scholarly journals Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 143 ◽  
Author(s):  
Enas Elmowafy ◽  
Marwa O. El-Derany ◽  
Francesca Biondo ◽  
Mattia Tiboni ◽  
Luca Casettari ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Spherical Shape ◽  
Aqueous Solubility ◽  
Biological Properties ◽  
Hepatoprotective Activity ◽  
Molar Ratio ◽  
Drug Release Profile ◽  
Sugar Esters

Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl4 intoxication and to carry out an antioxidant effect.

scholarly journals Novel Leu-Val Based Dipeptide as Antimicrobial and Antimalarial Agents: Synthesis and Molecular Docking

2020 ◽  
Vol 8 ◽  
Author(s):  
James A. Ezugwu ◽  
Uchechukwu C. Okoro ◽  
Mercy A. Ezeokonkwo ◽  
China R. Bhimapaka ◽  
Sunday N. Okafor ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Condensation Reaction ◽  
Biological Properties ◽  
Health Issues ◽  
Protein Residues ◽  
Antimalarial Agents ◽  
Antimalarial Resistance ◽  
Microbial Strains

The increase of antimicrobial resistance (AMR) and antimalarial resistance are complex and severe health issues today, as many microbial strains have become resistant to market drugs. The choice for the synthesis of new dipeptide-carboxamide derivatives is as a result of their wide biological properties such as antimicrobial, anti-inflammatory, and antioxidant activities. The condensation reaction of substituted benzenesulphonamoyl pentanamides with the carboxamide derivatives using peptide coupling reagents gave targeted products (8a-j). The in silico antimalarial and antibacterial studies showed good interactions of the compounds with target protein residues and a higher dock score in comparison with standard drugs. In the in vivo study, compound 8j was the most potent antimalarial agent with 61.90% inhibition comparable with 67% inhibition for Artemisinin. In the in vitro antimicrobial activity, compounds 8a and 8b (MIC 1.2 × 10−3 M and 1.1 × 10−3 M) were most potent against S. aureus; compound 8a, 8b, and 8j with MIC 6.0 × 10−3 M, 5.7 × 10−4 M, and 6.5 × 10−4 M, respectively, were the most active against B. subtilis; compound 8b (MIC 9.5 × 10−4 M) was most active against E.coli while 8a, 8b and 8d were the most active against S. typhi. Compounds 8c and 8h (MIC 1.3 × 10−3 M) each were the most active against C. albicans, while compound 8b (MIC 1.3 × 10−4 M) was most active against A. niger.

Hepatoprotective activity of a purified methanol extract and saponins from the roots of Chenopodium bonus-henricus L.

2019 ◽  
Vol 74 (11-12) ◽  
pp. 329-337 ◽  
Author(s):  
Zlatina Kokanova-Nedialkova ◽  
Paraskev Nedialkov ◽  
Magdalena Kondeva-Burdina ◽  
Rumyana Simeonova
Keyword(s):  
High Performance ◽  
High Resolution Mass Spectrometry ◽  
Antioxidant Activities ◽  
Rat Hepatocytes ◽  
Hepatoprotective Activity ◽  
Cellular Damage ◽  
Medicagenic Acid ◽  
Hepatoprotective Agents

Abstract An ultra-high-performance liquid chromatography-high-resolution mass spectrometry based profiling of a purified MeOH extract (PME) from the roots of Chenopodium bonus-henricus L. (Amaranthaceae) tentatively identified 15 saponins of six sapogenins. The PME exerts hepatoprotective and antioxidant activities comparable to those of flavonoid complex silymarin in in vitro (1 and 10 μg/mL) and in vivo (200 mg/kg/daily for 7 days) models of hepatotoxicity, induced by CCl4. The main constituents of PME, respectively saponins bonushenricoside A (1), 3-O-β-D-glucuronopyranosyl-bayogenin-28-O-β-D-glucopyranosyl ester (2), 3-O-β-D-glucuronopyranosyl-medicagenic acid-28-O-β-D-xylopyranosyl (1→4)-α-L-rhamnopyranosyl(1→2)-α-L-arabinopyranosyl ester (3), 3-O-β-D-glucuronopyranosyl-2β-hydroxygypsogenin-28-O-β-D-glucopyranosyl ester (4), 3-O-α-L-rabinopyranosyl-bayogenin-28-O-β-D-glucopyranosyl ester (6) and bonushenricoside B (8) (3 μg/mL each), compared to silymarin (5 and 50 μg/mL), significantly reduced the cellular damage caused by CCl4 in rat hepatocytes, preserved cell viability and glutathione level, decreased lactate dehydrogenase leakage and reduced lipid damage. The experimental data suggest that the glycosides of phytolaccagenin, bayogenin, medicagenic acid, 2β-hydroxygypsogenin, 2β-hydroxyoleanoic acid and oleanoic acid are a promising and safe class of hepatoprotective agents.

scholarly journals CO-CRYSTALS OF ACTIVE PHARMACEUTICAL INGREDIENT-IBUPROFEN LYSINE

2020 ◽  
pp. 22-32
Author(s):  
ALPANA KULKARNI ◽  
RITESH BACHHAV ◽  
VISHAL HOL ◽  
SWAPNIL SHETE
Keyword(s):  
Analgesic Activity ◽  
Physical Stability ◽  
Aqueous Solubility ◽  
Active Pharmaceutical Ingredient ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Compression Properties ◽  
Lattice Arrangement

Objective: Co-crystal is defined as a crystalline complex of two or more neutral molecules bound together primarily by hydrogen bonding or other non-covalent interactions. The pharmaceutical co-crystal involves crystal lattice arrangement between an Active Pharmaceutical Ingredient (API) with another pharmaceutically acceptable molecule. Co-crystals of API are preferred since they depict improved solubility, dissolution, stability, compressibility in comparison with API. Ibuprofen lysine (IL), frequently used analgesic and the anti-inflammatory drug has poor aqueous solubility and compressibility. This work shows the feasibility and optimal conditions for the preparation of co-crystals of ibuprofen lysine using Polyvivylpyrrolidone K25 (PK 25) and Polyvivylpyrrolidone K30 (PK 30) as co-formers. Methods: In this study, we prepared and studied the solubility, drug content, flow properties, physical stability of novel co-crystal, consisting of IL and PK 25/PK 30. The co-crystal IL: PK 30 (at a molar ratio of 0.29:0.5) and IL: PK 25 (at a molar ratio of 0.58:1) were characterized by X-ray analysis, infrared spectroscopy and thermal analysis. Furthermore, the tablet formulations of the co-crystals were subjected to in vitro dissolution and in vivo analgesic activity, with the goal of comparing the co-crystals with IL and the marketed tablet of ibuprofen (Brufen®) respectively. Results: The IL: PK co-crystals demonstrated superior solubility and the dissolution properties over IL. The compression properties of the co-crystals were similar to IL. The co-crystals exhibited higher analgesic activity than the marketed tablet.  Conclusion: The results indicated the use of PK 25 and PK 30 as safe and promising co-crystal formers.

Preparation and In Vivo Characterization of Niosomal Carriers of the Antidiabetic Drug Repaglinide

2015 ◽  
Vol 8 (1) ◽  
pp. 2756-2767 ◽  
Author(s):  
Shrishti Namdev ◽  
Kishore Gujar ◽  
Satish Mandlik ◽  
Preeti Jamkar
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Span 60

The objective of this study is to prepare and characterise repaglinide niosomes using the Factorial Design strategy.Repaglinide is a potent second-generation oral hypoglycemic agent and has short half-life of 1 hour and oral bioavailability of 50%. Preparing Niosomal drugdelivery of repaglinide may increase its bioavailability which would lead to better therapeutic effects, reduce the frequency of dosing from twice a day to once a day and decrease side effects. The preliminary study was carried out for selection of surfactant and method of preparation based on least particle size and highest entrapment efficiency. For niosome preparation, organic solvent injection method was selected and span 60, cholesterol were selected as variable. A32 factorial design was used to optimize the effect of amounts of span 60(X1) and cholesterol (X2) which were the independent variables. Particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Relation between the dependent and independent variables were drawn out from the mathematical equations and response surface plots.Statistical analysis was performed using ANOVA which was found to be significant and quadratic equation was obtained by MLRA. The particle size was found to be in range of 144-497 nm and entrapment efficiency between 54-88%. Scanning electron microscopy indicated the spherical shape of the niosomes and formation of vesicle. Zeta potential analysis showed negatively charged surface with value of-36.7 mV. In vitro drug release profile showed that drug released fast initially followed by a slow release. In vivo pharmacokinetic study revealed that the niosomal preparation showed significant decrease in blood glucose level when compared to free repaglinide. The developed niosomal system also has potential of maintaining therapeutic level of RPG for longer period of time.Thus,the niosomes could be promising carriers for delivery ofrepaglinide with increased 

Formulation and evaluation of α-Pinene loaded Self-emulsifying nanoformulation for in-vivo anti-Parkinson’s activity

2021 ◽  
Vol 15 ◽  
Author(s):  
Rajnish Srivastava ◽  
P.K. Choudhury ◽  
Suresh Kumar Dev ◽  
Vaibhav Rathore
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Neuroprotective Effect ◽  
Spherical Shape ◽  
Tween 80 ◽  
In Vivo Studies ◽  
Drug Release Profile

Aim: The aim of the present study was to develop and optimize the self-nanoemulsifying drug delivery system of α-pinene (ALP-SNEDDS) and to evaluate its in-vivo anti-Parkinson’s activity. Background: Different lipid-based drug delivery technologies have been researched to upgrade the bioavailability of such drug candidates and to expand their clinical adequacy upon oral administration. Self-emulsifying drug delivery system (SEDDS) have pulled in expanding interests and, specifically, self-nanoemulsifying drug delivery system (SNEDDS). Objective: The present work was an attempt in order to improve the bioavailability of the ALP via defining the role of self-nanoemulsifying formulations for its neuroprotective effect. Method: Miscibility of the ALP was estimated in various excipient components to select the optimized combination. Self-nanoemulsification, thermodynamic stability, effect of dilution on robustness, optical clarity, viscosity and conductivity tests were performed. The in-vivo anti-Parkinson’s activity of the ALP-SNEEDS formulations were done by using Pilocarpine antagonism induced Parkinsonism in rodents. Behavioural tests like tremulous jaw movements, body temperature, salivation and lacrimation are performed. Result: Two optimized formulation, composed of Anise oil, Tween 80 and Transcutol-HP of Oil: Smix ratio (4:6 and 3:7) were selected. The Smix ratio for both the formulation was 2:1. The particle size was found to consistent with the increase in dilution. The mean negative zeta potential of the formulations was found to be increased with increase in dilution. The TEM images of the formulations reveals spherical shape of the droplet. The in-vitro drug release profile was found to be significant as compared to plain ALP suspension. Conclusion: The results form in-vivo studies indicate that nanosizing and enhanced solubilisation of oral ALP-SNEDDS formulations significantly improved the behavioural activities as compared to plain ALP suspension.

scholarly journals Optimization and Evaluation of Piperine Loaded Herbosomes for their Antioxidant and Hepatoprotective Potential

2022 ◽  
Vol 34 (2) ◽  
pp. 383-388
Author(s):  
Gayatri Joshi ◽  
Abhishek Tiwari ◽  
Prashant Upadhyay
Keyword(s):  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Hepatoprotective Activity ◽  
The Body ◽  
Oral Dosage ◽  
Serum Glutamic Oxaloacetic Transaminase ◽  
Homogeneous Population ◽  
Ic50 Value

Piperine is classified as a class II drug in the biopharmaceutical classification system due to its low aqueous solubility. As a result, piperine herbosomes were created to improve the dissolution rate and in vivo liver protecting activity of piperine and physico-chemical characteristics were used to confirm herbosome formation. The piperine-herbosome formulation revealed spherical particle size of all formulations from P1-P10 and found142.4 ± 0.98 nm for best piperine-herbosome formulation (P2) and a PDI value of 0.237, indicating a homogeneous population of piperine loaded vesicles. In vitro drug release rate and percent entrapment efficiency were determined for all formulations P1-P25 and found to be 95.306 ± 0.21 and 97.306 ± 0.65 in 12 h, respectively for best piperine-herbosome formulation (P2). It exemplifies the complex’s long-term releasing capability. This information suggests that it may have a longer retention time inside the body, extending the duration of effect. The antioxidant potential of pure piperine was determined using the DPPH scavenging method, with an IC50 value of 107.59 ± 0.11 g/mL compared to a formulation with an IC50 value of 93.926 ± 0.03 g/mL. Swiss albino mice of either sex were utilized for the evaluation of hepatoprotective activity. On the 8th day, the hepatotoxicity was caused by giving a single oral dosage of CCl4 (0.5 mL) and the parameters were evaluated on the 9th day. This formulation has the best optimized based on drug content and drug entrapment. Serum glutamic oxaloacetic transaminase (SGOT), serum glutamic-pyruvic transaminase (SGPT), alkaline phosphatase (ALP) and total bilirubin were among the biochemical markers measured. In comparison to normal control (161 ± 0.31 IU/L, 52.78 ± 0.28 IU/L, 121.12 ± 0.14 IU/L and 0.633 ± 1.44 IU/L) and P2 formulation (163.23 ± 0.49 IU/L, 66.9 ± 0.05 IU/L, 128.3 ± 1.15 IU/L and 0.645 ± 0.67 IU/L respectively).

scholarly journals CHRISIN: A REVIEW OF ITS THERAPEUTIC APPLICATIONS

2019 ◽  
Vol 16 (33) ◽  
pp. 1-9
Author(s):  
T. W. KULTZ ◽  
E. A. ROZISCA ◽  
L. E. A. CAMARGO
Keyword(s):  
Antioxidant Activities ◽  
Great Part ◽  
Biological Properties ◽  
Future Research ◽  
Therapeutic Applications ◽  
In Vivo Assays ◽  
Wide Range ◽  
Therapeutic Properties

The chrysin, flavonoid mainly encountered in plants and beekeeping products, has awakened the interest between researchers from all over the world, due the wide range of therapeutic properties, like anti inflammatory and antioxidant activities and also your potent antitumor effect. The goal of this task was investigate the various therapeutic applications of chrysin, relating in vitro and in vivo assays, as well as your applications in nanotecnology field. Because of that, this article has been developed with researches relating keywords in scientific search sites, like PubMed, Scielo, Google Scholar, etc. Gathering great part of recent literature, it could be seen that the biological properties of chrysin, such as anti inflamatory, antioxidant and antitumoral activities, can be verified by using plants extracts properly treated and purified, or in applications using nanotecnology as being an alternative for a directly and precise use of these activities. Thus, it has been verified the uses against breast cancer, thyroid cancer and uterine colon cancer. Therefore, concludes that chrysin features numerous activities and therapeutic properties tested by in vitro and in vivo assays, in addition to all its nanoapplication potential. These results show and justify the importance of this research for society and for the scientific scope. The differential of this article is the combination of nanotechnology studies and the therapeutic properties of chrysin, which contributes to future research on the topics.

In vitro and in vivo antioxidant activities of the leaves of Chrysophyllum albidum

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
AH Adebayo ◽  
AO Abolaji ◽  
OO Ayepola ◽  
TB Olorunfemi ◽  
OS Taiwo
Keyword(s):  
Antioxidant Activities

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Nanodrugs as a new approach in therapy of cardiovascular diseases and cancer with tumor-associated angiogenesis

2020 ◽  
Vol 28 ◽  
Author(s):  
Justyna Hajtuch ◽  
Karolina Niska ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Cardiovascular Disease ◽  
Cardiovascular Diseases ◽  
Controlled Drug Release ◽  
Biological Properties ◽  
Comprehensive Information ◽  
Conventional Drug ◽  
Key Factor ◽  
Functionalized Materials

Background: Cancer along with cardiovascular diseases are globally defined as leading causes of death. Importantly, some risk factors are common to these diseases. The process of angiogenesis and platelets aggregation are observed in cancer development and progression. In recent years, studies have been conducted on nanodrugs in these diseases that have provided important information on the biological and physicochemical properties of nanoparticles. Their attractive features are that they are made of biocompatible, well-characterized and easily functionalized materials. Unlike conventional drug delivery, sustained and controlled drug release can be obtained by using nanomaterials. Methods: In this article, we review the latest research to provide comprehensive information on nanoparticle-based drugs for the treatment of cancer, cardiovascular disease associated with abnormal haemostasis, and the inhibition of tumorassociated angiogenesis. Results: The results of the analysis of data based on nanoparticles with drugs confirm their improved pharmaceutical and biological properties, which gives promising antiplatelet, anticoagulant and antiangiogenic effects. Moreover, the review included in vitro, in vivo research and presented nanodrugs with chemotherapeutics approved by Food and Drug Administration. Conclusion: By the optimization of nanoparticles size and surface properties, nanotechnology are able to deliver drugs with enhanced bioavailability in treatment of cardiovascular disease, cancer and inhibition of cancer-related angiogenesis. Thus, nanotechnology can improve the therapeutic efficacy of the drug, but there is a need for a better understanding of the nanodrugs interaction in the human body, because this is a key factor in the success of potential nanotherapeutics.

Sign in / Sign up

Export Citation Format

Share Document