scholarly journals Antiulcerogenic Potential Activity of Free and NanoencapsulatedPassiflora serratodigitataL. Extracts

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Marc Strasser ◽  
Peky Noriega ◽  
Raimar Löbenberg ◽  
Nádia Bou-Chacra ◽  
Elfriede M. Bacchi
Keyword(s):  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Residual Water ◽  
Flavonoid Content ◽  
Organic Extract ◽  
Water Fraction ◽  
Physical Chemical ◽  
Potential Activity ◽  
Antiulcerogenic Activity ◽  
Herbal Formulations

This paper provides evidence that the leaves and stem ofPassiflora serratodigitataL. dry crude extract (DCE), ethylacetate fraction (EAF), and residual water fraction show potential antiulcerogenic activity. Interestingly, the polymeric nanocapsule loaded with EAF had 10-fold more activity than the free EAF. Furthermore, the polymer nanoparticles provided homogeneous colloidal drug delivery systems and allowed overcoming challenges such as poor aqueous solubility as well as the physical-chemical instability of the organic extract, which presented 90% (w/w) of the flavonoid content. The entrapment efficiency of the total flavonoid was 90.6 ± 2.5% (w/v) for the DCE and 79.9 ± 2.7% (w/v) for the EAF. This study shows that nanoencapsulation improves both the physicochemical properties and the efficacy of the herbal formulations. Therefore, free and encapsulated extracts have the potential to be suitable drug design candidates for the therapeutic management of ulcer.

scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

scholarly journals The activity of extracts chara vulgaris against promastigotes of leishmania tropica.

2018 ◽  
Vol 12 (2) ◽  
pp. 66-72
Author(s):  
Ban Hussein Ali ◽  
Thaer A. Saleh ◽  
Mohammed M. Al-Halbosiy
Keyword(s):  
Major Health Problem ◽  
Organic Extract ◽  
Major Health ◽  
Treatment Groups ◽  
Chara Vulgaris ◽  
Incubation Periods ◽  
Potential Activity ◽  
Diphenyl Tetrazolium Bromide ◽  
Better Than

            Leishmaniasis is a widespread parasitic disease caused by Leishmania parasite, this disease considers as a major health problem worldwide. The available therapy is unsatisfactory expensive with a cytotoxic side effects. Studies of marine algae as a source of pharmacological active compounds have increased worldwide.  This study was aimed to investigate the effect of a type of green algae (Chara vulgaris) on promastigotes of L. tropica, by using. various concentrations (500, 250, 125, 62.5, 31.25, 15.6 µg/mL) in vitro by MTT assay [3-(4.5-dimethylthiazol-2-yl)- 2.5-diphenyl tetrazolium bromide)], to investigate its effect on the proliferation of promastigotes, by three incubation periods (24, 48, 72 hr.) The results showed a significant (p< 0.05)   decrease in survived of promastigotes in treatment groups with concentrations that ranged between 15 to 500 μg/ ml.  This study revealed a major growth inhibition effect of the organic extract of C. vulgaris against L. tropica promastigotes, and the extract of ethyl acetate showed potential activity is better than the aqueous extract.

scholarly journals Enhanced Therapeutic Efficacy of Vincristine Sulfate for Lymphoma Using Niosome-Based Drug Delivery

2020 ◽  
Vol 15 (3) ◽  
Author(s):  
Mohammad Reza Mehrabi ◽  
Mohammad Ali Shokrgozar ◽  
Tayebeh Toliyat ◽  
Masoomeh Shirzad ◽  
Azadeh Izadyari ◽  
...  
Keyword(s):  
Side Effects ◽  
Zeta Potential ◽  
Anticancer Activity ◽  
Performance Test ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Diffusion Method ◽  
Vincristine Sulfate ◽  
Lymphoma Cells

: Clinical application of vincristine sulfate as a chemotherapeutic agent is limited because of its low aqueous solubility and severe side effects. This study aimed to improve the bioavailability and reduce side effects of vincristine sulfate through entrapping in PEGylated niosomes. We evaluated the anticancer activity of PEGylated niosomal vincristine sulfate (PEG-nVCR) in a mouse model of lymphoma induced by BCL1 clone 5B1b cell line. PEG-nVCR was prepared by the thin-film hydration method. The prepared niosomes were characterized by size, zeta potential, and entrapment efficiency. The drug release pattern, neurotoxicity experiment, and in vivo anticancer activity of PEG-nVCR were evaluated by the dialysis diffusion method, rotarod performance test, and flow cytometry, respectively. The mean particle size, zeta potential, and entrapment efficiency of nisomes were obtained around 220 nm, -19 mV, and 81%, respectively. A sustained release behavior was indicated by PEG-nVCR so that the maximum release of VCR from niosomes reached to 69% after 36h of incubation. After the treatment of mice by different formulations, a significant reduction in lymphoma cells in the spleen was obtained for the PEG-nVCR, as compared to the free vincristine sulfate. In the neurotoxicity experiment, a 2.5-fold lower motor incoordination effect was observed for the PEG-nVCR group with respect to the free VCR group. According to these findings, it can be concluded that the PEGylated niosomal formulation could be a suitable carrier for the delivery of VCR to the lymphoma cells or other related cancer cells.

scholarly journals Analysis and design of wastewater treatment

2018 ◽  
Vol 2 (3) ◽  
pp. 121-135
Author(s):  
Jordan Andres P. Pinoargote ◽  
Jennifer Tatiana R. Alcivar ◽  
Carlos G. Villacreses Viteri
Keyword(s):  
Wastewater Treatment ◽  
Structural Design ◽  
Treatment System ◽  
Residual Water ◽  
Analysis And Design ◽  
Agricultural Engineering ◽  
Physical Chemical ◽  
Technical University ◽  
The Cost ◽  
The City

The work proposes the reuse of wastewater from the Faculty of Agronomic Engineering of the Technical University of Manabí, located in the Lodana parish in the city of Portoviejo, to irrigate the diversity of plantations that exist in the institution as a banana, cocoa and lemon. In the work, the results of the physical-chemical and bacteriological analysis carried out on the residual water generated in the institution are offered, being able to verify that it does not meet the parameters required to be used in the irrigation of crops. The technical scheme of the proposed treatment system is shown, specifying the structure of the zeolite filter. The calculations made for the technical and structural design of each of the devices that make up the proposed treatment system are provided. The analysis of the performance of the system that is illustrated with a series of data reflected in tables is exposed and where an efficiency between 84% and 88% can be verified. A review of compliance with environmental regulations is carried out and an economic analysis is provided on the cost of the investment for the introduction of the system in the Faculty of Agricultural Engineering of the Technical University of Manabí.

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 Development of pasteurized coffee-flavored dairy beverage added with mint extract (Mentha x piperita)

2020 ◽  
Vol 42 ◽  
pp. e48474
Author(s):  
Bruno Fischer ◽  
Jean Carlo Rauschkolb ◽  
Rogério Luis Cansian ◽  
Ilizandra Aparecida Fernandes ◽  
Alexander Junges ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Flavonoid Content ◽  
Color Intensity ◽  
Product Analysis ◽  
Sensory Acceptance ◽  
Mentha X Piperita ◽  
Physical Chemical ◽  
Development And Validation ◽  
Phenolic And Flavonoid ◽  
Phenolic And Flavonoid Compounds

The aim of this work was to evaluate different concentrations of ethanol on antioxidant (phenolic and flavonoid) compounds extraction of Mentha x Piperita aiming at applying the extract in whey-based dairy beverages. The extracts were obtained by cold maceration using water and ethanol as solvents. The extract using water and 70% ethanol had a 13.83 (w w-1) yield, 61.72 mg GAE g-1 phenolic compounds extract, 37.27 mg QE g-1 flavonoid content extract and 0.056 mg mL-1 antioxidant activities. The dairy beverage formulations followed a 22 factorial design in order to evaluate the effect of whey/milk and starch addition on the physical-chemical (pH, acidity, moisture, ash, fat, protein, viscosity, and color) and sensorial characteristics (acceptability) of the product. Analysis of variance (ANOVA) allowed for the development and validation of mathematical models for ash content, lipids, viscosity, and luminosity of the dairy beverage. The effects of whey/milk and starch variables on such characteristics were analyzed by the elaboration of contour curves. The product presented a lower color intensity at the highest whey concentration (75%). The product had a good sensory acceptance, and the 50 whey and 50% milk formulation presented a 7.16 points average and 79.51% acceptance index, suggesting that 50% of whey could be added up to the product’s formulation.

Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design

2014 ◽  
Vol 3 (7) ◽  
pp. 301-308 ◽  
Author(s):  
Apoorva Agarwal ◽  
Vandana Kharb ◽  
Vikas Anand Saharan
Keyword(s):  
Water Solubility ◽  
Maximum Yield ◽  
Statistical Design ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Pharmaceutical Journal ◽  
Response Surfaces ◽  
Stoichiometric Ratio ◽  
Box Behnken Design ◽  
Quadratic Response

With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.DOI: http://dx.doi.org/10.3329/icpj.v3i7.19079 International Current Pharmaceutical Journal, June 2014, 3(7): 301-308

scholarly journals Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles

2018 ◽  
Vol 8 (6-s) ◽  
pp. 63-69
Author(s):  
Sandip Akaram Bandgar ◽  
Pranali Dhavale ◽  
Pravin Patil ◽  
Sardar Shelake ◽  
Shitalkumar Patil
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Solid Lipid Nanoparticle ◽  
Bioavailability Enhancement ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Optimum Stability

Solid Lipid Nanoparticles (SLN) are rapidly developing field of nanotechnology with several potential application in drug delivery and research. Drugs having low aqueous solubility not only give low oral bioavailability but provide high inter-and intra subject variability. The purpose of the present study was to investigate the bioavailability enhancement of Prazosin Hydrochloride drug by formulating solid lipid nanoparticle. Prazosin Hydrochloride Drug is an antihypertensive drug with limited bioavailability so that solid lipid nanoparticle (SLN) is one of the approaches to improve bioavailability. SLN were prepared using glyceryl monostearate by hot homogenization followed by Solvent emulsification-ultrasonication. Prazosin Hydrochloride loaded SLN were characterized and optimized by parameters like particle size, zeta potential, XRD, DSC. Proposing Hydrochloride loaded SLN having the particle size 263.8±1.88 and entrapment efficiency 89.29±0.65% shows better bioavailability and optimum stability in studies. The SLN studies prepared using glyceryl mono stearate   as a lipid and Polaxamer 407 as a polymer leads to improve bioavailability of the drug. Keywords: Prazosin Hydrochloride, Solid Lipid Nanoparticles, Entrapment efficiency, DSC

scholarly journals Design and Synthesis of Lactose, Galactose and Cholic Acid Related Dual Conjugated Chitosan Derivatives as Potential Anti Liver Cancer Drug Carriers

Polymers ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 2939
Author(s):  
Yili Ding ◽  
Wutong Cui ◽  
Chamakura V. N. S. Vara Prasad ◽  
Bingyun Wang
Keyword(s):  
Liver Cancer ◽  
Cholic Acid ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Fold Increase ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Chitosan Derivatives ◽  
Design And Synthesis ◽  
Electron Microscope Image

Cholic acid and galactose or lactose dual conjugated chitosan derivatives were designed and synthesized as potential anti liver cancer drug carriers, their structures were characterized through proton NMR spectra, elemental analysis, size distribution, zeta potential, and scanning electron microscope image studies. The ability of the dual conjugates to enhance the aqueous solubility of the cancer drug sorafenib was evaluated. The entrapment efficiency (EE%) and drug content (DC%) of sorafenib in the inclusion complexes were measured. The chitosan dual conjugate with cholic acid and galactose was found to be best in enhancing the aqueous solubility of sorafenib. The solubility of sorafenib in water has increased from 1.7 µg/mL to 1900 µg/mL which is equal to 1117-fold increase in its solubility due to the inclusion complex with chitosan conjugate.

scholarly journals Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate

2015 ◽  
Vol 14 (9) ◽  
pp. 1549-1556
Author(s):  
P Kommavarapu ◽  
A Maruthapillai ◽  
K Palanisamy
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Solvent Injection ◽  
Injection Method ◽  
Solid Lipid ◽  
Enhanced Solubility

Purpose: To enhance the aqueous solubility and dissolution rate of elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles (SLNs) using solvent injection method.Methods: EVG-loaded SLNs were prepared by solvent injection method. Four different formulations of SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous phase. The SLNs were characterized for various physical properties, including particle size, zeta potential, polydispersity, release profile and entrapment efficiency.Results: The yield of SLNs was in the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes were observed in mean particle size (nm), Z - potential (mV) and polydispersity index (PDI) of the SLNs by varying the  concentration of cryoprotectant. EVG – SLNs demonstrated a 800 – 1030-fold enhancement in aqueous solubility compared with plain EVG. The dissolution efficiency (DE) for SLNs was > 63 % in all cases and increased up to 83 % with increasing lipid load.Conclusion: Successful preparation and characterization of elvitegravir–loaded solid lipid nanoparticles by solvent injection method has been accomplished in this study.Keywords: Elvitegravir, Solid lipid nanoparticles, Cryoprotectant, Lipid load, Entrapment efficiency

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