scholarly journals Bupivacaine-loaded nanostructured lipid carriers prepared with beeswax, lavender or melaleuca oil: characterization and physico-chemical stability

2019 ◽  
Author(s):  
Gabriela Geronimo ◽  
Eneida de Paula ◽  
Gustavo Henrique Rodrigues da Silva ◽  
Lígia Nunes de Morais Ribeiro
Keyword(s):  
Therapeutic Efficacy ◽  
Nanostructured Lipid Carriers ◽  
Physico Chemical ◽  
In Vivo Tests ◽  
Oil Characterization ◽  
New Applications

Although bupivacaine (BVC) is one of the most widely used anesthetics worldwide, improving its therapeutic efficacy without increasing the clinical doses may open possibilities for new applications for this drug. In this study, we prepared innovative formulations: nanostructured lipid carriers (NLC) functionalized with beeswax, lavender or melaleuca oil in order to increase the anesthetic efficiency of BVC. For this, after preparation and characterization of the NLC by dynamic light scattering and determination of the encapsulation efficiency (% EE), stability was monitored during 12 months. The NLC showed appropriate physical-chemical features, with high %EE and stability. The developed formulations proved to be good candidates to increase the therapeutic efficacy of BVC so that further in vitro and in vivo tests are under course to evaluate their advantages, in comparison to the commercial BVC formulation.

scholarly journals Characterization of a New Chitosanase from a Marine Bacillus sp. and the Anti-Oxidant Activity of Its Hydrolysate

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 126
Author(s):  
Chunrui Ma ◽  
Xiao Li ◽  
Kun Yang ◽  
Shangyong Li
Keyword(s):  
Radical Scavenging ◽  
Maximal Activity ◽  
Hydroxyl Groups ◽  
Bacillus Sp ◽  
Low Molecular Weight Chitosan ◽  
Anti Oxidant

Chitooligosaccharide (COS) has been recognized to exhibit efficient anti-oxidant activity. Enzymatic hydrolysis using chitosanases can retain all the amino and hydroxyl groups of chitosan, which are necessary for its activity. In this study, a new chitosanase encoding gene, csnQ, was cloned from the marine Bacillus sp. Q1098 and expressed in Escherichia coli. The recombinant chitosanase, CsnQ, showed maximal activity at pH 5.31 and 60 °C. Determination of CsnQ pH-stability showed that CsnQ could retain more than 50% of its activity over a wide pH, from 3.60 to 9.80. CsnQ is an endo-type chitosanase, yielding chitodisaccharide as the main product. Additionally, in vitro and in vivo analyses indicated that chitodisaccharide possesses much more effective anti-oxidant activity than glucosamine and low molecular weight chitosan (LMW-CS) (~5 kDa). Notably, to our knowledge, this is the first evidence that chitodisaccharide is the minimal COS fragment required for free radical scavenging.

scholarly journals Biodistribution of Nanostructured Lipid Carriers in Mice Atherosclerotic Model

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3499 ◽  
Author(s):  
Devel ◽  
Almer ◽  
Cabella ◽  
Beau ◽  
Bernes ◽  
...  
Keyword(s):  
Colloidal Stability ◽  
Ex Vivo ◽  
Particle Diameter ◽  
Nanostructured Lipid Carriers ◽  
Atherosclerotic Plaques ◽  
Particle Uptake ◽  
Atherosclerotic Lesions ◽  
Physico Chemical

Atherosclerosis is a major cardiovascular disease worldwide, that could benefit from innovative nanomedicine imaging tools and treatments. In this perspective, we here studied, by fluorescence imaging in ApoE-/- mice, the biodistribution of non-functionalized and RXP470.1-targeted nanostructured lipid carriers (NLC) loaded with DiD dye. RXP470.1 specifically binds to MMP12, a metalloprotease that is over-expressed by macrophages residing in atherosclerotic plaques. Physico-chemical characterizations showed that RXP-NLC (about 105 RXP470.1 moieties/particle) displayed similar features as non-functionalized NLC in terms of particle diameter (about 60-65 nm), surface charge (about −5 — −10 mV), and colloidal stability. In vitro inhibition assays demonstrated that RXP-NLC conserved a selectivity and affinity profile, which favored MMP-12. In vivo data indicated that NLC and RXP-NLC presented prolonged blood circulation and accumulation in atherosclerotic lesions in a few hours. Twenty-four hours after injection, particle uptake in atherosclerotic plaques of the brachiocephalic artery was similar for both nanoparticles, as assessed by ex vivo imaging. This suggests that the RXP470.1 coating did not significantly induce an active targeting of the nanoparticles within the plaques. Overall, NLCs appeared to be very promising nanovectors to efficiently and specifically deliver imaging agents or drugs in atherosclerotic lesions, opening avenues for new nanomedicine strategies for cardiovascular diseases.

In Vitro Studies on Physiological and Chemical Stability of New LE404-Derivatives with Extended Half-Life

Drug Research ◽  
2018 ◽  
Vol 68 (09) ◽  
pp. 514-520
Author(s):  
Stephanie Zergiebel ◽  
Andreas Seeling
Keyword(s):  
Pharmacokinetic Parameters ◽  
Lead Structure ◽  
Lack Of Information ◽  
Gastrointestinal Fluid ◽  
In Vivo Tests ◽  
Dopamine And Serotonin Receptors ◽  
The Stability

AbstractDibenzoazecines are a class of potential neuroleptics with high affinity to dopamine and serotonin receptors. The efficacy and high therapeutic range has already been demonstrated in vivo with the lead structure 7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecin-3-ol (LE404) and selected derivatives. There is a variety of new synthesized structurally different dibenzoazecine derivatives with the aim to improve pharmacokinetic parameters, all of which contain the lead structure LE404. For a multitude of these substances is still a lack of information, inclusive of stability, physicochemical parameters, pharmacokinetics and metabolism. Therefore, the present study investigated the stability properties of 17 new azecine derivatives, including esterase cleavage, stability in simulated gastrointestinal fluid, stability at different pH-values and determination of octanol/water-partition coefficients. These findings, in correlation to the properties and efficacy of the already in vivo tested substances, will be useful for safety and efficacy in further in vivo tests.

Casuarina equisetifoliaExtract Loaded Phytosomes: Optimization, Characterization andIn vivoEvaluation of Antidiabetic and Antihyperlipidemic Activities in Wistar Rats

2019 ◽  
Vol 9 (2) ◽  
pp. 116-133 ◽  
Author(s):  
Anjana Rani ◽  
Sunil Kumar ◽  
Roop K. Khar
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Therapeutic Efficacy ◽  
Entrapment Efficiency ◽  
Herbal Extract ◽  
Casuarina Equisetifolia ◽  
Novel Drug

Background:Herbal extracts have brilliant in-vitro activity but less in-vivo action in light of their macromolecular size and poor lipid solubility bringing about poor absorption and low bioavailability. These issues can be corrected by designing novel drug delivery systems. Phytosomes provide better absorption and bioavailability when compared to conventional herbal extract.Objective:This paper deals with the preparation, optimization and characterization of Phytosome of plant extract and in vivo assessment of antidiabetic and antihyperlipidemic activity for improved therapeutic efficacy having sufficient stability.Methods:Preliminary distinctive strategies were utilized to get ready Phytosome and antisolvent precipitation method was chosen. The formulation was guided by a full factorial design to study the effect of Independent variable on various dependent variables and resulted in an optimised product. Response contour plots were generated for each response factor to predict a phytosomal composition that yields phytosome formulation having least particle size and maximum entrapment efficiency.Results:Mean particle size, entrapment efficiency and Span value were found to be 295 ± 0.53nm, 82.43 ± 1.65% and 0.34 ± 0.14 respectively. Zeta potential was found to be 19.35mv, indicating the formation of stable formulation. In vitro release study described that the drug release follows the Korsmeyer- Peppas kinetic model. The results proved that Phytosomes of Casuarina equisetifolia extract exhibited more antidiabetic potential and antihyperlipidemic properties as compared to crude Casuarina extract.Conclusion:Phytosomes of Casuarina equestifolia extract was successfully formulated having good entrapment efficiency and physico-chemical characterization of the optimized product, confirming the formation of stable formulation. In vivo antidiabetic activity confirmed better potential of the optimised formulation. Consequently, it has been presumed that Phytosomes of Casuarina equisetifolia extract serve as a useful novel drug delivery system and provide more therapeutic efficacy than conventional plant extracts.

Simultaneous Determination of Absorption Coefficients for Skin and Muscle Tissues Using Spatially Resolved Measurements

2011 ◽  
Vol 222 ◽  
pp. 309-312 ◽  
Author(s):  
Hiroshi Suzuki ◽  
Masatsugu Niwayama ◽  
Toshitaka Yamakawa ◽  
Masaki Ohkubo ◽  
Ryotaro Kime ◽  
...  
Keyword(s):  
Near Infrared ◽  
Absorption Coefficients ◽  
Calculation Algorithm ◽  
Spatially Resolved ◽  
Muscle Tissues ◽  
In Vivo Tests ◽  
Deep Layers

We present a method for simultaneous measurement of optical absorption coefficients for skin (μas) and muscle (μam) tissues using spatially resolved near-infrared spectroscopy (SRS). A novel calculation algorithm was developed to determine the absorption coefficients of superficial and deep layers within a three-layered structure using Monte Carlo simulation. A method for measuring the skin and muscle absorption coefficients was proposed based on this algorithm. In vitro experiments with tissue-like phantom and in vivo tests were performed using the SRS system with four separate detectors. The results show that the absorption coefficients for both skin and muscle tissues were obtained accurately.

Mitochondrial Neurogastrointestinal Encephalomyopathy (MNGIE): Biochemical Features and Therapeutic Approaches

2007 ◽  
Vol 27 (1-3) ◽  
pp. 151-163 ◽  
Author(s):  
M. C. Lara ◽  
M. L. Valentino ◽  
J. Torres-Torronteras ◽  
M. Hirano ◽  
R. Martí
Keyword(s):  
Molecular Genetic ◽  
In Vivo Studies ◽  
Gene Encoding ◽  
Mitochondrial Neurogastrointestinal Encephalomyopathy ◽  
Mtdna Replication ◽  
Biochemical Features

Over the last 15 years, important research has expanded our knowledge of the clinical, molecular genetic, and biochemical features of mitochondrial neurogastrointestinal encephalomyopathy (MNGIE). The characterization of mitochondrial involvement in this disorder and the seminal determination of its genetic cause, have opened new possibilities for more detailed and deeper studies on the pathomechanisms in this progressive and fatal disease. It has been established that MNGIE is caused by mutations in the gene encoding thymidine phosphorylase (TP), which lead to absolute or nearly complete loss of its catalytic activity, producing systemic accumulations of its substrates, thymidine (dThd) and deoxyuridine (dUrd). Findings obtained from in vitro and in vivo studies indicate that the biochemical imbalances specifically impair mitochondrial DNA (mtDNA) replication, repair, or both leading to mitochondrial dysfunction. We have proposed that therapy for MNGIE should be aimed at reducing the concentrations of these toxic nucleosides to normal or nearly normal levels. The first treatment, allogeneic stem-cell transplantation (alloSCT) reported in 2006, produced a nearly full biochemical correction of the dThd and dUrd imbalances in blood. Clinical follow-up of this and other patients receiving alloSCT is necessary to determine whether this and other therapies based on a permanent restoration of TP will be effective treatment for MNGIE.

scholarly journals Characterization of Fibrous Mordenite: A First Step for the Evaluation of Its Potential Toxicity

Crystals ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 769 ◽  
Author(s):  
Dario Di Giuseppe
Keyword(s):  
Surface Characteristics ◽  
International Agency ◽  
Precautionary Approach ◽  
Adverse Health Effects ◽  
In Vivo Tests ◽  
Pathogenic Agents ◽  
Geological Formations

In nature, a huge number of unregulated minerals fibers share the same characteristics as asbestos and therefore have potential adverse health effects. However, in addition to asbestos minerals, only fluoro-edenite and erionite are currently classified as toxic/pathogenic agents by the International Agency for Research on Cancer (IARC). Mordenite is one of the most abundant zeolites in nature and commonly occurs with a fibrous crystalline habit. The goal of this paper is to highlight how fibrous mordenite shares several common features with the well-known carcinogenic fibrous erionite. In particular, this study has shown that the morphology, biodurability, and surface characteristics of mordenite fibers are similar to those of erionite and asbestos. These properties make fibrous mordenite potentially toxic and exposure to its fibers can be associated with deadly diseases such as those associated with regulated mineral fibers. Since the presence of fibrous mordenite concerns widespread geological formations, this mineral fiber should be considered dangerous for health and the precautionary approach should be applied when this material is handled. Future in vitro and in vivo tests are necessary to provide further experimental confirmation of the outcome of this work.

scholarly journals Development, in vitro and in vivo evaluations of novel lipid drug delivery system of Newbouldia laevis (P. Beauv.)

2016 ◽  
Vol 3 ◽  
pp. 184954351667344
Author(s):  
Chukwuebuka Umeyor ◽  
Emmanuel Anaka ◽  
Franklin Kenechukwu ◽  
Chinazom Agbo ◽  
Anthony Attama
Keyword(s):  
Encapsulation Efficiency ◽  
Folk Medicine ◽  
Research Work ◽  
Lipid Matrix ◽  
Solid Lipid ◽  
Development In Vitro

Newbouldia laevis (P. Beauv.) is a tropical rainforest plant used in traditional folk medicine for the treatment of malaria, cough, joint pains, stomach ache, oedema and inflammation. The main thrust of this research work was to study the analgesic/anti-nociceptive properties of N. laevis-loaded solid lipid microdispersions. N. laevis leaves were extracted using ethanol, and the extract was formulated into solid lipid microdispersions using lipid matrix comprising a rational blend of Precirol® ATO 5 and Softisan® 154. Characterization of the solid lipid microdispersions include determination of morphology, particle size, pH, thermal property, encapsulation efficiency percentage and analgesic/anti-nociceptive property. The results obtained showed that the particles were spherical with sizes ranging from 40 µm to 125 µm. The solid lipid microdispersions maintained a stable pH within the acidic region of 5–6 with insignificant variations ( p > 0.05) over a period of 90 days. Thermal analysis showed that N. laevis was entrapped in the lipid matrix used for the formulations. Solid lipid microdispersions recorded a maximum encapsulation efficiency up to 88.1%. N. laevis-loaded solid lipid microdispersions also produced good analgesic/anti-nociceptive property comparable with the standard diclofenac potassium. N. laevis-loaded solid lipid microdispersions showed good analgesic/anti-nociceptive effect and could be used in the treatment and management of pain.

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