Search results for "030226 pharmacology & pharmacy"
showing 10 items of 317 documents
GABAA agonist muscimol ameliorates learning/memory deficits in streptozocin-induced Alzheimer’s disease non-transgenic rat model
2015
Background: GABAergic inhibitory action regulates learning/memory processes and contributes to neurotransmission (Gong et al., 2009). Existing evidence suggests GABAergic system is involved in pathophysiology of Alzheimer’s disease (AD) via inhibitory interneuron deficits (Verret et al., 2012) and decrease in functional GABAA receptors (Limon et al., 2012). In vitro, GABA and muscimol (GABAA receptor agonist) blocked neuronal death induced by Aβ in rat hippocampal and cortical neurons (Paula-Lima et al., 2005). Our concept: low doses of muscimol may prevent learning/memory deficits in intracerebroventricular (icv) streptozocin (STZ)-induced AD non-transgenic rat model. Methods. Wistar male …
Micellar liquid chromatography determination of rivaroxaban in plasma and urine. Validation and theoretical aspects.
2019
A Micellar Chromatographic method to determine rivaroxaban in plasma and urine has been developed. The samples were dissolved in the mobile phase (SDS 0.05 M – 1-propanol 12.5%, phosphate buffered at pH 7) and 20 μL directly injected, avoiding the extraction and purification steps. Using a C18 column and running under isocratic mode at 1 mL/min, analyte was eluted without interference from the matrix in <6.0 min. The detection absorbance wavelength was set to 250 nm. The procedure was validated by Food and Drug Administration guidelines in terms of: system suitability, calibration range (0.05–5 mg/L), linearity, sensitivity, robustness, carry-over effect, specificity, accuracy (−11.1 to 4.2…
Computer simulations for bioequivalence trials: Selection of analyte in BCS class II and IV drugs with first-pass metabolism, two metabolic pathways …
2018
A semi-physiological two compartment pharmacokinetic model with two active metabolites (primary (PM) and secondary metabolites (SM)) with saturable and non-saturable pre-systemic efflux transporter, intestinal and hepatic metabolism has been developed. The aim of this work is to explore in several scenarios which analyte (parent drug or any of the metabolites) is the most sensitive to changes in drug product performance (i.e. differences in in vivo dissolution) and to make recommendations based on the simulations outcome. A total of 128 scenarios (2 Biopharmaceutics Classification System (BCS) drug types, 2 levels of KM Pgp, in 4 metabolic scenarios at 2 dose levels in 4 quality levels of t…
Relationship between particle size and dissolution rate of bulk powders and sieving characterized fractions of two qualities of orthoboric acid
1996
Drug Dev. Ind. Pharm. ISI Document Delivery No.: VN279 Times Cited: 1 Cited Reference Count: 22 Tromelin, A Habillon, S Andres, C Pourcelot, Y Chaillot, B; International audience; We have carried out a study of the particle size distribution and aqueous dissolution rate of two commercially available qualities of orthoboric acid, labeled ''crystal'' (ABC) and ''powder'' (ABP). In a previous work, we have shown that the two commercial qualities of orthoboric acid chosen as model compound (''powder'' and ''crystal'') are related to the same crystal network in spite of their different names. However, these two qualities have very different size particle distributions, as previously determined b…
The Effect of Methanolic Leaf Extract of Boerhavia diffusa Linn. (Nictaginaceae) on the Activities of Antidiabetic, Anti-inflammatory and Antioxidant…
2018
Diabetic therapeutic potentiality of methanol extract of stem leaves of Boerhavia diffusa was investigated following in-vivo study models in streptozotocin-induced diabetic rat. Methanol extract of stem leaves of Boerhavia diffusa exerted the glucose lowering effect an increase in serum insulin level on 28st day of postadministration. In addition to a higher expression of insulin receptor A. The extract treatment or glibenclamide for 28 days significantly (p<0.05) reduced HbA1c. Boerhavia diffusa L. or glibenclamide for 28 days show no damaging effect on red blood count and hemoglobin when compared to the control group. Significant (p<0.05) increase in platelet count and white blood cell c…
Mucoadhesive Polymeric Films to Enhance Barbaloin Penetration Into Buccal Mucosa: a Novel Approach to Chemoprevention.
2018
Nowadays, chemoprevention by administering natural supplements is considered an attractive strategy to reverse, suppress, or prevent the evolution of premalignant oral lesions. In particular, Barbaloin exhibits anti-proliferative, anti-inflammatory, and anti-cancer properties, and it results useful in multi-therapy with classic chemotherapeutics. Therefore, in this work, mucoadhesive buccal films, as locoregional drug delivery system able to provide a targeted and efficient therapeutic delivery of Barbaloin, are proposed. Thus, Aloin extract-loaded Eudragit (R) RL100 or Eudragit (R) RS100-based buccal films were designed in order to obtain an easily self-administrable formulation capable of…
Innovative strategies to treat skin wounds with mangiferin: fabrication of transferosomes modified with glycols and mucin
2020
Aim: The moisturizing properties of glycerol, the penetration enhancing capability of propylene glycol and the bioadhesive properties of mucin were combined to improve the carrier capabilities of transfersomes and the efficacy of mangiferin in the treatment of skin lesions. Materials & methods: Mangiferin was incorporated in transfersomes and glycoltransfersomes, which were also modified with mucin. The physico–chemical features were assessed, along with the efficacy against oxidative stress and skin wounds in vitro and in vivo. Results: Glycoltransfersomes promoted the deposition of mangiferin in epidermis and dermis, protected fibroblasts from oxidative stress and stimulated their pr…
Effect of actively targeted copolymer coating on solid tumors eradication by gold nanorods-induced hyperthermia.
2020
Efforts in the field of anticancer therapy are increasingly focusing on the development of localized and selective treatments. Photothermal therapy (PTT) can lead to a spatially confined death of cancer cells, exploiting an increasing in temperature generated after UV-NIR irradiation of peculiar materials. Herein, a new actively targeted gold-based drug delivery system, named PHEA-LA-Fol-AuNRs/Iri, was explored for hyperthermia and chemotherapy colon cancer treatment. Gold nanorods were stabilized using a folate-derivative of α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA-LA-PEG-FA) as coating agent and then loaded with the antineoplastic drug irinotecan (Iri). The efficacy of empty and i…
Effect of endothelial cell heterogeneity on nanoparticle uptake.
2020
Endothelial cells exhibit distinct properties in morphology and functions in different organs that can be exploited for nanomedicine targeting. In this work, endothelial cells from different organs, i.e. brain, lung, liver, and kidney, were exposed to plain, carboxylated, and amino-modified silica. As expected, different protein coronas were formed on the different nanoparticle types and these changed when foetal bovine serum (FBS) or human serum were used. Uptake efficiencies differed strongly in the different endothelia, confirming that the cells retained some of their organ-specific differences. However, all endothelia showed higher uptake for the amino-modified silica in FBS, but, inter…
Effects of the dual sodium-glucose linked transporter inhibitor, licogliflozinvsplacebo or empagliflozin in patients with type 2 diabetes and heart f…
2020
Aims Explore the efficacy, safety and tolerability of the dual sodium-glucose cotransporter (SGLT) 1 and 2 inhibitor, licogliflozin in patients with type-2 diabetes mellitus (T2DM) and heart failure. Methods This multicentre, parallel-group phase IIA study randomized 125 patients with T2DM and heart failure (New York Heart Association II-IV; plasma N-terminal pro b-type natriuretic peptide [NT-proBNP] >300 pg/mL) to licogliflozin (2.5 mg, 10 mg, 50 mg) taken at bedtime, empagliflozin (25 mg) or placebo (44 patients completed the study). The primary endpoint was change from baseline in NT-proBNP after 12 weeks. Secondary endpoints included change from baseline in glycated haemoglobin, fas…