.001 at 400 mg/kg, P &lt; 0.01 at 200 mg/kg) than AGBM. The conditioned avoidance response was significantly higher in the groups treated with high doses of LEBM and MEBM than AGBM. There were significant decreases in brain noradrenaline (P &lt; 0.001) and 5-hydroxytryptamine (P &lt; 0.01) levels and an increase in dopamine levels (P &lt; 0.05) in the LEBM-treated groups compared with the stress control group.

Conclusions
The proposed LEBM is solvent free, does not have the shortcomings associated with conventional extraction, and had comparable nootropic activity to the MEBM.
The relation between moisture-induced aggregation and structural changes in lyophilized insulin
Authors: Flores-Fernández Giselle M , Solá Ricardo J , Griebenow Kai 
Published: October 2010

Abstract

Objectives
Long-term stability is a critical factor in the successful development of protein pharmaceuticals. Due to the relative instability of proteins in aqueous solutions, they are formulated frequently and stored as lyophilized powders. Exposure of such powders to moisture constitutes a substantial storage problem leading to aggregation and inactivation. We have investigated the structural consequences of moisture sorption by lyophilized insulin under controlled humidity conditions by employing Fourier transform-infrared (FT-IR) microscopy.

Methods
Lyophilized insulin samples were stored in humidity chambers under controlled conditions at 50°C. Protein aggregation studies were carried out by redissolving the insulin samples and measuring the amount of both soluble protein and insoluble aggregates. Near-UV circular dichroism spectra were collected to assess the tertiary structure. FT-IR microscopy studies were carried out to investigate secondary structural changes in solid-state insulin after incubation at different relative humidities.

Key findings
It was found that sorption of moisture was accompanied by small structural changes in lyophilized insulin at low levels of relative humidity (i.e. 11%). At higher relative humidity levels, structural changes were becoming more pronounced and were characterized by a loss in the α-helix and increase in β-sheet content. The magnitude of the structural changes in tendency paralleled the solid-state instability data (i.e. formation of buffer-insoluble aggregates and loss in tertiary structure upon reconstitution).

Conclusions
The results support the hypothesis that water sorption by lyophilized proteins enables structural transitions which can lead to protein aggregation and other deleterious phenomena.
Protective effects of sodium para-amino salicylate on manganese-induced neuronal death: the involvement of reactive oxygen species
Authors: Yoon Hyonok , Kim Do-Sung , Lee Geum-Hwa , Kim Ji Ye , Kim Diana H , Kim Kee-Won , Chae Soo-Wan , You Wan-Hee , Lee Yong Chul , Park Seoung Ju , Kim Hyung-Ryong , Chae Han-Jung 
Published: October 2010

Abstract

Objectives
This study tested whether sodium para-amino salicylic dihydrate, an antibacterial drug for tuberculosis, could block manganese-induced apoptosis in SK-N-MC neurons.

Methods
Cell viability, Hoechst staining, dichlorofluorescin diacetate analysis for reactive oxygen species measurement, and immunoblotting were performed.

Key findings
In vitro, manganese chloride significantly decreased the viability of SK-N-MC cells, accompanied by apoptotic features such as changes in nuclear morphology. Sodium para-amino salicylic dihydrate inhibited these apoptotic characteristics through reducing intracellular reactive oxygen species generation, protecting mitochondrial membrane potential and caspase-3 activation.

Conclusions
Sodium para-amino salicylic dihydrate inhibits manganese-induced apoptosis in neurons and may reduce manganese-mediated neurodegeneration.
Chitosan-tripolyphosphate nanoparticles as a possible skin drug delivery system for aciclovir with enhanced stability
Authors: Hasanovic Amra , Zehl Martin , Reznicek Gottfried , Valenta Claudia 
Published: October 2010

Abstract

Objectives
The aim of the present study was to create a skin delivery system based on chitosan-tripolyphosphate nanoparticles for aciclovir with enhanced chemical stability.

Methods
Nanoparticles were formed spontaneously using ionotropic gelation with tripolyphosphate. Two different sizes of aciclovir-loaded nanoparticles were characterised in terms of zeta potential, particle size and polydispersity index.

Key findings
Standard diffusion experiments using Franz-type diffusion cells showed reasonable skin permeability that depended on particle size and chitosan content. The larger the nanoparticle, having a higher chitosan content, the better the aciclovir permeation through porcine skin. Differential scanning calorimetry studies showed a remarkable decrease in the typical transition temperature, indicating an interaction between skin lipid bilayer and the nanoparticles. Moreover, the chemical stability of aciclovir was significantly increased by the nanoparticle system. After the observation period of 5 weeks, aciclovir incorporated into nanoparticles had undergone photo-oxidation to a significantly lower extent than pure aqueous solution. This degradation product of aciclovir was analysed using LC/MS, and its identity established.

Conclusions
These studies demonstrate that incorporation of aciclovir into chitosan-tripolyphosphate nanoparticles significantly improves its chemical stability. Moreover, skin diffusion studies in vitro showed improved permeation of aciclovir from the nanoparticle system, especially from nanoparticles with higher chitosan content.
Collagen-based wound dressing for doxycycline delivery: in-vivo evaluation in an infected excisional wound model in rats
Authors: Adhirajan Natarajan , Shanmugasundaram Natesan , Shanmuganathan Seetharaman , Babu Mary 
Published: October 2010

Abstract

Objectives
A novel collagen-based dressing consisting of 2,3-dihydroxybenzoic-acid-modified gelatin microspheres loaded with doxycycline has previously been reported to address both infection and matrix degradation. In the present study the potential benefits of the dressing were investigated in an excisional wound model in rats challenged with Pseudomonas aeruginosa.

Methods
A full-thick excisional wound (1.5 times 1.5 cm) was created on the dorsum of the rats and infection induced by injecting 105 colony-forming units (CFU) of P. aeruginosa. The healing pattern was assessed from wound reduction, matrix metalloprotease (MMP) levels, CFU reduction and histological and biochemical analysis.

Key findings
The treated group exhibited complete healing by day 15, compared with day 24 in the control group. Early subsidence of infection (99.9% by day 9) resulted in faster epidermal resurfacing and fibroplasias, whereas the microbial load exceeded 103 CFU even on day 15 in the control group and caused severe inflammation. Biochemical analysis showed that the expression of both collagen and hexosamine was significantly increased in the treated group. Gelatin zymography revealed prolonged expression of MMPs 2, 8 and 9 in the control group compared with the treated group.

Conclusions
The study indicates that the developed dressing attenuated both infection and metalloprotease levels, and may therefore have potential application in wound healing.
Evaluation of supercritical fluid engineered budesonide powder for respiratory delivery using nebulisers
Authors: Amani Amir , Chrystyn Henry , Clark Brian J , Abdelrahim Mohamed E , York Peter 
Published: October 2010

Abstract

Objectives
Currently, suspensions prepared from micronised drug substances are the only delivery system marketed for nebulisation of steroids, and reported inconsistent or low bioavailability arising from their use provides a rationale for researching alternative formulations. Supercritical fluid processing of drug substances to obtain respirable-sized particles has been used over the last decade to formulate dry powder inhalers. We aimed thus to process budesonide powder to improve its deposition characteristics.

Methods
In an attempt to overcome the limitations of nebuliser suspensions when prepared from micronised drug particles, budesonide powder was processed using a supercritical fluid based process and suspended using Tween 80 as a surfactant to provide an aqueous nebuliser formulation. The in-vitro characteristics of the emitted dose on nebulisation for the prepared suspension were then compared to a commercially available suspension formulation of budesonide using a jet and a vibrating mesh nebuliser.

Key findings
The results showed a significant improvement of the in-vitro deposition properties of the suspension containing supercritical fluid engineered budesonide particles.

Conclusions
The results indicated the benefit of such materials compared with traditionally micronised drug powders.
Preparation, characterization and taste-masking properties of microspheres containing azithromycin
Authors: Hu Liandong , Pan Jianbin , Liu Ci , Xu Hongxin , Luo Liangzhao 
Published: October 2010

Abstract

Objectives
The aim of this study was to prepare a microsphere formulation in order to mask the bitter taste of azithromycin.

Methods
Microspheres of azithromycin with ethyl cellulose were prepared by the modified solvent diffusion method. The microspheres were mixed with other excipients to form orally dry suspensions and the sensory test for taste masking was evaluated.

Key findings
Results demonstrated that the suspension could significantly mask the bitter taste of azithromycin and the relative bioavailability of suspensions to reference preparations was 102.7%.

Conclusions
The results indicate that the microsphere formulation can be a promising drug carrier for masking the bitter taste of azithromycin.