Search results for: micelles
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 53

Search results for: micelles

23 Purification of Bacillus Lipopeptides for Diverse Applications

Authors: Vivek Rangarajan, Kim G. Clarke

Abstract:

Bacillus lipopeptides are biosurfactants with wide ranging applications in the medical, food, agricultural, environmental and cosmetic industries. They are produced as a mix of three families, surfactin, iturin and fengycin, each comprising a large number of homologues of varying functionalities. Consequently, the method and degree of purification of the lipopeptide cocktail becomes particularly important if the functionality of the lipopeptide end-product is to be maximized for the specific application. However, downstream processing of Bacillus lipopeptides is particularly challenging due to the subtle variations observed in the different lipopeptide homologues and isoforms. To date, the most frequently used lipopeptide purification operations have been acid precipitation, solvent extraction, membrane ultrafiltration, adsorption and size exclusion. RP-HPLC (reverse phase high pressure liquid chromatography) also has potential for fractionation of the lipopeptide homologues. In the studies presented here, membrane ultrafiltration and RP-HPLC were evaluated for lipopeptide purification to different degrees of purities for maximum functionality. Batch membrane ultrafiltration using 50 kDa polyether sulphone (PES) membranes resulted in lipopeptide recovery of about 68% for surfactin and 82 % for fengycin. The recovery was further improved to 95% by using size-conditioned lipopeptide micelles. The conditioning of lipopeptides with Ca2+ ions resulted in uniformly sized micelles with average size of 96.4 nm and a polydispersity index of 0.18. The size conditioning also facilitated removal of impurities (molecular weight ranging between 2335-3500 Da) through operation of the system under dia-filtration mode, in a way similar to salt removal from protein by dialysis. The resultant purified lipopeptide was devoid of macromolecular impurities and could ideally suit applications in the cosmetic and food industries. Enhanced purification using RP-HPLC was carried out in an analytical C18 column, with the aim to fractionate lipopeptides into their constituent homologues. The column was eluted with mobile phase comprising acetonitrile and water over an acetonitrile gradient, 35% - 80%, over 70 minutes. The gradient elution program resulted in as many as 41 fractions of individual lipopeptide homologues. The efficacy test of these fractions against fungal phytopathogens showed that first 21 fractions, identified to be homologues of iturins and fengycins, displayed maximum antifungal activities, suitable for biocontrol in the agricultural industry. Thus, in the current study, the downstream processing of lipopeptides leading to tailor-made products for selective applications was demonstrated using two major downstream unit operations.

Keywords: bacillus lipopeptides, membrane ultrafiltration, purification, RP-HPLC

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22 Targeted Nano Anti-Cancer Drugs for Curing Cancers

Authors: Imran Ali

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General chemotherapy for cancer treatment has many side and toxic effects. A new approach of targeting nano anti-cancer drug is under development stage and only few drugs are available in the market today. The unique features of these drugs are targeted action on cancer cells only without any side effect. Sometimes, these are called magic drugs. The important molecules used for nano anti-cancer drugs are cisplatin, carboplatin, bleomycin, 5-fluorouracil, doxorubicin, dactinomycin, 6-mercaptopurine, paclitaxel, topotecan, vinblastin and etoposide etc. The most commonly used materials for preparing nano particles carriers are dendrimers, polymeric, liposomal, micelles inorganic, organic etc. The proposed lecture will comprise the-of-art of nano drugs in cancer chemo-therapy including preparation, types of drugs, mechanism, future perspectives etc.

Keywords: cancer, nano-anti-cancer drugs, chemo-therapy, mechanism of action, future perspectives

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21 Loss in Efficacy of Viscoelastic Ionic Liquid Surfactants under High Salinity during Surfactant Flooding

Authors: Shilpa K. Nandwani, Mousumi Chakraborty, Smita Gupta

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When selecting surfactants for surfactant flooding during enhanced oil recovery, the most important criteria is that the surfactant system should reduce the interfacial tension between water and oil to ultralow values. In the present study, a mixture of ionic liquid surfactant and commercially available binding agent sodium tosylate has been used as a surfactant mixture. Presence of wormlike micelles indicates the possibility of achieving ultralow interfacial tension. Surface tension measurements of the mixed surfactant system have been studied. The emulsion size distribution of the mixed surfactant system at varying salinities has been studied. It has been found that at high salinities the viscoelastic surfactant system loses their efficacy and degenerate. Hence the given system may find application in low salinity reservoirs, providing good mobility to the flood during tertiary oil recovery process.

Keywords: ionic liquis, interfacial tension, Na-tosylate, viscoelastic surfactants

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20 Application of Low Frequency Ac Magnetic Field for Controlled Delivery of Drugs by Magnetic Nanoparticles

Authors: K. Yu Vlasova, M. A. Abakumov, H. Wishwarsao, M. Sokolsky, N. V. Nukolova, A. G. Majouga, Y. I. Golovin, N. L. Klyachko, A. V. Kabanov

Abstract:

Introduction:Nowadays pharmaceutical medicine is aimed to create systems for combined therapy, diagnostic, drug delivery and controlled release of active molecules to target cells. Magnetic nanoparticles (MNPs) are used to achieve this aim. MNPs can be applied in molecular diagnostics, magnetic resonance imaging (T1/T2 contrast agents), drug delivery, hyperthermia and could improve therapeutic effect of drugs. The most common drug containers, containing MNPs, are liposomes, micelles and polymeric molecules bonded to the MNPs surface. Usually superparamagnetic nanoparticles are used (the general diameter is about 5-6 nm) and all effects of high frequency magnetic field (MF) application are based on Neel relaxation resulting in heating of surrounded media. In this work we try to develop a new method to improve drug release from MNPs under super low frequency MF. We suppose that under low frequency MF exposures the Brown’s relaxation dominates and MNPs rotation could occur leading to conformation changes and release of bioactive molecules immobilized on MNPs surface.The aim of this work was to synthesize different systems with active drug (biopolymers coated MNPs nanoclusters with immobilized enzymes and doxorubicin (Dox) loaded magnetic liposomes/micelles) and investigate the effect of super low frequency MF on these drug containers. Methods: We have synthesized MNPs of magnetite with magnetic core diameter 7-12 nm . The MNPs were coated with block-copolymer of polylysine and polyethylene glycol. Superoxide dismutase 1 (SOD1) was electrostatically adsorbed on the surface of the clusters. Liposomes were prepared as follow: MNPs, phosphatidylcholine and cholesterol were dispersed in chloroform, dried to get film and then dispersed in distillated water, sonicated. Dox was added to the solution, pH was adjusted to 7.4 and excess of drug was removed by centrifugation through 3 kDa filters. Results: Polylysine coated MNPs formed nanosized clusters (as observed by TEM) with intensity average diameter of 112±5 nm and zeta potential 12±3 mV. After low frequency AC MF exposure we observed change of immobilized enzyme activity and hydrodynamic size of clusters. We suppose that the biomolecules (enzymes) are released from the MNPs surface followed with additional aggregation of complexes at the MF in medium. Centrifugation of the nanosuspension after AC MF exposures resulted in increase of positive charge of clusters and change in enzyme concentration in comparison with control sample without MF, thus confirming desorption of negatively charged enzyme from the positively charged surface of MNPs. Dox loaded magnetic liposomes had average diameter of 160±8 nm and polydispersity index (PDI) 0.25±0.07. Liposomes were stable in DW and PBS at pH=7.4 at 370C during a week. After MF application (10 min of exposure, 50 Hz, 230 mT) diameter of liposomes raised to 190±10 nm and PDI was 0.38±0.05. We explain this by destroying and/or reorganization of lipid bilayer, that leads to changes in release of drug in comparison with control without MF exposure. Conclusion: A new application of low frequency AC MF for drug delivery and controlled drug release was shown. Investigation was supported by RSF-14-13-00731 grant, K1-2014-022 grant.

Keywords: magnetic nanoparticles, low frequency magnetic field, drug delivery, controlled drug release

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19 Influence of Cationic Surfactant (TTAB) on the Rate of Dipeptide (Gly-DL-Asp) Ninhydrin Reaction in Absence and Presence of Organic Solvents

Authors: Mohd. Akram, A. A. M. Saeed

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Surfactants are widely used in our daily life either directly in household and personal care products or indirectly in the industrial processes. The kinetics of the interaction of glycyl-DL-aspartic acid (Gly-DL-Asp) with ninhydrin has been investigated spectrophotometrically in aqueous and organic-solvent media in the absence and presence of cationic surfactant of tetradecyltrimethylammonium bromide (TTAB). The study was carried out under different experimental conditions. The first and fractional order-rate were observed for [Gly-DL-Asp] and [ninhydrin], respectively. The reaction was enhanced about four-fold by TTAB micelles. The effect of organic solvents was studied at a constant concentration of TTAB and showed an increase in the absorbance as well as the rate constant for the formation of product (Ruhemann's purple). The results obtained in micellar media are treated quantitatively in terms of pseudo-phase and Piszkiewicz cooperativity models. The Arrhenius and Eyring equations are valid for the reaction over the range of temperatures used and different activation parameters (Ea, ∆H#, ∆S#, and ∆G#) have been evaluated.

Keywords: glycyl-DL-aspartic acid, ninhydrin, organic solvents, TTAB

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18 Starch-Based Systems for the Nano-Delivery of Quercetin

Authors: Fernando G. Torres, Omar P. Troncoso

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Quercetin is a naturally occurring polyphenol found in many vegetables, such as onion, with antioxidant properties. It is a dietary component with a documented role in reducing different human cancers. However, its low bioavailability, poor water solubility, and chemical instability limit its applications. Different nano-delivery systems such as nanoparticles, micelles, and nanohydrogels have been studied in order to improve the bioavailability of quercetin. Nanoparticles based on natural polymers such as starch have the advantage of being biocompatible, biodegradable, and non-toxic. In this study, quercetin was loaded into starch nanoparticles using a nanoprecipitation method. Different routes, using sodium tripolyphosphate and Tween® 80 as tensioactive agents, were tested in order to obtain an optimized starch-based nano-delivery system. The characterization of the nanoparticles loaded with quercetin was assessed by Fourier Transform Infrared Spectroscopy, Dynamic Light Scattering, Zeta potential, and Differential scanning calorimetry. UV-vis spectrophotometry was used to evaluate the loading efficiency and capacity of the samples. The results showed that starch-based systems could be successfully used for the nano-delivery of quercetin.

Keywords: starch nanoparticles, nanoprecipitation, quercetin, biomedical applications

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17 Host-Assisted Delivery of a Model Drug to Genomic DNA: Key Information From Ultrafast Spectroscopy and in Silico Study

Authors: Ria Ghosh, Soumendra Singh, Dipanjan Mukherjee, Susmita Mondal, Monojit Das, Uttam Pal, Aniruddha Adhikari, Aman Bhushan, Surajit Bose, Siddharth Sankar Bhattacharyya, Debasish Pal, Tanusri Saha-Dasgupta, Maitree Bhattacharyya, Debasis Bhattacharyya, Asim Kumar Mallick, Ranjan Das, Samir Kumar Pal

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Drug delivery to a target without adverse effects is one of the major criteria for clinical use. Herein, we have made an attempt to explore the delivery efficacy of SDS surfactant in a monomer and micellar stage during the delivery of the model drug, Toluidine Blue (TB) from the micellar cavity to DNA. Molecular recognition of pre-micellar SDS encapsulated TB with DNA occurs at a rate constant of k1 ~652 s 1. However, no significant release of encapsulated TB at micellar concentration was observed within the experimental time frame. This originated from the higher binding affinity of TB towards the nano-cavity of SDS at micellar concentration which does not allow the delivery of TB from the nano-cavity of SDS micelles to DNA. Thus, molecular recognition controls the extent of DNA recognition by TB which in turn modulates the rate of delivery of TB from SDS in a concentration-dependent manner.

Keywords: DNA, drug delivery, micelle, pre-micelle, SDS, toluidine blue

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16 Surfactant-Free O/W-Emulsion as Drug Delivery System

Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

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Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability

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15 Direct Visualization of Shear Induced Structures in Wormlike Micellar Solutions by Microfluidics and Advanced Microscopy

Authors: Carla Caiazza, Valentina Preziosi, Giovanna Tomaiuolo, Denis O'Sullivan, Vincenzo Guida, Stefano Guido

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In the last decades, wormlike micellar solutions have been extensively used to tune the rheological behavior of home care and personal care products. This and other successful applications underlie the growing attention that both basic and applied research are devoting to these systems, and to their unique rheological and flow properties. One of the key research topics is the occurrence of flow instabilities at high shear rates (such as shear banding), with the possibility of appearance of flow induced structures. In this scenario, microfluidics is a powerful tool to get a deeper insight into the flow behavior of a wormlike micellar solution, as the high confinement of a microfluidic device facilitates the onset of the flow instabilities; furthermore, thanks to its small dimensions, it can be coupled with optical microscopy, allowing a direct visualization of flow structuring phenomena. Here, the flow of a widely used wormlike micellar solution through a glass capillary has been studied, by coupling the microfluidic device with μPIV techniques. The direct visualization of flow-induced structures and the flow visualization analysis highlight a relationship between solution structuring and the onset of discontinuities in the velocity profile.

Keywords: flow instabilities, flow-induced structures, μPIV, wormlike micelles

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14 Nano-emulsion/Nano-suspension as Precursors for Oral Dissolvable Film to Enhance Bioavalabilty for Poor-water Solubility Drugs

Authors: Yuan Yang, Mickey Lam

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Oral dissolvable films have been considered as a unique alternative approach to conventional oral dosage forms. The films could be administrated via the gastrointestinal tract as conventional dosages or through sublingual/buccal mucosa membranes, which could enhance drug bioavailability by avoiding the first-pass effect and improving permeability due to high blood flow and lymphatic circulation. This work has described a state-of-art technic using nano-emulsion/nano-suspension as a precursor for the film to enhance the bioavailability of BCS class II drugs. The drug molecules are consequentially processed through the emulsification, gelation, and film-casting processes. The gelation process is critical to stabilizing the nano-emulsion for the film-casting as well as controlling the drug release process. Furthermore, the size of the nanoparticle on the film has a strong correlation with the size of the micelles in the precursor and the condition of the gelation process. It has been discovered that nanoparticle from 200 nm to 300 nm has shown the highest permeability for sublingual administration. In one example shown in work, the bioavailability of a low solubilize drug has been increased from 10% to 24% via sublingual administration of the film. The increasing of the bioavailability was thought to be associated with the enhancement of the diffusion process of the drug in the saliva layer above the mucosa membrane and the fact that the presents of the emulsifier help lose the rigid junction of the mucosa cells.

Keywords: oral dissolvable film, nano-suspension, nano-emulsion, bioavailability

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13 Reorientation of Anisotropic Particles in Free Liquid Microjets

Authors: Mathias Schlenk, Susanne Seibt, Sabine Rosenfeldt, Josef Breu, Stephan Foerster

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Thin liquid jets on micrometer scale play an important role in processing such as in fiber fabrication, inkjet printing, but also for sample delivery in modern synchrotron X-ray devices. In all these cases the liquid jets contain solvents and dissolved materials such as polymers, nanoparticles, fibers pigments or proteins. As liquid flow in liquid jets differs significantly from flow in capillaries and microchannels, particle localization and orientation will also be different. This is of critical importance for applications, which depend on well-defined homogeneous particle and fiber distribution and orientation in liquid jets. Investigations of particle orientation in liquid microjets of diluted solutions have been rare, despite their importance. With the arise of micro-focused X-ray beams it has become possible to scan across samples with micrometer resolution to locally analyse structure and orientation of the samples. In the present work, we used this method to scan across liquid microjets to determine the local distribution and orientation of anisotropic particles. The compromise wormlike block copolymer micelles as an example of long flexible fibrous structures, hectorite materials as a model of extended nanosheet structures, and gold nanorods as an illustration of short stiff cylinders to comprise all relevant anisotropic geometries. We find that due to the different velocity profile in the liquid jet, which resembles plug flow, the orientation of the particles which was generated in the capillary is lost or changed into non-oriented or bi-axially orientations depending on the geometrical shape of the particle.

Keywords: anisotropic particles, liquid microjets, reorientation, SAXS

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12 Spectroscopic Studies on Solubilization of Polycyclic Aromatic Hydrocarbons in Structurally Different Gemini Surfactants

Authors: Toshikee Yadav, Deepti Tikariha, Jyotsna Lakra, Kallol K. Ghosh

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Polycyclic aromatic hydrocarbons (PAHs) are potent atmospheric pollutants that consist of two or more benzene rings. PAHs have low solubility in water. Their slow dissolution can contaminate large amounts of ground water for long period. They are hydrophobic, non-polar and neutral in nature and are known to have potential mutagenic or carcinogenic activity. In current scenario their removal from the environment, water and soil is still a great challenge and scientists worldwide are engaged to invent and design novel separation technology and decontaminating systems. Various physical, chemical, biological and their combined technologies have been applied to remediate organic-contaminated soils and groundwater. Surfactants play a vital role in the solubilization of these hydrophobic organic compounds. In the present investigation Solubilization capabilities of structurally different gemini surfactants i.e. butanediyl-1,4-bis(dimethyldodecylammonium bromide) (C12-4-C12,2Br−), 2-butanol-1,4-bis (dimethyldodecylammonium bromide) (C12-4(OH)-C12,2Br−), 2,3-butanediol-1,4-bis (dimethyldodecylammonium bromide) (C12-4(OH)2-C12,2Br−) for three polycyclic aromatic hydrocarbons (PAHs); phenanthrene (Phe),fluorene (Fluo) and acenaphthene (Ace) have been studied spectrophotometrically at 300 K. The result showed that the solubility of PAHs increases linearly with increasing surfactant concentration, as an implication of association between the PAHs and micelles. Molar solubilization ratio (MSR), micelle–water partition coefficient (Km) and Gibb's free energy of solubilization (ΔG°s) for PAHs have been determined in aqueous medium. (C12-4(OH)2-C12,2Br−) shows the higher solubilization for all PAHs. Findings of the present investigation may be useful to understand the role of appropriate surfactant system for the solubilization of toxic hydrophobic organic compounds.

Keywords: gemini surfactant, molar solubilization ratio, polycyclic aromatic hydrocarbon, solubilization

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11 The Hydrotrope-Mediated, Low-Temperature, Aqueous Dissolution of Maize Starch

Authors: Jeroen Vinkx, Jan A. Delcour, Bart Goderis

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Complete aqueous dissolution of starch is notoriously difficult. A high-temperature autoclaving process is necessary, followed by cooling the solution below its boiling point. The cooled solution is inherently unstable over time. Gelation and retrogradation processes, along with aggregation-induced by undissolved starch remnants, result in starch precipitation. We recently observed the spontaneous gelatinization of native maize starch (MS) in aqueous sodium salicylate (NaSal) solutions at room temperature. A hydrotropic mode of solubilization is hypothesized. Differential scanning calorimetry (DSC) and polarized optical microscopy (POM) of starch dispersions in NaSal solution were used to demonstrate the room temperature gelatinization of MS at different concentrations of MS and NaSal. The DSC gelatinization peak shifts to lower temperatures, and the gelatinization enthalpy decreases with increasing NaSal concentration. POM images confirm the same trend through the disappearance of the ‘Maltese cross’ interference pattern of starch granules. The minimal NaSal concentration to induce complete room temperature dissolution of MS was found to be around 15-20 wt%. The MS content of the dispersion has little influence on the amount of NaSal needed to dissolve it. The effect of the NaSal solution on the MS molecular weight was checked with HPSEC. It is speculated that, because of its amphiphilic character, NaSal enhances the solubility of MS in water by association with the more hydrophobic MS moieties, much like urea, which has also been used to enhance starch dissolution in alkaline aqueous media. As such small molecules do not tend to form micelles in water, they are called hydrotropes rather than surfactants. A minimal hydrotrope concentration (MHC) is necessary for the hydrotropes to structure themselves in water, resulting in a higher solubility of MS. This is the case for the system MS/NaSal/H₂O. Further investigations into the putative hydrotropic dissolution mechanism are necessary.

Keywords: hydrotrope, dissolution, maize starch, sodium salicylate, gelatinization

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10 Aggregation-Induced-Active Stimuli-Responsive Based Nano-Objects for Wastewater Treatment Application

Authors: Parvaneh Eskandari, Rachel O'Reilly

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In the last years, controlling the self-assembly behavior of stimuli-responsive nano-objects, including micelles, vesicles, worm-like, etc., at different conditions is considered a pertinent challenge in the polymer community. The aim of the project was to synthesize aggregation-induced emission (AIE)-active stimuli-responsive polymeric nano-objects to control the self-assemblies morphologies of the prepared nano-objects. Two types of nanoobjects, micelle and vesicles, including PDMAEMA-b-P(BzMA-TPEMA) [PDMAEMA: poly(N,Ndimethylaminoethyl methacrylate); P(BzMA-TPEMA): poly[benzyl methacrylate-co- tetraphenylethene methacrylate]] were synthesized by using reversible addition−fragmentation chain-transfer (RAFT)- mediated polymerization-induced self-assembly (PISA), which combines polymerization and self-assembly in a single step. Transmission electron microscope and dynamic light scattering (DLS) analysis were used to confirm the formed self-assemblies morphologies. The controlled self-assemblies were applied as nitrophenolic compounds (NPCs) adsorbents from wastewater, thanks to their CO2-responsive part, PDMAEMA. Moreover, the fluorescence-active part of the prepared nano-objects, P(BzMA-TPEMA), played a key role in the detection of the NPCs at the aqueous solution. The optical properties of the prepared nano-objects were studied by UV/Vis and fluorescence spectroscopies. For responsivity investigations, the hydrodynamic diameter and Zeta-potential (ζ-potential) of the sample's aqueous solution were measured by DLS. In the end, the prepared nano-objects were used for the detection and adsorption of different NPCs.

Keywords: aggregation-induced emission polymers, stimuli-responsive polymers, reversible addition−fragmentation chain-transfer polymerization, polymerization-induced self-assembly, wastewater treatment

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9 Surface Functionalized Biodegradable Polymersome for Targeted Drug Delivery

Authors: Susmita Roy, Madhavan Nallani

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In recent years' polymersomes, self-assembled polymeric vesicles emerge from block copolymers, have been widely investigated due to their enhance stability and unique advantageous properties compared to their phospholipid counterpart, liposomes, dendrimers, and micelles. It provides a distinctive platform for advanced therapeutics and the creation of complex (bio) catalytically active systems for research in Nanomedicine and synthetic biology. Inspired by nature, where compartmentalization of biological components is all ubiquitous, we are interested in developing a platform technology of self-assembled multifunctional compartments with applications in areas from targeted drug/gene delivery, biosensing, pharmaceutical to cosmetics. Polymersome surfaces can be a proper choice of derivatization with a controlled amount of functional groups. To achieve site-specific targeting of polymersomes, biological recognition motives can be attached to the polymersomes surface by standard bioconjugation techniques, (like esterification, amidation, thiol-maleimide coupling, click-chemistry routes or other coupling methods). Herein, we are developing easy going, one-step bioconjugation strategies for site-specific surface functionalized biodegradable polymeric and/or polymer-lipid hybrid vesicles for targeted drug delivery. Biodegradable polymer, polycaprolactone-b-polyethylene glycol (PCL-PEG), polylactic acid-b-polyethylene glycol (PLA-PEG) and phospholipid, 1-palmitoyl-2- oleoyl-sn-glycero-3-phosphocholine (POPC) has been widely used for numerous vesicle formulations. Some of these drug-loaded formulations are being tested on mice for controlled release. These surface functionalized polymersomes are also appropriate for membrane protein reconstitution/insertion, antibodies conjugation and various bioconjugation with diverse targeted molecules for controlled drug delivery.

Keywords: drug delivery, membrane protein, polymersome, surface modification

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8 Application of Gold Nanorods in Cancer Photothermaltherapy

Authors: Mehrnaz Mostafavi

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Lung cancer is one of the most harmful forms of cancer. The long-term survival rate of lung cancer patients treated by conventional modalities such as surgical resection, radiation, and chemotherapy remains far from satisfactory. Systemic drug delivery is rarely successful because only a limited amount of the chemotherapeutic drug targets lung tumor sites, even when administered at a high dose. Targeted delivery of drug molecules to organs or special sites is one of the most challenging research areas in pharmaceutical sciences. By developing colloidal delivery systems such as liposomes, micelles and nanoparticles a new frontier was opened for improving drug delivery. Nanoparticles with their special characteristics such as small particle size, large surface area and the capability of changing their surface properties have numerous advantages compared with other delivery systems. Targeted nanoparticle delivery to the lungs is an emerging area of interest.Multimodal or combination therapy represents a promising new method to fight disease. Therefore, a combination of different therapeutic strategies may be the best alternative to improve treatment outcomes for lung cancer. Photothermal therapy was proposed as a novel approach to treatment. In this work, photothermal therapy with gold nanoparticles and near infrared laser (NIR) irradiation was investigated.Four types of small (<100nm), NIR absorbing gold nanoparticles (nanospheres, nanorods) were synthesized using wet chemical methods and characterized by transmission electron microscopy, dynamic light scattering and UV-vis spectroscopy. Their synthesis and properties were evaluated, to determine their feasibility as a photothermal agent for clinical applications. In vitro cellular uptake studies of the nanoparticles into lung cancer cell lines was measured using light scattering microscopy.Small gold nanorods had good photothermal properties and the greatest cellular uptake, and were used in photothermal studies. Under 4W laser irradiation, an increase in temperature of 10°C and decrease in cell viability of up to 80% were obtained.

Keywords: photothermal, therapy, cancer, gold nanorods

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7 Synthesis and Characterization of Polycaprolactone for the Delivery of Rifampicin

Authors: Evelyn Osehontue Uroro, Richard Bright, Jing Yang Quek, Krasimir Vasilev

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Bacterial infections have been a challenge both in the public and private sectors. The colonization of bacteria often occurs in medical devices such as catheters, heart valves, respirators, and orthopaedic implants. When biomedical devices are inserted into patients, the deposition of macromolecules such as fibrinogen and immunoglobin on their surfaces makes it easier for them to be prone to bacteria colonization leading to the formation of biofilms. The formation of biofilms on medical devices has led to a series of device-related infections which are usually difficult to eradicate and sometimes cause the death of patients. These infections require surgical replacements along with prolonged antibiotic therapy, which would incur additional health costs. It is, therefore, necessary to prevent device-related infections by inhibiting the formation of biofilms using intelligent technology. Antibiotic resistance of bacteria is also a major threat due to overuse. Different antimicrobial agents have been applied to microbial infections. They include conventional antibiotics like rifampicin. The use of conventional antibiotics like rifampicin has raised concerns as some have been found to have hepatic and nephrotoxic effects due to overuse. Hence, there is also a need for proper delivery of these antibiotics. Different techniques have been developed to encapsulate and slowly release antimicrobial agents, thus reducing host cytotoxicity. Examples of delivery systems are solid lipid nanoparticles, hydrogels, micelles, and polymeric nanoparticles. The different ways by which drugs are released from polymeric nanoparticles include diffusion-based release, elution-based release, and chemical/stimuli-responsive release. Polymeric nanoparticles have gained a lot of research interest as they are basically made from biodegradable polymers. An example of such a biodegradable polymer is polycaprolactone (PCL). PCL degrades slowly by hydrolysis but is often sensitive and responsive to stimuli like enzymes to release encapsulants for antimicrobial therapy. This study presents the synthesis of PCL nanoparticles loaded with rifampicin and the on-demand release of rifampicin for treating staphylococcus aureus infections.

Keywords: enzyme, Staphylococcus aureus, PCL, rifampicin

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6 Magnetic Biomaterials for Removing Organic Pollutants from Wastewater

Authors: L. Obeid, A. Bee, D. Talbot, S. Abramson, M. Welschbillig

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The adsorption process is one of the most efficient methods to remove pollutants from wastewater provided that suitable adsorbents are used. In order to produce environmentally safe adsorbents, natural polymers have received increasing attention in recent years. Thus, alginate and chitosane are extensively used as inexpensive, non-toxic and efficient biosorbents. Alginate is an anionic polysaccharide extracted from brown seaweeds. Chitosan is an amino-polysaccharide; this cationic polymer is obtained by deacetylation of chitin the major constituent of crustaceans. Furthermore, it has been shown that the encapsulation of magnetic materials in alginate and chitosan beads facilitates their recovery from wastewater after the adsorption step, by the use of an external magnetic field gradient, obtained with a magnet or an electromagnet. In the present work, we have studied the adsorption affinity of magnetic alginate beads and magnetic chitosan beads (called magsorbents) for methyl orange (MO) (an anionic dye), methylene blue (MB) (a cationic dye) and p-nitrophenol (PNP) (a hydrophobic pollutant). The effect of different parameters (pH solution, contact time, pollutant initial concentration…) on the adsorption of pollutant on the magnetic beads was investigated. The adsorption of anionic and cationic pollutants is mainly due to electrostatic interactions. Consequently methyl orange is highly adsorbed by chitosan beads in acidic medium and methylene blue by alginate beads in basic medium. In the case of a hydrophobic pollutant, which is weakly adsorbed, we have shown that the adsorption is enhanced by adding a surfactant. Cetylpyridinium chloride (CPC), a cationic surfactant, was used to increase the adsorption of PNP by magnetic alginate beads. Adsorption of CPC by alginate beads occurs through two mechanisms: (i) electrostatic attractions between cationic head groups of CPC and negative carboxylate functions of alginate; (ii) interaction between the hydrocarbon chains of CPC. The hydrophobic pollutant is adsolubilized within the surface aggregated structures of surfactant. Figure c shows that PNP can reach up to 95% of adsorption in presence of CPC. At highest CPC concentrations, desorption occurs due to the formation of micelles in the solution. Our magsorbents appear to efficiently remove ionic and hydrophobic pollutants and we hope that this fundamental research will be helpful for the future development of magnetically assisted processes in water treatment plants.

Keywords: adsorption, alginate, chitosan, magsorbent, magnetic, organic pollutant

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5 Synthesis of Temperature Sensitive Nano/Microgels by Soap-Free Emulsion Polymerization and Their Application in Hydrate Sediments Drilling Operations

Authors: Xuan Li, Weian Huang, Jinsheng Sun, Fuhao Zhao, Zhiyuan Wang, Jintang Wang

Abstract:

Natural gas hydrates (NGHs) as promising alternative energy sources have gained increasing attention. Hydrate-bearing formation in marine areas is highly unconsolidated formation and is fragile, which is composed of weakly cemented sand-clay and silty sediments. During the drilling process, the invasion of drilling fluid can easily lead to excessive water content in the formation. It will change the soil liquid plastic limit index, which significantly affects the formation quality, leading to wellbore instability due to the metastable character of hydrate-bearing sediments. Therefore, controlling the filtrate loss into the formation in the drilling process has to be highly regarded for protecting the stability of the wellbore. In this study, the temperature-sensitive nanogel of P(NIPAM-co-AMPS-co-tBA) was prepared by soap-free emulsion polymerization, and the temperature-sensitive behavior was employed to achieve self-adaptive plugging in hydrate sediments. First, the effects of additional amounts of AMPS, tBA, and cross-linker MBA on the microgel synthesis process and temperature-sensitive behaviors were investigated. Results showed that, as a reactive emulsifier, AMPS can not only participate in the polymerization reaction but also act as an emulsifier to stabilize micelles and enhance the stability of nanoparticles. The volume phase transition temperature (VPTT) of nanogels gradually decreased with the increase of the contents of hydrophobic monomer tBA. An increase in the content of the cross-linking agent MBA can lead to a rise in the coagulum content and instability of the emulsion. The plugging performance of nanogel was evaluated in a core sample with a pore size distribution range of 100-1000nm. The temperature-sensitive nanogel can effectively improve the microfiltration performance of drilling fluid. Since a combination of a series of nanogels could have a wide particle size distribution at any temperature, around 200nm to 800nm, the self-adaptive plugging capacity of nanogels for the hydrate sediments was revealed. Thermosensitive nanogel is a potential intelligent plugging material for drilling operations in natural gas hydrate-bearing sediments.

Keywords: temperature-sensitive nanogel, NIPAM, self-adaptive plugging performance, drilling operations, hydrate-bearing sediments

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4 Detailed Analysis of Mechanism of Crude Oil and Surfactant Emulsion

Authors: Riddhiman Sherlekar, Umang Paladia, Rachit Desai, Yash Patel

Abstract:

A number of surfactants which exhibit ultra-low interfacial tension and an excellent microemulsion phase behavior with crude oils of low to medium gravity are not sufficiently soluble at optimum salinity to produce stable aqueous solutions. Such solutions often show phase separation after a few days at reservoir temperature, which does not suffice the purpose and the time is short when compared to the residence time in a reservoir for a surfactant flood. The addition of polymer often exacerbates the problem although the poor stability of the surfactant at high salinity remains a pivotal issue. Surfactants such as SDS, Ctab with large hydrophobes produce lowest IFT, but are often not sufficiently water soluble at desired salinity. Hydrophilic co-solvents and/or co-surfactants are needed to make the surfactant-polymer solution stable at the desired salinity. This study focuses on contrasting the effect of addition of a co-solvent in stability of a surfactant –oil emulsion. The idea is to use a co-surfactant to increase stability of an emulsion. Stability of the emulsion is enhanced because of creation of micro-emulsion which is verified both visually and with the help of particle size analyzer at varying concentration of salinity, surfactant and co-surfactant. A lab-experimental method description is provided and the method is described in detail to permit readers to emulate all results. The stability of the oil-water emulsion is visualized with respect to time, temperature, salinity of the brine and concentration of the surfactant. Nonionic surfactant TX-100 when used as a co-surfactant increases the stability of the oil-water emulsion. The stability of the prepared emulsion is checked by observing the particle size distribution. For stable emulsion in volume% vs particle size curve, the peak should be obtained for particle size of 5-50 nm while for the unstable emulsion a bigger sized particles are observed. The UV-Visible spectroscopy is also used to visualize the fraction of oil that plays important role in the formation of micelles in stable emulsion. This is important as the study will help us to decide applicability of the surfactant based EOR method for a reservoir that contains a specific type of crude. The use of nonionic surfactant as a co-surfactant would also increase the efficiency of surfactant EOR. With the decline in oil discoveries during the last decades it is believed that EOR technologies will play a key role to meet the energy demand in years to come. Taking this into consideration, the work focuses on the optimization of the secondary recovery(Water flooding) with the help of surfactant and/or co-surfactants by creating desired conditions in the reservoir.

Keywords: co-surfactant, enhanced oil recovery, micro-emulsion, surfactant flooding

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3 Pickering Dry Emulsion System for Dissolution Enhancement of Poorly Water Soluble Drug (Fenofibrate)

Authors: Nitin Jadhav, Pradeep R. Vavia

Abstract:

Poor water soluble drugs are difficult to promote for oral drug delivery as they demonstrate poor and variable bioavailability because of its poor solubility and dissolution in GIT fluid. Nowadays lipid based formulations especially self microemulsifying drug delivery system (SMEDDS) is found as the most effective technique. With all the impressive advantages, the need of high amount of surfactant (50% - 80%) is the major drawback of SMEDDS. High concentration of synthetic surfactant is known for irritation in GIT and also interference with the function of intestinal transporters causes changes in drug absorption. Surfactant may also reduce drug activity and subsequently bioavailability due to the enhanced entrapment of drug in micelles. In chronic treatment these issues are very conspicuous due to the long exposure. In addition the liquid self microemulsifying system also suffers from stability issues. Recently one novel approach of solid stabilized micro and nano emulsion (Pickering emulsion) has very admirable properties such as high stability, absence or very less concentration of surfactant and easily converts into the dry form. So here we are exploring pickering dry emulsion system for dissolution enhancement of anti-lipemic, extremely poorly water soluble drug (Fenofibrate). Oil moiety for emulsion preparation was selected mainly on the basis of higher solubility of drug. Captex 300 was showed higher solubility for fenofibrate, hence selected as oil for emulsion. With Silica (solid stabilizer); Span 20 was selected to improve the wetting property of it. Emulsion formed by Silica and Span20 as stabilizer at the ratio 2.5:1 (silica: span 20) was found very stable at the particle size 410 nm. The prepared emulsion was further preceded for spray drying and formed microcapsule evaluated for in-vitro dissolution study, in-vivo pharmacodynamic study and characterized for DSC, XRD, FTIR, SEM, optical microscopy etc. The in vitro study exhibits significant dissolution enhancement of formulation (85 % in 45 minutes) as compared to plain drug (14 % in 45 minutes). In-vivo study (Triton based hyperlipidaemia model) exhibits significant reduction in triglyceride and cholesterol with formulation as compared to plain drug indicating increasing in fenofibrate bioavailability. DSC and XRD study exhibit loss of crystallinity of drug in microcapsule form. FTIR study exhibit chemical stability of fenofibrate. SEM and optical microscopy study exhibit spherical structure of globule coated with solid particles.

Keywords: captex 300, fenofibrate, pickering dry emulsion, silica, span20, stability, surfactant

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2 Recent Advances in Research on Carotenoids: From Agrofood Production to Health Outcomes

Authors: Antonio J. Melendez-Martinez

Abstract:

Beyond their role as natural colorants, some carotenoids are provitamins A and may be involved in health-promoting biological actions and contribute to reducing the risk of developing non-communicable diseases, including several types of cancer, cardiovascular disease, eye conditions, skin disorders or metabolic disorders. Given the versatility of carotenoids, the COST-funded European network to advance carotenoid research and applications in agro-food and health (EUROCAROTEN) is aimed at promoting health through the diet and increasing well-being by means. Stakeholders from 38 countries participate in this network, and one of its main objectives is to promote research on little-studied carotenoids. In this contribution, recent advances of our research group and collaborators in the study of two such understudied carotenoids, namely phytoene and phytofluene, the colorless carotenoids, are outlined. The study of these carotenoids is important as they have been largely neglected despite they are present in our diets, fluids, and tissues, and evidence is accumulating that they may be involved in health-promoting actions. More specifically, studies on their levels in diverse tomato and orange varieties were carried out as well as on their potential bioavailability from different dietary sources. Furthermore, the potential effect of these carotenoids on an animal model subjected to oxidative stress was evaluated. The tomatoes were grown in research greenhouses, and some of them were subjected to regulated deficit irrigation, a sustainable agronomic practice. The citrus samples were obtained from an experimental field. The levels of carotenoids were assessed using HPLC according to routine methodologies followed in our lab. Regarding the potential bioavailability (bioaccessibility) studies, different products containing colorless carotenoids, like fruits, juices, were subjected to simulated in vitro digestions, and their incorporation into mixed micelles was assessed. The effect of the carotenoids on oxidative stress was evaluated on the Caenorhabditis elegans model. For that purpose, the worms were subjected to oxidative stress by means of a hydrogen peroxide challenge. In relation to the presence of colorless carotenoids in tomatoes and orange varieties, it was observed that they are widespread in such products and that there are mutants with very high quantities of them, for instance, the Cara Cara or Pinalate mutant oranges. The studies on their bioaccessibility revealed that, in general, phytoene and phytofluene are more bioaccessible than other common dietary carotenoids, probably due to their distinctive chemical structure. About the in vivo antioxidant capacity of phytoene and phytofluene, it was observed that they both exerted antioxidant effects at certain doses. In conclusion, evidence on the importance of phytoene and phytofluene as dietary easily bioavailable and antioxidant carotenoids has been obtained in recent studies from our group, which can be important shortly to innovate in health-promotion through the development of functional foods and related products.

Keywords: carotenoids, health, functional foods, nutrition, phytoene, phytofluene

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1 Magnesium Nanoparticles for Photothermal Therapy

Authors: E. Locatelli, I. Monaco, R. C. Martin, Y. Li, R. Pini, M. Chiariello, M. Comes Franchini

Abstract:

Despite the many advantages of application of nanomaterials in the field of nanomedicine, increasing concerns have been expressed on their potential adverse effects on human health. There is urgency for novel green strategies toward novel materials with enhanced biocompatibility using safe reagents. Photothermal ablation therapy, which exploits localized heat increase of a few degrees to kill cancer cells, has appeared recently as a non-invasive and highly efficient therapy against various cancer types; anyway new agents able to generate hyperthermia when irradiated are needed and must have precise biocompatibility in order to avoid damage to healthy tissues and prevent toxicity. Recently, there has been increasing interest in magnesium as a biomaterial: it is the fourth most abundant cation in the human body, and it is essential for human metabolism. However magnesium nanoparticles (Mg NPs) have had limited diffusion due to the high reduction potential of magnesium cations, which makes NPs synthesis challenging. Herein, we report the synthesis of Mg NPs and their surface functionalization for the obtainment of a stable and biocompatible nanomaterial suitable for photothermal ablation therapy against cancer. We synthesized the Mg crystals by reducing MgCl2 with metallic lithium and exploiting naphthalene as an electron carrier: the lithium–naphthalene complex acts as the real reducing agent. Firstly, the nanocrystal particles were coated with the ligand 12-ethoxy ester dodecanehydroxamic acid, and then entrapped into water-dispersible polymeric micelles (PMs) made of the FDA-approved PLGA-b-PEG-COOH copolymer using the oil-in-water emulsion technique. Lately, we developed a more straightforward methodology by introducing chitosan, a highly biocompatible natural product, at the beginning of the process, simultaneously using lithium–naphthalene complex, thus having a one-pot procedure for the formation and surface modification of MgNPs. The obtained MgNPs were purified and fully characterized, showing diameters in the range of 50-300 nm. Notably, when coated with chitosan the particles remained stable as dry powder for more than 10 months. We proved the possibility of generating a temperature rise of a few to several degrees once MgNPs were illuminated using a 810 nm diode laser operating in continuous wave mode: the temperature rise resulted significant (0-15 °C) and concentration dependent. We then investigated potential cytotoxicity of the MgNPs: we used HN13 epithelial cells, derived from a head and neck squamous cell carcinoma and the hepa1-6 cell line, derived from hepatocellular carcinoma and very low toxicity was observed for both nanosystems. Finally, in vivo photothermal therapy was performed on xenograft hepa1-6 tumor bearing mice: the animals were treated with MgNPs coated with chitosan and showed no sign of suffering after the injection. After 12 hours the tumor was exposed to near-infrared laser light. The results clearly showed an extensive damage to tumor tissue after only 2 minutes of laser irradiation at 3Wcm-1, while no damage was reported when the tumor was treated with the laser and saline alone in control group. Despite the lower photothermal efficiency of Mg with respect to Au NPs, we consider MgNPs a promising, safe and green candidate for future clinical translations.

Keywords: chitosan, magnesium nanoparticles, nanomedicine, photothermal therapy

Procedia PDF Downloads 242