Journal of Drug Delivery Science and Technology最新文献

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Application of six typical microalgae in the treatment of lung adenocarcinoma 六种典型微藻在肺腺癌治疗中的应用
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-05 DOI: 10.1016/j.jddst.2025.107250
Chengyu Liu , Keying Cui , Yuejiao Liu , Jinlong Dai , Yinghui Chai , Wen Chen
{"title":"Application of six typical microalgae in the treatment of lung adenocarcinoma","authors":"Chengyu Liu ,&nbsp;Keying Cui ,&nbsp;Yuejiao Liu ,&nbsp;Jinlong Dai ,&nbsp;Yinghui Chai ,&nbsp;Wen Chen","doi":"10.1016/j.jddst.2025.107250","DOIUrl":"10.1016/j.jddst.2025.107250","url":null,"abstract":"<div><div>Due to its advantages in structure, composition, and function, microalgae hold broad application prospects in the biomedical field, particularly in tumor treatment. However, microalgae are a group of tiny algae, and recent research has primarily focused on advanced modifications, with less attention paid to the functional differences among various species of microalgae. In this study, we selected six typical microalgae, including <em>Chlorella</em>, <em>H. pluvialis</em>, <em>C. reinhardtii</em>, <em>Spirulina</em>, <em>E. gracilis and D. salina</em>, and investigated their effects on lung adenocarcinoma. In the RPMI1640 medium containing 10 % FBS, all microalgaes maintained good morphology and motility for over 48 h. <em>In vitro</em> experiments revealed that all microalgae species are capable of inhibiting the proliferation and invasion of adenocarcinoma cells, while inducing their apoptosis. Among them, <em>Spirulina</em> and <em>E. gracilis</em> exhibit the strongest anticancer effects. We further constructed tumor-bearing animal models and found that all microalgae inhibited the growth of transplanted tumors, without any significant adverse effects on surrounding normal tissues and vital organs. Among them, <em>Spirulina</em> and <em>E. gracilis</em> can exert anticancer effects by activating anti-tumor immunity. Our research also indicates that in the absence of light, <em>Spirulina</em> and <em>E. gracilis</em> did not affect microvascular density and hypoxia in vivo. In summary, <em>Spirulina</em> and <em>E. gracilis</em> may be more suitable as drug delivery carriers for targeted tumor therapy. Our research provides important data support for the medical application of microalgae.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107250"},"PeriodicalIF":4.5,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144579652","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}
引用次数: 0
Developing thermoresponsive p(NIPAAm-HMAAm) electrospun nanofibers for on-demand drug release of doxorubicin 制备热敏p(NIPAAm-HMAAm)电纺丝纳米纤维用于阿霉素按需释放
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-04 DOI: 10.1016/j.jddst.2025.107244
Adriana Gonçalves , Susete N. Fernandes , A. Sofia Pádua , Jorge Carvalho Silva , João Paulo Borges , Miguel Castilho , Paula I.P. Soares
{"title":"Developing thermoresponsive p(NIPAAm-HMAAm) electrospun nanofibers for on-demand drug release of doxorubicin","authors":"Adriana Gonçalves ,&nbsp;Susete N. Fernandes ,&nbsp;A. Sofia Pádua ,&nbsp;Jorge Carvalho Silva ,&nbsp;João Paulo Borges ,&nbsp;Miguel Castilho ,&nbsp;Paula I.P. Soares","doi":"10.1016/j.jddst.2025.107244","DOIUrl":"10.1016/j.jddst.2025.107244","url":null,"abstract":"<div><div>On-demand drug delivery carriers enable a controlled and localized release of chemotherapeutic drugs, reducing the severe side effects associated with their systemic administration. Thermoresponsive drug delivery vehicles are particularly interesting due to their ability to perform remote-controlled targeted drug release in response to a temperature variation. This study presents the synthesis of a thermoresponsive copolymer, poly (N-isopropylacrylamide-co-hydroxymethylacrylamide), p (NIPAAm-HMAAm), and its processing via electrospinning for localized and on-demand drug release. The polymer's lower critical solution temperature (LCST) was tuned to approximately 40 °C, allowing remote control over its conformational structure under physiological conditions. Fibers crosslinked at 150 °C retained up to 70 % of their initial weight after 28 days in PBS. Swelling assays showed a 20-fold increase in membrane weight after immersion in PBS at 25 °C, which decreased approximately 10 times when the temperature exceeded the LCST by 10 °C, confirming thermoresponsiveness. Doxorubicin release from the fibers is significantly influenced by their crosslinking time and is enhanced at temperatures above the LCST, in acidic tumor conditions (pH 6.5). Additionally, temperature cycles further enhanced drug release by 10 % following the initial burst release, under acidic conditions. Thermoresponsive membranes exhibited no signs of cytotoxicity to PC3 cells, and <em>in vitro</em> drug release studies revealed that DOX-loaded membranes reduced cell viability below 80 % at a released concentration of approximately 5 μg mL<sup>−1</sup>. The results highlight the potential of p (NIPAAm-HMAAm) fibers as effective thermoresponsive carriers for localized, on-demand drug delivery in the postoperative treatment of solid tumors.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107244"},"PeriodicalIF":4.5,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144579653","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}
引用次数: 0
Optimized PEGylated carbon nanotubes for enhanced drug delivery and antimicrobial performance against gram-negative bacteria 优化聚乙二醇碳纳米管增强药物传递和抗革兰氏阴性细菌的抗菌性能
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-04 DOI: 10.1016/j.jddst.2025.107249
Jasra Gul , Samina Perveen , Shahida Muhammad Habib , Asia Naz Awan , Muhammad Raza Shah
{"title":"Optimized PEGylated carbon nanotubes for enhanced drug delivery and antimicrobial performance against gram-negative bacteria","authors":"Jasra Gul ,&nbsp;Samina Perveen ,&nbsp;Shahida Muhammad Habib ,&nbsp;Asia Naz Awan ,&nbsp;Muhammad Raza Shah","doi":"10.1016/j.jddst.2025.107249","DOIUrl":"10.1016/j.jddst.2025.107249","url":null,"abstract":"<div><div>Primary challenges in antibiotic treatment include misuse and overuse, adverse effects, multidrug resistance, potential allergic reactions, improper administration, and lack of new therapeutic development. Approximately two-thirds of bacterial infections are linked with biofilm formation. <em>Escherichia coli</em> (<em>E. coli</em>) and <em>Pseudomonas aeruginosa</em> (<em>P. aeruginosa</em>) are the most common prevalent gram-negative pathogens associated with biofilm formation in medical devices. However, improving the potency of existing antibacterial agents <em>via</em> combination therapy and other nanotechnology-based drug delivery strategies can accelerate drug development. In this study, we developed ceftriaxone (CFT) loaded on PEG functionalized multi-wall carbon nanotubes (PEG-OMC) nanocomposite to enhance its efficacy against <em>E. coli</em> and <em>P. aeruginosa</em>. The carbon nanotubes (CNTs) were initially oxidized and subsequently functionalized <em>via</em> ester coupling and drug entrapment to obtain the nanoformulation (CFT-PEG-OMC) which were further characterized using TGA, SEM, FTIR, % Entrapment Efficiency (%EE), DLS, <em>in vitro</em> drug release study, bacterial biofilm morphology <em>via</em> AFM as well as cytotoxic and antibacterial evaluation. The findings demonstrated that CFT-PEG-OMC showed maximum drug %EE, nano-range hydrodynamic size, negative surface charge with low PDI, and enhanced thermal stability as compared to its counterparts. FTIR analysis of the CFT-PEG-OMC confirmed the possible molecular interaction between the CFT and PEG-OMC. The designed formulation showed prolonged drug release and non-cytotoxicity against normal cell lines (NIH/3T3 cells). The antibacterial studies of CFT-PEG-OMC against gram-negative bacteria showed improved bactericidal potency as compared to pure CFT. Additionally, AFM microscopy confirmed morphological disruption and damage to the bacterial cell surfaces following treatment with CFT-PEG-OMC. The findings of this study confirmed the applicability of the developed CFT-PEG-OMC nanoformulation for enhanced antibacterial activity of CFT against gram-negative bacteria.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107249"},"PeriodicalIF":4.5,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144613776","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}
引用次数: 0
Optimization and bactericidal inhibitory activities of nanostructured lipid carrier-mediated Co-delivery of myricetin and amoxicillin for eradication of Helicobacter pylori in vitro 纳米结构脂质载体介导的杨梅素和阿莫西林共递送体外根除幽门螺杆菌的优化和杀菌抑制活性
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-04 DOI: 10.1016/j.jddst.2025.107233
Tehsin Ullah Khan , Qiao Shiyue , Mohamed Sharaf , Busati Ahmed , Zhe Chi , Chen-Guang Liu
{"title":"Optimization and bactericidal inhibitory activities of nanostructured lipid carrier-mediated Co-delivery of myricetin and amoxicillin for eradication of Helicobacter pylori in vitro","authors":"Tehsin Ullah Khan ,&nbsp;Qiao Shiyue ,&nbsp;Mohamed Sharaf ,&nbsp;Busati Ahmed ,&nbsp;Zhe Chi ,&nbsp;Chen-Guang Liu","doi":"10.1016/j.jddst.2025.107233","DOIUrl":"10.1016/j.jddst.2025.107233","url":null,"abstract":"<div><div><em>Helicobacter pylori</em> is a major contributor to peptic ulcer disease and gastric cancer, with rising global infection rates. This study explores the potential of optimized nanostructured lipid carriers (NLCs) loaded with Myr and AMO as a co-delivery system, Notably, the unloaded NLCs themselves exhibited intrinsic bactericidal activity against <em>H. pylori</em>, highlighting their potential as both a drug carrier and an active antibacterial agent<em>,</em> offering a promising alternative to combat antibiotic-resistant infections. The formulation was optimized using the Box-Behnken design (BBD) technique, taking into account three AIVs (particle size, PDI, and zeta potential) and three CIVs (solid lipid concentration, liquid lipid concentration, and surfactant concentration). The optimized unloaded NLCs had a particle size of ∼86 nm, PDI of 0.343, and ZP of −18.8 mV. The Myr-AMO@NLCs had a particle size of ∼140 nm, PDI of 0.353, and ZP of −32.9 mV, with encapsulation efficiencies of 85 % for Myr and 90 % for AMO. Transmission electron microscopy (TEM) confirmed the spherical shape and surface characteristics of both unloaded and loaded NLCs. Continuous release of Myr over 72 h indicated long-term therapeutic efficacy. Myr-AMO@NLCs demonstrated significantly enhanced antibacterial activity against <em>H. pylori</em> 26995 (p &lt; 0.01), outperforming unloaded NLCs and pure drugs (p &lt; 0.05). Bioimaging studies, including scanning electron microscopy (SEM), confocal light scattering microscopy (CLSM), and flow cytometry, showed that NLCs adhered to the bacterial membrane, causing membrane disruption, cytoplasmic leakage, and enzyme inhibition. The simultaneous delivery of Myr and AMO using NLCs is an effective strategy to combat <em>H. pylori</em> infections, with promising potential as an alternative treatment.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107233"},"PeriodicalIF":4.5,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144605813","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}
引用次数: 0
Microbubble encapsulation of monocarboxylate transporter 1 inhibitor AZD3965 for ultrasound mediated delivery to head and neck squamous cell carcinoma 微泡包封单羧酸转运蛋白1抑制剂AZD3965用于超声介导给药头颈部鳞状细胞癌
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-04 DOI: 10.1016/j.jddst.2025.107245
Brian E. Oeffinger , Valeria Arango-Aliaga , Corinne E. Wessner , Hebah Falatah , Quezia Lecerda , Ankit S. Patel , Gagan Kaushal , Ji-Bin Liu , Ubaldo E. Martinez-Outschoorn , John R. Eisenbrey , Margaret A. Wheatley , Joseph M. Curry
{"title":"Microbubble encapsulation of monocarboxylate transporter 1 inhibitor AZD3965 for ultrasound mediated delivery to head and neck squamous cell carcinoma","authors":"Brian E. Oeffinger ,&nbsp;Valeria Arango-Aliaga ,&nbsp;Corinne E. Wessner ,&nbsp;Hebah Falatah ,&nbsp;Quezia Lecerda ,&nbsp;Ankit S. Patel ,&nbsp;Gagan Kaushal ,&nbsp;Ji-Bin Liu ,&nbsp;Ubaldo E. Martinez-Outschoorn ,&nbsp;John R. Eisenbrey ,&nbsp;Margaret A. Wheatley ,&nbsp;Joseph M. Curry","doi":"10.1016/j.jddst.2025.107245","DOIUrl":"10.1016/j.jddst.2025.107245","url":null,"abstract":"<div><div>Many solid tumors, including head and neck squamous cell carcinoma (HNSCC), are characterized by the dysregulation of metabolic functions, including accelerated glycolysis. This results in accumulation of intracellular lactate, which in turn leads to an increased expression of monocarboxylate transporters (MCT) family members to export lactate. The MCT 1 inhibitor AZD3965 has been developed as a targeted therapy, as it can increase intracellular lactate concentration resulting in tumor cell death, however translation into clinical trials has been challenging due to off target toxicity. The goal of this work was to develop a platform for targeted delivery of AZD3965 utilizing a surfactant stabilized microbubble (SE61) and ultrasound. AZD3965 was successfully loaded into SE61, resulting in a microbubble mean size of 1.58 ± 0.08 μm, a mean microbubble concentration of 5.58 ± 1.44 × 10<sup>8</sup> microbubbles/mL and an average AZD3965 loading of 45.2 ± 3.5 μg/mL of SE61 microbubbles. The initial tolerability and ability to improve tumor control by ultrasound mediated microbubble delivery of the MCT 1 inhibitor to HNSCC tumor model was also evaluated <em>in vivo</em>. SE61 microbubbles loaded with AZD3965 were well tolerated, were imaged and successfully destroyed at tumor sites using ultrasound. Future studies will likely require a combination of multiple treatment doses, increased drug loading, and/or multiple inhibitors as no significant tumor response to treatment was observed <em>in vivo</em>. Overall, this study showed the feasibility of loading the MCT 1 inhibitor AZD3965 onto the SE61 microbubble platform for targeted ultrasound mediated delivery to HNSCC.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107245"},"PeriodicalIF":4.5,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144571016","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}
引用次数: 0
Quercetin-magnesium nanoparticles as a multifunctional nanoplatform for wound Healing: Modulating macrophage polarization and promoting angiogenesis 槲皮素-镁纳米颗粒作为伤口愈合的多功能纳米平台:调节巨噬细胞极化和促进血管生成
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-03 DOI: 10.1016/j.jddst.2025.107246
Saige Meng , Guangzhou Zhao , De-zhi Lu , Shandan Ouyang
{"title":"Quercetin-magnesium nanoparticles as a multifunctional nanoplatform for wound Healing: Modulating macrophage polarization and promoting angiogenesis","authors":"Saige Meng ,&nbsp;Guangzhou Zhao ,&nbsp;De-zhi Lu ,&nbsp;Shandan Ouyang","doi":"10.1016/j.jddst.2025.107246","DOIUrl":"10.1016/j.jddst.2025.107246","url":null,"abstract":"<div><div>Effective wound healing requires the regulation of oxidative stress, inflammation, and angiogenesis. In this study, we developed quercetin-magnesium nanoparticles (Que-Mg NPs) as a multifunctional nanoplatform to modulate macrophage polarization and enhance vascular regeneration for improved wound healing. The nanoparticles were synthesized <em>via</em> metal-polyphenol coordination, exhibiting a uniform size of approximately 50 nm and pH-responsive drug release, which facilitated accelerated quercetin release under acidic conditions. <em>In vitro</em> studies demonstrated that Que-Mg NPs possessed excellent biocompatibility, effectively scavenged reactive oxygen species, and alleviated oxidative stress-induced cellular damage. Moreover, Que-Mg NPs significantly downregulated pro-inflammatory cytokines (TNF-α, IL-1β, IL-6), while upregulating the anti-inflammatory cytokine IL-10, indicating potent immunoregulatory effects. Furthermore, Que-Mg NPs promoted macrophage polarization toward the M2 phenotype and enhanced their phagocytic function, contributing to an anti-inflammatory microenvironment conducive to tissue repair. Additionally, Que-Mg NPs facilitated endothelial cell migration and tube formation, potentially activating the VEGF signaling pathway to stimulate angiogenesis. Collectively, these findings highlight the potential of Que-Mg NPs as a promising nanotherapeutic strategy for wound healing by simultaneously modulating oxidative stress, inflammation, and vascular regeneration.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107246"},"PeriodicalIF":4.5,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144557601","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}
引用次数: 0
Development and evaluation of niosomes containing amphotericin B and clove oil for the improvement of antifungal and antiparasitic therapies 含有两性霉素B和丁香油的ni质体的开发和评价,以提高抗真菌和抗寄生虫的治疗效果
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-03 DOI: 10.1016/j.jddst.2025.107243
Tatielle do Nascimento , Verônica da Silva Cardoso , Ralph Santos-Oliveira , Debora Ferreira Barreto-Vieira , Alane Beatriz Vermelho , Eduardo Ricci-Júnior
{"title":"Development and evaluation of niosomes containing amphotericin B and clove oil for the improvement of antifungal and antiparasitic therapies","authors":"Tatielle do Nascimento ,&nbsp;Verônica da Silva Cardoso ,&nbsp;Ralph Santos-Oliveira ,&nbsp;Debora Ferreira Barreto-Vieira ,&nbsp;Alane Beatriz Vermelho ,&nbsp;Eduardo Ricci-Júnior","doi":"10.1016/j.jddst.2025.107243","DOIUrl":"10.1016/j.jddst.2025.107243","url":null,"abstract":"<div><div>Nanotechnology has been used to encapsulate drugs in nanosystems, increasing therapeutic efficacy and reducing adverse effects. Niosomes can be used to encapsulate lipophilic drugs and facilitate their solubilization in aqueous media. Potential drugs for encapsulation have problems with their physicochemical characteristics, such as low water solubility and poor bioavailability. One of these drugs is amphotericin B, a broad-spectrum antifungal agent widely used in the treatment of infectious diseases. The main objectives of this work are to develop niosomes containing amphotericin B and clove oil, and to evaluate its antileishmania and anticandida activities. Niosomes were produced by the lipid film hydration method, using poloxamer 184 and tween 80® as non-ionic surfactants, as well as cholesterol and clove oil to stabilize the system. Vesicles with a size of around 70 nm and a polydispersity index below 0.2 were obtained. The amphotericin B encapsulation content was 92.3 % ± 4.3684. The <em>in vitro</em> release test demonstrated a prolonged release profile, with approximately 15 % of the drug released from the niosomes within 72 h. Stability studies confirmed that niosomes are most stable at temperatures around 8 °C, maintaining their size and polydispersity index for 150 days. <em>In vitro</em> results showed that the encapsulation of amphotericin in niosomes containing clove oil increased the efficacy of the drug by decreasing the mean inhibitory concentration in tests with <em>Candida</em> and <em>Leishmania</em> species (<em>C. albicans</em>, <em>C.</em> auris, <em>L. amazonensis</em> and <em>L. infantum</em>). Cytotoxicity tests showed that niosomes were less toxic to macrophages when compared to the free form of amphotericin.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107243"},"PeriodicalIF":4.5,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144570936","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}
引用次数: 0
Dissolution enhancement of indapamide in binary and ternary stable combinations with perindopril and amlodipine drugs in oral tablets 吲达帕胺与培哚普利、氨氯地平二、三元稳定联合口服片剂溶出度的提高
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-03 DOI: 10.1016/j.jddst.2025.107239
Sami Jebali , Sana Yakoubi , Emna Amira , Monia Ouni , Haykel Galai
{"title":"Dissolution enhancement of indapamide in binary and ternary stable combinations with perindopril and amlodipine drugs in oral tablets","authors":"Sami Jebali ,&nbsp;Sana Yakoubi ,&nbsp;Emna Amira ,&nbsp;Monia Ouni ,&nbsp;Haykel Galai","doi":"10.1016/j.jddst.2025.107239","DOIUrl":"10.1016/j.jddst.2025.107239","url":null,"abstract":"<div><div>Management of hypertension often requires a combination therapy approach, with fixed-dose formulations supporting patient adherence for better outcomes. However, some challenges need addressing concerning their solubility, the limitations posed by dissolution rates, and the possible drug-drug interaction, the key obstacles in optimizing the efficacy and the stability of these formulations. This study evaluates the physicochemical stability and solubility enhancement of indapamide in mono formulation as well as the combined form with perindopril and amlodipine. A rapid UPLC-DAD method was established and validated for profiling dissolution across three media mimicking physiological pH: 1.2, 4.5, and 6.8. The best separation was performed using a Waters UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm) in a run time less than 3 min, the mobile phase was optimized to a 65:35 (v/v) ratio of 0.1 % trifluoroacetic acid in water (pH = 2) and acetonitrile. Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) techniques were utilized to assess physical and chemical stability while molecular docking simulations offered insight into drug-drug interactions as well as toxicity risks associated. For solubility enhancement and bioavailability improvement of indapamide, two amorphization techniques, quench cooling and milling, were investigated. The relative bioavailability was notably increased with the co-formulation of indapamide (BCS II) with perindopril (BCS III) and amlodipine (BCS I); in conjunction, stability studies assessed that no significant degradation or adverse interaction has taken place. Computational modeling elaborated on the contributions of hydrogen bonding and hydrophobic interactions to a combined formulation stability and pharmacokinetic behavior. These will provide insight necessary for a rational design of fixed-dose combinations for the treatment of hypertension: enhanced bioavailability, stability, and therapeutic efficacy.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107239"},"PeriodicalIF":4.5,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144570933","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}
引用次数: 0
Eprosartan loaded mesoporous silica nanoparticles embedded in mucoadhesive buccal films: A strategy for improved bioavailability 负载依伯沙坦的介孔二氧化硅纳米颗粒嵌入黏附口腔膜:一种提高生物利用度的策略
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-03 DOI: 10.1016/j.jddst.2025.107248
Menna M. Abdellatif , Rana M. Gebreel
{"title":"Eprosartan loaded mesoporous silica nanoparticles embedded in mucoadhesive buccal films: A strategy for improved bioavailability","authors":"Menna M. Abdellatif ,&nbsp;Rana M. Gebreel","doi":"10.1016/j.jddst.2025.107248","DOIUrl":"10.1016/j.jddst.2025.107248","url":null,"abstract":"<div><div>Eprosartan is a selective angiotensin receptor blocker used to treat essential hypertension. However, it has a low oral bioavailability of only 13 % as it is categorized as BCS class II and undergoes first-pass metabolism. Therefore, incorporating eprosartan into mesoporous silica nanoparticles (MSNs)-loaded buccal film might augment its bioavailability. The MSNs were formulated using the incipient wetness method, and an I-optimal design was utilized for optimization purposes. The independent variables were the drug-to-mesoporous silica ratio and the type of mesoporous silica. The entrapment efficiency percent (EE %), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and percentage of drug released after 6 h (Q6 %) were assessed. The optimized MSNs formula was assessed by evaluating its morphology, Fourier-transform infrared spectroscopy (FTIR), and thermal analysis. Then, the optimized MSNs formula was embedded into a mucoadhesive buccal film, which was characterized via ex vivo permeation and pharmacokinetics studies. The optimized MSNs formula was spherical and had EE % of 99.50 ± 0.54 %, PS of 197.9 ± 2.2 nm, PDI of 0.442 ± 0.008, ZP of −16.21 ± 0.87 mV, and Q6 % of 93.00 ± 1.9 %. The FTIR ensured the drug's uptake by the porous structure, while thermal analysis confirmed its amorphous state after loading into MSNs. The MSNs-loaded buccal film augmented the apparent permeability coefficient by 4.88 folds compared to free-drug film. The C<sub>max</sub> and AUC<sub>0-t</sub> of MSNs-loaded buccal film were 2.88-fold and 2.63-fold, respectively, compared to the oral eprosartan, while the T<sub>max</sub> was shortened to 0.5 h instead of 1 h. This study confirmed the capability of MSNs-loaded buccal film to enhance the bioavailability of eprosartan.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107248"},"PeriodicalIF":4.5,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144562873","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}
引用次数: 0
Development and evaluation of fusidic acid myrrh oil organogel for the reversal of Gram-negative bacterial resistance and improvement of wound-healing potential 富西地酸没药油有机凝胶逆转革兰氏阴性菌耐药和提高创面愈合潜力的研制与评价
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-07-03 DOI: 10.1016/j.jddst.2025.107247
Faisal R. Aljohani , Amer A. Alanazi , Abdulelah Z.A. Albalawi , Ghareb M. Soliman , Mona Qushawy , Mona F. Arafa , Nehal Elsherbiny , Huda M. Atif , Helal F. Hetta , Yasmin N. Ramadan , Mohamed A. Safwat , Mohamed M. Badran , Ayman Salama
{"title":"Development and evaluation of fusidic acid myrrh oil organogel for the reversal of Gram-negative bacterial resistance and improvement of wound-healing potential","authors":"Faisal R. Aljohani ,&nbsp;Amer A. Alanazi ,&nbsp;Abdulelah Z.A. Albalawi ,&nbsp;Ghareb M. Soliman ,&nbsp;Mona Qushawy ,&nbsp;Mona F. Arafa ,&nbsp;Nehal Elsherbiny ,&nbsp;Huda M. Atif ,&nbsp;Helal F. Hetta ,&nbsp;Yasmin N. Ramadan ,&nbsp;Mohamed A. Safwat ,&nbsp;Mohamed M. Badran ,&nbsp;Ayman Salama","doi":"10.1016/j.jddst.2025.107247","DOIUrl":"10.1016/j.jddst.2025.107247","url":null,"abstract":"<div><div>Bacterial resistance to antibiotics remains a major challenge, reducing the effectiveness of affected antibiotics and posing a serious risk to patient health. Fusidic acid (FA) is an antibiotic with pleiotropic beneficial properties, including antibacterial, antioxidant, and anti-inflammatory. However, the inherent resistance of Gram-negative bacteria limits its wound-healing efficacy. This study aimed to tackle this hurdle and improve its wound-healing properties through formulation with myrrh oil into an organogel formulation, taking advantage of their shared beneficial pharmacological properties. Three organogelators with three concentrations each, were tested to reach an optimum formulation in terms of stability and drug delivery attributes. The optimum formulation containing Span 60 had a shear thinning behavior and good spreadability. It sustained FA release, enhanced its antibacterial activity against Gram-positive bacteria compared with FA alone, myrrh oil alone or the commercial FA cream. Additionally, this formulation reversed the inherent Gram-negative bacterial resistance. <em>In vivo</em> wound-healing studies in a rat wound model revealed improved efficacy compared with myrrh oil organogel and the commercial FA cream. A series of pharmacodynamics studies revealed that these improved wound-healing properties were due to the combined antibacterial, antioxidant, and anti-inflammatory properties of FA and myrrh oil. They also improved collagen deposition and cellular proliferation in the wound area. These results suggest that combining natural active ingredients, such as myrrh oil, with FA in a single formulation could have improved wound healing and antibacterial properties, thereby increasing their potential for combating bacterial resistance and treating chronic wounds.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"112 ","pages":"Article 107247"},"PeriodicalIF":4.5,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144596150","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}
引用次数: 0
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