scholarly journals CUR-CA-THIONE: A NOVEL CURCUMIN CONCOCTION WITH ENHANCED WATER SOLUBILITY AND BRAIN BIO-AVAILABILITY

2016 ◽  
Vol 8 (12) ◽  
pp. 265 ◽  
Author(s):  
Devang Y. Shelat ◽  
Sanjeev R Acharya
Keyword(s):  
Wistar Rats ◽  
Water Solubility ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Systemic Circulation ◽  
Oral Route ◽  
Male Wistar Rats ◽  
Dialysis Bag

<p><strong>Objective: </strong>Curcumin, is widely studied as a potential drug in treating various disorders but lacks applicability due to poor water solubility and tissue bioavailability. The main objective of the study was to develop a formulation of curcumin that has enhanced water solubility and brain bioavailability.</p><p><strong>Methods: </strong>A curcumin concoction was prepared using solvent evaporation technique taking casein and glutathione as vectors. Various process parameters were identified namely time, temperature, pH and vector while formulation parameters included drug entrapment, anti-oxidant activity, and water solubility. The concoctions were evaluated for <em>in vitro</em> release kinetics at three pH i.e. 1.2, 4.5 and 6.2 at six-time intervals i.e. 10, 20, 30, 40, 60, 120 min using dialysis bag membrane. The same kinetics was further validated using same time points with wistar rats and giving concoction at a single dose of 2 g/kg via the oral route.</p><p><strong>Results: </strong>A concoction i.e. CUR-CA-THIONE having significant entrapment efficiency (77.83%, 97.75%, 90.19%), water solubility (40, 350 and 45 times than normal curcumin) and DPPH activity (IC<sub>50</sub>: 28.91, 25.07 and 27.89) was evaluated in concoctions CUR-CA-THIONE-T.1, CUR-CA-THIONE-T.2 and CUR-CA-THIONE-T.3 respectively. These formulations were then carried out for <em>in vitro</em> release profile at different pH with average release obtained between 20-30 min. <em>In vivo</em> kinetics was studied by isolating tissues like brain, liver, lung, kidney and spleen in male wistar rats and maximum brain bioavailability was observed for CUR-CA-THIONE-T.3 at 30 min with 75 ng/g of brain tissue.</p><p><strong>Conclusion: </strong>The experiment helps in concluding that CUR-CA-THIONE has improved its water solubility and is able to by-pass systemic circulation to targeted activity.</p>

scholarly journals Development and Evaluation of Solid Lipid Nanoparticles of Raloxifene Hydrochloride for Enhanced Bioavailability

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Anand Kumar Kushwaha ◽  
Parameswara Rao Vuddanda ◽  
Priyanka Karunanidhi ◽  
Sanjay Kumar Singh ◽  
Sanjay Singh
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Dsc Studies ◽  
Solid Lipid ◽  
Raloxifene Hydrochloride ◽  
Dialysis Bag

Raloxifene hydrochloride (RL-HCL) is an orally selective estrogen receptor modulator (SERM) with poor bioavailability of nearly 2% due to its poor aqueous solubility and extensive first pass metabolism. In order to improve the oral bioavailability of raloxifene, raloxifene loaded solid lipid nanoparticles (SLN) have been developed using Compritol 888 ATO as lipid carrier and Pluronic F68 as surfactant. Raloxifene loaded SLN were prepared by solvent emulsification/evaporation method, and different concentrations of surfactant, and homogenization speed were taken as process variables for optimization. SLN were characterized for particle size, zeta potential, entrapment efficiency, surface morphology, and crystallinity of lipid and drug.In vitrodrug release studies were performed in phosphate buffer of pH 6.8 using dialysis bag diffusion technique. Particle sizes of all the formulations were in the range of 250 to 1406 nm, and the entrapment efficiency ranges from 55 to 66%. FTIR and DSC studies indicated no interaction between drug and lipid, and the XRD spectrum showed that RL-HCL is in amorphous form in the formulation.In vitrorelease profiles were biphasic in nature and followed Higuchi model of release kinetics. Pharmacokinetics of raloxifene loaded solid lipid nanoparticles after oral administration to Wistar rats was studied. Bioavailability of RL-HCL loaded SLN was nearly five times than that of pure RL-HCL.

scholarly journals Drug Release Kinetics of Electrospun PHB Meshes

Materials ◽  
2019 ◽  
Vol 12 (12) ◽  
pp. 1924 ◽  
Author(s):  
Vojtech Kundrat ◽  
Nicole Cernekova ◽  
Adriana Kovalcik ◽  
Vojtech Enev ◽  
Ivana Marova
Keyword(s):  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Toxic Substances ◽  
Antimicrobial Efficiency ◽  
Vis Spectroscopy ◽  
Model Drug ◽  
Phosphate Buffered Saline ◽  
Kinetics Of

Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.

Concomitant release of sialic acids and calcium by neuraminidase from rat aorta in situ

1988 ◽  
Vol 235 (1279) ◽  
pp. 139-144 ◽  
Keyword(s):  
Sialic Acid ◽  
Wistar Rats ◽  
Rat Aorta ◽  
Sialic Acids ◽  
Molar Ratio ◽  
Male Wistar Rats

Male Wistar rats were heparinized and killed with pentobarbital. The upper and lower ends of the aortae were cannulated and the blood was washed out with saline until the washings contained calcium and sialic-acid-reacting material at minimal concentrations. The aortae were perfused with neuraminidase for 15 min. This caused the appearance of calcium as well as of sialic acids in the perfusate in total amounts of about 5.3 nmol and about 3.6 nmol per aorta respectively. The molar ratio of about 1.5 is sufficiently close to that determined for the association of calcium with sialic acids in vitro to suggest that their association is similar in vivo .

scholarly journals Synthesis of Some Novel Derivatives of 2-(9H-purin-6-ylsulfanyl) Acetohydrazide as Potential Antithyroid Agents

2017 ◽  
Vol 56 (4) ◽  
Author(s):  
Ismat Fatima ◽  
Munawar A. Munawar ◽  
Waqar Nasir ◽  
Misbahul A. Khan ◽  
Affia Tasneem ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Male Wistar Rats ◽  
Antithyroid Agents ◽  
Derivatives Of

Some novel derivatives of 2-(9<em>H</em>-Purin-6-ylsulfanyl)acetohydrazide were synthesized by reacting it with respective aldehydes in ethanol. The antithyroid effect of these compounds was ascertained <em>in vitro</em> by studying their complexation with iodine spectrophotometrically. <em>In vivo</em>, the hormonal as well as histological variations in male Wistar rats demonstrated significant antithyroid potential (p ≤ 0.05) of these compounds.

Ibuprofen loaded nano-ethanolic liposomes carbopol gel system: in vitro characterization and anti-inflammatory efficacy assessment in Wistar rats

2018 ◽  
Vol 38 (3) ◽  
pp. 291-298 ◽  
Author(s):  
Atefeh Afshar Moghaddam ◽  
Abdul Ahad ◽  
Mohd. Aqil ◽  
Farhan J. Ahmad ◽  
Yasmin Sultana ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Wistar Rats ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
In Vitro Characterization ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
The Stability

AbstractThe objective of the present study was to develop and characterize nano-ethanolic liposomes (NEL) for transdermal delivery of ibuprofen (IBU). The NEL for transdermal delivery of IBU were prepared by thin film hydration technique and evaluated for vesicle size, shape, entrapment efficiency, transdermal flux, andin vivoanti-inflammatory activity in Wistar rats. The NEL optimized formulation (NEL-Opt) presented vesicle sizes of 32.85±1.98 nm and entrapment efficiency of 86.40±0.55% with improved transdermal flux. The presence of ethanol and flexibility of NEL could be the reasons for better permeation enhancement of IBU via rat’s skin.In vivoanti-inflammatory study of IBU-loaded NEL-Opt gel showed significant reduction (41.18%) of edema in carrageenan-induced rat paw edema as compared to conventional gel of IBU, where reduction of edema was found to be 12.50%. Our results suggest that developed NEL formulations are efficient systems for transdermal IBU delivery against inflammation. The stability study confirmed that the NEL-Opt gel formulation was considerably stable at refrigerator temperature. Our results concluded that NEL are an efficient carrier for transdermal delivery of IBU.

scholarly journals Endothelium/Nitric Oxide Mediates the Vasorelaxant and Antihypertensive Effects of the Aqueous Extract from the Stem Bark ofMammea africanaSabine (Guttiferae)

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Elvine Pami Nguelefack-Mbuyo ◽  
Alain Bertrand Dongmo ◽  
Télesphore Benoît Nguelefack ◽  
Albert Kamanyi ◽  
Pierre Kamtchouing ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Response Curve ◽  
Wistar Rats ◽  
Antihypertensive Effect ◽  
Stem Bark ◽  
Male Wistar Rats ◽  
Vasorelaxant Activity ◽  
Concentration Response Curve

This study evaluates the vasorelaxant and antihypertensive effects of the aqueous extract from the stem bark ofM. africana(AEMA). AEMA was testedin vitroon intact or endothelium-denuded rats’ aorta rings precontracted with KCl or norepinephrine in absence or in presence of L-NAME or glibenclamide. The effect of a single concentration (300 μg/mL) of AEMA was also examined on the concentration-response curve of KCl.In vivo, the antihypertensive effects of AEMA (200 mg/kg/day) were evaluated in male Wistar rats treated with L-NAME (40 mg/kg/day) for 4 weeks. AEMA relaxed aorta rings precontracted with NE or KCl with respective EC50 values of 0.36 μg/mL and 197.60 μg/mL. The destruction of endothelium or pretreatment of aorta rings with L-NAME shifted the EC50 of AEMA from 0.36 μg/mL to 40.65 μg/mL and 20.20 μg/mL, respectively. The vasorelaxant activity ofM. africanawas significantly inhibited in presence of glibenclamide. AEMA also significantly inhibited the concentration-response curve of KCl. Administered orally, AEMA induced acute and chronic antihypertensive effects and normalized renal NO level. These results show that the vasorelaxant activity of AEMA might be mediated by the activation of the NO-cGMP-ATP-dependent potassium channels pathway and might predominantly account for its antihypertensive effect.

scholarly journals Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine

Materials ◽  
2021 ◽  
Vol 14 (19) ◽  
pp. 5759
Author(s):  
Hussam I. Kutbi ◽  
Hani Z. Asfour ◽  
Ahmed K. Kammoun ◽  
Alaa Sirwi ◽  
Simona Cavalu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Water Solubility ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Structural Features ◽  
Transmission Electron ◽  
Mean Size ◽  
Therapeutic Activities

Various perspectives had been utilized to enhance the poor intestinal permeability and bioavailability of drugs with low water solubility. Berberine (Brb) is a unique molecule that possesses multiple therapeutic activities such as antimicrobial, anti-inflammatory, antioxidant and anti-hyperglycemic effects. To improve Brb permeability and bioavailability, this study presents a newly developed formulation, namely Brb hyaluronate-based liposomes, prepared by using film hydration method and characterized by dynamic light scattering measurements, entrapment efficiency percentage (EE%), transmission electron microscope (TEM), in vitro drug release and physical stability. The bioavailability of the selected formulations was assessed in vivo after oral administration to rats. The results revealed an enhanced effect of hyaluronic acid on the entrapment efficiency, reaching 78.1 ± 0.1% with mean size 520.7 ± 19.9 nm. Sustained release of Brb was recorded up to 24 h in comparison to Brb solution. Physical stability was maintained for three months at refrigeration temperature. Results of pharmacokinetics studies indicated the potential of the liposomal formulation to increase the oral bioavailability of Brb and to accelerate its entry into the bloodstream. The obtained results are accredited to the lipophilic nature of the prepared system, resembling the structural features of bio-membrane, in addition to their small size that enhances intestinal penetration.

The irreversible binding of benzo[a]pyrene to rat liver macromolecules in vivo and in vitro: Effects of agents that influence benzo[a]pyrene metabolism

1979 ◽  
Vol 57 (11) ◽  
pp. 1238-1245 ◽  
Author(s):  
L. S. Gontovnick ◽  
S. Ng ◽  
G. D. Bellward
Keyword(s):  
Wistar Rats ◽  
Methadone Treatment ◽  
Intraperitoneal Administration ◽  
Time Dependent ◽  
Diethyl Maleate ◽  
Irreversible Binding ◽  
Male Wistar Rats ◽  
In Vitro Effects

The present study was carried out to determine the effects of agents that influence benzo[a]-pyrene(BP)metabolism in vitro on the irreversible binding of BP to rat hepatic macromolecules in vivo. The irreversible binding of [3H]BP was found to be both dose and time dependent after its intraperitoneal administration to male Wistar rats. The SKF 525-A, at doses of 50 and 75 mg/kg, ip, 3 h before BP, decreased the level of binding from control by 31 and 34%, respectively. At 35 mg/kg, SKF 525-A had no effect. Diethyl maleate (0.6 mL/kg, ip) and cysteine (150 mg/kg, ip), 30 and 5 min before BP, respectively, did not alter the binding of BP from control. Oral methadone treatment, previously shown to increase selectively epoxide hydrase activity in male Wistar rats, also failed to alter the amount of BP bound to hepatic macromolecules. 3-Methylcholanthrene (20 mg/kg per day, ip, for 2 days) administered 24 h before BP, decreased the level of binding from control by.30%. Parallel in vitro studies were carried out with the various agents used in vivo.

scholarly journals Identification of Compounds With Vasoactive Properties in a Pitaya Juice Extract (Stenocereus griseus)

2021 ◽  
Vol 5 (Supplement_2) ◽  
pp. 362-362
Author(s):  
Yadira Ramírez Rodríguez ◽  
Karina Robledo Márquez ◽  
Ricardo Espinosa Tanguma ◽  
Alejandra Medina Hernández ◽  
Francisco Bautista-Redonda ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Wistar Rats ◽  
In Vitro Models ◽  
Physiological Solution ◽  
Action Mechanism ◽  
Vasodilator Effect ◽  
Funding Sources ◽  
Male Wistar Rats

Abstract Objectives The objective of this study is to identify the vasoactive compounds present in the pitaya juice extract (PJE) and evaluate its effect using in vivo and in vitro models. Methods First, the pitaya juice was obtained from the fruit of Stenocereus Griseus, centrifuged to obtain PJE. Six hundred mL of PJE was frozen until its use and other 600 mL was lyophilized and stored. The lyophilized PJE was analyzed by HPLC-PAD. The wavelengths for detection in the PAD system were 535 and 480 nm for betalains, and 370 and 280 nm for phenolic compounds. On the other hand, the vasoactive effect of PJE was evaluated in isolated rings of thoracic aortas, with (n = 5) and without endothelium (n = 5), of male Wistar rats (250–350 g) previously contracted with phenylephrine (10 mM to 10 μmol/L), followed by the administration of a concentration of 20 mg/mL of lyophilized PJE and 1 mL physiological solution, as a control (30 min of treatment). Results The profiling of lyophilized PJE by HPLC-PAD showed 16 types of betalains and 31 types of phenolic compounds, which will be analyzed by mass spectrometry. Isolated aortic rings (in presence and absence of the endothelium) administered with PJE showed 8-fold greater vasodilation compared to the control (54.3% ± 14.1 vs 6.7% ± 3.7), suggesting that the compounds present in the PJE may exert a vasodilator effect, of which its action mechanism will be investigated. Conclusions Pitaya juice extract contains vasoactive compounds such as betalains and phenolic compounds, which could be responsible for PJE exerting a vasodilator effect that was observed in assays of isolated rat aortic rings. Funding Sources 1. Consejo Nacional de Ciencia y Tecnología (CONACYT) 2. Instituto Potosino de Investigación Científica y Tecnológica A.C. (IPICYT).

scholarly journals Effect of Recrystallization Technique on Oral Bioavailability of Valsartan

2021 ◽  
Vol 11 (6) ◽  
pp. 88-93
Author(s):  
TP Rao ◽  
N. Nalluri
Keyword(s):  
Oral Bioavailability ◽  
Wistar Rats ◽  
Relative Bioavailability ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Type I ◽  
Dissolution Properties ◽  
Male Wistar Rats

Valsartan (VAL) is a widely prescribed anti-hypertensive agent with angiotensin II type I receptor antagonistic activity. VAL belongs to BCS class II having a low and variable oral bioavailability (10-35%) and its absorption is dissolution rate limited. Recrystallization of VAL from different organic solvents improved VAL aqueous solubility and thereby in vitro dissolution properties. In this investigation in vivo oral bioavailability (BA) of VAL and its recrystallized products with methanol and ethanol (VMET and VETH respectively) solvents was evaluated in male Wistar rats. Also, a rapid, economical and reliable RP-HPLC-PDA method was developed for the estimation of VAL in rat plasma samples and validated according to ICH guidelines. Chromatographic separation was achieved on an Agilent eclipse C18 column (150×4.6mm, 5µ) with a mobile phase composition of 10mM ammonium acetate: acetonitrile (75:25%v/v) at a flow rate of 1.2 mL/min. The retention time of VAL was found to be 2.9 min and showed good linearity (R2>0.996) in the selected concentration range of 0.5-25µg/mL. A 2.9, 2.8 folds increase in Cmax and a relative bioavailability of 320, 305% was observed with VMET and VETH respectively, when compared to that of untreated VAL. Thus it can be inferred that recrystallization is easy and economical technique for enhancing the pharmaceutical properties like solubility, dissolution properties and oral BA of poorly water soluble drugs like VAL. Keywords: Bioanalytical method, Bioavailability, Male Wistar rats, Valsartan, Recrystallization

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