scholarly journals TOPICAL DELIVERY OF QUERCETIN LOADED TRANSFERSOMES FOR WOUND TREATMENT: IN VITRO AND IN VIVO EVALUATION

2021 ◽  
pp. 189-197
Author(s):  
MARWA ABDALLAH ◽  
DEMIANA I. NESEEM ◽  
OMAIMA N. ELGAZAYERLY ◽  
ALY A. ABDELBARY
Keyword(s):  
Wistar Rats ◽  
Spherical Shape ◽  
The Other ◽  
Wound Treatment ◽  
In Vivo Evaluation ◽  
Skin Deposition ◽  
Significant Difference ◽  
Male Wistar Rats

Objective: To design topical Quercetin (Qc)-loaded transfersomes (TFs) for wound treatment. Methods: Qc-loaded TFs were prepared by thin-film hydration technique using 2241full factorial design and the optimum formula was selected. In vivo skin, deposition and cutaneous wound induction studies were performed for four groups of male wistar rats. At the end of the experiment, biochemical parameters were measured in the healed tissues (total proteins (TP), total antioxidant capacity (TAC), glutathione reductase (GSH), nitric oxide (NO), and malonaldehyde (MDA). Two in vivo histopathological experiments using male wistar rats were performed; the first study was done for the healed tissues of the above experiment and the second was to confirm the safety of formulations. Results: Qc optimum TFs (F6) showed EE% of 91.1%, PS of 695.35 nm, PDI of 0.592, and ZP of-11.1 mV, and spherical shape. In vivo skin deposition study showed that drug percentage retained in the skin from Qc optimum TFs was significantly higher than that from Qc suspension and Qc liposomes (p<0.05). There was no significant difference in the values of TP, TAC and MDA between the treated groups (p>0.05). GSH in TFs treated groups was significantly higher than the other groups (p<0.05) while NO in TFs treated groups was significantly lower than the other treated groups (p<0.05). Histopathological experiments showed that wounds treated by TFs healed better than those treated by both liposomes and Qc suspension. Conclusion: Qc-loaded TFs can be used as successful drug-delivery system for wound healing.

scholarly journals PENGARUH EKSTRAK DAGING LIDAH BUAYA (Aloe Vera) TERHADAP PENYEMBUHAN ULSERASI MUKOSA MULUT PADA MALE WISTAR RATS

2015 ◽  
Vol 1 (1) ◽  
pp. 25
Author(s):  
Laila Fitrotuz Zahroh ◽  
Rahmawati Sri Praptiningsih ◽  
Moh. Baehaqi
Keyword(s):  
Oral Mucosa ◽  
Wistar Rats ◽  
Healing Process ◽  
Research Result ◽  
Aloe Vera ◽  
Control Group ◽  
Control Group Design ◽  
Significant Difference ◽  
Male Wistar Rats

Background: Oral mucosa ulceration which often occurs usually in the form of white-yellowish spot with concave surface, reddish edge and pain. Based on previous research, Aloe vera process anti-inflammation substance that could help quickening ulceration healing process. This research aims to know the effect of Aloe vera flesh extract on Male wistar rats oral mucosa ulceration in-vivo. Method: this research was quasi experimental research with the post-test only control group design using Male wistar rats as the testing animal. In the research, there were three treatment groups: The first groups which was given aquadest treatment, second groups with Aloe vera flesh extract, and third groups which was given chlorhexidine gluconate 0,2% treatment. The data collecting was based on histopathology observation concerning the increase of fibroblast quantity. Result: The research result based on comparison test among the three groups with One Way Anova showed that on Day 3th, the average quantity of fibroblast didn't have significant difference between the treatment group and control group positive that was p>0,05, meanwhile on Day 7th every group showed significant difference p<0,05. Conclusion: It concluded that Aloe vera flesh extract has influence on the healing of Male wistar rats oral mucosa ulceration as shown by fibroblast increasing quantity.

scholarly journals Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Rajni Bala ◽  
Sushil Khanna ◽  
Pravin Pawar
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Content Uniformity ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
Significant Difference ◽  
Film Formulation ◽  
Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

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.

scholarly journals Effect of single clove garlic on clinical symptoms of photoaging in wistar rats exposed with UV-B

2019 ◽  
Vol 2 (2) ◽  
pp. 40-44
Author(s):  
Nyoman Pratiwi Hapsari Dewi ◽  
I Gusti Ayu Dewi Ratnayanti ◽  
I Gusti Kamasan Nyoman Arijana ◽  
Ni Made Linawati
Keyword(s):  
Clinical Symptom ◽  
Wistar Rats ◽  
Clinical Symptoms ◽  
Light Exposure ◽  
Premature Aging ◽  
The Other ◽  
Control Group ◽  
Control Group Design ◽  
Significant Difference ◽  
Male Wistar Rats

Background: Photoaging is a premature aging that occurs on skin due to the ultraviolet light exposure that causes the emergence of clinical symptoms, one of which is wrinkle. One kind of material that can prevent photoaging is antioxidant. A single clove garlic has the highest antioxidant activity compared to the other materials. Aim: This research aimed at investigating the effectivity of single clove garlic in inhibiting the clinical symptom of photoaging. Method: This research was an experimental research, utilizing pre-post-test control group design. The used sample were 30 male wistar rats which were divided into 6 experimental groups. All groups were exposed to UV-B light with the amount of 840 mJ/cm2. Control group (P1) was only exposed to UV-B while the other groups were treated with placebo cream (P2), sunblock (P3), 5% garlic cream (P4), 10% garlic cream (P5) and 20% garlic cream (P6) respectively. The clinical symptom in the form of wrinkle was observed by using dermascope and the observations were categorized based on Glogau Scale. The statistical analysis utilized Wilcoxon and Kruskal Wallis test which was followed by Mann Whitney test. Result: The result of the research showed that there was significant difference on the apparent wrinkle on P1 group and P3, P5 and P6. Meanwhile the comparison between P1, P2 and P4 was not significant. Conclusion: The single clove garlic extract can prevent photoaging and has the similar protective effect for the skin as of sunblock.

Pharmacokinetic Profile of Oxaliplatin-Loaded pH-Responsive Hydrogels in Rabbits

2020 ◽  
Vol 26 (44) ◽  
pp. 5755-5763
Author(s):  
Kaleem Ullah ◽  
Shujaat Ali Khan ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Ghulam Murtaza
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Oral Solution ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Platinum Compound ◽  
In Vivo Evaluation ◽  
Significant Difference

Background: Oxaliplatin (OXP), a 3rd generation platinum compound, which causes severe side effects due to; impulse high concentration in the bloodstream thereby exposing healthy cells at a high ratio, nonspecific delivery at the target site and non-compliance is administered intravenously. Objective: The project was aimed at the development, characterization, and in-vitro and in-vivo evaluation of pHresponsive hydrogels for oral administration of OXP. Methods: Hydrogel formulations were synthesized through a free radical polymerization technique followed by brief characterization using various techniques. The hydrogels were investigated for various in-vitro studies such as sol-gel, drug loading, swelling, drug release, and MTT-assay. While in-vivo studies such as oral tolerability, histopathology, and hematology studies were performed on rabbits. A simple and sensitive HPLC-UV method was optimized and the comparative pharmacokinetic study was performed in rabbits using OXP-oral solution and OXP-loaded hydrogels. Results: In-vitro characterization confirmed that the reactant was successfully crosslinked to form thermally stable hydrogels with decreased crystallinity and rough surface. Swelling and drug release showed that hydrogels were more responsive to basic pH (6.8 and 7.4) in comparison with pH 1.2. The blank hydrogels were cytocompatible as more than 95% of the cells were viable while free OXP and OXP-loaded hydrogels displayed dosedependent cytotoxic effect. In-vivo studies confirmed that chitosan and gelatin hydrogel suspension was well tolerable up to 3800 mg/kg and 4000 mg/kg of body weight, respectively. Hematology and serum chemistry reports were well within the range suggesting normal liver and kidney functions. Similarly, histopathology slides of rabbit vital organs were also found normal without causing any histopathological change. Conclusion: HPLC-UV method was successfully optimized for OXP detection in oral solution and hydrogels administered to rabbits. A significant difference was found among various pharmacokinetic parameters by comparing the two groups including half-life (t1/2), tmax, Cmax, AUCtot MRT, Vz, and Lz.

scholarly journals Design and in vivo Evaluation of Manidipine by Self-Nanoemulsifying Drug Delivery Systems

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
S Srikanth Reddy ◽  
G Suresh
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Spherical Shape ◽  
Pharmacokinetic Studies ◽  
In Vivo Evaluation ◽  
Enhanced Solubility ◽  
Pure Drug

The current research is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of Manidipine for enhanced solubility and oral bioavailability. The Manidipine SNEDDS are formulated with excipients comprising of Capmul MCM (oil phase), Transcutol P (surfactant) Lutrol L 300 as co-surfactant. The prepared fifteen formulations of Manidipine SNEDDS analysed for emulsification time, percentage transmittance, particle size, in vitro drug release, and stability studies. In vivo pharmacokinetic studies of the optimized formulation were carried out in Wistar rats in comparison with control (pure drug). The morphology of Manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 is 98.24 ± 5.14%. The particle size F14 formulation was 22.4 nm and Z-Average 23.3 nm. The PDI and zeta potential of Manidipine SNEDDS optimized formulation (F14) were 0.313 and-5.1mV respectively. From in vivo bioavailability data the optimized formulation exhibited a significantly greater Cmax and Tmax of the SNEDDS was found to be 3.42 ± 0.46ng/ml and 2.00 ± 0.05 h respectively. AUC0-∞ infinity for formulation was significantly higher (11.25 ± 3.45 ng.h/ml) than pure drug (7.45 ± 2.24ng. h/ml). Hence a potential SNEDDS formulation of Manidipine developed with enhanced solubility and bioavailability.

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 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.

Sign in / Sign up

Export Citation Format

Share Document