Journal of Drug Delivery Science and Technology最新文献

{"title":"Design and in vitro cytotoxicity of docetaxel-loaded hyaluronic acid-coated nanostructured lipid carriers in breast cancer cells","authors":"Isabel Rheinfranck Peleje ,&nbsp;Leonardo Delello Di Filippo ,&nbsp;Marcela Tavares Luiz ,&nbsp;Giovanna Capaldi Fortunato ,&nbsp;Deivys Leandro Portuondo ,&nbsp;Mônica Freitas da Silva ,&nbsp;Iracilda Zeppone Carlos ,&nbsp;Jonatas Lobato Duarte ,&nbsp;Marlus Chorilli","doi":"10.1016/j.jddst.2025.107077","DOIUrl":"10.1016/j.jddst.2025.107077","url":null,"abstract":"<div><div>Breast cancer is one of the most prevalent types of cancer globally. Among the treatment options, docetaxel (DTX) is frequently used as chemotherapy, but its clinical efficacy is limited due to adverse effects and low bioavailability. To minimize toxicity and improve drug delivery to cancer cells, nanostructured lipid carriers (NLC) have been explored. Modifying their surface with hyaluronic acid (HA) can target the drug to CD44 receptors, overexpressed in many cancers like breast cancer, increasing drug accumulation in the target tissue and reducing non-target toxicity. This work aimed to develop and evaluate the <em>in vitro</em> cytotoxicity and cellular uptake of HA-coated NLCs encapsulating docetaxel (HA-NLC-DTX) in breast cancer cells. NLCs were obtained using capric/caprylic acid triglycerides (CCTG) as liquid lipid, glyceryl behenate (Compritol®) as solid lipid, polysorbate 80 (P80) and cetyltrimethylammonium bromide (CTAB) as surfactants, and an aqueous phase composed of ultra-purified water. The HA coating was mediated by electrostatic interactions with a by adding a cationic surfactant (CTAB). The formulations were characterized regarding particle size, polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency, differential scanning calorimetry, infrared spectroscopy, and <em>in vitro</em> release profile. Cytotoxicity was evaluated using the MCF-7 breast adenocarcinoma cell line and L929 cell line. Different formulations were developed varying the proportions of surfactant, solid, and liquid lipid. The particle sizes ranged from 40 nm to 247 nm, with ZP from −23 mV to −8 mV and PDI between 0.27 and 0.76. For CTAB, the concentration of 0.1 % w/v (of total formulation) proved to be the most promising for adding HA, presenting homogeneous particles and lower PDI, which can favor the colloidal stability and optimize drug delivery, showing a positive ZP. Considering the desired colloidal properties, F5 (CCTG 25 mg, Compritol® 35 mg, P80 5 mg, CTAB 1 mg, DTX 1 mg) was selected for subsequent studies. For HA concentrations, 1 mg/ml and 0.5 mg/ml were tested, with ratios ranging from 1:1 to 8:1. Release studies showed a cumulative and controlled release of DTX from NLC, especially HA-coated NLC. In cytotoxicity assays, free DTX showed an IC₅₀ of 91.12 nM after 72 h. The formulation HA-NLC-DTX showed a greater cytotoxic effect than free DTX, with an IC50 of 49.80 nM. Additionally, HA-NLC was successfully internalized by MCF-7 cells as confirmed by flow cytometry. The results confirm that the HA-coated NLC provides a controlled and effective release of DTX, with increased cytotoxicity in breast cancer cells, demonstrating the promising potential of HA-coating in breast cancer-targeted therapies.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107077"},"PeriodicalIF":4.5,"publicationDate":"2025-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144155172","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lipid and polymeric nanocarriers as an approach to enhance the anti-inflammatory activity of essential oils","authors":"Cynthia Camila Ziech,&nbsp;Douglas dos Santos Porto,&nbsp;Thiago Caon","doi":"10.1016/j.jddst.2025.107079","DOIUrl":"10.1016/j.jddst.2025.107079","url":null,"abstract":"<div><div>Essential oils (EOs), which are mixtures of volatile compounds extracted from aromatic plants, have received attention as anti-inflammatory agents due to their ability to modulate multiple signaling pathways (e.g., the arachidonic acid pathway, cannabinoid receptors and cytokine regulation) and to reduce or even avoiding toxic side effects of synthetic drugs. Oregano, peppermint, clove, wintergreen, rosemary, tea tree, lavender, thyme and erva baleeira EOs have been widely used in this context. Despite the high efficiency, high volatility, hydrophobicity and oxidation of many terpenes found in these EOs, many challenges are found formulation development step, which have motivated the application of nanotechnologies such as lipid or polymeric nanocarriers. Lipid-based systems have the benefit of providing high encapsulation efficiency of hydrophobic terpenes and can improve interaction with cells or biological tissues. Polymeric nanoparticles, in turn, often result in more stable particles with greater release control. In addition to these advantages, enhanced anti-inflammatory activity can be achieved, which was exploited in detail in this review. Several topical formulations containing EO nanoparticles have been demonstrated to provide an <em>in vivo</em> anti-inflammatory effect similar or even higher than reference drugs such as indomethacin and dexamethasone, encouraging clinical trials. Besides anti-inflammatory effects, some EOs have antimicrobial and/or analgesic properties, making it possible to reduce the number of drugs used in inflammatory disorders associated with infection or pain (an important aspect from a safety standpoint). Another point that still deserves to be explored is the synergism of the anti-inflammatory action of EOs.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107079"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144168841","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Internal force-controlled (IFC) sonication with tunable conditions for the large-scale preparation of porous silicon nanoparticles","authors":"Nam Cheol Hwang ,&nbsp;Seung Woo Baek ,&nbsp;Dongjae Choi ,&nbsp;Hwajun Jeong ,&nbsp;Dokyoung Kim","doi":"10.1016/j.jddst.2025.107095","DOIUrl":"10.1016/j.jddst.2025.107095","url":null,"abstract":"<div><div>Porous silicon nanoparticles (pSiNPs) have garnered significant attention for various applications, including drug delivery and biosensing. Conventionally, their production has been restricted to small-scale synthesis, often resulting in nanoparticles of variable sizes, which has limited their commercialization and practical use. In this study, we present a novel method for the scalable production of pSiNPs on a gram scale in a relatively short time using internal force-controlled (IFC) sonication. IFC sonication ensures power adjustment (from 60 W to 300 W), short processing times (&lt;3 h), high yield (63.0 ± 4.18 %), and high reproducibility. This method produces nanoparticles with a superior degree of uniformity and consistent sizes, thereby addressing size variation challenges observed in previous approaches. These advancements facilitate large-scale production and enhance the reproducibility and applicability of pSiNPs in various fields.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107095"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144169328","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bergamot waste derived lipid nanosystems as novel excipients for (trans)dermal drug delivery","authors":"Paola Volonté ,&nbsp;Caterina Ricci ,&nbsp;Sebastiano Arnoldi ,&nbsp;Gabriella Roda ,&nbsp;Elena Del Favero ,&nbsp;Francesco Puoci ,&nbsp;Paola Minghetti ,&nbsp;Silvia Franzè ,&nbsp;Francesco Cilurzo","doi":"10.1016/j.jddst.2025.107085","DOIUrl":"10.1016/j.jddst.2025.107085","url":null,"abstract":"<div><div>Inedible waste from the bergamot processing industry is typically used to produce essential oil, parfums, pectin etc. Nevertheless, the discarded bergamot peels can still serve as a valuable source of novel lipid ingredients. This study explores the potential of using lipid components from bergamot peels (BLCs) to create lipid-based nanosystems (LBNs) for skin application.</div><div>BLCs were extracted and characterized by GC/MS and ATR-FTIR. LBNs were prepared by hot melt homogenization, and their ultrastructure was studied by cryo-EM and SAXS. Ibuprofen (IB) was chosen as model drug. The <em>in vitro</em> skin permeation pattern of IB either loaded in LBNs (IB-LBNs) or co-administered with empty LBNs was studied using porcine skin.</div><div>The LBNs had a mean diameter of about 150 nm and a core-shell structure. LBNs increased the IB flux through porcine skin by a factor of three, both in IB-LBNs form and after co-administration with the free drug solution. This data suggests that BLCs act as skin penetration enhancers rather than drug carriers. ATR-FTIR results further indicated that BLCs perturb the structure of stratum corneum lipids, likely due to the presence of unsaturated fatty acid esters in BLCs extract.</div><div>In conclusion, BLCs could be promising novel and natural excipients for the design of cutaneous preparations.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107085"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144169327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Microfluidic fabrication of rivastigmine-loaded chitosan-hyaluronic acid nanoparticles using 3D-Printed devices","authors":"Esmaeil Atashbasteh ,&nbsp;Mohsen Nasr Esfahany ,&nbsp;Parham Reisi ,&nbsp;Mohsen Minaiyan ,&nbsp;Azade Taheri","doi":"10.1016/j.jddst.2025.107084","DOIUrl":"10.1016/j.jddst.2025.107084","url":null,"abstract":"<div><div>This research investigates the combination of 3D printing and microfluidic technologies to create innovative drug delivery systems for neurodegenerative conditions. Fused Deposition Modeling (FDM) was utilized to design and produce four different microfluidic channel configurations (Y-shaped, T-shaped, Baffle, and Staggered Herringbone Micromixers). These channels were used to prepare chitosan-hyaluronic acid polyelectrolyte nanoparticles encapsulating rivastigmine hydrogen tartrate, a therapeutic agent for Alzheimer's disease. SEM and digital imaging confirmed the high structural accuracy and functionality of the fabricated microchannels. By optimizing nanoparticle preparation conditions, particles with consistent size (309.9–476.36 nm), narrow polydispersity index, and high encapsulation efficiency (up to 94.76 %) were achieved. Electrostatic interactions between chitosan, hyaluronic acid, and rivastigmine facilitated nanoparticle formation without covalent bonding. The optimized formulation was obtained using the Staggered Herringbone Micromixers channel, with a flow rate of 1 mL/min, 0.5 % w/v chitosan concentration, and 0.25 % w/v hyaluronic acid concentration with maximum particle uniformity and drug loading efficiency. <em>In vitro</em> drug release studies demonstrated a biphasic release pattern, with an initial burst phase followed by sustained release over 24 h. This study demonstrates the potential of combining 3D printing and microfluidics for the reproducible, scalable, and cost-effective production of electrostatic nanoparticulate drug delivery systems, offering a promising platform for treating Alzheimer's and other neurodegenerative diseases.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107084"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144169347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of antioxidant, antimicrobial, anti-inflammatory properties and cytotoxicity of copper-doped NiO nanoparticles synthesized using biomass extract","authors":"Abdullahi Dahiru Datti ,&nbsp;Shivangi Parhi ,&nbsp;Abanindra Nath Sarkar ,&nbsp;Rahul Narayanan ,&nbsp;Archana M ,&nbsp;Ejjurothu Ramya Lakshmi Keerthana ,&nbsp;Sudeshna Saha ,&nbsp;Paulomi Ghosh ,&nbsp;M. Muthuraj ,&nbsp;Dipankar Das","doi":"10.1016/j.jddst.2025.107102","DOIUrl":"10.1016/j.jddst.2025.107102","url":null,"abstract":"<div><div>Biomass extract-mediated production of nanoparticles (NPs) is a beneficial substitute for the conventional approach because it is sustainable and inexpensive. This work reports on the preparation of nickel oxide NPs and copper-doped nickel oxide nanoparticles (Cu-doped-NiO NPs) through the precipitation method using <em>Calotropis gigantea</em> flower extract (CGFE) and the assessment of their bioactivities. Different techniques are employed to characterize the NiO NPs and Cu-doped-NiO NPs. X-ray diffraction shows that the NiO NPs are face-centered cubic with 27.3 nm average crystallite size, whereas the Cu-doped NiO NPs are between 18.8 and 43.3 nm. Microscopy images reveal that the NiO NPs and Cu-doped-NiO NPs have blunt needle-like shapes. X-ray photoelectron spectroscopy analysis ascertains the formation of the NiO and the successful doping of NiO with copper. Mass spectrometric analysis of the extract reveals the presence of various phytochemicals. The antioxidant property was evaluated by ABTS and DPPH assays. The CGFE-mediated NiO NPs are effective against <em>Staphylococcus aureus</em> and <em>Escherichia coli</em>, while copper doping improves the antibacterial properties at a concentration of 3 and 4 mg/mL. The antifungal activity of the Cu-doped NiO NPs lasts more than 90 h against <em>C. albicans</em>, while its potential starts to decline after 24 h against <em>A. niger</em>. The anti-inflammatory activity of the Cu-doped NiO NPs is 80.1 %. The Cu-doped NiO NPs show an IC₅₀ value of 125.9 ± 2.1 μg/mL against fibroblast cells. The outcomes implied that the biosynthesized Cu-doped-NiO NPs could actively be used as a potent antimicrobial, antioxidant, and anti-inflammatory agent.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107102"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194827","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel siRNA delivery system targeting β-catenin in colorectal cancer Cells: Synergistic effect with 5-fluorouracil","authors":"Ahmad Ghareeb ,&nbsp;Noura Ghazal ,&nbsp;Mohyeddin Assali ,&nbsp;Naim Kittana ,&nbsp;Ahmed Khader ,&nbsp;Mariam Daraghmeh","doi":"10.1016/j.jddst.2025.107082","DOIUrl":"10.1016/j.jddst.2025.107082","url":null,"abstract":"<div><div>Short interference RNA (siRNA) has emerged as a promising approach for the treatment of many diseases that require controlling protein expression such as cancer. Effective delivery of siRNA into cells is a challenge. This project aimed to develop a guided delivery system based on multi-walled carbon nanotubes (MWCNTs) that can deliver siRNA preferentially into colorectal cancer (CRC) cells (Caco-2) to knock down β-catenin. MWCNTs were functionalized with a tetra-amine linker to load siRNA (<em>f</em>-MWCNTs (8)), which was in the next stage functionalized with mannose sugar as a targeting agent (<em>f</em>-MWCNTs (12)). Loads of amine on <em>f</em>-MWCNTs (8) and <em>f</em>-MWCNTs (12) were 12.7 × 10³ and 40 × 10³ nmol/mg respectively. The amount of loaded mannose in <em>f</em>-MWCNTs (12) was 1.109 μg/mg. The optimum N/P ratio for loading siRNA was 5:1 for the <em>f</em>-MWCNTs (8) and 15:1 for the <em>f</em>-MWCNTs (12). siRNA-<em>f</em>-MWCNTs (8) knocked down β-catenin protein by about 20 % and reduced the cell viability by about 10 %, while siRNA-<em>f</em>-MWCNTs (12) knocked down β-catenin protein by 50 % and reduced the cell viability by 32 %. A combination of siRNA-<em>f</em>-MWCNTs (12) with the anticancer drug 5-fluorouracil (5-FU) reduced the cell viability by around 80 % compared to 25 % by monotherapy with 5-FU, while the combination with <em>f</em>-MWCNTs (8) did not show a significant effect. In conclusion, the functionalization of MWCNT with mannose increases the efficiency of siRNA delivery into Caco-2 cells and the knockdown of β-catenin can improve the sensitivity of Caco-2 cells to 5-FU.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107082"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144189995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation of pH-sensitive ZIF-8 (MOF) impregnated amino-chitosan biocomposite beads for sustained release of 5-fluorouracil","authors":"Ahmed M. Omer ,&nbsp;Eman M. Abd El-Monaem ,&nbsp;Heba S. Hassan ,&nbsp;Mahmoud A. Elmeligy ,&nbsp;Angela Kleinová ,&nbsp;Abdelazeem S. Eltaweil ,&nbsp;Abolfazl Heydari","doi":"10.1016/j.jddst.2025.107099","DOIUrl":"10.1016/j.jddst.2025.107099","url":null,"abstract":"<div><div>pH-sensitive carriers have emerged as an optimal choice for the oral administration of anticancer drugs, exhibiting the desired release performance. This study aims to develop biocomposite beads for the sustained release of the anticancer drug 5-fluorouracil (5-FU). Here, 5-FU was encapsulated within a ZIF-8 metal-organic framework (MOF), which was subsequently impregnated into amino-chitosan beads. The resulting Am-CS@ZIF-8 biocomposite beads were characterized for their chemical structure, surface morphology, elemental composition, crystallinity, surface charges, and mechanical properties utilizing Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), zeta potential analysis, and a texture analyzer, respectively. The developed beads exhibited a textured surface, denser composition, and a positively charged surface with a maximum zeta potential of +12.4 at pH 7.4. In comparison to Am-CS beads, the Am-CS@ZIF-8 biocomposite beads demonstrated superior mechanical properties, achieving a maximum stress value of 5.668 MPa compared to the 1.874 MPa recorded for pure Am-CS beads. pH sensitivity was assessed through the investigation of water uptake behavior at pH 1.2 and pH 7.4. The Am-CS@ZIF-8 biocomposite beads demonstrated a high encapsulation efficiency of approximately 81.6 % for 5-FU. They exhibited pH-responsive release behavior, with only 17 % of the drug released at pH 1.2 after 2 h and a sustained release of 52 % at pH 7.4 over 24 h. The release mechanism was predominantly governed by Fickian diffusion, as closely fitted by the Peppas-Sahlin kinetic model. The formulated carrier confirmed its biodegradability under enzymatic physiological conditions, suggesting its potential applicability as an effective system for the oral delivery of anticancer drugs.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107099"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144189996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhanced bioavailability of betulinic acid using a self-nanoemulsifying drug delivery system (SNEDDS) with fish oil","authors":"Laura R. Ochoa-Rodríguez ,&nbsp;Diego A. Bravo-Alfaro ,&nbsp;Cecilia D. Treviño-Quintanilla ,&nbsp;Alaina A. Esperon-Rojas ,&nbsp;Angélica A. Ochoa-Flores ,&nbsp;Reina Araceli Mauricio-Sánchez ,&nbsp;Miguel A. Gómez-Lim ,&nbsp;Luis Medina-Torres ,&nbsp;Rogelio Rodriguez-Rodriguez ,&nbsp;Gabriel Luna-Bárcenas ,&nbsp;Hugo S. García","doi":"10.1016/j.jddst.2025.107080","DOIUrl":"10.1016/j.jddst.2025.107080","url":null,"abstract":"<div><div>Betulinic acid (BA) is a naturally occurring pentacyclic triterpene compound that exhibits various biological activities such as anticancer, antiviral, anti-inflammatory, anti-hyperlipidemic, and hepatoprotective. Because of its lupane-like chemical structure, this compound exhibits low solubility in aqueous media, leading to low bioavailability and a short half-life in systemic circulation when administered orally. To solve solubility and bioavailability problems, nanotechnology offers the design of encapsulation systems based on lipids, such as self-nanoemulsifying drug delivery systems (SNEDDS). Limited reports show that low-energy techniques prepare betulinic acid encapsulation systems. Therefore, in the present work, the development of SNEDDS is proposed for the encapsulation of betulinic acid using fish oil as the oil phase, Cremophor EL® as surfactant, and Labrafil M1944CS® as co-surfactant. The results showed that fish oil was the one that solubilized more significant amounts of BA (12.96 mg BA/g of oil). The systems with fish oil showed average droplet sizes between 19.44 and 40.33 nm, while the PDI ranged from 0.037 to 0.144 and was allowed to encapsulate from 0.73 to 2.82 mg of BA with 94.1 % encapsulation efficiency. The system evaluated <em>in vitro</em> exhibited no substantial change in particle size throughout the study, but there was a significant change in the polydispersity index (PDI). Finally, in the <em>in vivo</em> evaluation with Wistar rats, a bioavailability of 17 times greater than free betulinic acid was obtained. These results show a significant increase in bioavailability when encapsulating BA using fish oil rich in DHA and EPA, which could be helpful for future applications in the medical field for the treatment of various pathologies such as cancer.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107080"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144169333","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synergistic antimicrobial effects of coffee green extract and oil microemulsions enhanced by photodynamic therapy: A strategy against antibiotic resistance","authors":"Paulinne M. Lima ,&nbsp;Catarina S. Guimarães ,&nbsp;Caroline V. Gonçalves ,&nbsp;Caio C. Pereira ,&nbsp;Laryana B. Garcia ,&nbsp;Isabela D. dos Santos ,&nbsp;Jayne F.S. Oliveira ,&nbsp;Micaela S.C. Silva ,&nbsp;Mateus F. Leite ,&nbsp;André L.M. Ruela ,&nbsp;Robson A.A. da Silva ,&nbsp;Gabriel A.B. Damasceno ,&nbsp;Denise B. da Silva ,&nbsp;Juliano G. Amaral","doi":"10.1016/j.jddst.2025.107094","DOIUrl":"10.1016/j.jddst.2025.107094","url":null,"abstract":"<div><div>Coffee is one of the main tropical crops, with Brazil accounting for more than a third of global production. It contains bioactive compounds such as chlorogenic acids that provide health benefits, such as antimicrobial activity, and is a natural alternative in combating antibiotic resistance, currently one of the major global threats to public health. Additionally, antimicrobial photodynamic therapy (aPDT) has also emerged as a way to overcome microbial resistance, using photosensitizers, light and oxygen to generate reactive species that eliminate microorganisms. Microemulsions were prepared by the spontaneous emulsification method, containing green coffee oil and extract, stabilized by surfactants. The dispersed systems obtained presented droplet size of approximately 25–60 nm, PDI of 0.088–0.290 and zeta potential of approximately −12 to −25 mV, at different temperatures and stability tests. In addition, they demonstrated Newtonian fluid behavior with a viscosity of approximately 30 cP. Furthermore, they were effective in treating microorganisms at lower doses than previously reported in the literature and were enhanced when associated with photodynamic therapy, acting at a minimum concentration of green coffee extract of 250 μg ml⁻¹ and when photoactivated, acting at 125 μg ml⁻¹, and they also exhibited activity in the absence of the incorporated extract. This study reveals a product that structures the use of plant-derived substances in the pharmaceutical industry, stimulating the bioeconomy and contributing to family farming, considering the economic importance of coffee in Brazil.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107094"},"PeriodicalIF":4.5,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144168838","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}