World Academy of Science, Engineering and Technology

Authors: Pranporn Kuropakornpong, Srisopa Ruangnoo, Arunporn Itharat

Abstract:

Liver cancer has the highest prevalence rate in the North and Northeast of Thailand. Four Thai medicinal plants such as resin of Ferula asafoetida Regel, latex of Aloe barbadensis Miller leaves, roots of Baliospermum manotanum, and latex of Garcinia hanburyi Hook are used in Thai traditional medicine as cathartic drug and detoxification in liver cancer patients. Thus, this research aimed to evaluate the cytotoxic activity of these plants against hepatocarcinoma (HepG2) and cholangiocarcinoma (KKU-M156) cells by SRB assay. These plants were macerated in 95% ethanol. The results showed that roots of Baliospermum manotanum and latex of Garcinia hanburyi Hook showed the strongest cytotoxicity against HepG2 (IC50 = 3.03+0.91 and 0.62+0.01µg/ml, respectively) and KKU-M156 (IC50 = 0.978+0.663 and 0.006+0.005 µg/ml, respectively). Latex of Garcinia hanburyi Hook also showed high cytotoxicity against normal cell line (IC50=8.86+0.31 µg/ml), and even though its selective values are high, dose of this herb should be limited.

Keywords: cholangiocarcinoma, cytotoxic activity, Garcinia hanburyi Hook, hepatocarcinoma

Procedia PDF Downloads 456

Authors: I. L. Ibrahim, A. Mann, B. A. Adam

Abstract:

This project involved screening for antibacterial activity, phytochemical and mineral properties of Leptadenia hastata by flame photometry. The result of phytochemical screening reveals that the presence of flavonoids, tannins, saponins, alkaloids, steroidal, and anthraquinones while the cardiac glycoside was absent. This justifies the plant been used as anti-bleeding and anti-inflammatory agents. The result of flame photometry revealed that 1.85 % (Na), 0.65% (K) and 1.85 % (Ca) which indicates the safe nature of the plant extract as such could be used to lower high blood pressure. The antibacterial properties of both the aqueous and ethanolic extract were studied against some bacteria, Escherichia coli, Bacillus Cercus, Pseudomonas aeruginas, and Enterobacter aerogegens, by disc diffusion method and the result reveals that there are very good activities against the organism while the ethanolic extract at concentration 1.0 – 1.2 mg/ml. the ethanolic extract showed in considerable zone inhibition against bacteria’s; Escherichia coli, Bacillus Cercus, pseudomonas aeruginosa andklebsellapnemuoniae. Minimum inhibitory concentration (MIC) and minimum Bacterial concentration (MBC) were conducted with fairly good significant effect of inhibition on the organism, therefore, plant extract could be a potential source of antibacterial agent.

Keywords: antibacterial activity, Leptadenia hastata, infectious diseases, phytochemical screening

Procedia PDF Downloads 590

Authors: Arunporn Itharat, Srisopa Ruangnoo, Pakakrong Thongdeeying

Abstract:

The rhizomes of Dioscorea membranacea (DM) has long been used in Thai Traditional medicine to treat cancer and inflammatory conditions such as rheumatism. The objective of this study was to investigate anti-inflammatory activity by determining the inhibitory effect on LPS-induced TNF-α from RAW264.7 cells of crude extracts and pure isolated compounds from DM. Three known dihydrophenantrene compounds were isolated by a bioassay guided isolation method from DM ethanolic extract [2,4 dimethoxy-5,6-dihydroxy-9,10-dihydrophenanthrene (1) and 5-hydroxy-2,4,6-trimethoxy-9,10-dihydrophenanthrene(2) and 5,6,2 -trihydroxy 3,4-methoxy, 9,10- dihydrophenanthrene (3)]. 1 showed the highest inhibitory effect on PGE2, followed by 3 and 1 (IC50 = 2.26, 4.97 and >20 μg/ml or 8.31,17.25 and > 20 µM respectively). These findings suggest that this plant showed anti-inflamatory effects by displaying an inhibitory effect on TNF-α release, hence, this result supports the usage of Thai traditional medicine to treat inflammation related diseases.

Keywords: Dioscorea membranacea, anti-inflammatory activity, TNF-Alpha , dihidrophenantrene compound

Procedia PDF Downloads 507

Authors: Kriyapa lairungruang, Arunporn Itharat

Abstract:

Limonia acidissima L. (LA) (Common name: wood apple, Thai name: ma-khwit) is a medicinal plant which has long been used in Thai traditional medicine. Its bark is used for treatment of diarrhea, abscess, wound healing and inflammation and it is also used in oral cancer. Thus, this research aimed to investigate antioxidant and cytotoxic activities of the LA bark extracts produced by various extraction methods. Different extraction procedures were used to extract LA bark for biological activity testing: boiling in water, maceration with 95% ethanol, maceration with 50% ethanol and water boiling of each the 95% and the 50% ethanolic residues. All extracts were tested for antioxidant activity using DPPH radical scavenging assay, cytotoxic activity against human laryngeal epidermoid carcinoma (HEp-2) cells and human oral epidermoid carcinoma (KB) cells using sulforhodamine B (SRB) assay. The results found that the 95% ethanolic extract of LA bark showed the highest antioxidant activity with EC50 values of 29.76±1.88 µg/ml. For cytotoxic activity, the 50% ethanolic extract showed the best cytotoxic activity against HEp-2 and KB cells with IC50 values of 9.55±1.68 and 18.90±0.86 µg/ml, respectively. This study demonstrated that the 95% ethanolic extract of LA bark showed moderate antioxidant activity and the 50% ethanolic extract provided potent cytotoxic activity against HEp-2 and KB cells. These results confirm the traditional use of LA for the treatment of oral cancer and laryngeal cancer, and also support its ongoing use.

Keywords: antioxidant activity, cytotoxic activity, Laryngeal epidermoid carcinoma, Limonia acidissima L., oral epidermoid carcinoma

Procedia PDF Downloads 479

Authors: Purnima Rawat, Divya Vohora, Sarika Gupta, Farhan J. Ahmad, Sushama Talegaonkar

Abstract:

Nanoparticles (NPs) that target bone tissue were developed using PLGA–mPEG (poly(lactic-co-glycolic-acid)–polyethylene glycol) diblock copolymers by using pamidronate as a bone-targeting moieties. These NPs are expected to enable the transport of hydrophilic drugs. The NP was prepared by in situ polymerization method, and their in- vitro characteristics were evaluated using dynamic light scattering, transmission electron microscopy (TEM) and in phosphate-buffered solution. The bone targeting potential of the NP was also evaluated on in-vitro pre-osteoblast MCT3E1 cell line using ALP activity, degree of mineralization and RT-PCR assay. The average particle size of the NP was 101.6 ± 3.7nm, zeta potential values were negative (-25±0.34mV) of the formulations and the entrapment efficiency was 93± 3.1 % obtained. The moiety of the PLGA–mPEG–pamidronate NPs exhibited the best apatite mineral binding ability in-vitro MCT3E1 pre-osteoblast cell line. Our results suggested that the developed nanoparticles may use as a delivery system for Pamidronate in bone repair and regeneration, warranting further evaluation of the treatment of bone disease.

Keywords: nanoparticle, pamidronate, in-situ polymerization, osteoblast

Procedia PDF Downloads 484

Authors: Fatemeh Soltani, Simindokht Shirvani Arani, Ali Bahrami Samani, Mahdi Sadeghi, Kamal Yavari

Abstract:

Cerium-141 [T1/2 = 32.501 days, Eβ (max) = 0.580 (29.8%) and 0.435(70.2%) MeV, Eγ=145.44 (48.2%) keV] possesses radionuclidic properties suitable for use in palliative therapy of bone metastases. 141Ce also has gamma energy of 145.44 keV, which resembles that of 99mTc. Therefore, the energy window is adjustable on the Tc-99m energy because of imaging studies. 141Ce can be produced through a relatively easy route that involves thermal neutron bombardment on natural CeO2 in medium flux research reactors (4–5×1013 neutrons/cm2•s). The requirement for an enriched target does not arise. Ethylenediamine tetramethylene phosphonic acid (EDTMP) was synthesized and radiolabeled with 141Ce. Complexation parameters were optimized to achieve maximum yields (>99%). The radiochemical purity of 141Ce-EDTMP was evaluated by radio-thin layer chromatography. The stability of the prepared formulation was monitored for one week at room temperature, and results showed that the preparation was stable during this period (>99%). Biodistribution studies of the complexes carried out in wild-type rats exhibited significant bone uptake with rapid clearance from blood. The properties of produced 141Ce-EDTMP suggest applying a new efficient bone pain palliative therapeutic agent to overcome metastatic bone pains.

Keywords: bone pain palliative, cerium-141, EDTMP, radiopharmaceutical

Procedia PDF Downloads 494

Authors: Arunporn Itharat, Kamonmas Srikwan, Srisopa Ruangnoo, Pakakrong Thongdeeying

Abstract:

Background: The rhizomes of Smilax glabra (SG) has long been used in Traditional Chinese and Thai herbal medicine to treat a variety of infectious diseases and immunological disorders. Objective: To investigate the in vitro anti-allergic activities of crude extracts and pure isolated flavonoid compounds from SG by determination of inhibitory effects on antigen-induced release of β-hexosaminidase from RBL-2H3 cells. Methods: The in vitro inhibitory effects of crude aqueous and organic extracts on beta-hexosaminidase release in RBL-2H3 cells were evaluated as an in vitro indication of possible anti-allergic activity in vivo. Bioassay-guided fractionation of extracts was used to isolate flavonoid compounds from the ethanolic extracts. Results: The 95% and 50% ethanolic extracts of SG showed remarkably high anti-allergic activity, with IC50 values of 5.74 ± 2.44 and 23.54 ± 4.75 μg/ml, much higher activity than that for Ketotifen (IC50 58.90 μM). The water extract had negligible activity (IC50 > 100 μg/ml). The two isolated flavonols, Engeletin and Astilbin, showed weak anti-allergic activity, IC50 values 97.46 ± 2.04 and > 100 μg/ml, respectively. Conclusions: The 95% and 50% ethanolic extracts of SG showed strong anti-allergic activity but two flavonol constituents did not show any significant anti-allergic activity. These findings suggest that a combination of effects of various phytochemicals in crude extracts used in traditional medicine are responsible for the purported anti-allergic activity of SG herbal preparations. The plethora of constituents in crude extracts, as yet unidentified, are likely to be acting synergistically to account for the strong observed anti-allergic in vitro activity.

Keywords: Smilax glabra, anti-allergic activity, RBL-2H3 cells, flavonoid compounds

Procedia PDF Downloads 670

Authors: Deepak Suresh Mohale, Anil V. Chandewar

Abstract:

Anxiety is defined as an exaggerated feeling of apprehension, uncertainty and fear. Nerium indicum is a well-known ornamental and medicinal plant belonging to the family Apocynaceae. A wide spectrum of biological activities has been reported with various constituents isolated from different parts of the plant. This study was conducted to investigate antianxiety activity of flower extract. Flowers were collected and dried in shade and coarsely powdered. Powdered mixture was extracted with ethyl acetate by maceration process. Extract of flowers obtained was subsequently dried in oven at 40-50 °C. This extract is then tested for antianxiety activity at low and high dose using elevated plus maze and light & dark model. Rats shown increased open arm entries and time spent in open arm in elevated Plus maze with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. In Light & dark Model, light box entries and time spent in light box increased with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. From result it is concluded that ethyl acetate extract of flower of Nerium indicum possess antianxiety activity at low and high dose.

Keywords: antianxiety, anxiety, kaner, nerium indicum, social isolation

Procedia PDF Downloads 398

Authors: A. Bhattacharya, Sanjay Gupta, S. H. Bodakhe

Abstract:

HbA1c is form of the haemoglobin that is used to measure the average plasma glucose concentration over prolonged periods of time. It is formed in a non-enzymatic glycation pathway by hemoglobin's exposure to plasma glucose. In diabetes mellitus, higher amounts of glycated hemoglobin, indicating poorer control of blood glucose levels, have been associated with cardiovascular disease, nephropathy, and retinopathy. Guraku’s basic components are nicotine and jaggery, jaggery is made up of sugarcane so can have a diabetogenic potential which is exacerbated in presence of nicotine. This work had done with the aim to find correlation between Diabetic cataract, HbA1c and Guraku. Subjects were enrolled according to the inclusion and exclusion criteria. In this study total 75 subjects were included. In the study it was found that people consuming Guraku had a high level of HbA1c thus are more prone to the development of diabetic cataract. Male subjects are the more than female subjects. Most of the subjects belong to the lower socioeconomical class and not very educated. It could be concluded that this type of study could be useful in indentifying number of subjects suffering from diabetic cataract whose condition get worse by use of nicotine product like Guraku and preventive measure to be taken in prevention of this type of diabetic complication.

Keywords: diabetic cataract, HbA1c, Guraku, diabetogenic potential

Procedia PDF Downloads 407

Authors: Ubaka Chukwuemeka Michael, Ukwe Chinwe Victoria

Abstract:

Background: The use of antipsychotic monotherapy remains the standard for schizophrenic disorders so also a prescription switch from older typical to newer atypical classes of antipsychotics on the basis of better efficacy and tolerability. However, surveys on the quality of antipsychotic drug use and substitution in developing countries are very scarce. This study was intended to evaluate quality and factors that drive the prescription and substitution of antipsychotic drugs among schizophrenic patients visiting a regional psychiatric hospital. Methods: Case files of patients visiting a federal government funded Neuropsychiatric Hospital between July 2012 and July 2014 were systematically retrieved. Patient demographic characteristics, clinical details and drug management data were collected and subjected to descriptive and inferential data analysis to determine quality and predictors of utilization. Results: Of the 600 case files used, there were more male patients (55.3%) with an overall mean age of 33.7±14.4 years. Typical antipsychotic agents accounted for over 85% of prescriptions, with majority of the patients receiving more than 2 drugs in at least a visit (80.9%). Fluphenazine (25.2%) and Haloperidol (18.8%) were mostly given as antipsychotics for treatment initiation while Olazenpine (23.0%) and Benzhexol (18.3%) were the most currently prescribed antipsychotics. Nearly half (42%, 252/600) of these patients were switched from one class to another, with 34.5% (207/600) of them switched from typical to atypical drug classes. No demographic or clinical factors influenced drug substitutions but a younger age and being married influenced being prescribed a polypharmacy regimen (more than 2 drugs) and an injectable antipsychotic agent. Conclusion: The prevalence of antipsychotic polypharmacy and use of typical agents among these patients was high. However, only age and marital status affected the quality of antipsychotic prescriptions among these patients.

Keywords: antipsychotics, drug substitution, pharmacoepidemiology, polypharmacy

Procedia PDF Downloads 477

Authors: Oluwafemi Ojo, Omotade Oloyede

Abstract:

This study seeks to investigate the antioxidative properties and the ability of aqueous, ethanolic and ethyl acetate extracts from Ocimum gratissimum (OG) leaves to inhibit some pro-oxidants (Fe2+ and sodium nitroprusside) induced lipid peroxidation in rat’s liver homogenates in vitro. The ability of the extracts to inhibit 25 µM FeSO4 and 7.0 µM sodium nitroprusside induced lipid peroxidation in isolated rat’s liver was determined. The results of the study revealed that both pro-oxidants caused a significantly decrease in (p < 0.05) accumulation of lipid peroxides. However, aqueous extract of OG shows a high ability to inhibit lipid production in the liver induced with SNP than Fe2+. Ethanolic and ethyl acetate extract of OG which shows a high ability to inhibit lipid production more when induced with Fe2+ than SNP. However, ethyl acetate fraction of OG shows a higher inhibitory effect on both Fe2+ and SNP induced lipid peroxidation in rat’s liver. This applies to its significantly higher extractable phytochemicals. Therefore, Fe II and sodium nitroprusside induced oxidative stress could be managed by dietary intake of Ocimum gratissimum leaves.

Keywords: antioxidative, pro-oxidants, lipid peroxidation, Ocimum gratissimum

Procedia PDF Downloads 484

Authors: Aghaei Amirkhizi Navideh, Sadjadi Soodeh Sadat, Moghaddam Banaem Leila, Athari Allaf Mitra, Johari Daha Fariba

Abstract:

Dendrimers are good candidates for preparing metal nanoparticles because they can structurally and chemically well-defined templates and robust stabilizers. Poly amidoamine (PAMAM) dendrimer-based multifunctional cancer therapeutic conjugates have been designed and synthesized in pharmaceutical industry. In addition, encapsulated nanoparticle surfaces are accessible to substrates so that catalytic reactions can be carried out. For preparation of dendimer-metal nanocomposite, a dendrimer solution containing an average of 55 Yb+3 ions per dendrimer was prepared. Prior to reduction, the pH of this solution was adjusted to 7.5 using NaOH. NaBH4 was used to reduce the dendrimer-encapsulated Yb+3 to the zerovalent metal. The pH of the resulting solution was then adjusted to 3, using HClO4, to decompose excess BH4-. The UV-Vis absorption spectra of the mixture were recorded to ensure the formation of Yb-G5-NH2 complex. High-resolution electron microscopy (HRTEM) and size distribution results provide additional information about dendimer-metal nanocomposite shape, size, and size distribution of the particles. The resulting mixture was irradiated in Tehran Research Reactor 2h and neutron fluxes were 3×1011 n/cm2.Sec and the specific activity was 7MBq. Radiochemical and chemical and radionuclide quality control testes were carried. Gamma Spectroscopy and High-performance Liquid Chromatography HPLC, Thin-Layer Chromatography TLC were recorded. The injection of resulting solution to solid tumor in mice shows that it could be resized the tumor. The studies about solid tumors and nano composites show that ytterbium encapsulated-dendrimer radiopharmaceutical could be introduced as a new therapeutic for the treatment of solid tumors.

Keywords: nano-radio pharmaceutical, ytterbium, PAMAM, dendrimers

Procedia PDF Downloads 505

Authors: Alaa E. El-sisi, Sherin Zakaria

Abstract:

Rebamipide is an antiulcer drug with unique properties such as anti-inflammatory action. It induces endogenous prostaglandin e2 (PGE2). PGE2 is considered as a potent physiological suppressor of liver fibrosis. Aim of study: This study investigated the effect of rebamipide on hepatic fibrosis. Material and Method: Hepatic fibrosis was induced by intraperitoneal injections (IP) injection of CCl4 (0.45 mL/kg) in corn oil 1:5 twice a week for 4 weeks. Rats were divided into four groups as follow: Group 1 treated with CCL4 only, group 2 and 3 treated with CCL4 and rebamipide 60 mg/kg/day (group2) or 100 mg/kg/day (group3), and the fourth group was considered as control group and treated with vehicles. ALT, AST, and Bilirubin were assayed in serum. Antioxidant markers such as malondialdhyde (MDA) and superoxide dismutase (SOD) and fibrotic markers such as hyaluronic acid (HA) and procollagen-III (procol-III) were evaluated in liver tissues. IL-10 as well as PGE2 were also assayed in liver tissues. Pathologic changes in the liver were detected by hematoxylin and eosin staining. Collagen precipitation in liver tissues was visualized using masson trichrom stain. Results: Rebamipide inhibit CCL4 induced increase in ALT and AST significantly (p < 0.05). Rebamipide exerted an antioxidant effect as it inhibits CCL4 induced increased MDA level and decreased SOD activity. Fibrotic markers assay revealed that repamipide (60 or 100 mg/kg/day) decreased the level of procol-III and HA compared to CCl4 (p < 0.05). Oral administration of Rebamipide was associated with a significant increase (p < 0.05) of PGE2 and IL-10. Rebamipide especially at the dose of (100 mg/kg/day) restores liver histology structure and abolish collagen precipitation in liver tissues. Conclusion: Rebamipide retards hepatic fibrosis induced by CCL4 may be through the induction of PGE2 level.

Keywords: fibrotic markers, hepatic fibrosis, PGE2, rebamipide

Procedia PDF Downloads 488

Authors: Flavia Laffleur

Abstract:

Summary: Biomaterials have gained immense interest in the pharmaceutical research in the last decades. Hyaluronic acid a carbohydrate and mucopolysaccharide was chemically modified in order to achieve and establish a promising platform for buccal drug delivery. Aim: Novel biomaterial was tested for its potential for buccal drug delivery. Background: Polysaccharide hyaluronic acid (HA) was chemically modified with cysteine ethyl ether (CYS). By immobilization of the thiol-bearing ligand on the polymeric backbone the thiolated bioconjugate HA-CYS was obtained. Methodology: Mucoadhesive, permeation enhancing and stability potential as well as mechanical, physicochemical properties further mucoadhesive strength, swelling index and residence time were investigated. The developed thiolated bioconjugate displayed enhanced mucoadhesiveness on buccal mucosa as well as permeation behavior and polymer stability. The near neutral pH and negative cytotoxicity studies indicated their non-irritability and biocompatible nature with biological tissues. Further, the model drug sulforhodamine 101 was incorporated to determine its drug release profiles. Results: The synthesized thiomer showed no toxicity. The mucoadhesion of thiolated hyaluronic acid on buccal mucosa was significantly improved in comparison to unmodified one. The biomaterial showed 2.5-fold higher stability in polymer structure. The release of sulforhodamine in the presence of thiolated hyaluronic acid was 2.3-fold increased compared to hyaluronic acid. Conclusion: Thus, the promising results encourage further investigations and exploitation of this versatile polysaccharide. So far, hyaluronic acid was not evaluated for buccal drug delivery.

Keywords: buccal delivery, hyaluronic acid, mucoadhesion, thiomers

Procedia PDF Downloads 505

Authors: Maryam Zahedi Fard, Nazia Abdul Majid, Hapipah Mohd Ali, Mahmood Ameen Abdulla

Abstract:

New quinazoline schiff base 3-(5-bromo-2-hydroxy-3-methoxybenzylideneamino)-2-(5-bromo-2-hydroxy-3-methoxyphenyl)-2,3-dihydroquinazolin-4(1H)-one was investigated for anticancer activity against MCF-7 human breast cancer cell line with involved mechanism of apoptosis. The compound demonstrated a remarkable antiproliferative effect, with an IC50 value of 3.41 ± 0.34, after 72 hours of treatment. Morphological apoptotic features in treated MCF-7 cells were observed by AO/PI staining. Furthermore, treated MCF-7 cells subjected to apoptosis death, as exhibited by perturbation of mitochondrial membrane potential and cytochrome c release as well as increase in ROS generation. We also found activation of caspases 3/7 and -9. Moreover, acute toxicity test demonstrated the nontoxic nature of the compound in mice. Our results showed the selected compound significantly induce apoptosis in MCF-7 cells via intrinsic pathway, which might be considered as a potent candidate for further in vivo and clinical breast cancer studies.

Keywords: antiproliferative effect, MCF-7 human breast cancer cell line, apoptosis, caspases

Procedia PDF Downloads 535

Authors: A. Mirzaei, S. Zolghadri, M. Athari-Allaf, H. Yousefnia, A. R. Jalilian

Abstract:

Rheumatoid arthritis is the most common autoimmune disease, leading to the destruction of the joints. The aim of this study was the preparation of 90Y-chitosan complex as a novel agent for radiosynovectomy. The complex was prepared in the diluted acetic acid solution. At the optimized condition, the radiochemical purity of higher than 99% was obtained by ITLC method on Whatman No. 1 and by using a mixture of methanol/water/acetic acid (4:4:2) as the mobile phase. The complex was stable in acidic media (pH=3) and its radiochemical purity was above 98% even after 48 hours. The biodistribution data in rats showed that there was no significant leakage of the injected activity even after 48 h. Considering all of the excellent features of the complex, 90Y-chitosan can be used to manipulate synovial inflammation effectively.

Keywords: chitosan, Y-90, radiosynovectomy, biodistribution

Procedia PDF Downloads 488

Authors: D. S. Mohale, A.V. Chandewar

Abstract:

Study was undertaken to investigate the effect of imipramine on various biochemical parameters and oxidative stress markers in short and long term depression on rats. Rats were subjected for short (21 days) and long term (84 days) social isolation for and checked for depression on force swim test and tail suspension method. Various markers of oxidative stress like lipid peroxidation (LPO), reduced glutathione (GSH), Supersoxide dismutase (SOD), catalase (CAT) and biochemical parameters like Serum glutamate oxaloacetate transaminase (SGOT), Serum glutamate pyruate transaminase (SGPT), and blood glucose were determined in depressed, control, imipramine and Vitamin E treated group. The rats displayed an increase in depression on force swim test and tail suspension method relative to control. There was significant increase in the level of LPO and decrease in the levels of GSH, SOD and CAT after short and long term depression. Increased oxidative stress in depression which may leads to alteration of biochemical parameters. Treatment with imipramine an tricyclic antidepressant significantly decreases in level of LPO, SGOT, SGPT and increase in the levels of GSH, SOD and CAT in long term depression.

Keywords: depression, oxidative stress, lipid peroxidation, reduced glutathione

Procedia PDF Downloads 504

Authors: Abhishek Kumar Sah, Preeti K. Suresh

Abstract:

Effective drug delivery to the eye is a massive challenge, due to complicated physiological ocular barriers, rapid washout by tear and nasolachrymal drainage. Thus, most of the conventional ophthalmic formulations face the problem of low ocular bioavailability. Ophthalmic drug therapy can be improved by enhancing the precorneal drug retention along with improved drug penetration. The aim of the present investigation was to develop and evaluate a biodegradable polymer poly (D, L-lactide-co-glycolide) (PLGA) coated nanoparticulate carrier of loteprednol etabonate. PLGA nanoparticles were prepared by modified emulsification/solvent diffusion method using high-speed homogenizer followed by sonication. The nanoparticles were characterized for various parameters such as particle size, zeta potential, polydispersity index, X-ray powder diffraction (XRD), Transmission electron microscopy (TEM), in vitro drug release profile and stability. The prepared nanocarriers displayed mean particle size in the range of 271.7 to 424.4 nm, with zeta potential less than –10 mV. In vitro release in simulated tear fluid (STF) nanocarrier showed an extended release profile of loteprednol etabonate. TEM confirmed the spherical morphology and smooth surface of the particles. All the prepared formulations were found to be stable at varying temperatures.

Keywords: drug delivery, ocular delivery, polymeric nanoparticles, loteprednol etabonate

Procedia PDF Downloads 555

Authors: Po-Chin Liang, Yung-Chu Chen, Chi-Feng Chiang, Yun-Ping Lin, Wen-Yuan Hsieh, Win-Li Lin

Abstract:

The aim of this study was to develop super paramagnetic iron oxide (SPIO) nano-particles comprised of a magnetic Fe3O4 core and a shell of aqueous stable self-doped polyethylene glycol (PEG) with a high loading of doxorubicin (SPIO-PEG-D) for tumor theranostics. The in-vivo MRI study showed that there was a stronger T2-weighted signal enhancement for the group under a magnetic field, and hence it indicated that this group had a better accumulation of SPIO-PEG than the group without a magnetic field. In the anticancer evaluation of SPIO-PEG-D, the group with a magnetic field displayed a significantly smaller tumor size than the group without. The overall results show that SPIO-PEG-D nanoparticles have the potential for the application of MRI/monitoring chemotherapy and the therapy can be locally enhanced by applying an external magnetic field.

Keywords: super paramagnetic iron oxide nano particles, doxorubicin, chemotherapy, MRI, magnetic fields

Procedia PDF Downloads 605

Authors: S. S. Patil, R. M. Mhetre, S. V. Patil

Abstract:

Lisinopril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and heart failure in prophylactic treatment after myocardial infarction and in diabetic nephropathy. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of lisinopril by formulating intranasal microspheres with Carbopol 974P NF and HPMC K4 M along with film forming polymer ethyl cellulose.The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, ex vivo mucoadhesion, drug release, ex vivo diffusion studies. All formulations has shown entrapment efficiency between 80 to more than 95%, mucoadhesion was more than 80 % and drug release up to 90 %. Ex vivo studies revealed tht the improved bioavailability of drug compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres shown better results than single carbopol based microspheres for the delivery of lisinopril.

Keywords: microspheres, lisinopril, nasal delivery, solvent evaporation method

Procedia PDF Downloads 532

Authors: S. V. Patil, P. S. Dounde, S. S. Patil

Abstract:

Emulgels have emerged as one of the most interesting topical delivery system as it has dual release control system that is gel and emulsion. The major objective behind this formulation is delivery of hydrophobic drugs to systemic circulation via skin. In fact presence of a gelling agent in water phase converts a classical emulsion in to emulgel. The emulgel for dermatological use has several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, non-staining, water-soluble, longer shelf life, bio-friendly, transparent and pleasing appearance. Various penetration enhancers can potentiate the effect. So this can be used as better topical drug delivery systems over present conventional systems available in market. Piroxicam is a non-steroidal anti-inflammatory drug that has major problems when administered orally; it is an insoluble drug and has irritant effect on gastro intestinal tract lead to ulceration and bleeding. The aim of this study was to overcoming these problems through preparation of topical emulgel of this drug. Emulgel of Piroxicam was prepared using Carbopol 940 along with mentha oil and clove oil as permeation enhancer. The prepared emulgel were evaluated for their physical appearance, pH determination, viscosity, spreadability, in vitro drug release, ex vivo permeation studies. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity and pH value. The emulgel was found to be stable with respect to physical appearance, pH, rheological properties and drug content at all temperature and conditions for three month.

Keywords: emulgel, piroxicam, menthe oil, clove oil

Procedia PDF Downloads 458

Authors: Nassim Belkacem, Amina Azzam, Dalila Haouchine, Kahina Bennacer, Samira Soufit

Abstract:

Objective: To evaluate the antioxidant activity of the methanolic extract along with the antimicrobial activity of the essential oil of the aerial parts of Rosmarinus officinalis L. collected in the region of Bejaia (northern center of Algeria). Materials and methods: The polyphenols and flavonoids contents of the methanolic extract were measured. The antioxidant activity was evaluated using two methods: the ABTS method and DPPH assay. The antimicrobial activity was studied by the agar diffusion method against five bacterial strains (Three Gram positive strains and two Gram negative strains) and one fungus. Results: The total polyphenol and flavonoid content was about 43.8 mg gallic acid equivalent per gram (GA Eq/g) and 7.04 mg quercetin equivalent per gram (Q Eq/g), respectively. In the ABTS assay, the rosemary extract has shown an inhibition of 98.02% at the concentration of 500ug/ml with a half maximal inhibitory concentration value (IC50) of 194.92ug/ml. The results of DPPH assay have shown that the rosemary extract has an inhibition of 94.67 % with an IC50 value of 17.87ug/ml, which is lower than that of Butylhydroxyanisol (BHA) about 6.03ug/ml and ascorbic acid about 1.24μg/ml. The yield in essential oil of rosemary obtained by hydrodistillation was 1.42%. Based on the determination of the diameter of inhibition, different antimicrobial activity of the essential oil was revealed against the six tested microbes. Escherichia coli from the University Hospital (UH), Streptococcus aureus (UH) and Pseudomonas aeruginosa ATCC have a minimum inhibitory concentration value (MIC) of 62.5µl/ml. However, Bacillus sp (UH) and Staphylococcus aureus ATCC have an MIC value of 125μl/ml. The inhibition zone against Candida sp was about 24 mm. The aromatograms showed that the essential oil of rosemary exercises an antifungal activity more important than the antibacterial one.

Keywords: Rosmarinus officinalis L., maceration, essential oil, antioxidant, antimicrobial activity

Procedia PDF Downloads 525

Authors: Abdelkader Basli, Jean-Claude Delaunay, Eric Pedrot, Jean-Michel Mérillon, Jean-Pierre Monti, Khodir Madani, Mohamed Chibane, Tristan Richard

Abstract:

The antioxidant and antimicrobial activities of Origanum glandulosum collected in Algeria have been studied. Extract was prepared from aerial part of endemic Algerian oregano. The produced extract has been characterized in terms of total phenols (using Folin method), total flavonoid, antioxidant activities (using the DPPH radical scavenging method and ORAC assay) and microbial activity against four bacteria: Streptococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae one yeast: Candida albicans and one fungi: Aspergillus niger. The results pointed the antioxidant activities of the extract of O. glandulosum and antimicrobial activities against all bacteria and C. Candida, but no effect on A. niger. High performance liquid chromatography combined with mass spectrometry (LC-MS) and nuclear magnetic resonance (LC-NMR) were used to separate and identify the major compounds present in the oregano extract. Rosmarinic acid, globoidnan A and B, lithospermic acid B and three flavonoids were identified.

Keywords: origanum glandulosum, antioxidant, microbial activity, polyphenol, LC-MS, LC-NMR

Procedia PDF Downloads 648

Authors: Travis J. Meyer, Jasodra Ramlall, Phyo Thu, Nidhi Gadura

Abstract:

For centuries humans have used the antimicrobial properties of copper to their advantage. Yet, after all these years the underlying mechanisms of copper mediated cell death in various microbes remain unclear. We had explored the hypothesis that copper mediated increased levels of lipid peroxidation in the membrane fatty acids is responsible for increased killing inEscherichia coli. In this study we show that in both gram positive (Staphylococcus aureus) and gram negative (Pseudomonas aeruginosa) bacteria there is a strong correlation between copper mediated cell death and increased levels of lipid peroxidation. Interestingly, the non-spore forming gram positive bacteria as well as gram negative bacteria show similar patterns of cell death, increased levels of lipid peroxidation, as well as genomic DNA degradation, however there is some difference inloss in membrane integrity upon exposure to copper alloy surface.

Keywords: antimicrobial, copper, gram positive, gram negative

Procedia PDF Downloads 485

Authors: Krutika K. Sawant, Anil Solanki

Abstract:

The present study deals with the preparation and optimization of ethyl cellulose-containing disopyramide phosphate loaded microspheres using solvent evaporation technique. A central composite design consisting of a two-level full factorial design superimposed on a star design was employed for optimizing the preparation microspheres. The drug:polymer ratio (X1) and speed of the stirrer (X2) were chosen as the independent variables. The cumulative release of the drug at a different time (2, 6, 10, 14, and 18 hr) was selected as the dependent variable. An optimum polynomial equation was generated for the prediction of the response variable at time 10 hr. Based on the results of multiple linear regression analysis and F statistics, it was concluded that sustained action can be obtained when X1 and X2 are kept at high levels. The X1X2 interaction was found to be statistically significant. The drug release pattern fitted the Higuchi model well. The data of a selected batch were subjected to an optimization study using Box-Behnken design, and an optimal formulation was fabricated. Good agreement was observed between the predicted and the observed dissolution profiles of the optimal formulation.

Keywords: disopyramide phosphate, ethyl cellulose, microspheres, controlled release, Box-Behnken design, factorial design

Procedia PDF Downloads 460

Authors: Zahid Manzoor, Shaukat Hussain Munawar, Zahid Iqbal, Imran Ahmad Khan, Abdul Aziz, Hafiz Muhammad Qasim

Abstract:

The present study was aimed to investigate the pharmacokinetics behavior and optimal dosage regimen of danofloxacin in 8 adult healthy buffaloes of local breed (Nili Ravi) following single intravenous administration at the dose of 2.5 mg/kg body weight. Plasma drug concentrations at various time intervals were measured by HPLC method. In vitro plasma protein binding was determined employing the ultrafiltration technique. The distribution and elimination of danofloxacin was rapid, as indicated by the values (Mean±SD) of distribution half-life (t1/2α = 0.25±0.09 hours) and elimination half life (t1/2β = 3.26±0.43 hours), respectively. Volume of distribution at steady state (Vss) was 1.14±0.12 L/kg, displaying its extensive distribution into various body fluids and tissues. The high value of AUC (9.80±2.14 µg/ml.hr) reflected the vast area of the body covered by drug concentration. The mean residence time was noted to be 4.78±0.52 hours. On the basis of pharmacokinetic parameters, a suitable intravenous regimen for danofloxacin in adult buffaloes would be 6.5 mg/kg to be repeated after 12 hours intervals. The present study is the foremost pharmacokinetic study of danofloxacin in the local species which would provide the valueable contribution in the local manufacturing of danofloxacin in Pakistan in future.

Keywords: danofloxacin, pharmacokinetics, plasma protein binding, buffaloes, dosage regimen

Procedia PDF Downloads 615

Authors: Hsiang-Ru Lin

Abstract:

Cholesterol plays an essential role in the regulation of the progression of numerous important diseases including atherosclerosis and Alzheimer disease so the generation of suitable cholesterol-lowering reagents is urgent to develop. Liver X receptor (LXR) is a ligand-activated transcription factor whose natural ligands are cholesterols, oxysterols and glucose. Once being activated, LXR can transactivate the transcription action of various genes including CYP7A1, ABCA1, and SREBP1c, involved in the lipid metabolism, glucose metabolism and inflammatory pathway. Essentially, the upregulation of ABCA1 facilitates cholesterol efflux from the cells and attenuates the production of beta-amyloid (ABeta) 42 in brain so LXR is a promising target to develop the cholesterol-lowering reagents and preventative treatment of Alzheimer disease. Engelhardia roxburghiana is a deciduous tree growing in India, China, and Taiwan. However, its chemical composition is only reported to exhibit antitubercular and anti-inflammatory effects. In this study, four compounds, engelheptanoxides A, C, engelhardiol A, and B isolated from the root of Engelhardia roxburghiana were evaluated for their agonistic activity against LXR by the transient transfection reporter assays in the HepG2 cells. Furthermore, their interactive modes with LXR ligand binding pocket were generated by molecular modeling programs. By using the cell-based biological assays, engelheptanoxides A, C, engelhardiol A, and B showing no cytotoxic effect against the proliferation of HepG2 cells, exerted obvious LXR agonistic effects with similar activity as T0901317, a novel synthetic LXR agonist. Further modeling studies including docking and SAR (structure-activity relationship) showed that these compounds can locate in LXR ligand binding pocket in the similar manner as T0901317. Thus, LXR is one of nuclear receptors targeted by pharmaceutical industry for developing treatments of Alzheimer and atherosclerosis diseases. Importantly, the cell-based assays, together with molecular modeling studies suggesting a plausible binding mode, demonstrate that engelheptanoxides A, C, engelhardiol A, and B function as LXR agonists. This is the first report to demonstrate that the extract of Engelhardia roxburghiana contains LXR agonists. As such, these active components of Engelhardia roxburghiana or subsequent analogs may show important therapeutic effects through selective modulation of the LXR pathway.

Keywords: Liver X receptor (LXR), Engelhardia roxburghiana, CYP7A1, ABCA1, SREBP1c, HepG2 cells

Procedia PDF Downloads 422

Authors: Rachmat Mauludin, Dita Sasri Primaviri, Irda Fidrianny

Abstract:

Propolis contains several antioxidant compounds which can be used in topical application to protect skin against free radical, prevent skin cancer and skin aging. Previous study showed that 70% ethanolic extract of propolis (EEP) provided the greatest antioxidant activity. Since EEP has very small solubility in water, the extract was prepared in nanoemulsion (NE). Nanoemulsion is chosen as cosmetic dosage forms according to its properties namely to decrease the risk of skin’s irritation, increase penetration, prolong its time to remain in our skin, and improve stability. Propolis was extracted using reflux methods and concentrated using rotavapor. EEP was characterized with several tests such as phytochemical screening, density, and antioxidant activity using DPPH method. Optimation of total surfactant, co-surfactant, oil, and amount of EEP that can be included in NE were required to get the best NE formulation. The evaluations included to organoleptic observation, globul size, polydispersity index, morphology using TEM, viscosity, pH, centrifuge, stability, Freeze and Thaw test, radical scavenging activity using DPPH method, and primary irritation test. The yield extracts was 11.12% from raw propolis contained of steroid/triterpenoid, flavonoid, and saponin based on phytochemical screening. EEP had the value of DPPH scavenging activity 61.14% and IC50 0.41629 ppm. The best NE formulation consisted of 26.25% Kolliphor RH40; 8.75% glycerine; 5% rice bran oil; and 3% EEP. NE was transparant, had globul size of 21.9 nm; polydispersity index of 0.338; and pH of 5.67. Based on TEM morphology, NE was almost spherical and has particle size below 50 nm. NE propolis revealed to be physically stable after stability test within 63 days at 25oC, centrifuged for 30 mins at 13.000 rpm, and passed 6 cycles of Freeze and Thaw test without separated. NE propolis reduced 58% of free radical DPPH similar to antioxidant activity of the original extracts. Antioxidant activity of NE propolis is relatively stable after stored for 6 weeks. NE Propolis was proven to be safe by primary irritation test with the value of primary irritation index (OECD) was 0. The best formulation for NE propolis contained of 26.25% Kolliphor RH40; 8.75% glycerine; 5% rice bran oil; and 3% EEP with globul size of 21.9 nm and polydispersity index of 0.338. NE propolis was stable and had antioxidant activity similar to EEP.

Keywords: propolis, antioxidant, nanoemulsion, irritation test

Procedia PDF Downloads 309

Authors: Rachmat Mauludin, Nurmazidah

Abstract:

Background and purpose: Famotidine is an H2 receptor blocker. Absorption orally is rapid enough, but famotidine can be degraded by stomach acid causing dose reduction until 35.8% after 50 minutes. This drug also undergoes first-pass metabolism which reduced its bio availability only until 40-50%. To overcome these problems, Solid Lipid Nano particles (SLNs) as alternative delivery systems can be formulated. SLNs is a lipid-based drug delivery technology with 50-1000 nm particle size, where the drug incorporated into the bio compatible lipids and the lipid particles are stabilized using appropriate stabilizers. When the particle size is 200 nm or below, lipid containing famotidine can be absorbed through the lymphatic vessels to the subclavian vein, so first-pass metabolism can be avoided. Method: Famotidine SLNs with various compositions of stabilizer was prepared using a high-speed homogenization and sonication method. Then, the particle size distribution, zeta potential, entrapment efficiency, particle morphology and in vitro release profiles were evaluated. Optimization of sonication time also carried out. Result: Particle size of SLN by Particle Size Analyzer was in range 114.6 up to 455.267 nm. Ultrasonicated SLNs within 5 minutes generated smaller particle size than SLNs which was ultrasonicated for 10 and 15 minutes. Entrapment efficiency of SLNs were 74.17 up to 79.45%. Particle morphology of the SLNs was spherical and distributed individually. Release study of Famotidine revealed that in acid medium, 28.89 up to 80.55% of famotidine could be released after 2 hours. Nevertheless in basic medium, famotidine was released 40.5 up to 86.88% in the same period. Conclusion: The best formula was SLNs which stabilized by 4% Poloxamer 188 and 1 % Span 20, that had particle size 114.6 nm in diameter, 77.14% famotidine entrapped, and the particle morphology was spherical and distributed individually. SLNs with the best drug release profile was SLNs which stabilized by 4% Eudragit L 100-55 and 1% Tween 80 which had released 36.34 % in pH 1.2 solution, and 74.13% in pH 7.4 solution after 2 hours. The optimum sonication time was 5 minutes.

Keywords: famotodine, SLN, high speed homogenization, particle size, release study

Procedia PDF Downloads 865

Authors: Hasan Demiroğlu, Uğur Avcıbaşı, Serhan Sakarya, Perihan Ünak

Abstract:

Implanted devices are progressively practiced in innovative medicine to relieve pain or improve a compromised function. Implant-associated infections represent an emerging complication, caused by organisms which adhere to the implant surface and grow embedded in a protective extracellular polymeric matrix, known as a biofilm. In addition, the microorganisms within biofilms enter a stationary growth phase and become phenotypically resistant to most antimicrobials, frequently causing treatment failure. In such cases, surgical removal of the implant is often required, causing high morbidity and substantial healthcare costs. Staphylococcus aureus is the most common pathogen causing implant-associated infections. Successful treatment of these infections includes early surgical intervention and antimicrobial treatment with bactericidal drugs that also act on the surface-adhering microorganisms. Linezolid is a promising anti-microbial with ant-staphylococcal activity, used for the treatment of MRSA infections. Linezolid is a synthetic antimicrobial and member of oxazolidinoni group, with a bacteriostatic or bactericidal dose-dependent antimicrobial mechanism against gram-positive bacteria. Intensive use of antibiotics, have emerged multi-resistant organisms over the years and major problems have begun to be experienced in the treatment of infections occurred with them. While new drugs have been developed worldwide, on the other hand infections formed with microorganisms which gained resistance against these drugs were reported and the scale of the problem increases gradually. Scientific studies about the production of bacterial biofilm increased in recent years. For this purpose, we investigated the activity of Lin, Lin radiolabeled with 131I (131I-Lin) and cold iodinated Lin (127I-Lin) against clinical strains of Staphylococcus aureus DSM 4910 in biofilm. In the first stage, radio and cold labeling studies were performed. Quality-control studies of Lin and iodo (radio and cold) Lin derivatives were carried out by using TLC (Thin Layer Radiochromatography) and HPLC (High Pressure Liquid Chromatography). In this context, it was found that the binding yield was obtained to be about 86±2 % for 131I-Lin. The minimal inhibitory concentration (MIC) of Lin, 127I-Lin and 131I-Lin for Staphylococcus aureus DSM 4910 strain were found to be 1µg/mL. In time-kill studies of Lin, 127I-Lin and 131I-Lin were producing ≥ 3 log10 decreases in viable counts (cfu/ml) within 6 h at 2 and 4 fold of MIC respectively. No viable bacteria were observed within the 24 h of the experiments. Biofilm eradication of S. aureus started with 64 µg/mL of Lin, 127I-Lin and 131I-Lin, and OD630 was 0.507±0.0.092, 0.589±0.058 and 0.266±0.047, respectively. The media control of biofilm producing Staphylococcus was 1.675±0,01 (OD630). 131I and 127I did not have any effects on biofilms. Lin and 127I-Lin were found less effectively than 131I-Lin at killing cells in biofilm and biofilm eradication. Our results demonstrate that the 131I-Lin have potent anti-biofilm activity against S. aureus compare to Lin, 127I-Lin and media control. This is suggested that, 131I may have harmful effect on biofilm structure.

Keywords: iodine-131, linezolid, radiolabeling, slime layer, Staphylococcus

Procedia PDF Downloads 564