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Department of Pharmaceutics, SVKM'S B.N. College of Pharmacy , Mumbai , India.
Context: Lipid based drug delivery systems have gained prominence in last decade for drugs with dissolution rate limited oral bioavailability. Objective: To improve the solubility, permeability and oral bioavailability of cefpodoxime proxetil, β-lactam antibiotic. It is BCS Class IV drug having solubility 400 µg/mL and 50% oral bioavailability. Materials and methods: Self-nanoemulsifying drug delivery system (SNEDDS) using various surfactant and cosurfactants such as tween 80, tocopheryl polyethylene glycol succinate (TPGS), propylene glycol and Capmul MCM as oil phase were prepared. Ternary phase diagrams were constructed to identify stable microemulsion region. Percent transmittance studies helped to shortlist the surfactant-cosurfactant combination. Results and discussion: Tween 80 and TPGS as surfactants and Capmul MCM as oil phase were found to produce stable nanoemulsions. Five formulations of SNEDDS had globule size of 55-60 nm and zeta potential of -4 to -11 mV. Self-emulsification time was between 221 and 370 s, while viscosity was dependent on composition of SNEDDS. Cloud point was above 70°C which indicated the retention of in vivo self-emulsifying properties. Average flux for cefpodoxime proxetil (CP) and SNEDDS was 0.104 and 0.985 µg/cm(2) min. Permeability was 19.72 and 206 for CP and SNEDDS. Liquid SNEDDS spray coated onto micropellets of microcrystalline cellulose (18-20#) were analysed by scanning electron microscope (SEM), self-emulsification and in vitro dissolution. A 5.36-fold increase in area under curve AUC(0-∞) was observed for CP-SNEDDS than plain drug. Minimum inhibitory concentration (MIC) was lower for SNEDDS. Liquid and SNEDDS micropellets were stable under accelerated conditions. Conclusion: SNEDDS formulations led to improved oral bioavailability due to enhanced solubilization of selected drug.
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Department of Industrial Biotechnology, Bharath University, Chennai 600073, India.
The present study was undertaken to test the chemopreventive effects of one herbal medicinal plant, Indigofera aspalathoides, on chemically induced carcinogenesis in rats. A well-known polyaromatic hydrocarbon, namely, 20-methylcholanthrene, which is a known carcinogenic substance, was used to induce fibrosarcoma in Wistar strain of male albino rats. Fibrosarcoma rats were treated with aqueous extracts of Indigofera aspalathoides. The rats were divided into four groups, each consisting of six animals. Group I served as normal control, Group II served as fibrosarcoma-induced animals, Group III were fibrosarcoma-bearing animals treated with aqueous extracts of Indigofera aspalathoides, and Group IV animals, which were normal healthy animals treated with Indigofera aspalathoides aqueous extract, served as drug control set. Group III and Group IV animals were treated with aqueous extract of Indigofera aspalathoides intraperitoneally at a dose of 250 mg/kg. b.w. for 30 days. The fibrosarcoma was proved by pathological examinations. The activity levels of nucleic acids such as total DNA and RNA and hexose, hexosamine, and sialic acid in liver and kidney of treated rats were used to monitor the chemopreventive role of the plant extract. The observed increase in the levels of DNA, RNA, hexose, hexosamine, and sialic acid in liver and kidney tissues of fibrosarcoma-bearing animals reached near normal state after the treatment with aqueous extracts of Indigofera aspalathoides, suggesting that Indigofera aspalathoides does have a chemotherapeutic role.
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Division of Biotechnology, Manipal Life Sciences Centre, Manipal University, Manipal -576104, Karnataka, India Biophysics Unit, Manipal Life Sciences Centre, Manipal University, Manipal - 576 104, Karnataka, India.
In the present study, the seeds of brinjal (Solanum melongena L.) var. Mattu Gulla were irradiated with single exposure of He-Ne laser at different doses of 5 to 40 J/cm(2) and germinated aseptically. Thirty days old seedlings were harvested and the germination, growth, physiological and biochemical parameters were estimated and compared to un-irradiated control seedlings. A significant enhancement in growth characters were noted with respect to length, fresh and dry weight of shoot and roots In addition, chlorophyll (a and b), carotenoid content, anthocyanin and amylases (α and β) activities were found to be altered. Significant alterations in percentage of seed germination (P<0.001) and time to 50% germination (P<0.001) were observed in the irradiated seeds compared to the un-irradiated controls. In conclusion, the results of the present study demonstrated that low dose (5-30 J/cm(2)) of He- Ne laser irradiation enhanced the germination process and altered growth, by positively influencing physiological and biochemical parameters of the brinjal seedlings compared to un-irradiated control under in vitro conditions. © 2012 Wiley Periodicals, Inc. Photochemistry and Photobiology © 2012 The American Society of Photobiology.
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Department of Chemistry, Indian Institute of Technology, Bombay, Powai, Mumbai 400 076, India.
We developed a simple, facile route for the synthesis of BF(2) complexes of prodigiosin type oligopyrroles and their cholesterol conjugates. This route gives an access to synthesize any desired meso-aryl-substituted 3-pyrrolyl BODIPYs which were not easily accessible earlier.
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Department of Biochemistry, Rabiammal Ahmed Maideen College for Women , Tamilnadu , India.
In humans, hypertension is considered a state of oxidative stress that can contribute to the development of atherosclerosis and other hypertension-induced organ damages. The objective of this study was to evaluate oxidative status, antioxidant activities, and oxidative stress by-products among Indian patients with various stages of hypertension. Lipid profile, enzymatic and non-enzymatic antioxidants, lipid peroxidation as thiobarbituric acid reactive substances (TBARS), C-reactive protein, electrolytes, and minerals were analyzed in the blood of newly diagnosed prehypertensives, stage I and II hypertensives (n = 20 in each group) and were compared to their age-matched normotensives. Elevated levels of lipid profile (except high density lipoprotein cholesterol [HDL-C]) were observed in stage I and II hypertensive patients. Enzymatic and non-enzymatic antioxidants were significantly (P < 0.05) lower, while TBARS and C-reactive protein were higher in prehypertensives, and stage I and II hypertensives. Significant (P <0.05) changes were also observed in the plasma Na(+) and K(+) concentrations among the hypertensive groups. Serum levels of zinc, copper, and magnesium were significantly (P < 0.05) lower in prehypertensives, and stage I and II hypertensives as compared to normotensives. The study indicated a strong association between blood pressure (BP) and oxidative stress-related parameters and suggests a possible role of oxidative stress in the development of elevated BP.
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Department of Pharmacology, N.E.T. Pharmacy College, Navodaya Nagar, Raichur - 584 103, Karnataka, India.
OBJECTIVES To evaluate the antiobesity effects of the ethanolic extract of Argyreia speciosa roots in rats fed with a cafeteria diet (CD). MATERIALS AND METHODS Obesity was induced in albino rats by feeding them a CD daily for 42 days, in addition to a normal diet. Body weight and food intake was measured initially and then every week thereafter. On day 42, the serum biochemical parameters were estimated and the animals were sacrificed with an overdose of ether. The, liver and parametrial adipose tissues were removed and weighed immediately. The liver triglyceride content was estimated. The influence of the extract on the pancreatic lipase activity was also determined by measuring the rate of release of oleic acid from triolein. RESULTS The body weight at two-to-six weeks and the final parametrial adipose tissue weights were significantly lowered (P < 0.01 and P < 0.05, respectively) in rats fed with the CD with Argyreia speciosa extract 500 mg/kg/day as compared to the CD alone. The extract also significantly reduced (P < 0.01) the serum contents of leptin, total cholesterol, low density lipoprotein (LDL), and triglycerides, which were elevated in rats fed with CD alone. In addition, the extract inhibited the induction of fatty liver with the accumulation of hepatic triglycerides. The extract also showed inhibition of pancreatic lipase activity by using triolein as a substrate. CONCLUSIONS The ethanolic extract of Argyreia speciosa roots produces inhibitory effects on cafeteria diet-induced obesity in rats.
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Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai 400 076, India.
A series of boron dipyrromethene (BODIPY) dyes containing two aldehyde functional groups at the 3 and 5 positions have been synthesized in low-to-decent yields in two steps. In the first step, the meso-aryl dipyrromethanes were treated with POCl(3) in N,N-dimethylformamide to afford 1,9-diformylated dipyrromethanes. In the second step, the diformylated dipyrromethanes were first in situ oxidized with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone and then reacted with BF(3)·OEt(2) to afford 3,5-diformylboron dipyrromethenes. The X-ray structural analysis indicated that the aldehyde groups are involved in intramolecular hydrogen bonding with fluoride atoms, which may be responsible for the stability of the diformylated BODIPY compounds. The presence of two formyl groups significantly alters the electronic properties, which is clearly evident in downfield shifts in the (1)H and (19)F NMR spectra, bathochromic shifts in the absorption and fluorescence spectra, better quantum yields, and increased lifetimes compared to 3,5-unsubstituted BODIPYs. Furthermore, 3,5-diformylboron dipyrromethenes are highly electron-deficient and undergo facile reductions compared to unsubstituted BODIPYs. These compounds exhibit pH-dependent on/off fluorescence and thus act as fluorescent pH sensors.
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Department of Industrial Biotechnology, Bharath University, Chennai, India *For correspondence : selvakumarmss@gmail.com.
A large number of active principles from traditional medicinal plants have been reported to have chemopreventive properties. In the present study, therapeutic efficacy of an aqueous extract of Indigofera aspalathoides against growth of transplanted experimental fibrosarcomas in Wistar strain male albino rats was tested. Tumors which appeared about six weeks after implantation were highly localized and were maintained by serial transplantation. Rats were divided into four groups. Group I served as normal control animals. Group II were fibrosarcoma bearing animals. Group III were animals with fibrosarcoma treated with Indigofera aspalathoides aqueous extracts at a dose of 250 mg/kg. b. w. per day for 30 days. Group IV animals were treated with aqueous extract of Indigofera aspalathoides alone. Reduction in tumor weight was noted in Group III as compared to II. The levels of cytochrome C in liver and kidney, the levels of cytochrome P450 and cytochrome b5 in liver microsomes, phase I biotransformation enzymes NADPH-cytochrome P450, NADPH-cytochrome b5, and aniline hydroxylase, and the phase II enzymes glutathione-S-transferase and UDP glucuronyl transferase indicated that their modulation played a role in the therapeutic efficacy of Indigofera aspalathoides against experimental fibrosarcoma.
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Department of Industrial Biotechnology, Bharath University, Chennai 600 073, India.
The anticancer and antioxidant effects of the aqueous extract of Indigofera aspalathoides on 20-methylcholanthrene (20-MCA) induced fibrosarcoma were investigated in male albino rats. The rats were divided into four different groups, each group consisting of six animals. Group I animals were served as normal control, Group II animals were fibrosarcoma-bearing animals after the incubation period, Group III animals were fibrosarcoma-bearing animals, treated with aqueous extract of I. aspalathoides intraperitoneally at a dose of 250 mg/kg b.w. for 30 days and Group IV animals were administered with the aqueous extract of I. aspalathoides alone, at a dose of 250 mg/kg b.w. for 30 days, served as drug control animals. After the experimental period, all the rats were weighed and killed by cervical decapitation. The serum was separated from the blood for analysis. The weights of the liver and the kidneys were noted. The fibrosarcoma was proved by pathological examinations. The liver and kidney tissues were excised and then homogenized in an ice-cold buffer. These tissues were used for biochemical analysis. The activities of antioxidant enzymes, e.g. catalase (CAT), glutathione peroxidase (GPx) and superoxide dismutase (SOD), in blood serum, liver, and kidney of control and experimental animals, respectively, have been reported. The present observations suggested that the aqueous extract of I. aspalathoides treatment enhanced the recovery from 20-MCA-induced fibrosarcoma due to its antioxidants and antineoplastic properties.
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Department of Yoga Research, Swami Vivekananda Yoga Anusandhana Samsthana, Bangalore, India.
OBJECTIVES This study compares the effects of an integrated yoga program with brief supportive therapy on distressful symptoms in breast cancer outpatients undergoing adjuvant radiotherapy. MATERIALS AND METHODS Eighty-eight stage II and III breast cancer outpatients were randomly assigned to receive yoga (n = 44) or brief supportive therapy (n = 44) prior to their radiotherapy treatment. Intervention consisted of yoga sessions lasting 60 min daily while the control group was imparted supportive therapy once in 10 days during the course of their adjuvant radiotherapy. Assessments included Rotterdam Symptom Check List and European Organization for Research in the Treatment of Cancer-Quality of Life (EORTC QoL C30) symptom scale. Assessments were done at baseline and after 6 weeks of radiotherapy treatment. RESULTS A GLM repeated-measures ANOVA showed a significant decrease in psychological distress (P = 0.01), fatigue (P = 0.007), insomnia (P = 0.001), and appetite loss (P = 0.002) over time in the yoga group as compared to controls. There was significant improvement in the activity level (P = 0.02) in the yoga group as compared to controls. There was a significant positive correlation between physical and psychological distress and fatigue, nausea and vomiting, pain, dyspnea, insomnia, appetite loss, and constipation. There was a significant negative correlation between the activity level and fatigue, nausea and vomiting, pain, dyspnea, insomnia, and appetite loss. CONCLUSION The results suggest beneficial effects with yoga intervention in managing cancer-and treatment-related symptoms in breast cancer patients.
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2012-05-23 08:26:58 © BioInfoBank Institute