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Keywords = self-emulsifying system

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13 pages, 3810 KB  
Article
Solar-Driven Selective Benzyl Alcohol Oxidation in Pickering Emulsion Stabilized by CNTs/GCN Hybrids Photocatalyst
by Yunyi Han, Yuwei Hou, Xuezhong Gong, Yu Zhang, Meng Wang, Pekhyo Vasiliy Ivanovich, Meili Guan and Jianguo Tang
Catalysts 2025, 15(8), 753; https://doi.org/10.3390/catal15080753 - 7 Aug 2025
Viewed by 511
Abstract
Herein, a bi-functional composite photocatalyst was synthesized by integrating carbon nanotubes (CNTs) and graphitic carbon nitride (GCN) via a facile electrostatic self-assembly strategy. The resulting CNTs/GCN composite served dual roles as both a solid emulsifier and a photocatalyst, enabling highly efficient photocatalytic benzyl [...] Read more.
Herein, a bi-functional composite photocatalyst was synthesized by integrating carbon nanotubes (CNTs) and graphitic carbon nitride (GCN) via a facile electrostatic self-assembly strategy. The resulting CNTs/GCN composite served dual roles as both a solid emulsifier and a photocatalyst, enabling highly efficient photocatalytic benzyl alcohol oxidation within a Pickering emulsion system. The relationship between emulsion droplet size and solid emulsifier dosage was investigated and optimized. The enhanced photocatalytic function was supported by an improved photocurrent response and reduced charge-transfer resistance, attributed to superior charge separation efficiency. Consequently, the benzyl alcohol conversion efficiency achieved in the Pickering emulsion system (58.9%) was three-fold of that observed in a traditional oil–water non-emulsion system (19.0%). Key active species were identified as photoholes, and an interfacial reaction mechanism was proposed. This work provides a new approach for extending photocatalytic applications in aqueous environments to diverse organic conversion reactions through the construction of multifunctional photocatalysts. Full article
(This article belongs to the Collection Catalysis in Advanced Oxidation Processes for Pollution Control)
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18 pages, 3268 KB  
Article
In Situ Emulsification Synergistic Self-Profile Control System on Offshore Oilfield: Key Influencing Factors and EOR Mechanism
by Liangliang Wang, Minghua Shi, Jiaxin Li, Baiqiang Shi, Xiaoming Su, Yande Zhao, Qing Guo and Yuan Yuan
Energies 2025, 18(14), 3879; https://doi.org/10.3390/en18143879 - 21 Jul 2025
Viewed by 338
Abstract
The in situ emulsification synergistic self-profile control system has wide application prospects for efficient development on offshore oil reservoirs. During water flooding in Bohai heavy oil reservoirs, random emulsification occurs with superimposed Jamin effects. Effectively utilizing this phenomenon can enhance the efficient development [...] Read more.
The in situ emulsification synergistic self-profile control system has wide application prospects for efficient development on offshore oil reservoirs. During water flooding in Bohai heavy oil reservoirs, random emulsification occurs with superimposed Jamin effects. Effectively utilizing this phenomenon can enhance the efficient development of offshore oilfields. This study addresses the challenges hindering water flooding development in offshore oilfields by investigating the emulsification mechanism and key influencing factors based on oil–water emulsion characteristics, thereby proposing a novel in situ emulsification flooding method. Based on a fundamental analysis of oil–water properties, key factors affecting emulsion stability were examined. Core flooding experiments clarified the impact of spontaneous oil–water emulsification on water flooding recovery. Two-dimensional T1–T2 NMR spectroscopy was employed to detect pure fluid components, innovating the method for distinguishing oil–water distribution during flooding and revealing the characteristics of in situ emulsification interactions. The results indicate that emulsions formed between crude oil and formation water under varying rheometer rotational speeds (500–2500 r/min), water cuts (30–80%), and emulsification temperatures (40–85 °C) are all water-in-oil (W/O) type. Emulsion viscosity exhibits a positive correlation with shear rate, with droplet sizes primarily ranging between 2 and 7 μm and a viscosity amplification factor up to 25.8. Emulsion stability deteriorates with increasing water cut and temperature. Prolonged shearing initially increases viscosity until stabilization. In low-permeability cores, spontaneous oil–water emulsification occurs, yielding a recovery factor of only 30%. For medium- and high-permeability cores (water cuts of 80% and 50%, respectively), recovery factors increased by 9.7% and 12%. The in situ generation of micron-scale emulsions in porous media achieved a recovery factor of approximately 50%, demonstrating significantly enhanced oil recovery (EOR) potential. During emulsification flooding, the system emulsifies oil at pore walls, intensifying water–wall interactions and stripping wall-adhered oil, leading to increased T2 signal intensity and reduced relaxation time. Oil–wall interactions and collision frequencies are lower than those of water, which appears in high-relaxation regions (T1/T2 > 5). The two-dimensional NMR spectrum clearly distinguishes oil and water distributions. Full article
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17 pages, 1364 KB  
Article
Droplet Size Reduction of Self-Emulsifying Drug Delivery System (SEDDS) Using the Hybrid of Medium and Long-Chain Triglycerides
by Kaijie Qian, Yuanyuan Lin, Bingxiang Zhao and Xiangrui Liu
Pharmaceutics 2025, 17(7), 822; https://doi.org/10.3390/pharmaceutics17070822 - 25 Jun 2025
Viewed by 723
Abstract
Background: Self-emulsifying drug delivery system (SEDDS) is widely used to improve the oral bioavailability of hydrophobic drugs. Emulsion droplet size was revealed to be a critical parameter that influences the thermodynamic stability, drug solubility, and drug absorption of the SEDDS. A high proportion [...] Read more.
Background: Self-emulsifying drug delivery system (SEDDS) is widely used to improve the oral bioavailability of hydrophobic drugs. Emulsion droplet size was revealed to be a critical parameter that influences the thermodynamic stability, drug solubility, and drug absorption of the SEDDS. A high proportion of surfactant and/or co-surfactant was usually employed to reduce the particle size, which may lead the low drug loading and undesirable gastrointestinal toxicity. Methods: This manuscript proposed a novel strategy to reduce the particle size of emulsions using the hybrid of medium and long-chain triglyceride (MCT and LCT) SEDDS without promoting the concentration of surfactants and co-surfactants. The composition of SEDDS was selected based on the drug solubility. Particle size distribution and zeta potential of emulsion particles were determined using the dynamic light scattering technique. The bioavailability of formulations was evaluated in a mouse model. Results: The particle size of the emulsion was reduced from 113.50 ± 0.34 nm (MCT SEDDS) and 371.60 ± 6.90 nm (LCT SEDDS) to 21.23 ± 0.30 nm (MCT&LCT SEDDS). Progesterone, a poorly water-soluble drug, was selected as the model drug in the investigation of SEDDS. The hybrid of MCT&LCT progesterone SEDDS exhibited reduced particle size, enlarged self-emulsifying ranges, and increased drug content in the aqueous phase after lipolysis compared with the conventional mono-MCT or LCT SEDDS. In addition, the bioavailability of progesterone in the MCT&LCT SEDDS formulation was 3.82-fold higher than that of Utrogestan® (a clinical oral administrated product) in a mouse model. Full article
(This article belongs to the Section Drug Delivery and Controlled Release)
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15 pages, 3020 KB  
Article
Metal Oxide-Modified PES Membranes for Efficient Separation of Oil-in-Water Emulsions and Trace Organic Compounds
by Jinze Li, Wensheng Yang, Yang Xu, Chengfeng Sun, Yingying Zhu and Geng Chen
Catalysts 2025, 15(6), 604; https://doi.org/10.3390/catal15060604 - 19 Jun 2025
Viewed by 597
Abstract
The efficient removal of emulsified oil and trace organic pollutants via forward osmosis (FO) technology remains challenging due to limited water flux and membrane fouling. In this study, a series of metal oxide-modified PES-based composite FO membranes were fabricated and systematically evaluated to [...] Read more.
The efficient removal of emulsified oil and trace organic pollutants via forward osmosis (FO) technology remains challenging due to limited water flux and membrane fouling. In this study, a series of metal oxide-modified PES-based composite FO membranes were fabricated and systematically evaluated to compare the effects of ZnO, Al2O3, and CuO nanoparticles on membrane structure and separation performance. The results demonstrated that the membrane modified with 0.04 g of ZnO nanoparticles achieved optimal synergy in terms of hydrophilicity, surface charge, and pore structure. The pure water flux increased from 5.48 L·m−2·h−1 for the pristine membrane to 18.5 L·m−2·h−1 for the ZnO-modified membrane, exhibiting a 237.5% increase in pure water flux compared to the pristine PES membrane, an oil rejection rate exceeding 97%, and over 95% rejection of typical negatively charged trace organic pollutants such as ibuprofen and tetracycline. Moreover, the ZnO-modified membrane showed excellent antifouling performance and structural stability in various organic solvent systems. This study not only optimized the interfacial chemistry and microstructure of the FO membrane but also enhanced pollutant repellence and the self-cleaning capability through increased hydrophilicity and surface negative charge density. These findings highlight the significant potential of ZnO modification for enhancing the overall performance of FO membranes and provide an effective strategy for developing high-performance, broadly applicable FO membranes for complex water purification. Full article
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57 pages, 5820 KB  
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 2 | Viewed by 1042
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, 1039 KB  
Article
Self-Emulsifying Drug Delivery System Enhances the Antidiabetic Activity of Passiflora ligularis Leaf Extract
by Sandra M. Echeverry, Diana P. Rey, Ivonne H. Valderrama, Ingrid A. Rodriguez, Paula M. Sepúlveda, Bibiana Verlindo de Araujo, Fátima Regina Mena Barreto Silva and Diana Marcela Aragón
Pharmaceutics 2025, 17(6), 730; https://doi.org/10.3390/pharmaceutics17060730 - 31 May 2025
Viewed by 621
Abstract
Background/Objectives: Previous studies have shown that unformulated extracts of Passiflora ligularis leaves exhibit promising antidiabetic activity. This research aimed to demonstrate that formulating the extract into a self-emulsifying drug delivery system (PLE-SEDDS) enhanced its antidiabetic activity in a high-fat-diet/streptozotocin-induced diabetic mouse model. Methods [...] Read more.
Background/Objectives: Previous studies have shown that unformulated extracts of Passiflora ligularis leaves exhibit promising antidiabetic activity. This research aimed to demonstrate that formulating the extract into a self-emulsifying drug delivery system (PLE-SEDDS) enhanced its antidiabetic activity in a high-fat-diet/streptozotocin-induced diabetic mouse model. Methods: Blood glucose levels (BGLs) of diabetic mice were monitored during 21 days of oral administration of P. ligularis extract (PLE) and PLE-SEDDS. Control groups included metformin (positive control), vehicle, and SEDDS vehicle (negative controls). The animals underwent an oral glucose tolerance test (OGTT). The oxidative stress markers superoxide dismutase (SOD), catalase (CAT), and lipid peroxidation quantified by malondialdehyde (MDA) levels were measured in the kidney, liver, and pancreas, complemented with histopathological analysis. Additionally, plasma lipid profile parameters were evaluated. Results: The PLE-SEDDS formulation demonstrated superior efficacy compared to the PLE extract in improving antidiabetic outcomes. Animals treated with PLE-SEDDS exhibited a minimal increase in blood glucose levels (11.5%) during the OGTT, compared to 27.4% with PLE and over 77% in the vehicle groups. PLE-SEDDS also showed greater enhancement of SOD and CAT activity, along with a more pronounced reduction in MDA levels, indicating stronger protection against oxidative stress. Histological analysis revealed significant preservation of pancreatic islets, and lipid profile analysis showed greater reductions in triglycerides, cholesterol, and LDL-C, alongside increased HDL-C levels. Conclusions: Altogether, these findings suggest that PLE-SEDDS exhibits superior antihyperglycemic, hypolipidemic, and antioxidant effects compared to the unformulated extract, making this novel formulation a promising option for treating type 2 diabetes mellitus. Full article
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14 pages, 5372 KB  
Article
Self-Crosslinking Waterborne Acrylate Modified Emulsified Asphalt via DAAM-ADH: A Dual-Enhanced Solution for Pavement Performance
by Jianhui Xu, Zhaoyi He, Haiying Li, Shutong Tang, Jie Wang, Jing Dang and Yuanyuan Li
Coatings 2025, 15(4), 420; https://doi.org/10.3390/coatings15040420 - 1 Apr 2025
Viewed by 465
Abstract
Emulsified asphalt is widely used for pavement maintenance due to its ease of application. However, its use is limited by poor high-temperature stability and low bonding strength. This study attempted to prepare a self-crosslinking waterborne acrylate (SWA)-type admixture using a diacetone acrylamide (DAAM)-adipic [...] Read more.
Emulsified asphalt is widely used for pavement maintenance due to its ease of application. However, its use is limited by poor high-temperature stability and low bonding strength. This study attempted to prepare a self-crosslinking waterborne acrylate (SWA)-type admixture using a diacetone acrylamide (DAAM)-adipic dihydrazide (ADH) crosslinking system and applied it to emulsified asphalt to ultimately obtain self-crosslinking waterborne acrylate-modified emulsified asphalt (AMEA). The research explored the effects of SWA on the fundamental properties, rheological characteristics, microscopic morphology, and bonding performance of AMEA. Results indicated that SWA undergoes self-crosslinking reactions during the demulsification process, forming a continuous and stable network structure that significantly enhances the strength of emulsified asphalt while improving softening point and high-temperature stability. Rheological analysis revealed that within the 10–15 phr dosage range, the influence of frequency on emulsified asphalt was minimized, with notable improvements in high-temperature elastic recovery and deformation resistance. Particularly when the dosage exceeds 10 phr, the material demonstrates adaptability to high-traffic environments. Pull-off tests demonstrated that SWA can increase the interlayer bonding strength of emulsified asphalt by over 50%. However, SWA exhibits some negative impact on the low-temperature ductility of emulsified asphalt, necessitating cautious dosage control during application. This novel self-crosslinking waterborne acrylate-modified emulsified asphalt, with its excellent bonding performance and superior high-temperature stability, emerges as a crucial material choice for pavement preventive maintenance. Full article
(This article belongs to the Special Issue Surface Treatments and Coatings for Asphalt and Concrete)
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28 pages, 6588 KB  
Article
Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System of Cannabidiol for Enhanced Solubility and Bioavailability
by Fengying Wu, Qing Ma, Guanghui Tian, Kaixian Chen, Rulei Yang and Jingshan Shen
Pharmaceutics 2025, 17(3), 340; https://doi.org/10.3390/pharmaceutics17030340 - 6 Mar 2025
Cited by 2 | Viewed by 2934
Abstract
Background/Objectives: This study aims to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) to enhance the solubility and oral bioavailability of cannabidiol (CBD). Methods: According to the solubility of CBD and pseudo-ternary phase diagrams of the different ingredients, an oil (medium-chain triglyceride, MCT), [...] Read more.
Background/Objectives: This study aims to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) to enhance the solubility and oral bioavailability of cannabidiol (CBD). Methods: According to the solubility of CBD and pseudo-ternary phase diagrams of the different ingredients, an oil (medium-chain triglyceride, MCT), mixed surfactants (Labrasol, Tween 80), and a co-surfactant (Transcutol) were selected for the SNEDDS. CBD-loaded SNEDDS formulations were prepared and characterized. The optimal SNEDDS was converted into solid SNEDDS powders via solid carrier adsorption and spray drying techniques. Various evaluations including flowability, drug release, self-emulsifying capacity, X-ray diffraction (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), morphology, and pharmacokinetic characteristics were conducted. Subsequently, the solid powders with fillers, disintegrants, and lubricants were added to the capsules for accelerated stability testing. Results: The investigations showed that the two S-SNEDDS formulations improved the CBD’s solubility and in vitro drug release, with good storage stability. The pharmacokinetic data of Sprague Dawley rats indicated that a single oral dose of L-SNEDDS and spray drying SNEDDS led to a quicker absorption and a higher Cmax of CBD compared to the two oil-based controls (CBD-sesame oil (similar to Epidiolex®) and CBD-MCT), which is favorable for the application of CBD products. Conclusions: SNEDDS is a prospective strategy for enhancing the solubility and oral bioavailability of CBD, and solid SNEDDS offers flexibility for developing more CBD-loaded solid formulations. Moreover, SNEDDS provides new concepts and methods for other poorly water-soluble drugs. Full article
(This article belongs to the Section Physical Pharmacy and Formulation)
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22 pages, 2878 KB  
Article
Protective Role and Enhanced Intracellular Uptake of Curcumin in Retinal Cells Using Self-Emulsifying Drug Delivery Systems (SNEDDS)
by Elide Zingale, Sebastiano Masuzzo, Tatu Lajunen, Mika Reinisalo, Jarkko Rautio, Valeria Consoli, Agata Grazia D’Amico, Luca Vanella and Rosario Pignatello
Pharmaceuticals 2025, 18(2), 265; https://doi.org/10.3390/ph18020265 - 17 Feb 2025
Cited by 1 | Viewed by 1313
Abstract
Background: Sirtuin-1 (SIRT1), a histone deacetylase enzyme expressed in ocular tissues with intracellular localization, plays a critical protective role against various degenerative ocular diseases. The link between reduced SIRT1 levels and diabetic retinopathy (DR) has prompted the exploration of natural therapeutic compounds that [...] Read more.
Background: Sirtuin-1 (SIRT1), a histone deacetylase enzyme expressed in ocular tissues with intracellular localization, plays a critical protective role against various degenerative ocular diseases. The link between reduced SIRT1 levels and diabetic retinopathy (DR) has prompted the exploration of natural therapeutic compounds that act as SIRT1 agonists. Curcumin (CUR), which has been shown to upregulate SIRT1 expression, is one such promising compound. However, effective delivery of CUR to the deeper ocular tissues, particularly the retina, remains a challenge due to its poor solubility and limited ocular penetration following topical administration. Within this context, the development of self-nanoemulsifying drug delivery systems (SNEDDS) for CUR topical ocular delivery represents a novel approach. Methods: In accordance with our prior research, optimized SNEDDS loaded with CUR were developed and characterized post-reconstitution with simulated tear fluid (STF) at a 1:10 ratio, showing suitable physicochemical and technological parameters for ocular delivery. Results: An entrapment efficiency (EE%) of approximately 99% and an absence of drug precipitation were noticed upon resuspension with STF. CUR-SNEDDS resulted in a better stability and release profile than free CUR under simulated ocular conditions. In vitro analysis of mucoadhesive properties revealed that CUR-SNEDDS, modified with a cationic lipid, demonstrated enhanced interactions with mucin, indicating the potential for improved ocular retention. Cytotoxicity tests demonstrated that CUR-SNEDDS did not affect the viability of human corneal epithelial (HCE) cells up to concentrations of 3 μM and displayed superior antioxidant activity compared to free CUR in an oxidative stress model using retinal pigment epithelial (ARPE-19) cells exposed to hydroquinone (HQ). Cell uptake studies confirmed an enhanced accumulation of CUR within the retinal cells following exposure to CUR-SNEDDS compared to neat CUR. CUR-SNEDDS, at lower concentrations, were found to effectively induce SIRT1 expression. Conclusions: The cytocompatibility, antioxidant properties, and enhanced cellular uptake suggest that these developed systems hold promise as formulations for the delivery of CUR to the retina. Full article
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15 pages, 1193 KB  
Review
The Use of Design of Experiments (DoE) Approaches for the Development of Self-Emulsifying Drug Delivery Systems (SEDDS)
by Ana Carolina Carvalho Lopes Serrano, Mateus Costa Viana, Natalha Vicentina Pinto, Eduardo Burgarelli Lages, Guilherme Carneiro and Gabriel Silva Marques Borges
Appl. Nano 2025, 6(1), 4; https://doi.org/10.3390/applnano6010004 - 12 Feb 2025
Viewed by 2099
Abstract
Self-emulsifying drug delivery systems (SEDDS) consist of isotropic mixtures of oils, surfactants, and solvents that after dispersion emulsify in the aqueous media of the gastrointestinal tract (GIT). SEDDS can deliver hydrophobic drugs, which could enhance their oral bioavailability by protecting them from precipitation [...] Read more.
Self-emulsifying drug delivery systems (SEDDS) consist of isotropic mixtures of oils, surfactants, and solvents that after dispersion emulsify in the aqueous media of the gastrointestinal tract (GIT). SEDDS can deliver hydrophobic drugs, which could enhance their oral bioavailability by protecting them from precipitation and degradation. However, it is important to find the appropriate ratio of their excipients to produce emulsions with the desirable physicochemical characteristics. In this sense, Design of Experiments (DoE) approaches such as central composite design (CCD) and Box–Behnken design (BBD) can reduce the number of experiments necessary to determine the best composition and preparation process of a SEDDS formulation. Therefore, this article aims to discuss drug delivery through SEDDS and how DoE approaches can aid researchers in achieving product quality specifications and optimizing the formulation preparation processes. For this, the most recent and relevant papers were analyzed. This review is expected to guide future research directions for more rational development of SEDDS. Full article
(This article belongs to the Collection Review Papers for Applied Nano Science and Technology)
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24 pages, 5097 KB  
Article
Development and Characterization of Innovative Nifurtimox Formulations as Therapeutic Alternative for Chagas Disease
by Ana Lia Mazzeti, Karolina Ribeiro Gonçalves, Patrícia Ferreira Boasquivis, Maria Terezinha Bahia and Vanessa Carla Furtado Mosqueira
Trop. Med. Infect. Dis. 2025, 10(2), 50; https://doi.org/10.3390/tropicalmed10020050 - 7 Feb 2025
Viewed by 1416
Abstract
Chagas disease, caused by Trypanosoma cruzi, remains a neglected tropical disease with limited and often suboptimal chemotherapeutic treatment options. The WHO recommends nifurtimox (NFX) for treating Chagas disease, which, although it is effective in the early stages of infection, has variable efficacy [...] Read more.
Chagas disease, caused by Trypanosoma cruzi, remains a neglected tropical disease with limited and often suboptimal chemotherapeutic treatment options. The WHO recommends nifurtimox (NFX) for treating Chagas disease, which, although it is effective in the early stages of infection, has variable efficacy in the chronic phase and induces adverse effects that frequently compromise the continuity of the treatment. This study focused on the development and characterization of innovative lipid-based self-emulsifying drug delivery systems (SEDDSs) and poly(ε-caprolactone) implants containing NFX. The SEDDS formulations modified the NFX release extent and rate. The implant characterization included thermal analysis, X-ray diffraction, thermo-optical analysis, and scanning electron microscopy, confirming the low interaction between NFX and the polymer. In vitro assays demonstrated the enhanced anti-T. cruzi activity of the NFX-SEDDS, with minimal cytotoxicity in mammalian cells. In vivo studies using T. cruzi-infected mice revealed that both formulations effectively suppressed parasitemia, achieving cure rates comparable to those of the standard oral NFX treatment. Additionally, the implants showed improved tolerability and sustained efficacy, delivering a prolonged effect equivalent to 40 oral doses. These findings highlight the potential of these innovative NFX formulations as promising alternatives for treating Chagas disease, particularly in the chronic phase, offering improved adherence and comparable efficacy to the existing therapies. Full article
(This article belongs to the Special Issue New Drug Formulations for Chagas's Disease Treatment)
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25 pages, 2673 KB  
Article
Development of Salvia officinalis–Based Self-Emulsifying Systems for Dermal Application: Antioxidant, Anti-Inflammatory, and Skin Penetration Enhancement
by Krisztina Bodnár, Boglárka Papp, Dávid Sinka, Pálma Fehér, Zoltán Ujhelyi, István Lekli, Richárd Kajtár, Fruzsina Nacsa, Ildikó Bácskay and Liza Józsa
Pharmaceutics 2025, 17(2), 140; https://doi.org/10.3390/pharmaceutics17020140 - 21 Jan 2025
Cited by 1 | Viewed by 2295
Abstract
Background/Objectives: The present study focused on the formulation and evaluation of novel topical systems containing Salvia officinalis (sage), emphasizing their antioxidant and anti-inflammatory properties. Sage, rich in carnosol, offers considerable therapeutic potential, yet its low water solubility limits its effectiveness in traditional formulations. [...] Read more.
Background/Objectives: The present study focused on the formulation and evaluation of novel topical systems containing Salvia officinalis (sage), emphasizing their antioxidant and anti-inflammatory properties. Sage, rich in carnosol, offers considerable therapeutic potential, yet its low water solubility limits its effectiveness in traditional formulations. The aim of our experimental work was to improve the solubility and thus bioavailability of the active ingredient by developing self-nano/microemulsifying drug delivery systems (SN/MEDDSs) with the help of Labrasol and Labrafil M as the nonionic surfactants, Transcutol HP as the co-surfactant, and isopropyl myristate as the oily phase. Methods: The formulations were characterized for droplet size, zeta potential, polydispersity index (PDI), encapsulation efficacy, and stability. The composition exhibiting the most favorable characteristics, with particle sizes falling within the nanoscale range, was incorporated into a cream and a gel, which were compared for their textural properties, carnosol penetration, biocompatibility and efficacy. Results: Release studies conducted using Franz diffusion cells demonstrated that the SNEDDS-based cream achieved up to 80% carnosol release, outperforming gels. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) test and enzyme-linked immunosorbent assays (ELISA) showed strong efficacy, with an in vivo carrageenan-induced rat paw edema model revealing that the SNEDDS-based cream significantly reduced inflammation. Conclusions: These findings highlight the potential of SNEDDS-enhanced topical formulations in improving therapeutic outcomes. Further research is warranted to confirm their long-term safety and efficacy. Full article
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33 pages, 2920 KB  
Review
Self-Emulsifying Drug Delivery Systems (SEDDS): Transition from Liquid to Solid—A Comprehensive Review of Formulation, Characterization, Applications, and Future Trends
by Prateek Uttreja, Indrajeet Karnik, Ahmed Adel Ali Youssef, Nagarjuna Narala, Rasha M. Elkanayati, Srikanth Baisa, Nouf D. Alshammari, Srikanth Banda, Sateesh Kumar Vemula and Michael A. Repka
Pharmaceutics 2025, 17(1), 63; https://doi.org/10.3390/pharmaceutics17010063 - 5 Jan 2025
Cited by 11 | Viewed by 10155
Abstract
Self-emulsifying drug delivery systems (SEDDS) represent an innovative approach to improving the solubility and bioavailability of poorly water-soluble drugs, addressing significant challenges associated with oral drug delivery. This review highlights the advancements and applications of SEDDS, including their transition from liquid to solid [...] Read more.
Self-emulsifying drug delivery systems (SEDDS) represent an innovative approach to improving the solubility and bioavailability of poorly water-soluble drugs, addressing significant challenges associated with oral drug delivery. This review highlights the advancements and applications of SEDDS, including their transition from liquid to solid forms, while addressing the formulation strategies, characterization techniques, and future prospects in pharmaceutical sciences. The review systematically analyzes existing studies on SEDDS, focusing on their classification into liquid and solid forms and their preparation methods, including spray drying, hot-melt extrusion, and adsorption onto carriers. Characterization techniques such as droplet size analysis, dissolution studies, and solid-state evaluations are detailed. Additionally, emerging trends, including 3D printing, hybrid systems, and supersaturable SEDDS (Su-SEDDS), are explored. Liquid SEDDS (L-SEDDS) enhance drug solubility and absorption by forming emulsions upon contact with gastrointestinal fluids. However, they suffer from stability and leakage issues. Transitioning to solid SEDDS (S-SEDDS) has resolved these limitations, offering enhanced stability, scalability, and patient compliance. Innovations such as personalized 3D-printed SEDDS, biologics delivery, and targeted systems demonstrate their potential for diverse therapeutic applications. Computational modeling and in silico approaches further accelerate formulation optimization. SEDDS have revolutionized drug delivery by improving bioavailability and enabling precise, patient-centric therapies. While challenges such as scalability and excipient toxicity persist, emerging technologies and multidisciplinary collaborations are paving the way for next-generation SEDDS. Their adaptability and potential for personalized medicine solidify their role as a cornerstone in modern pharmaceutical development. Full article
(This article belongs to the Special Issue Microemulsion Utility in Pharmaceuticals)
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19 pages, 5132 KB  
Article
Double Hydrophilic Hyperbranched Copolymer-Based Lipomer Nanoparticles: Copolymer Synthesis and Co-Assembly Studies
by Angelica Maria Gerardos and Stergios Pispas
Polymers 2024, 16(22), 3129; https://doi.org/10.3390/polym16223129 - 9 Nov 2024
Cited by 2 | Viewed by 1603
Abstract
Double hydrophilic, random, hyperbranched copolymers were synthesized via reversible addition–fragmentation chain transfer (RAFT) polymerization of oligo(ethylene glycol) methyl ether methacrylate (OEGMA) and 2-(dimethylamino)ethyl methacrylate (DMAEMA) utilizing ethylene glycol dimethacrylate (EGDMA) as the branching agent. The resulting copolymers were characterized in terms of their [...] Read more.
Double hydrophilic, random, hyperbranched copolymers were synthesized via reversible addition–fragmentation chain transfer (RAFT) polymerization of oligo(ethylene glycol) methyl ether methacrylate (OEGMA) and 2-(dimethylamino)ethyl methacrylate (DMAEMA) utilizing ethylene glycol dimethacrylate (EGDMA) as the branching agent. The resulting copolymers were characterized in terms of their molecular weight and dispersity using size exclusion chromatography (SEC), and their chemical structure was confirmed using FT-IR and 1H-NMR spectroscopy techniques. The choice of the two hydrophilic blocks and the design of the macromolecular structure allowed the formation of self-assembled nanoparticles, partially due to the pH-responsive character of the DMAEMA segments and their interaction with -COOH end groups remaining from the chain transfer agent. The copolymers showed pH-responsive properties, mainly due to the protonation–deprotonation equilibria of the DMAEMA segments. Subsequently, a nanoscopic polymer–lipid (lipomer) mixed system was formulated by complexing the synthesized copolymers with cosmetic amphiphilic emulsifiers, specifically glyceryl stearate (GS) and glyceryl stearate citrate (GSC). This study aims to show that developing lipid–polymer hybrid nanoparticles can effectively address the limitations of both liposomes and polymeric nanoparticles. The effects of varying the ionic strength and pH on stimuli-sensitive polymeric and mixed polymer–lipid nanostructures were thoroughly investigated. To achieve this, the structural properties of the hybrid nanoparticles were comprehensively characterized using physicochemical techniques providing insights into their size distribution and stability. Full article
(This article belongs to the Special Issue Block Copolymers: Self-Assembly and Applications, 2nd Edition)
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34 pages, 3009 KB  
Review
Lipid-Based Nanoformulations for Drug Delivery: An Ongoing Perspective
by Mubashar Rehman, Nayab Tahir, Muhammad Farhan Sohail, Muhammad Usman Qadri, Sofia O. D. Duarte, Pedro Brandão, Teresa Esteves, Ibrahim Javed and Pedro Fonte
Pharmaceutics 2024, 16(11), 1376; https://doi.org/10.3390/pharmaceutics16111376 - 26 Oct 2024
Cited by 15 | Viewed by 5593
Abstract
Oils and lipids help make water-insoluble drugs soluble by dispersing them in an aqueous medium with the help of a surfactant and enabling their absorption across the gut barrier. The emergence of microemulsions (thermodynamically stable), nanoemulsions (kinetically stable), and self-emulsifying drug delivery systems [...] Read more.
Oils and lipids help make water-insoluble drugs soluble by dispersing them in an aqueous medium with the help of a surfactant and enabling their absorption across the gut barrier. The emergence of microemulsions (thermodynamically stable), nanoemulsions (kinetically stable), and self-emulsifying drug delivery systems added unique characteristics that make them suitable for prolonged storage and controlled release. In the 1990s, solid-phase lipids were introduced to reduce drug leakage from nanoparticles and prolong drug release. Manipulating the structure of emulsions and solid lipid nanoparticles has enabled multifunctional nanoparticles and the loading of therapeutic macromolecules such as proteins, nucleic acid, vaccines, etc. Phospholipids and surfactants with a well-defined polar head and carbon chain have been used to prepare bilayer vesicles known as liposomes and niosomes, respectively. The increasing knowledge of targeting ligands and external factors to gain control over pharmacokinetics and the ever-increasing number of synthetic lipids are expected to make lipid nanoparticles and vesicular systems a preferred choice for the encapsulation and targeted delivery of therapeutic agents. This review discusses different lipids and oil-based nanoparticulate systems for the delivery of water-insoluble drugs. The salient features of each system are highlighted, and special emphasis is given to studies that compare them. Full article
(This article belongs to the Special Issue Liposomes Applied in Drug Delivery Systems)
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