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1.
Curr Drug Metab ; 21(11): 885-901, 2020.
Article in English | MEDLINE | ID: mdl-33032505

ABSTRACT

BACKGROUND: Surfactants are an important category of additives that are used widely in most of the formulations as solubilizers, stabilizers, and emulsifiers. Current drug delivery systems comprise of numerous synthetic surfactants (such as Cremophor EL, polysorbate 80, Transcutol-P), which are associated with several side effects though used in many formulations. Therefore, to attenuate the problems associated with conventional surfactants, a new generation of surface-active agents is obtained from the metabolites of fungi, yeast, and bacteria, which are termed as biosurfactants. OBJECTIVES: In this article, we critically analyze the different types of biosurfactants, their origin along with their chemical and physical properties, advantages, drawbacks, regulatory status, and detailed pharmaceutical applications. METHODS: 243 papers were reviewed and included in this review. RESULTS: Briefly, Biosurfactants are classified as glycolipids, rhamnolipids, sophorolipids, trehalolipids, surfactin, lipopeptides & lipoproteins, lichenysin, fatty acids, phospholipids, and polymeric biosurfactants. These are amphiphilic biomolecules with lipophilic and hydrophilic ends and are used as drug delivery vehicles (foaming, solubilizer, detergent, and emulsifier) in the pharmaceutical industry. Despite additives, they have some biological activity as well (anti-cancer, anti-viral, anti-microbial, P-gp inhibition, etc.). These biomolecules possess better safety profiles and are biocompatible, biodegradable, and specific at different temperatures. CONCLUSION: Biosurfactants exhibit good biomedicine and additive properties that can be used in developing novel drug delivery systems. However, more research should be driven due to the lack of comprehensive toxicity testing and high production cost which limits their use.


Subject(s)
Lipids , Pharmaceutical Vehicles , Surface-Active Agents , Animals , Humans , Lipids/classification , Lipids/pharmacology , Pharmaceutical Vehicles/classification , Pharmaceutical Vehicles/pharmacology , Surface-Active Agents/classification , Surface-Active Agents/pharmacology
2.
Braz J Microbiol ; 51(2): 691-700, 2020 Jun.
Article in English | MEDLINE | ID: mdl-31612432

ABSTRACT

The use of dispersants in marine environments is a common practice worldwide for oil spill remediation. While the effects of chemical dispersants have been extensively studied, those of biosurfactants, mainly surfactin that is considered one of the most effective surfactants produced by bacteria, have been less considered. We constructed microcosms containing marine water collected from Grumari beach (W_GB, Brazil) and from Schiermonnikoog beach (W_SI, The Netherlands) with the addition of oil (WO), Ultrasperse II plus oil (WOS), surfactin plus oil (WOB), and both dispersants (WS or WB) individually. In these treatments, the composition of bacterial communities and their predictive biodegradation potential were determined over time. High-throughput sequencing of the rrs gene encoding bacterial 16S rRNA revealed that Bacteroidetes (Flavobacteria class) and Proteobacteria (mainly Gammaproteobacteria and Alphaproteobacteria classes) were the most abundant phyla found among the W_GB and W_SI microbiomes, and the relative abundance of the bacterial types in the different microcosms varied based on the treatment applied. Non-metrical multidimensional scaling (NMDS) revealed a clear clustering based on the addition of oil and on the dispersant type added to the GB or SI microcosms, i.e., WB and WOB were separated from WS and WOS in both marine ecosystems studied. The potential presence of diverse enzymes involved in oil degradation was indicated by predictive bacterial metagenome reconstruction. The abundance of predicted genes for degradation of petroleum hydrocarbons increased more in surfactin-treated microcosms than those treated with Ultrasperse II, mainly in the marine water samples from Grumari beach.


Subject(s)
Microbiota , Seawater/microbiology , Surface-Active Agents/metabolism , Water Microbiology , Water Pollutants, Chemical/metabolism , Bacteria/classification , Bacteria/metabolism , Biodegradation, Environmental , Brazil , Metagenome , Petroleum/metabolism , Petroleum Pollution , Seawater/analysis , Surface-Active Agents/classification
3.
J Basic Microbiol ; 59(3): 277-287, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30614549

ABSTRACT

Bioemulsifiers (BE) and biosurfactants (BS) are considered as multifunctional biomolecules of 21st century because of their functional abilities and eco-friendly properties. They are produced by various microorganisms under versatile and extreme environmental conditions. They have tremendous applications in various industries such as petroleum, food, medicine, pharmaceutical, chemical, paper & pulp, textile, and cosmetics. Currently, they are also considered as "green molecules" because of their wide applications in bioremediation of soil. Their importance has been increasing day by day in the global market as they are the natural resources with high-aggregate value. Although, there are numerous reports on BE and BS production by different bacteria, Acinetobacter spp. acquired special attention among all. This is because it is the earliest member known for the production of bioemulsifier. Emulsan and Alasan are the best examples of the commercially used BE produced by Acinetobacter spp. These BE are mainly used in microbial enhanced oil recovery and biodegradation of toxic compounds. This review is focused on BE and BS produced by Acinetobacter spp., their characterization and applications in different fields. This is the first review on genus Acinetobacter which defines independently about different types of BE and BS produced by it. It will also address the need of exploration of these molecules from various sources and their applications for the benefit of mankind and sustainable environment.


Subject(s)
Acinetobacter/metabolism , Emulsifying Agents/metabolism , Surface-Active Agents/metabolism , Acinetobacter/classification , Anti-Infective Agents , Antineoplastic Agents , Biodegradation, Environmental , Biological Control Agents , Detergents , Emulsifying Agents/chemistry , Emulsifying Agents/classification , Free Radical Scavengers , Hydrocarbons/metabolism , Petroleum/metabolism , Surface-Active Agents/chemistry , Surface-Active Agents/classification
4.
Appl Microbiol Biotechnol ; 103(2): 589-602, 2019 Jan.
Article in English | MEDLINE | ID: mdl-30456577

ABSTRACT

Biosurfactants are surface-active molecules that are synthesised non-ribosomally by a wide range of microorganisms including bacteria, yeast and filamentous fungi. The bacterial genus Serratia is gaining international interest, as biosurfactants produced by this genus have emerged as a promising source of antimicrobial, antifouling and antitumour compounds that possess emulsification and surface activity. Various species of Serratia have been identified as biosurfactant producers, including Serratia marcescens, Serratia rubidaea and Serratia surfactantfaciens. Members of the Serratia genus have been reported to principally produce two classes of biosurfactants, namely lipopeptides and glycolipids. Lipopeptides produced by Serratia species include serrawettins and stephensiolides, while identified glycolipids include rubiwettins and rhamnolipids. This review will primarily focus on the classification of biosurfactants produced by Serratia species and the genes and mechanisms involved in the biosynthesis of these biosurfactant compounds. Thereafter, an indication of the primary growth conditions and nutrient composition required for the optimum production of biosurfactants by this genus will be outlined. An overview of the latest advances and potential applications of the biosurfactants produced by Serratia in the medical, pharmaceutical, agricultural and petroleum industries is also provided.


Subject(s)
Glycolipids/chemistry , Glycolipids/metabolism , Lipopeptides/chemistry , Lipopeptides/metabolism , Serratia/metabolism , Surface-Active Agents/chemistry , Surface-Active Agents/metabolism , Anti-Infective Agents/chemistry , Anti-Infective Agents/classification , Anti-Infective Agents/metabolism , Antineoplastic Agents/chemistry , Antineoplastic Agents/classification , Antineoplastic Agents/metabolism , Glycolipids/classification , Lipopeptides/classification , Surface-Active Agents/classification
5.
Cutan Ocul Toxicol ; 37(2): 103-111, 2018 Jun.
Article in English | MEDLINE | ID: mdl-28693384

ABSTRACT

AIM: To evaluate eye irritation potential of palm-based methyl ester sulphonates (MES) of different chain lengths; C12, C14, C16, C16:18. METHODS: The Bovine Corneal Opacity and Permeability test method (BCOP), OECD Test Guideline 437, was used as an initial step to study the inducing effect of palm-based MES on irreversible eye damage. The second assessment involved the use of reconstructed human corneal-like epithelium test method, OECD Test Guideline 492 using SkinEthic™ Human Corneal Epithelium to study the potential effect of palm-based MES on eye irritancy. The palm-based MES were prepared in 10% solution (w/v) in deionized water and tested as a liquid and surfactant test substances whereby both test conducted according to the liquid/surfactant treatment protocol. RESULTS: The preliminary BCOP results showed that palm-based MES; C12, C14, C16, C16:18 were not classified as severe eye irritants test substances with in vitro irritancy score between 3 and the threshold level of 55. The second evaluation using SkinEthic™ HCE model showed that palm-based MES; C12, C14, C16, C16:18 and three commercial samples were potentially irritants to the eyes with mean tissue viability ≤ 60% and classified as Category 2 according to United Nations Globally Harmonized System of Classification and Labelling of Chemicals. However, there are some limitations of the proposed ocular irritation classification of palm-based MES due to insolubility of long chain MES in 10% solution (w/v) in deionized water. CONCLUSION: Therefore, future studies to clarify the eye irritation potential of the palm-based MES will be needed, and could include; methods to improve the test substance solubility, use of test protocol for solids, and/or inclusion of a benchmark anionic surfactant, such as sodium dodecyl sulphate within the study design.


Subject(s)
Cornea/drug effects , Irritants/toxicity , Palm Oil , Sulfonic Acids/toxicity , Surface-Active Agents/toxicity , Animal Testing Alternatives , Animals , Cattle , Cornea/metabolism , Cornea/pathology , Corneal Opacity , Humans , In Vitro Techniques , Irritants/classification , Permeability , Sulfonic Acids/classification , Surface-Active Agents/classification
6.
Int J Pharm ; 490(1-2): 146-54, 2015 Jul 25.
Article in English | MEDLINE | ID: mdl-26002566

ABSTRACT

The application of self-nanoemulsified drug delivery system (SNEDDS) to improve bioavailability of diacerein (D) has been hampered by its large dose and limited solubility. This work aimed to prepare diacerein loaded self nanoemulsifying self nanosuspension (D-SNESNS) containing high drug load. D-SNESNS was prepared by homogenizing D into Maisine™-based SNEDDS that gave the highest drug solubility. D-SNESNS was evaluated for particle size, zeta potential and in vitro dissolution. Significant increase of D solubility was observed from D-SNESNS (∼ 309 µg/mL) than traditional SNEDDS (∼162µg/mL) due to the spontaneous simultaneous formation of nanoemulsion and nanosuspension (top-down approach). When exposed to water with mild agitation, the drug microparticles in D-SNESNS are temporarily surrounded by unsaturated aqueous layer (containing optimum concentrations of surfactant and co-solvent) that facilitates the erosion of the suspended drug particles into nanosized ones. Nanoemulsion-based nanosuspension (NENS) was confirmed using transmission electron microscopy and particle size analysis. D-SNESNS equivalent to 50mg D exhibited complete and very rapid dissolution after 15 min in phosphate buffer pH 6.8 due to the existence of D as solubilized molecules inside nanoemulsion globules and nanosized suspended drug particles forming D-NENS. The relative bioavailabilities of rhein from D-SNESNS in rats with normal and blocked chylomicron flow were about 210% and 164%, respectively in comparison to aqueous D suspension. The significant increase in the dissolution, portal absorption and lymphatic delivery of D propose that SNESNS could be promising to improve oral bioavailability of poorly water soluble drugs that have limited drug load in SNEDDS.


Subject(s)
Anthraquinones/chemistry , Anthraquinones/pharmacokinetics , Emulsions/chemistry , Emulsions/pharmacokinetics , Nanoparticles/chemistry , Suspensions/chemistry , Suspensions/pharmacokinetics , Administration, Oral , Animals , Anthraquinones/administration & dosage , Biological Availability , Chemistry, Pharmaceutical/methods , Drug Carriers/administration & dosage , Drug Carriers/chemistry , Drug Delivery Systems/methods , Emulsions/administration & dosage , Male , Nanoparticles/administration & dosage , Particle Size , Rats , Rats, Wistar , Solubility , Surface-Active Agents/administration & dosage , Surface-Active Agents/chemistry , Surface-Active Agents/classification , Suspensions/administration & dosage
7.
Eur J Pharm Biopharm ; 94: 152-9, 2015 Aug.
Article in English | MEDLINE | ID: mdl-26004819

ABSTRACT

Structural traits of permeation enhancers are important determinants of their capacity to promote enhanced drug absorption. Therefore, in order to obtain a better understanding of structure-activity relationships for permeation enhancers, a Quantitative Structural Activity Relationship (QSAR) model has been developed. The random forest-QSAR model was based upon Caco-2 data for 41 surfactant-like permeation enhancers from Whitehead et al. (2008) and molecular descriptors calculated from their structure. The QSAR model was validated by two test-sets: (i) an eleven compound experimental set with Caco-2 data and (ii) nine compounds with Caco-2 data from literature. Feature contributions, a recent developed diagnostic tool, was applied to elucidate the contribution of individual molecular descriptors to the predicted potency. Feature contributions provided easy interpretable suggestions of important structural properties for potent permeation enhancers such as segregation of hydrophilic and lipophilic domains. Focusing on surfactant-like properties, it is possible to model the potency of the complex pharmaceutical excipients, permeation enhancers. For the first time, a QSAR model has been developed for permeation enhancement. The model is a valuable in silico approach for both screening of new permeation enhancers and physicochemical optimisation of surfactant enhancer systems.


Subject(s)
Computer Simulation , Intestinal Absorption/drug effects , Intestinal Mucosa/drug effects , Models, Chemical , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Caco-2 Cells , Electric Impedance , Humans , Intestinal Mucosa/metabolism , Molecular Structure , Permeability , Quantitative Structure-Activity Relationship , Reproducibility of Results , Surface-Active Agents/classification , Technology, Pharmaceutical/methods
8.
Biopolymers ; 104(3): 129-47, 2015 May.
Article in English | MEDLINE | ID: mdl-25808118

ABSTRACT

Lipopeptides are microbial surface active compounds produced by a wide variety of bacteria, fungi, and yeast. They are characterized by high structural diversity and have the ability to decrease the surface and interfacial tension at the surface and interface, respectively. Surfactin, iturin, and fengycin of Bacillus subtilis are among the most popular lipopeptides. Lipopepetides can be applied in diverse domains as food and cosmetic industries for their emulsification/de-emulsification capacity, dispersing, foaming, moisturizing, and dispersing properties. Also, they are qualified as viscosity reducers, hydrocarbon solubilizing and mobilizing agents, and metal sequestering candidates for application in environment and bioremediation. Moreover, their ability to form pores and destabilize biological membrane permits their use as antimicrobial, hemolytic, antiviral, antitumor, and insecticide agents. Furthermore, lipopeptides can act at the surface and can modulate enzymes activity permitting the enhancement of the activity of certain enzymes ameliorating microbial process or the inhibition of certain other enzymes permitting their use as antifungal agents. This article will present a detailed classification of lipopeptides biosurfactant along with their producing strain and biological activities and will discuss their functional properties and related applications.


Subject(s)
Bacillus subtilis/chemistry , Bacterial Proteins/chemistry , Bacterial Proteins/classification , Lipopeptides/chemistry , Lipopeptides/classification , Surface-Active Agents/chemistry , Surface-Active Agents/classification , Animals , Humans
9.
J Mater Sci Mater Med ; 25(12): 2677-89, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25091188

ABSTRACT

Bone tissue engineering literature conveys investigations regarding biodegradable polymers where bioactive inorganic materials are added either before or after electrospinning process. The goal is to mimic the composition of bone and enhance the biocompatibility of the materials. Yet, most polymeric materials are hydrophobic in nature; therefore, their surfaces are not favorable for human cellular adhesion. In this sense, modifications of the hydrophobic surface of electrospun polymer fibers with hydrophilic and bioactive nanoparticles are beneficial. In this work, dispersion of hydroxyapatite (HAp), which is similar to the mineral component of natural bone, within biodegradable and biocompatible polymer poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) with the aid of a surfactant has been investigated. Non-ionic TWEEN20 and 12-hydroxysteric acid (HSA), cationic dodecyl trimethyl ammonium bromide (DTAB) and anionic sodium deoxycholate and sodium dodecyl sulfate (SDS) surfactants were used for comparison in order to prepare stable and homogenous nanocomposite suspensions of HAp/PHBV for the electrospinning process. Continuous and uniform composite nanofibers were generated successfully within a diameter range of 400-1,000 nm by the mediation of all surfactant types. Results showed that incorporation of HAp and any of the surfactant types strongly activates the precipitation rate of the apatite-like particles and decreases percent crystallinity of the HAp/PHBV mats. Mineralization was greatly enhanced on the fibers produced by using DTAB, HSA, and especially SDS on where also osteoblastic metabolic activity was similarly increased. The produced HAp/PHBV nanofibrous composite scaffolds would be a promising candidate as an osteoconductive bioceramic/polymer composite material for tissue engineering applications.


Subject(s)
Biocompatible Materials/chemical synthesis , Durapatite/chemistry , Nanofibers/chemistry , Osteoblasts/cytology , Polyesters/chemistry , Surface-Active Agents/chemistry , Tissue Scaffolds , 3T3 Cells , Animals , Bone Substitutes/chemical synthesis , Cell Differentiation/physiology , Electroplating/methods , Equipment Design , Equipment Failure Analysis , Materials Testing , Mice , Nanocomposites/chemistry , Nanocomposites/ultrastructure , Nanofibers/ultrastructure , Osteoblasts/physiology , Osteogenesis/physiology , Rotation , Surface-Active Agents/classification
10.
Ying Yong Sheng Tai Xue Bao ; 24(8): 2319-24, 2013 Aug.
Article in Chinese | MEDLINE | ID: mdl-24380354

ABSTRACT

By using the standard test methods in Experimental Guideline for Environmental Safety Evaluation of Chemical Pesticide to aquatic organisms, a comparative study was conducted on the acute toxicity of 39 nonionic, 6 anionic, and 3 cationic surfactants to Daphnia magna. The acute toxicity of three cationic surfactants 1427, 1227 and C8-10 to D. magna belonged to virulent level, and the toxicity of 1427 was the highest, with the EC50 value being 0.97 x 10(-2) mg x L(-1). The acute toxicity of nonionic surfactants polyoxyethylene ether castor oil EL, Tween, and Span emulsifiers belonged to low level, but the toxicity of alkylphenol polyoxyethylene ether and fatty alcohol polyoxyethylene ether surfactants was relatively high, of which, AEO-7 and AEO-5 displayed high toxicity, with the EC50 value being 0.82 and 0.97 mg x L(-1), respectively. In these surfactants, the more liposolubility, the higher the toxicity was. Most of the anionic surfactants were medium in toxicity, but the acute toxicity of NNO belonged to high toxicity, with the EC50 value being 0.17 mg x L(-1).


Subject(s)
Daphnia/drug effects , Pesticides/toxicity , Surface-Active Agents/toxicity , Animals , Pesticides/classification , Surface-Active Agents/classification , Toxicity Tests, Acute
11.
Polim Med ; 42(1): 17-27, 2012.
Article in English | MEDLINE | ID: mdl-22783729

ABSTRACT

There are many methods to increase solubility of a substance. These include, inter alia, preparation of solid dispersions, i.e. eutectic mixtures, solid solutions, glassy solutions and suspensions. When compared to the individual constituents prior to dispersion formation solid dispersion components are better soluble in water. Therefore, solid solutions became one of the most promising ways to modify solubility, ensuring improved bioavailability and consequently therapeutic efficacy of a substance. In this part of the publication solid dispersions were classified and described in regard to their properties and preparation methods, i.e. melting method, melt evaporation and melt extrusion methods, lyophilisation technique, melt agglomeration process as well as SCF technology and electrospinning.


Subject(s)
Chemistry, Pharmaceutical/methods , Administration, Oral , Biological Availability , Freeze Drying/methods , Solubility , Surface-Active Agents/chemistry , Surface-Active Agents/classification , Suspensions/chemistry , Suspensions/classification
12.
PLoS One ; 6(11): e24139, 2011.
Article in English | MEDLINE | ID: mdl-22125591

ABSTRACT

The omnipresent group of pesticide adjuvants are often referred to as "inert" ingredients, a rather misleading term since consumers associate this term with "safe". The upcoming new EU regulation concerning the introduction of plant protection products on the market (EC1107/2009) includes for the first time the demand for information on the possible negative effects of not only the active ingredients but also the used adjuvants. This new regulation requires basic toxicological information that allows decisions on the use/ban or preference of use of available adjuvants. In this study we obtained toxicological relevant information through a multiple endpoint reporter assay for a broad selection of commonly used adjuvants including several solvents (e.g. isophorone) and non-ionic surfactants (e.g. ethoxylated alcohols). The used assay allows the toxicity screening in a mechanistic way, with direct measurement of specific toxicological responses (e.g. oxidative stress, DNA damage, membrane damage and general cell lesions). The results show that the selected solvents are less toxic than the surfactants, suggesting that solvents may have a preference of use, but further research on more compounds is needed to confirm this observation. The gene expression profiles of the selected surfactants reveal that a phenol (ethoxylated tristyrylphenol) and an organosilicone surfactant (ethoxylated trisiloxane) show little or no inductions at EC(20) concentrations, making them preferred surfactants for use in different applications. The organosilicone surfactant shows little or no toxicity and good adjuvant properties. However, this study also illustrates possible genotoxicity (induction of the bacterial SOS response) for several surfactants (POEA, AE, tri-EO, EO FA and EO NP) and one solvent (gamma-butyrolactone). Although the number of compounds that were evaluated is rather limited (13), the results show that the used reporter assay is a promising tool to rank commonly used agricultural adjuvants based on toxicity and toxic mode of action data.


Subject(s)
Escherichia coli/drug effects , Gene Expression Regulation, Bacterial/drug effects , Solvents/toxicity , Surface-Active Agents/toxicity , Analysis of Variance , Dose-Response Relationship, Drug , Escherichia coli/genetics , Escherichia coli/growth & development , Escherichia coli Proteins/genetics , Gene Expression Profiling , Inhibitory Concentration 50 , Microbial Viability/drug effects , Microbial Viability/genetics , Solvents/classification , Surface-Active Agents/classification , Toxicity Tests/methods
13.
Adv Colloid Interface Sci ; 166(1-2): 60-86, 2011 Aug 10.
Article in English | MEDLINE | ID: mdl-21652020

ABSTRACT

During our investigations of two-phase flow in long hydrophobic minitubes and capillaries, we have observed transformation of the main rivulet into different new hydrodynamic modes with the use of different kinds of surfactants. The destabilization of rivulet flow at air velocities <80 m/s occurs primarily due to the strong branching off of sub-rivulets from the main rivulet during the downstream flow in the tube. The addition of some surfactants of not-so-high surface activity was found to increase the frequency of sub-rivulet formation and to suppress the Rayleigh and sinuous instabilities of the formed sub-rivulets. Such instabilities result in subsequent fragmentation of the sub-rivulets and in the formation of linear or sinuous arrays of sub-rivulet fragments (SRFs), which later transform into random arrays of SRFs. In the downstream flow, SRFs further transform into large sliding cornered droplets and linear droplet arrays (LDAs), a phenomenon which agrees with recent theories. At higher surface activity, suppression of the Rayleigh instability of sub-rivulets with surfactants becomes significant, which prevents sub-rivulet fragmentation, and only the rivulet and sub-rivulets can be visualized in the tube. At the highest surface activity, the bottom rivulet transforms rapidly into an annular liquid film. The surfactant influence on the behavior of the rivulets in minitubes is incomparably stronger than the classic example of the known surfactant stabilizing influence on a free jet. The evolution of a rivulet in the downstream flow inside a long minitube includes the following sequence of hydrodynamic modes/patterns: i) single rivulet; ii) rivulet and sub-rivulets; and iii) rivulet, sub-rivulets, sub-rivulet fragments, cornered droplets, linear droplet arrays, linear arrays of sub-rivulet fragments and annular film. The formation of these many different hydrodynamic patterns downstream is in drastic contrast with the known characteristics of two-phase flow, which demonstrates one mode for the entire tube length. Recent achievements in fluid mechanics regarding the stability of sliding thin films and in wetting dynamics have allowed us to interpret many of our findings. However, the most important phenomenon of the surfactant influence on sub-rivulet formation remains poorly understood. To achieve further progress in this new area, an interdisciplinary approach based on the use of methods of two-phase flow, wetting dynamics and interfacial rheology will be necessary.


Subject(s)
Hydrodynamics , Surface-Active Agents/chemistry , Air , Computer Simulation , Hydrophobic and Hydrophilic Interactions , Image Processing, Computer-Assisted , Surface Properties , Surface-Active Agents/classification
14.
Acta Pharm Hung ; 81(4): 151-63, 2011.
Article in Hungarian | MEDLINE | ID: mdl-22329302

ABSTRACT

Surface active agents can be classified 60 years ago with the introduction of the HLB system. The characterization of emulgents allowed their common use in the practice. The objective of the review is to summarize the research in the field of surface active agents and HLB-value. The basic principles and relationships related to HLB are detailed such as the predicting and experimental methods for the determination, as well as the achievements of development and applications of surface active agents.


Subject(s)
Emulsifying Agents , Technology, Pharmaceutical , Emulsifying Agents/classification , Mathematical Computing , Surface-Active Agents/classification , Technology, Pharmaceutical/methods
15.
J Pharm Pharmacol ; 62(11): 1622-36, 2010 Nov.
Article in English | MEDLINE | ID: mdl-21039546

ABSTRACT

OBJECTIVES: The aim of this review is to highlight relevant considerations when implementing a rational strategy for the development of lipid and surfactant based drug delivery system and to discuss shortcomings and challenges to the current classification of these delivery systems. We also aim to offer suggestions for an improved classification system that will accommodate lipid based formulations that are not currently accommodated in the lipid formulation classification system. KEY FINDINGS: When categorising lipid and surfactant based drug delivery systems, the current Lipid Formulations Classifications System is a useful tool. However, it does not apply to all marketed lipid and surfactant systems or those reported in research papers. A more profound understanding of the functionalities of lipids and surfactants and their role in emulsion formation will enable a rational development strategy and will create the basis for a revised classification system encompassing all employed lipid and surfactant drug delivery systems. SUMMARY: The ever-increasing number of poorly soluble compounds in drug discovery and development calls for the serious need for effective and affordable drug delivery strategies that will enhance bioavailability and decrease variability. Lipid and surfactant based drug delivery systems offer these advantages; however, the development of these systems requires proper understanding of the physicochemical nature of the compound as well as the lipid excipients and gastrointestinal digestion. One major challenge of lipid excipients and delivery systems is the varying range of compounds they contain. This has contributed to the challenge of proper characterisation and evaluation of these delivery systems, their stability, classification and regulatory issues, which consequently have affected the number of these formulations that eventually reach the market. Suggestions as to proper classification of these delivery systems based on their main lipid component and recommended use are put forward. The prospect of these delivery systems looks promising.


Subject(s)
Drug Delivery Systems , Lipids/chemistry , Pharmaceutical Preparations/administration & dosage , Surface-Active Agents/chemistry , Administration, Oral , Biological Availability , Drug Delivery Systems/classification , Emulsions/chemistry , Emulsions/classification , Lipids/classification , Pharmaceutical Preparations/chemistry , Solubility , Surface-Active Agents/classification , Technology, Pharmaceutical/methods
16.
Adv Exp Med Biol ; 672: 54-64, 2010.
Article in English | MEDLINE | ID: mdl-20545273

ABSTRACT

Biosurfactant or microbial surfactants produced by microbes are structurally diverse and heterogeneous groups of surface-active amphipathic molecules. They are capable of reducing surface and interfacial tension and have a wide range of industrial and environmental applications. The present chapter reviews the biochemical properties of different classes of microbial surfactants and their potential application in different industrial sectors.


Subject(s)
Biological Products/chemistry , Surface-Active Agents/chemistry , Agriculture , Biological Products/classification , Detergents/chemistry , Environmental Restoration and Remediation , Food Industry , Industry , Molecular Biology , Pesticides/chemistry , Petroleum , Surface-Active Agents/classification
17.
Adv Exp Med Biol ; 672: 102-20, 2010.
Article in English | MEDLINE | ID: mdl-20545277

ABSTRACT

Surfactants are the amphiphilic molecules that tend to alter the interfacial and surface tension. The fundamental property related to the structure of surfactant molecules is their self-aggregation resulting in the formation of association colloids. Apart from the packing of these molecules into closed structures, the structural network also results in formation of extended bilayers, which are thermodynamically stable and lead to existence of biological membranes and vesicles. From biological point of view the development of new knowledge and techniques in the area of vesicles, bilayers and multiplayer membranes and their polymerizable analogue provide new opportunities for research in the respective area. 'Green Surfactants' or the biologically compatible surfactants are in demand to replace some of the existing surfactants and thereby reduce the environmental impact, in general caused by classic surfactants. In this context, the term 'natural surfactants or biosurfactants' is often used to indicate the natural origin of the surfactant molecules. Most important aspect of biosurfactants is their environmental acceptability, because they are readily biodegradable and have low toxicity than synthetic surfactants. Some of the major applications of biosurfactants in pollution and environmental control are microbial enhanced oil recovery, hydrocarbon degradation, hexa-chloro cyclohexane (HCH) degradation and heavy-metal removal from contaminated soil. In this chapter, we tried to make a hierarchy from vital surfactant molecules toward understanding their behavioral aspects and application potential thereby ending into the higher class of broad spectrum 'biosurfactants'. Pertaining to the budding promise offered by these molecules, the selection of the type and size of each structural moiety enables a delicate balance between surface activity and biological function and this represents the most effective approach of harnessing the power of molecular self-assembly.


Subject(s)
Biological Products/chemistry , Biomimetic Materials/chemistry , Surface-Active Agents/chemistry , Animals , Biodegradation, Environmental , Biological Products/classification , Biological Products/toxicity , Biomimetic Materials/classification , Colloids/chemistry , Environmental Restoration and Remediation , Humans , Surface-Active Agents/classification , Surface-Active Agents/toxicity
18.
Adv Exp Med Biol ; 672: 236-49, 2010.
Article in English | MEDLINE | ID: mdl-20545287

ABSTRACT

Biosurfactants are surface-active compounds from biological sources, usually extracellular, produced by bacteria, yeast or fungi. Research on biological surfactant production has grown significantly due to the advantages they present over synthetic compounds such as biodegradability, low toxicity, diversity of applications and functionality under extreme conditions. Although the majority of microbial surfactants have been reported in bacteria, the pathogenic nature of some producers restricts the wide application of these compounds. A growing number of aspects related to the production of biosurfactants from yeasts have been the topic of research during the last decade. Given the industrial importance of yeasts and their potential to biosurfactant production, the goal of this chapter is to review the biosurfactants identified up to present, focusing the relevant parameters that influence biosurfactant production by yeasts and its characteristics, revealing the potential of application of such compounds in the industrial field and presenting some directions for the future development of this area, taking into account the production costs.


Subject(s)
Biological Products/biosynthesis , Surface-Active Agents/chemistry , Yeasts/metabolism , Biological Products/chemistry , Biological Products/classification , Carbon/metabolism , Culture Media , Kinetics , Nitrogen/metabolism , Surface-Active Agents/classification
19.
Biochemistry ; 48(49): 11606-8, 2009 Dec 15.
Article in English | MEDLINE | ID: mdl-19908902

ABSTRACT

Bolaamphiphile-class surfactants composed of two hydrophilic (maltoside) headgroups connected by long saturated alkyl chains were tested for their ability to stabilize a solubilized membrane protein, Escherichia coli diacylglycerol kinase (DAGK), and to sustain its native function. Members of this "Bis-MALT-C(18-28)" series were poor solubilizers of DAGK in the absence of conventional detergent. However, mixed micelles of the bolaamphiphiles with either dodecylphosphocholine or beta-n-decyl maltoside were more effective and enhanced DAGK's thermal stability relative to corresponding detergent-only conditions. Moreover, certain bolaamphiphiles were seen to be lipidlike by providing partial activation of DAGK's catalytic activity. Finally, addition of bolaamphiphiles to micellar NMR samples of DAGK did not result in a degradation of spectral quality, indicating their compatibility with high-resolution structural studies. To the best of our knowledge, this work represents the first documentation of the potential of bolaamphiphile-class surfactants for use in biochemical and biophysical studies of MPs.


Subject(s)
Diacylglycerol Kinase/chemistry , Furans/chemistry , Furans/classification , Membrane Proteins/chemistry , Pyridones/chemistry , Pyridones/classification , Surface-Active Agents/chemistry , Surface-Active Agents/classification , Diacylglycerol Kinase/physiology , Escherichia coli Proteins/chemistry , Escherichia coli Proteins/physiology , Membrane Proteins/physiology , Micelles , Protein Stability , Solubility , Solutions , Thermodynamics
20.
J Colloid Interface Sci ; 335(2): 242-9, 2009 Jul 15.
Article in English | MEDLINE | ID: mdl-19403142

ABSTRACT

The effect of surfactants on the solubility of a new phosphate salt of carvedilol was investigated at different biorelevent pH to evaluate their solubilization capacity. Solutions of different classes of surfactants viz., anionic-sodium dodecyl sulfate (SDS) and sodium taurocholate (STC), cationic-cetyltrimethylammonium bromide (CTAB) and non-ionic-Tween 80 (T80) were prepared in the concentration range of 5-35 mmol dm(-3) in buffer solutions of pH 1.2, 3.0, 4.5, 5.8, 6.8 and 7.2. The solubility data were used to calculate the solubilization characteristics viz. molar solubilization capacity, water micelle partition coefficient, free energy of solubilization and binding constant. Solubility enhancement in basic pH was in following order: CTAB>T80>SDS>STC. CTAB and T80 showed remarkable solubility enhancement in acidic pH as well. Among the anionic surfactants, solubility in acidic medium was retarded except at pH 1.2 in case of SDS. Cationic and non-ionic surfactants were found to be suitable for enhancing the solubility of CP which can be employed for maintaining the in vitro sink condition in the basic dissolution medium. While anionic surfactants showed solubility retardant behavior which may be exploited in increasing the drug entrapment efficiency of a colloidal drug delivery system formulated by emulsification technique.


Subject(s)
Carbazoles/chemistry , Hydrogen-Ion Concentration , Propanolamines/chemistry , Surface-Active Agents/chemistry , Buffers , Carvedilol , Solubility , Surface-Active Agents/classification
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