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Search Results (442)

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Keywords = micelle stabilization

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21 pages, 7777 KiB  
Article
Physicochemical and Computational Study of the Encapsulation of Resv-4′-LA and Resv-4′-DHA Lipophenols by Natural and HP-β-CDs
by Ana Belén Hernández-Heredia, Dennis Alexander Silva-Cullishpuma, José Pedro Cerón-Carrasco, Ángel Gil-Izquierdo, Jordan Lehoux, Léo Faion, Céline Crauste, Thierry Durand, José Antonio Gabaldón and Estrella Núñez-Delicado
Int. J. Mol. Sci. 2025, 26(15), 7454; https://doi.org/10.3390/ijms26157454 (registering DOI) - 1 Aug 2025
Abstract
This study investigates the self-assembly and host–guest complexation behaviour of novel resveratrol-based lipophenols (LipoResv)—resveratrol-4′-linoleate (Resv-4′-LA) and resveratrol-4′-docosahexaenoate (Resv-4′-DHA)—with hydroxypropyl-β-cyclodextrins (HP-β-CDs). These amphiphilic molecules display surfactant-like properties, forming micellar aggregates in aqueous media. Fluorescence spectroscopy was used to determine the critical micelle concentration (CMC), [...] Read more.
This study investigates the self-assembly and host–guest complexation behaviour of novel resveratrol-based lipophenols (LipoResv)—resveratrol-4′-linoleate (Resv-4′-LA) and resveratrol-4′-docosahexaenoate (Resv-4′-DHA)—with hydroxypropyl-β-cyclodextrins (HP-β-CDs). These amphiphilic molecules display surfactant-like properties, forming micellar aggregates in aqueous media. Fluorescence spectroscopy was used to determine the critical micelle concentration (CMC), revealing that LipoResv exhibit significantly lower CMC values than their free fatty acids, indicating higher hydrophobicity. The formation of inclusion complexes with HP-β-CDs was evaluated based on changes in CMC values and further confirmed by dynamic light scattering (DLS) and molecular modelling analyses. Resv-4′-LA formed 1:1 complexes (Kc = 720 M−1), while Resv-4′-DHA demonstrated a 1:2 stoichiometry with lower affinity constants (K1 = 17 M−1, K2 = 0.18 M−1). Environmental parameters (pH, temperature, and ionic strength) significantly modulated CMC and binding constants. Computational docking and molecular dynamics simulations supported the experimental findings by revealing the key structural determinants of the host–guest affinity and micelle stabilization. Ligand efficiency (LE) analysis further aligned with the experimental data, favouring the unmodified fatty acids. These results highlight the versatile encapsulation capacity of HP-β-CDs for bioactive amphiphile molecules and support their potential applications in drug delivery and functional food systems. Full article
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21 pages, 5748 KiB  
Article
Potential and Challenges of a Targeted Membrane Pre-Fouling: Process Performance of Milk Protein Fractionation After the Application of a Transglutaminase Treatment of Casein Micelles
by Michael Reitmaier, Ulrich Kulozik and Petra Först
Foods 2025, 14(15), 2682; https://doi.org/10.3390/foods14152682 - 30 Jul 2025
Viewed by 143
Abstract
The covalent cross-linking of caseins by the enzyme transglutaminase (Tgase) stabilizes the structure of casein micelles. In our study, the effects of a pretreatment of skim milk (SM) by Tgase on milk protein fractionation by microfiltration were tested. Tgase was found to induce [...] Read more.
The covalent cross-linking of caseins by the enzyme transglutaminase (Tgase) stabilizes the structure of casein micelles. In our study, the effects of a pretreatment of skim milk (SM) by Tgase on milk protein fractionation by microfiltration were tested. Tgase was found to induce amount-dependent modifications of all milk proteins in SM and a reduction in deposit resistance for laboratory dead-end filtrations of up to 20%. This improvement in process performance could partially be confirmed in pilot-scale cross-flow filtrations of Tgase-pretreated SM and micellar casein solutions (MCC). These comparative trials with untreated retentates under a variation of ΔpTM (0.5–2 bar) at 10 and 50° revealed distinct differences in deposit behavior and achieved the reduction in deposit resistance in a range of 0–20%. The possibility of pre-fouling with enzymatically pretreated MCC prior to SM filtration was also investigated. Under different pre-fouling conditions, practical modes of retentate change, and pre-foulant compositions, a switch to untreated SM consistently resulted in an immediate and major increase in deposit resistance by 50–150%. This was partially related to the change in the ionic environment and the protein fraction. Nevertheless, our results underline the potential of Tgase pretreatment and pre-fouling approaches to alter filtration performance for different applications. Full article
(This article belongs to the Special Issue Membranes for Innovative Bio-Food Processing)
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24 pages, 2320 KiB  
Article
Glucoselipid Biosurfactant Biosynthesis Operon of Rouxiella badensis DSM 100043T: Screening, Identification, and Heterologous Expression in Escherichia coli
by Andre Fahriz Perdana Harahap, Chantal Treinen, Leonardo Joaquim Van Zyl, Wesley Trevor Williams, Jürgen Conrad, Jens Pfannstiel, Iris Klaiber, Jakob Grether, Eric Hiller, Maliheh Vahidinasab, Elvio Henrique Benatto Perino, Lars Lilge, Anita Burger, Marla Trindade and Rudolf Hausmann
Microorganisms 2025, 13(7), 1664; https://doi.org/10.3390/microorganisms13071664 - 15 Jul 2025
Viewed by 390
Abstract
Rouxiella badensis DSM 100043T had been previously proven to produce a novel glucoselipid biosurfactant which has a very low critical micelle concentration (CMC) as well as very good stability against a wide range of pH, temperature, and salinity. In this study, we [...] Read more.
Rouxiella badensis DSM 100043T had been previously proven to produce a novel glucoselipid biosurfactant which has a very low critical micelle concentration (CMC) as well as very good stability against a wide range of pH, temperature, and salinity. In this study, we performed a function-based library screening from a R. badensis DSM 100043T genome library to identify responsible genes for biosynthesis of this glucoselipid. The identified open reading frames (ORFs) were cloned into several constructs in Escherichia coli for gene permutation analysis and the individual products were analyzed using high-performance thin-layer chromatography (HPTLC). Products of interest from positive expression strains were purified and analyzed by liquid chromatography/electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) and nuclear magnetic resonance (NMR) for further structure elucidation. Function-based screening of 5400 clones led to the identification of an operon containing three ORFs encoding acetyltransferase GlcA (ORF1), acyltransferase GlcB (ORF2), and phosphatase/HAD GlcC (ORF3). E. coli pCAT2, with all three ORFs, resulted in the production of identical R. badensis DSM 100043T glucosedilipid with Glu-C10:0-C12:1 as the main congener. ORF2-deletion strain E. coli pAFP1 primarily produced glucosemonolipids, with Glu-C10:0,3OH and Glu-C12:0 as the major congeners, predominantly esterified at the C-2 position of the glucose moiety. Furthermore, fed-batch bioreactor cultivation of E. coli pCAT2 using glucose as the carbon source yielded a maximum glucosedilipid titer of 2.34 g/L after 25 h of fermentation, which is 55-fold higher than that produced by batch cultivation of R. badensis DSM 100043T in the previous study. Full article
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34 pages, 4581 KiB  
Review
Nanoradiopharmaceuticals: Design Principles, Radiolabeling Strategies, and Biomedicine Applications
by Andrés Núñez-Salinas, Cristian Parra-Garretón, Daniel Acuña, Sofía Peñaloza, Germán Günther, Soledad Bollo, Francisco Arriagada and Javier Morales
Pharmaceutics 2025, 17(7), 912; https://doi.org/10.3390/pharmaceutics17070912 - 14 Jul 2025
Viewed by 544
Abstract
Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental [...] Read more.
Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental design principles, radiolabeling techniques, and biomedical applications of nanoradiopharmaceuticals, with a particular focus on their expanding role in precision oncology. It explores key areas, including single- and multi-modal imaging modalities (SPECT, PET), radionuclide therapies involving beta, alpha, and Auger emitters, and integrated theranostic systems. A diverse array of nanocarriers is examined, including liposomes, micelles, albumin nanoparticles, PLGA, dendrimers, and gold, iron oxide, and silica-based platforms, with an assessment of both preclinical and clinical research outcomes. Theranostic nanoplatforms, which integrate diagnostic and therapeutic functions within a single system, enable real-time monitoring and personalized dose optimization. Although some of these systems have progressed to clinical trials, several obstacles remain, including formulation stability, scalable manufacturing, regulatory compliance, and long-term safety considerations. In summary, nanoradiopharmaceuticals represent a promising frontier in personalized medicine, particularly in oncology. By combining diagnostic and therapeutic capabilities within a single nanosystem, they facilitate more individualized and adaptive treatment approaches. Continued innovation in formulation, radiochemistry, and regulatory harmonization will be crucial to their successful routine clinical use. Full article
(This article belongs to the Special Issue Nanosystems for Advanced Diagnostics and Therapy)
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37 pages, 8085 KiB  
Review
Scaling Amphiphilicity with Janus Nanoparticles: A New Frontier in Nanomaterials and Interface Science
by Mirela Honciuc and Andrei Honciuc
Nanomaterials 2025, 15(14), 1079; https://doi.org/10.3390/nano15141079 - 11 Jul 2025
Viewed by 383
Abstract
Janus nanoparticles (JNPs) extend the concept of amphiphilicity beyond classical molecular surfactants into the nanoscale. Amphiphilic behavior is defined by the presence of hydrophobic and hydrophilic moieties within a single molecular structure. Traditionally, such molecular structures are known as surfactants or amphiphiles and [...] Read more.
Janus nanoparticles (JNPs) extend the concept of amphiphilicity beyond classical molecular surfactants into the nanoscale. Amphiphilic behavior is defined by the presence of hydrophobic and hydrophilic moieties within a single molecular structure. Traditionally, such molecular structures are known as surfactants or amphiphiles and are capable of reducing interfacial tension, adsorbing spontaneously at interfaces, stabilizing emulsions and foams, and forming micelles, bilayers, or vesicles. Recent experimental, theoretical, and computational studies demonstrate that these behaviors are scalable to nanostructured colloids such as JNPs. Amphiphilic JNPs, defined by anisotropic surface chemistry on distinct hemispheres, display interfacial activity driven by directional wetting, variable interfacial immersion depth, and strong interfacial anchoring. They can stabilize liquid/liquid and liquid/gas interfaces, and enable templated or spontaneous self-assembly into supra-structures, such as monolayer sheets, vesicles, capsules, etc., both in bulk and at interfaces. Their behavior mimics the “soft” molecular amphiphiles but also includes additional particularities given by their “hard” structure, as well as contributions from capillary, van der Waals, hydrophobic, and shape-dependent forces. This review focuses on compiling the evidence supporting amphiphilicity as a scalable property, discussing how JNPs function as colloidal amphiphiles and how geometry, polarity contrast, interfacial interactions, and environmental parameters influence their behavior. By comparing surfactant behavior and JNP assembly, this work aims to clarify the transferable principles, the knowledge gap, as well as the emergent properties associated with amphiphilic Janus colloids. Full article
(This article belongs to the Special Issue Morphological Design and Synthesis of Nanoparticles (Second Edition))
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24 pages, 1920 KiB  
Review
Advances in Doxorubicin Chemotherapy: Emerging Polymeric Nanocarriers for Drug Loading and Delivery
by Abhi Bhadran, Himanshu Polara, Godwin K. Babanyinah, Sruthy Baburaj and Mihaela C. Stefan
Cancers 2025, 17(14), 2303; https://doi.org/10.3390/cancers17142303 - 10 Jul 2025
Viewed by 639
Abstract
Background/Objectives: Effective and targeted delivery of doxorubicin (DOX) remains a significant challenge due to its dose-limiting cardiotoxicity and systemic side effects. Liposomal formulations like Doxil® have improved tumor targeting and reduced toxicity, but issues such as limited stability, poor release control, and [...] Read more.
Background/Objectives: Effective and targeted delivery of doxorubicin (DOX) remains a significant challenge due to its dose-limiting cardiotoxicity and systemic side effects. Liposomal formulations like Doxil® have improved tumor targeting and reduced toxicity, but issues such as limited stability, poor release control, and insufficient site-specific delivery persist. As a result, there is a growing interest in advanced drug delivery systems, particularly polymeric nanocarriers, which offer biocompatibility, tunable properties, and ease of fabrication. Methods: This review is organized into two key sections. The first section provides a comprehensive overview of DOX, including its mechanism of action, clinical challenges, and the limitations of current chemotherapy approaches. The second section highlights recent advances in polymeric nanocarriers for DOX delivery, focusing on polymeric micelles as well as other promising systems like hydrogels, dendrimers, polymersomes, and polymer–drug conjugates. Results: Initial discussions explore current strategies enhancing DOX’s clinical translation, including methods to address cardiotoxicity and multidrug resistance. The latter part presents recent studies that report improved drug loading efficiency in polymeric nanocarriers through techniques such as core/shell modifications, enhanced hydrophobic interactions, and polymer–drug conjugation. Conclusions: Despite notable progress in polymeric nanocarrier-based DOX delivery, challenges like limited circulation time, immunogenicity, and manufacturing scalability continue to hinder clinical application. Continued innovation in this field is crucial for the development of safe, effective, and clinically translatable polymeric nanocarriers for cancer therapy. Full article
(This article belongs to the Section Cancer Drug Development)
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23 pages, 9287 KiB  
Article
Emulsifying Stability, Digestive Sustained Release, and Cellular Uptake of Alcohol-Soluble Artemisia argyi Flavonoids Were Improved by Glycosylation of Casein Micelles with Oat Glucan
by Ye Zhang, Dongliang Wang, Mengling Peng, Min Yang, Ya Yu, Mengting Yuan, Yanan Liu, Bingyu Zhu, Xiuheng Xue and Juhua Wang
Foods 2025, 14(14), 2435; https://doi.org/10.3390/foods14142435 - 10 Jul 2025
Viewed by 340
Abstract
Flavonoids, widely present in Artemisia argyi (AA), offer potential health benefits but are limited in food applications because of their bitter taste, inadequate absorption, and stability. Casein micelles encapsulation can enhance the flavonoid absorption, stability, and bioactivity. In this study, Artemisia argyi flavonoids [...] Read more.
Flavonoids, widely present in Artemisia argyi (AA), offer potential health benefits but are limited in food applications because of their bitter taste, inadequate absorption, and stability. Casein micelles encapsulation can enhance the flavonoid absorption, stability, and bioactivity. In this study, Artemisia argyi flavonoids (AAFs) were extracted using ultrasound-assisted extraction (UAE) to optimize the process. The glycosylation reaction between casein (CN) micelles and oat β-glucan (OBG) was employed to improve AAF’s emulsifying stability, sustained release during digestion, and cellular uptake. The maximum glycosylation degree of 32.33% was achieved at a CN-to-OBG ratio of 1:2, 120 min browning time, and 95 °C temperature. This glycosylated delivery system enhanced the emulsifying properties of the AAFs, digestive sustained release, and cellular uptake, showing potential as a cross-linking material for fat-soluble substances and medicines. Full article
(This article belongs to the Section Food Physics and (Bio)Chemistry)
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25 pages, 3317 KiB  
Article
Biosurfactant Produced by Bacillus subtilis UCP 1533 Isolated from the Brazilian Semiarid Region: Characterization and Antimicrobial Potential
by Antônio P. da C. Albuquerque, Hozana de S. Ferreira, Yali A. da Silva, Renata R. da Silva, Carlos V. A. de Lima, Leonie A. Sarubbo and Juliana M. Luna
Microorganisms 2025, 13(7), 1548; https://doi.org/10.3390/microorganisms13071548 - 1 Jul 2025
Viewed by 348
Abstract
The increasing resistance of pathogenic microorganisms to antimicrobials has driven the search for safe and sustainable alternatives. In this context, microbial biosurfactants have gained prominence due to their antimicrobial activity, low toxicity, and high stability under extreme conditions. This study presents the production [...] Read more.
The increasing resistance of pathogenic microorganisms to antimicrobials has driven the search for safe and sustainable alternatives. In this context, microbial biosurfactants have gained prominence due to their antimicrobial activity, low toxicity, and high stability under extreme conditions. This study presents the production and characterization of a biosurfactant with antimicrobial potential, obtained from Bacillus subtilis isolated from soil, for application in the control of resistant strains. Bacterial identification was performed using mass spectrometry (MALDI-TOF), confirming it as Bacillus subtilis. The strain B. subtilis UCP 1533 was cultivated using different carbon sources (glucose, soybean oil, residual frying oil, and molasses) and nitrogen sources (ammonium chloride, sodium nitrate, urea, and peptone), with evaluations at 72, 96, and 120 h. The best condition involved a mineral medium supplemented with 2% soybean oil and 0.12% corn steep liquor, resulting in the production of 16 g·L−1 of biosurfactant, with a critical micelle concentration (CMC) of 0.3 g·L−1 and a reduction in water surface tension to 25 mN·m−1. The biosurfactant showed an emulsification index of 100% for used motor oil and ranged from 50% to 100% for different vegetable oils, maintaining stability across a wide range of pH, salinity, and temperature. FT-IR and NMR analyses confirmed its lipopeptide nature and anionic charge. Toxicity tests with Tenebrio molitor larvae showed 100% survival at all the tested concentrations. In phytotoxicity assays, seed germination rates above 90% were recorded for Solanum lycopersicum and Lactuca sativa. Antimicrobial tests revealed inhibitory activity against resistant strains of Escherichia coli and Pseudomonas aeruginosa, as well as against species of the genus Candida (C. glabrata, C. lipolytica, C. bombicola, and C. guilliermondii), highlighting the biosurfactant as a promising alternative in combating antimicrobial resistance (AMR). These results indicate the potential application of this biosurfactant in the development of antimicrobial agents for pharmaceutical formulations and sustainable strategies for phytopathogen control in agriculture. Full article
(This article belongs to the Section Antimicrobial Agents and Resistance)
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20 pages, 5107 KiB  
Article
Controlled Synthesis of N-Doped Hierarchical Porous Carbon Spheres Through Polydopamine for CO2 Adsorption and High-Performance Supercapacitors
by Xiaoqi Jin, Jinlong Ge, Zhong Wu, Linlin Zhu, Mingwen Xiong, Jiahui Qi and Chengxiu Ruan
Molecules 2025, 30(13), 2747; https://doi.org/10.3390/molecules30132747 - 26 Jun 2025
Viewed by 352
Abstract
Hierarchical porous N-doped carbon spheres featuring a combination of micropores, mesopores and macropores as well as tuneable properties were synthesised using dopamine as a carbon precursor and triblock copolymers (F127, P123 and F127/P123 composites) as templates via direct polymerisation-induced self-assembly. The structures and [...] Read more.
Hierarchical porous N-doped carbon spheres featuring a combination of micropores, mesopores and macropores as well as tuneable properties were synthesised using dopamine as a carbon precursor and triblock copolymers (F127, P123 and F127/P123 composites) as templates via direct polymerisation-induced self-assembly. The structures and textures of these materials were characterised using X-ray diffraction, scanning electron microscopy, transmission electron microscopy, N2 adsorption–desorption isotherm analysis, Fourier-transform infrared spectroscopy, Raman spectroscopy and X-ray photoelectron spectroscopy. The sample synthesised at an F127:P123 molar ratio of 1:3 (NCS-FP3) exhibited the highest surface area (463 m2/g) and pore volume (0.27 cm3/g). The hydrophobic/hydrophilic molar ratios of the templates were adjusted to control the morphology of the corresponding micelles and hence the porous structures and morphologies of the carbon spheres, which exhibited high CO2 capture capacities (2.90–3.46 mmol/g at 273 K and 760 mmHg) because of their developed microporous structures and N doping. Additionally, NCS-FP3 exhibited an outstanding electrochemical performance, achieving a high specific capacitance (328.3 F/g at a current density of 0.5 A/g) and outstanding cycling stability (99.2% capacitance retention after 10,000 cycles). These high CO2 capture and electrochemical performances were ascribed to the beneficial effects of pore structures and surface chemistry features. Full article
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26 pages, 8375 KiB  
Article
Water-Soluble Formulations of Curcumin and Eugenol Produced by Spray Drying
by Iskra Z. Koleva, Katya Kamenova, Petar D. Petrov and Christo T. Tzachev
Pharmaceuticals 2025, 18(7), 944; https://doi.org/10.3390/ph18070944 - 23 Jun 2025
Viewed by 561
Abstract
Background/Objectives: In this study, we present a green, scalable platform for the production of water-dispersible powders co-encapsulating the lipophilic bioactives curcumin (Cur) and eugenol (Eug) within the amphiphilic polymer Soluplus® (SP) via low-temperature spray drying. Methods: The amount of Cur [...] Read more.
Background/Objectives: In this study, we present a green, scalable platform for the production of water-dispersible powders co-encapsulating the lipophilic bioactives curcumin (Cur) and eugenol (Eug) within the amphiphilic polymer Soluplus® (SP) via low-temperature spray drying. Methods: The amount of Cur (1%, 5%, and 10%) and Eug (5%, 10%, 15%, and 20%) was varied to achieve single- and double-loaded water-soluble powders with the maximum amount of active substances. The powders containing a higher loading of Cur, 5% and 10% (and Eug), were obtained from water/ethanol mixtures (2:1 and 5:1 v/v ratio), while the formulation with 1% of Cur was spray-dried by using water as a solvent. Results: By leveraging aqueous or aqueous–ethanolic feed systems, we achieved high loading of the bioactive substances—up to 10% Cur and 20% Eug (w/w)—while minimizing organic solvent use. Myo-inositol was incorporated as a stabilizing excipient to modulate particle morphology, improve powder flowability, and enhance redispersibility. Physicochemical characterization revealed nanoscale micellization (53–127 nm), amorphization of both actives as confirmed by XRD and DSC, and the absence of crystalline residue. Encapsulation efficiencies exceeded 95% for Cur and 93% for Eug. Dissolution tests demonstrated a rapid release from the 5% Cur/5% Eug formulation (>85% in 5 min), while higher-loaded single-formulations showed progressively slower release (up to 45 min). Conclusions: This work demonstrates a robust and environmentally responsible encapsulation strategy, suitable for delivering poorly water-soluble phytochemicals with potential applications in oral nutraceuticals and pharmaceutical dosage forms. Full article
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16 pages, 1726 KiB  
Article
Cationic Polymer Micelles as Carriers of Bioactive Sesquiterpene Lactones from Inula Helenium L. for Effective Treatment of Bacterial Biofilms
by Rumena Stancheva, Tsvetozara Damyanova, Tsvetelina Paunova-Krasteva, Ralitsa Veleva, Tanya Topouzova-Hristova, Viktoria Ivanova, Antoaneta Trendafilova, Ivaylo Dimitrov, Stanislav Rangelov and Emi Haladjova
Pharmaceutics 2025, 17(6), 800; https://doi.org/10.3390/pharmaceutics17060800 - 19 Jun 2025
Viewed by 573
Abstract
Objectives: Nanosized polymeric micelles (PMs) with an average size of about 80 nm and moderately positive ζ potential, based on an amphiphilic poly(4-methyl-piperazin-1-yl)-propenone)-b-polylactide (PMPP-PLA) block copolymer, were prepared. They were used as platforms for the delivery of bioactive sesquiterpene lactones from Inula helenium [...] Read more.
Objectives: Nanosized polymeric micelles (PMs) with an average size of about 80 nm and moderately positive ζ potential, based on an amphiphilic poly(4-methyl-piperazin-1-yl)-propenone)-b-polylactide (PMPP-PLA) block copolymer, were prepared. They were used as platforms for the delivery of bioactive sesquiterpene lactones from Inula helenium L. root extract. Methods: The PMs were characterized with good encapsulation efficiency as a maximum value of 72% was reached at a polymer-to-extract mass ratio of 10:1. The loaded micelles exhibited good colloidal stability. An in vitro release was performed showing a burst release profile. The biocompatibility of the resulting PMs was confirmed by assessing their cytotoxic effect on human keratinocytes in vitro by colorimetric assay and flow cytometry. Results: The systems demonstrated the capability to reduce the biomass of pre-formed Gram-positive and Gram-negative bacterial biofilms. Conclusions: The obtained data clearly determine a trend for a strong combined effect between the PMs and the root extract, distinguishing them with an excellent anti-biofilm potential and prospects for future applications in medical practice. Full article
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28 pages, 3006 KiB  
Article
Self-Assembling Amphiphilic ABA Triblock Copolymers of Hyperbranched Polyglycerol with Poly(tetrahydrofuran) and Their Nanomicelles as Highly Efficient Solubilization and Delivery Systems of Curcumin
by Dóra Fecske, György Kasza, Gergő Gyulai, Kata Horváti, Márk Szabó, András Wacha, Zoltán Varga, Györgyi Szarka, Yi Thomann, Ralf Thomann, Rolf Mülhaupt, Éva Kiss, Attila Domján, Szilvia Bősze, Laura Bereczki and Béla Iván
Int. J. Mol. Sci. 2025, 26(12), 5866; https://doi.org/10.3390/ijms26125866 - 19 Jun 2025
Viewed by 598
Abstract
Delivering of hydrophobic drugs by polymeric nanoparticles is an intensively investigated research and development field worldwide due to the insufficient solubility of many existing and potential new drugs in aqueous media. Among polymeric nanoparticles, micelles of biocompatible amphiphilic block copolymers are among the [...] Read more.
Delivering of hydrophobic drugs by polymeric nanoparticles is an intensively investigated research and development field worldwide due to the insufficient solubility of many existing and potential new drugs in aqueous media. Among polymeric nanoparticles, micelles of biocompatible amphiphilic block copolymers are among the most promising candidates for solubilization, encapsulation, and delivery of hydrophobic drugs to improve the water solubility and thus the bioavailability of such drugs. In this study, amphiphilic ABA triblock copolymers containing biocompatible hydrophilic hyperbranched (dendritic) polyglycerol (HbPG) outer and hydrophobic poly(tetrahydrofuran) (PTHF) inner segments were synthesized using amine-telechelic PTHF as a macroinitiator for glycidol polymerization. These hyperbranched–linear–hyperbranched block copolymers form nanosized micelles with 15–20 nm diameter above the critical micelle concentration. Coagulation experiments proved high colloidal stability of the aqueous micellar solutions of these block copolymers against temperature changes. The applicability of block copolymers as drug delivery systems was investigated using curcumin, a highly hydrophobic, water-insoluble, natural anti-cancer agent. High and efficient drug solubilization up to more than 3 orders of magnitude to that of the water solubility of curcumin (>1500-fold) is achieved with the HbPG-PTHF-HbPG block copolymer nanomicelles, locating the drug in amorphous form in the inner PTHF core. Outstanding stability of and sustained curcumin release from the drug-loaded block copolymer micelles were observed. The in vitro bioactivity of the curcumin-loaded nanomicelles was investigated on U-87 glioblastoma cell line, and an optimal triblock copolymer composition was found, which showed highly effective cellular uptake and no toxicity. These findings indicate that the HbPG-PTHF-HbPG triblock copolymers are promising candidates for advanced drug solubilization and delivery systems. Full article
(This article belongs to the Special Issue Design, Synthesis and Applications of Dendrimer Materials)
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57 pages, 5820 KiB  
Review
Surfactant-Enabled Nanocarriers in Breast Cancer Therapy: Targeted Delivery and Multidrug Resistance Reversal
by Ashirwad Jadhav and Karuppiah Nagaraj
Pharmaceutics 2025, 17(6), 779; https://doi.org/10.3390/pharmaceutics17060779 - 13 Jun 2025
Cited by 1 | Viewed by 737
Abstract
Breast cancer remains a leading cause of cancer-related morbidity and mortality among women worldwide. Its treatment is complicated by molecular heterogeneity and the frequent development of multidrug resistance (MDR). Conventional drug delivery approaches are often limited by poor aqueous solubility, rapid systemic clearance, [...] Read more.
Breast cancer remains a leading cause of cancer-related morbidity and mortality among women worldwide. Its treatment is complicated by molecular heterogeneity and the frequent development of multidrug resistance (MDR). Conventional drug delivery approaches are often limited by poor aqueous solubility, rapid systemic clearance, non-specific biodistribution, and off-target toxicity. This review will critically explore the possibility of surfactant-based drug delivery systems (DDSs) in addressing the constraints of standard breast cancer treatments. It focuses on the mechanisms by which surfactants promote solubility, facilitate cellular uptake, and overcome drug resistance, while also analyzing current therapeutic success and future directions. A thorough review of preclinical and clinical investigations was undertaken, focusing on important surfactant-based DDSs such as polymeric micelles, nanoemulsions, liposomes, and self-emulsifying systems (SEDDSs). Mechanistic insights into surfactant functions, such as membrane permeabilization and efflux pump inhibition, were studied alongside delivery systems incorporating ligands and co-loaded medicines. Pluronic® micelles, TPGS-based systems, biosurfactant-stabilized nanoparticles, and lipid-based carrier surfactant platforms improve medication solubility, stability, and delivery. Genexol® are examples of formulations demonstrating effective use and FDA translational potential. These systems now incorporate stimuli-responsive release mechanisms—such as pH, temperature, redox, immuno- and photodynamic treatment—artificial intelligence treatment design, and tailored treatment advancement, and responsive tailoring. Surfactant-enabled DDSs can improve breast cancer care. Innovative approaches for personalized oncology treatment are countered by the enduring challenges of toxicity, regulatory hurdles, and diminished scalability. Full article
(This article belongs to the Special Issue Natural Nanoparticle for Cancer Diagnosis and Treatment, 2nd Edition)
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16 pages, 2637 KiB  
Article
Polyoxyethylene Group-Dependent Surface Properties and Aggregation Behavior in Oleyl-Based Sulfosuccinate Systems
by Ping Li, Zhengwei Zhang, Jie Chai, Yuan Liu, Siqi Han and Peixin Bai
Molecules 2025, 30(11), 2321; https://doi.org/10.3390/molecules30112321 - 26 May 2025
Viewed by 502
Abstract
Three oleyl-based sulfosuccinates with different polyoxyethylene (EO) chain length (MS-OEn, where n = 3, 5, 7) were synthesized, and their structure were confirmed using FT-IR and ¹H NMR analyses. The surfactant’s adsorption properties, aggregation behavior and practical performance were systematically investigated. [...] Read more.
Three oleyl-based sulfosuccinates with different polyoxyethylene (EO) chain length (MS-OEn, where n = 3, 5, 7) were synthesized, and their structure were confirmed using FT-IR and ¹H NMR analyses. The surfactant’s adsorption properties, aggregation behavior and practical performance were systematically investigated. Equilibrium surface tension measurements elucidated the surface adsorption properties such as critical micelle concentration (cmc) values and the corresponding surface tensions at cmc (γcmc). Dynamic surface tension analysis indicated slower adsorption kinetics for surfactants with longer EO chains. Aggregation studies demonstrated that MS-OE3 formed vesicles, whereas no such vesicular structures were observed in the aqueous solutions of MS-OE5 and MS-OE7 at equivalent concentrations. Further, it was observed that foam stability decreased with an increase in EO units, while MS-OE3 exhibited the best wetting ability. Notably, the liquid crystal emulsion formulated with MS-OE7 demonstrated exceptional long-term stability. Full article
(This article belongs to the Section Materials Chemistry)
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23 pages, 1422 KiB  
Review
Harnessing the Power of Nanocarriers to Exploit the Tumor Microenvironment for Enhanced Cancer Therapy
by Bandar Aldhubiab, Rashed M. Almuqbil and Anroop B. Nair
Pharmaceuticals 2025, 18(5), 746; https://doi.org/10.3390/ph18050746 - 19 May 2025
Viewed by 826
Abstract
The tumor microenvironment (TME) has a major role in malignancy and its complex nature can mediate tumor survival, metastasis, immune evasion, and drug resistance. Thus, reprogramming or regulating the immunosuppressive TME has a significant contribution to make in cancer therapy. Targeting TME with [...] Read more.
The tumor microenvironment (TME) has a major role in malignancy and its complex nature can mediate tumor survival, metastasis, immune evasion, and drug resistance. Thus, reprogramming or regulating the immunosuppressive TME has a significant contribution to make in cancer therapy. Targeting TME with nanocarriers (NCs) has been widely used to directly deliver anticancer drugs to control TME, which has revealed auspicious outcomes. TME can be reprogrammed by using a range of NCs to regulate immunosuppressive factors and activate immunostimulatory cells. Moreover, TME can be ameliorated via regulating the redox environment, oxygen content, and pH value of the tumor site. NCs have the capacity to provide site-specific delivery of therapeutic agents, controlled release, enhanced solubility and stability, decreased toxicities, and enhanced pharmacokinetics as well as biodistribution. Numerous NCs have demonstrated their potential by inducing distinct anticancer mechanisms by delivering a range of anticancer drugs in various preclinical studies, including metal NCs, liposomal NCs, solid lipid NCs, micelles, nanoemulsions, polymer-based NCs, dendrimers, nanoclays, nanocrystals, and many more. Some of them have already received US Food and Drug Administration approval, and some have entered different clinical phases. However, there are several challenges in NC-mediated TME targeting, including scale-up of NC-based cancer therapy, rapid clearance of NCs by the mononuclear phagocyte system, and TME heterogeneity. In order to harness the full potential of NCs in tumor treatment, there are several factors that need to be carefully studied, including optimization of drug loading into NCs, NC-associated immunogenicity, and biocompatibility for the successful translation of NC-based anticancer therapies into clinical practice. In this review, a range of NCs and their applications in drug delivery to remodel TME for cancer therapy are extensively discussed. Moreover, findings from numerous preclinical and clinical studies with these NCs are also highlighted. Full article
(This article belongs to the Special Issue Recent Advances in Nanocarriers for Drug Delivery)
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