Sinapic Acid Release at the Cell Level by Incorporation into Nanoparticles: Experimental Evidence Using Biomembrane Models

Sinapic acid (SA), belonging to the phenylpropanoid family, and its derivatives are secondary metabolites found in the plant kingdom. In recent years, they have drawn attention because of their various biological activities, including neuroprotective effects. In this study, SA was incorporated into two different nanoparticle systems, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). The influence of different concentrations of SA on the nanoparticle systems was evaluated. It was studied the efficacy of the nanoparticle systems to release the active ingredient at cell level through the use of models of biological membranes represented by multilamellar vesicles (MLV) of dimyristoylphosphatidylcholine (DMPC) and conducting kinetic studies by placing in contact SLN and NLC, both unloaded and loaded with two different amounts of SA, with the same biological membrane model. Differential scanning calorimetry (DSC) was used for these studies. The results indicated a different distribution of SA within the two nanoparticle systems and that NLC are able to incorporate and release SA inside the structure of the biological membrane model.

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β-Cyclodextrins influence on E-3,5,4′-trimethoxystilbene absorption across biological membrane model: A differential scanning calorimetry evidence

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2009.12.048 ◽

2010 ◽

Vol 388 (1-2) ◽

pp. 144-150 ◽

Cited By ~ 5

Author(s):

Maria Grazia Sarpietro ◽

Sara Ottimo ◽

Maria Chiara Giuffrida ◽

Carmela Spatafora ◽

Corrado Tringali ◽

...

Keyword(s):

Differential Scanning Calorimetry ◽

Biological Membrane ◽

Membrane Model ◽

Scanning Calorimetry

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pH-Dependent Thermal Stability of Vibrio cholerae L-asparaginase

Protein and Peptide Letters ◽

10.2174/0929866526666190617092944 ◽

2019 ◽

Vol 26 (10) ◽

pp. 743-750 ◽

Cited By ~ 1

Author(s):

Remya Radha ◽

Sathyanarayana N. Gummadi

Keyword(s):

Vibrio Cholerae ◽

Conformational Changes ◽

Kinetic Studies ◽

Structural Features ◽

Structure Stability ◽

Kcal Mole ◽

Scanning Calorimetry ◽

Wide Range ◽

Ph Dependent ◽

Ph Range

Background:pH is one of the decisive macromolecular properties of proteins that significantly affects enzyme structure, stability and reaction rate. Change in pH may protonate or deprotonate the side group of aminoacid residues in the protein, thereby resulting in changes in chemical and structural features. Hence studies on the kinetics of enzyme deactivation by pH are important for assessing the bio-functionality of industrial enzymes. L-asparaginase is one such important enzyme that has potent applications in cancer therapy and food industry.Objective:The objective of the study is to understand and analyze the influence of pH on deactivation and stability of Vibrio cholerae L-asparaginase.Methods:Kinetic studies were conducted to analyze the effect of pH on stability and deactivation of Vibrio cholerae L-asparaginase. Circular Dichroism (CD) and Differential Scanning Calorimetry (DSC) studies have been carried out to understand the pH-dependent conformational changes in the secondary structure of V. cholerae L-asparaginase.Results:The enzyme was found to be least stable at extreme acidic conditions (pH< 4.5) and exhibited a gradual increase in melting temperature from 40 to 81 °C within pH range of 4.0 to 7.0. Thermodynamic properties of protein were estimated and at pH 7.0 the protein exhibited ΔG37of 26.31 kcal mole-1, ΔH of 204.27 kcal mole-1 and ΔS of 574.06 cal mole-1 K-1.Conclusion:The stability and thermodynamic analysis revealed that V. cholerae L-asparaginase was highly stable over a wide range of pH, with the highest stability in the pH range of 5.0–7.0.

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Neuroprotective Effects, Biological Activities and Therapeutic Potential of Phytochemicals: A Comprehensive Review

10.31487/j.ajmc.2020.01.04 ◽

2020 ◽

pp. 1-11

Author(s):

Xi-jun Wang ◽

Shi Qiu ◽

Aihua Zhang ◽

Jian-hua Miao ◽

Hui Sun ◽

...

Keyword(s):

Natural Products ◽

Neurological Disorders ◽

Chemical Biology ◽

Therapeutic Potential ◽

Biological Activities ◽

Therapeutic Agents ◽

Neuroprotective Effects ◽

Alternative Medicines ◽

Pharmacological Targets ◽

The World

The incidence of neurological disorders is growing in the world together with an increased lifespan. Nowadays, there are still no effective treatments for neurodegenerative pathology, which make necessary to search for new therapeutic agents. Natural products, most of them used in phytochemicals from herbal medicine, are considered promising alternatives for the treatment of neurodegenerative diseases. Numerous herbs have been applied to neurodegenerative disease treatments as complementary and alternative medicines. In the 21st century, omics-coupled functional pharmacology was developed for neurodegenerative drug discovery from natural products. In this article, we firstly provide the latest understanding of neurological disorders on risk factors, category, diagnosis and treatment, and then specially present an overview of natural products in neuroprotective effects research from chemical biology to pharmacological targets, and also discuss the natural products application and future challenge.

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Naringenin Release to Biomembrane Models by Incorporation into Nanoparticles. Experimental Evidence Using Differential Scanning Calorimetry

Surfaces ◽

10.3390/surfaces4040025 ◽

2021 ◽

Vol 4 (4) ◽

pp. 295-305

Author(s):

Cristina Torrisi ◽

Marco Di Guardia ◽

Francesco Castelli ◽

Maria Grazia Sarpietro

Keyword(s):

Differential Scanning Calorimetry ◽

Heart Tissue ◽

Protective Role ◽

Delivery Systems ◽

Free Radical Scavenger ◽

Radical Scavenger ◽

Drug Bioavailability ◽

Cell Level ◽

Scanning Calorimetry ◽

Beneficial Effects

Naringenin (4′,5,7-trihydroxyflavanone-7-rhamnoglucosideor naringenin-7-rhamnoglucoside), a flavonoid present in large quantities in citrus, has different beneficial effects on human health as an antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator. Different studies have shown that this substance also has a hypoglycemic and antihypertensive effect, reduces cholesterol and triglycerides, and plays an important protective role in the heart tissue; moreover, it provides neuroprotection against various neurological disorders such as Parkinson’s disease and unpredictable chronic stress-induced depression. Despite these advantages, Naringenin is poorly absorbed, and the small percentage absorbed is rapidly degraded by the liver, as a result losing its activity. Several approaches have been attempted to overcome these obstacles, among them, nanotechnology, with the use of Drug Delivery Systems (DDS) as Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC). DDS can, in fact, improve the drug bioavailability. The aim of this study was to develop and characterize SLN and NLC containing Naringenin and to evaluate the ability of these nanoparticles to release Naringenin at the cell level using biomembrane models represented by Multilamellar Vesicles (MLV). These studies were performed using Differential Scanning Calorimetry, a powerful technique to detect the interaction of drugs and delivery systems with MLV. It was shown that Naringenin could be better incorporated into NLC with respect to SLN and that Naringenin could be released by NLC into the biomembrane model. Therefore, suggesting the administration of Naringenin loaded into nanoparticles could help avoid the disadvantages associated with the use of the free molecule.

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Spatial structure of beta-amyloid Aβ<sub>1-40</sub> in complex with a biological membrane model

Advances in Alzheimer s Disease ◽

10.4236/aad.2012.13004 ◽

2012 ◽

Vol 01 (03) ◽

pp. 22-29 ◽

Cited By ~ 1

Author(s):

Konstantin S. Usachev ◽

Andrey V. Filippov ◽

Oleg N. Antzutkin ◽

Vladimir V. Klochkov

Keyword(s):

Spatial Structure ◽

Biological Membrane ◽

Beta Amyloid ◽

Membrane Model ◽

Amyloid Aβ

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Effect of The Surfactant and Liquid Lipid Type in The Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210222143716 ◽

2021 ◽

Vol 09 ◽

Author(s):

Mona Qushawy

Keyword(s):

Drug Release ◽

Factorial Design ◽

Biological Membrane ◽

Entrapment Efficiency ◽

Tween 80 ◽

Full Factorial Design ◽

Nanostructured Lipid Carrier ◽

Class Iii ◽

Scanning Calorimetry ◽

Full Factorial

Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) which is characterized by high solubility and low permeability. Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane. Method: 22 full factorial design was used to make the design of MF-NLCs formulations. MF-NLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80). Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of (0.253±0.01 to 0.496±0.02). The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7 % for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to the optimized formulation with the best responses. Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.

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The biophysical interaction of ferulic acid with liposomes as biological membrane model: The effect of the lipid bilayer composition

Journal of Molecular Liquids ◽

10.1016/j.molliq.2020.114689 ◽

2020 ◽

pp. 114689

Author(s):

Stéphanie Andrade ◽

Maria João Ramalho ◽

Joana Angélica Loureiro ◽

Maria Carmo Pereira

Keyword(s):

Ferulic Acid ◽

Lipid Bilayer ◽

Biological Membrane ◽

Membrane Model

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Steroidal pyrazolines as a promising scaffold in drug discovery

Future Medicinal Chemistry ◽

10.4155/fmc-2019-0325 ◽

2020 ◽

Vol 12 (10) ◽

pp. 949-959

Author(s):

Ranju Bansal ◽

Ranjit Singh

Keyword(s):

Drug Discovery ◽

Broad Spectrum ◽

Chemical Reactivity ◽

Biological Activities ◽

Antimicrobial Activities ◽

Review Article ◽

Pharmacological Activities ◽

Neuroprotective Effects ◽

Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

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Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

Royal Society Open Science ◽

10.1098/rsos.191184 ◽

2019 ◽

Vol 6 (10) ◽

pp. 191184 ◽

Cited By ~ 5

Author(s):

Fangbin Hu ◽

Weikang Liu ◽

Liuliu Yan ◽

Fanhui Kong ◽

Kun Wei

Keyword(s):

Electron Microscopy ◽

Glycolic Acid ◽

Water Solubility ◽

Skin Diseases ◽

Biological Activities ◽

Drug Loading ◽

Synthesis Method ◽

Hacat Cells ◽

Scanning Calorimetry

Astaxanthin is a xanthophyll carotenoid with high beneficial biological activities, such as antioxidant function and scavenging oxygen free radicals, but its application is limited because of poor water solubility and low bioavailability. Here, we prepared and optimized poly(lactic-co-glycolic acid) (PLGA) nanoparticles loaded with astaxanthin using the emulsion solvent evaporation technique and investigated the anti-photodamage effect in HaCaT cells. The four-factor three-stage Box–Behnken design was used to optimize the nanoparticle formulation. The experimental determination of the optimal nanoparticle size was 154.4 ± 0.35 nm, the zeta potential was 22.07 ± 0.93 mV, encapsulation efficiency was 96.42 ± 0.73% and drug loading capacity was 7.19 ± 0.12%. The physico-chemical properties of the optimized nanoparticles were characterized by dynamic light scattering, scanning electron microscopy, transmission electron microscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry and thermo-gravimetric analyser. In vitro study exhibited the excellent cell viability and cellular uptake of optimized nanoparticles on HaCaT cells. The anti-photodamage studies (cytotoxicity assay, reactive oxygen species content and JC-1 assessment) demonstrated that the optimized nanoparticles were more effective and safer than pure astaxanthin in HaCaT cells. These results suggest that our PLGA-coated astaxanthin nanoparticles synthesis method was highly feasible and can be used in cosmetics or the treatment of skin diseases.

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Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Biomolecules ◽

10.3390/biom9060241 ◽

2019 ◽

Vol 9 (6) ◽

pp. 241 ◽

Cited By ~ 1

Author(s):

Walter Ferreira da Silva Júnior ◽

Danielle Lima Bezerra de Menezes ◽

Luana Carvalho de Oliveira ◽

Letícia Scherer Koester ◽

Patrícia Danielle Oliveira de Almeida ◽

...

Keyword(s):

Inclusion Complexes ◽

Biological Activities ◽

Physicochemical Characterization ◽

Inflammatory Activity ◽

Scanning Calorimetry ◽

Promising Alternative ◽

Wide Range ◽

Natural Mixture ◽

Anti Inflammatory

α, β amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD’s as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both βCD and HPβCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.

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