RSC Pharmaceutics最新文献

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Polymer-lipid hybrid nanoparticles co-encapsulating fucoxanthin and carbon dots for targeted anti-inflammatory therapy in Alzheimer's disease 聚合物-脂质混合纳米颗粒共包封岩藻黄素和碳点用于阿尔茨海默病的靶向抗炎治疗
RSC Pharmaceutics Pub Date : 2026-03-19 DOI: 10.1039/D6PM00008H
J. Horacio Silvestre-Martínez, Lorna G. Yañez-Algandar, Karina del Carmen Lugo-Ibarra and Ana B. Castro-Ceseña
{"title":"Polymer-lipid hybrid nanoparticles co-encapsulating fucoxanthin and carbon dots for targeted anti-inflammatory therapy in Alzheimer's disease","authors":"J. Horacio Silvestre-Martínez, Lorna G. Yañez-Algandar, Karina del Carmen Lugo-Ibarra and Ana B. Castro-Ceseña","doi":"10.1039/D6PM00008H","DOIUrl":"https://doi.org/10.1039/D6PM00008H","url":null,"abstract":"<p >Alzheimer's disease (AD) is a long-term brain disorder characterized by the buildup of proteins like amyloid-beta (Aβ) and Tau. This disease process can start up to 20 years before symptoms such as memory loss, language problems, changes in personality, and eventually dementia appear. Currently, AD has no cure, and available treatments only ease symptoms, making it a major global health concern. Developing new therapies is urgently needed. Nanomedicine presents promising solutions, especially for overcoming challenges like delivering drugs across the blood–brain barrier (BBB). In this study, we explored polymer-lipid hybrid nanoparticles (NPs) decorated with transferrin (Tf) to help them cross the BBB. These NPs were loaded with carbon dots (CDs) and fucoxanthin (Fx), which have antioxidant and anti-inflammatory qualities that may benefit neurodegenerative disease treatment. The resulting nanoparticle formulation (NPs-CDFx) had encapsulation efficiencies of 45% for Fx and 10% for CDs, with an average particle size of about 88.74 nm. The safety of these NPs was tested using an <em>in vitro</em> model with lipopolysaccharide (LPS) stimulated rat astrocytes, where high cell viability (92.18%) was observed. qPCR analysis showed that NPs-CDFx significantly lowered the expression of genes linked to neuroinflammation and disease progression, such as APP, GFAP, and S100β. To further confirm delivery, the NPs were injected into five-day-old zebrafish larvae, where confocal microscopy detected the CDs’ fluorescence in the brain, indicating successful targeted delivery across the BBB. Overall, these findings suggest that the nanoparticles can efficiently deliver therapeutic agents to the brain, reduce neuroinflammatory gene expression, and demonstrate the effectiveness of polymer-lipid hybrid nanoparticles for targeted brain drug delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 669-681"},"PeriodicalIF":0.0,"publicationDate":"2026-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d6pm00008h?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011766","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Kinetic modelling and in vitro release mechanism of levodopa from sporopollenin-based microcapsules in human blood plasma 左旋多巴微胶囊在人血浆中的动力学模型及体外释放机制
RSC Pharmaceutics Pub Date : 2026-03-10 DOI: 10.1039/D5PM00261C
Shwan Abdullah Hamad, Zhila Salam Othman, Shilan Hiwa Hama Salih and Trefa Mohammed Abdullah
{"title":"Kinetic modelling and in vitro release mechanism of levodopa from sporopollenin-based microcapsules in human blood plasma","authors":"Shwan Abdullah Hamad, Zhila Salam Othman, Shilan Hiwa Hama Salih and Trefa Mohammed Abdullah","doi":"10.1039/D5PM00261C","DOIUrl":"https://doi.org/10.1039/D5PM00261C","url":null,"abstract":"<p >Levodopa (LD) remains the most effective therapy for Parkinson's disease; however, its short plasma half-life necessitates frequent dosing and contributes to fluctuating drug levels and motor complications. In this study, we systematically investigated the <em>in vitro</em> release behaviour of LD from sporopollenin exine microcapsules (SECs) in a clinically relevant biological medium, human blood plasma, and applied kinetic modelling to elucidate the governing release mechanism. LD-loaded sporopollenin microcapsules (0.5 g) were prepared by vacuum-assisted, pH-triggered precipitation and incubated in human plasma at 37 °C under moderate agitation (50 rpm). Release experiments were conducted over 12 h, with sequential sampling and medium replacement to maintain constant volume and sink conditions. LD concentrations were quantified by UV-Vis spectrophotometry using validated plasma-matched calibration curves. The release profile exhibited a reproducible biphasic pattern, characterised by a rapid initial phase within the first 30 min, followed by a prolonged and stable release phase extending to 12 h. Despite low fractional release, the system rapidly established a therapeutically relevant equilibrium LD concentration in plasma, indicative of reservoir-controlled drug availability rather than depletion-driven release. Kinetic modelling demonstrated that the Higuchi model provided the best fit to the concentration-time data (<em>R</em><small><sup>2</sup></small> = 0.9955 ± 0.0008). In contrast, the Korsmeyer–Peppas model yielded a low release exponent (<em>n</em> = 0.209 ± 0.002), consistent with diffusion-dominated, Fickian transport. Peppas–Sahlin analysis further confirmed the predominance of diffusional mechanisms, with minimal contribution from matrix relaxation. These findings demonstrate that SECs function as stable, reservoir-type carriers that provide both rapid initial LD availability and sustained plasma concentrations under physiologically relevant conditions. This work, to our knowledge, represents the first detailed kinetic analysis of LD release from SECs in human blood plasma and highlights the potential of this natural biopolymer as a bio-regulated platform for improved LD delivery in Parkinson's disease.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 799-808"},"PeriodicalIF":0.0,"publicationDate":"2026-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00261c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Needle-free transdermal delivery of mRNA vaccine with ionic liquid crystals and effective tumor growth inhibition 离子液晶mRNA疫苗的无针透皮递送和有效的肿瘤生长抑制
RSC Pharmaceutics Pub Date : 2026-03-10 DOI: 10.1039/D5PM00327J
Tomohiro Higashi, Keisuke Tanaka, Kiyohiro Toyofuku, Rie Wakabayashi, Yoshirou Kawaguchi, Noriho Kamiya and Masahiro Goto
{"title":"Needle-free transdermal delivery of mRNA vaccine with ionic liquid crystals and effective tumor growth inhibition","authors":"Tomohiro Higashi, Keisuke Tanaka, Kiyohiro Toyofuku, Rie Wakabayashi, Yoshirou Kawaguchi, Noriho Kamiya and Masahiro Goto","doi":"10.1039/D5PM00327J","DOIUrl":"https://doi.org/10.1039/D5PM00327J","url":null,"abstract":"<p >mRNA vaccines have emerged as a promising therapeutic option based on their ability to elicit a strong immune response, the reduced risk of genomic integration, and the potential to produce various vaccine candidates using the same manufacturing process. However, current mRNA vaccines primarily rely on injection-based administration, which is an invasive procedure that requires a healthcare professional. To address these limitations, transdermal delivery has been proposed as a non-invasive alternative. However, the stratum corneum (SC) acts as a formidable barrier to biopharmaceuticals penetration, necessitating innovative approaches for effective transdermal vaccination. In this study, we developed a novel ionic liquid crystal (ILC), which was formulated from a lyotropic liquid crystal (LLC) using ionic liquids (ILs) with amphiphilic molecular properties. ILC formulations were prepared by mixing ILs with ultrapure water and demonstrated optimal viscoelastic properties for transdermal application. <em>In vitro</em> skin permeation assays revealed the superior mRNA penetration of ILC formulations compared with aqueous mRNA solutions. Furthermore, <em>in vivo</em> evaluation using a tumor-bearing mouse model revealed that transdermal mRNA delivery <em>via</em> ILCs significantly suppressed tumor growth and promoted CD8+ T-cell infiltration into tumor tissues, indicating a potent antitumor effect. These findings highlight the potential of ILC-based transdermal mRNA delivery as a promising strategy for the development of next-generation mRNA vaccine administration methods.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 659-668"},"PeriodicalIF":0.0,"publicationDate":"2026-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00327j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
QbD-optimized HA–Pluronic nanomicelles for the targeted repurposing of tofacitinib in breast cancer qbd优化的HA-Pluronic纳米胶束用于靶向重新利用托法替尼治疗乳腺癌
RSC Pharmaceutics Pub Date : 2026-03-06 DOI: 10.1039/D5PM00391A
Suchita Waghmare, Rohini Palekar, Pratiksha Bramhe, Nilesh Rarokar and Pramod Khedekar
{"title":"QbD-optimized HA–Pluronic nanomicelles for the targeted repurposing of tofacitinib in breast cancer","authors":"Suchita Waghmare, Rohini Palekar, Pratiksha Bramhe, Nilesh Rarokar and Pramod Khedekar","doi":"10.1039/D5PM00391A","DOIUrl":"https://doi.org/10.1039/D5PM00391A","url":null,"abstract":"<p >Tofacitinib, a Janus kinase (JAK) inhibitor clinically approved for rheumatoid arthritis, holds significant potential for repurposing in breast cancer therapy due to its ability to suppress the oncogenic STAT3 signaling pathway; however, its therapeutic application is hindered by poor aqueous solubility, rapid systemic clearance, and non-specific distribution. To address these limitations, this study aimed to develop hyaluronic acid (HA)-decorated Pluronic F127 (PF127) micelles to enhance the solubility, bioavailability, and targeted delivery of Tofacitinib to CD44-overexpressing breast cancer cells. A Quality by Design (QbD) approach utilizing a Box–Behnken design (BBD) was employed to systematically optimize critical process parameters—drug-to-polymer ratio, polymer concentration, and stirring temperature—to minimize particle size and polydispersity index (PDI) while maximizing entrapment efficiency. The optimized micelles exhibited a uniform particle size of 159.2 ± 3.8 nm, a narrow PDI of 0.221, a high entrapment efficiency of 91.14%, and a negative zeta potential of −24.6 mV, ensuring colloidal stability. <em>In vitro</em> evaluation demonstrated a sustained, diffusion-controlled drug release profile and significantly enhanced cytotoxicity against MCF-7 breast cancer cells (IC<small><sub>50</sub></small> 14.2 µg mL<small><sup>−1</sup></small>) compared to the free drug (IC<small><sub>50</sub></small> 46.8 µg mL<small><sup>−1</sup></small>), attributed to CD44-mediated cellular uptake. Furthermore, <em>in vivo</em> pharmacokinetic analysis in Wistar rats revealed a 4.3-fold increase in oral bioavailability and a prolonged elimination half-life compared to free Tofacitinib, while histopathological studies confirmed the formulation's biocompatibility and safety in major organs. These findings collectively support the viability of the QbD-optimized HA–PF127 micellar system as a promising nanocarrier platform for the effective oral repurposing of Tofacitinib in breast cancer treatment.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 749-767"},"PeriodicalIF":0.0,"publicationDate":"2026-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00391a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011753","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
nor-MC3 and nor-KC2: cationic ionizable lipids for the delivery of therapeutic nucleic acids 非mc3和非kc2:用于输送治疗性核酸的阳离子电离脂质
RSC Pharmaceutics Pub Date : 2026-03-04 DOI: 10.1039/D5PM00350D
Deaglan Arnold, Nagavenkata Durga Prasad Atmuri, Fariba Saadati, Ardalan Nabi, Daniel Z. Kurek, Anthony Tam, Taniya Adak, Dominik Witzigmann, Glenn Sammis, Pieter R. Cullis, Jayesh Kulkarni and Marco A. Ciufolini
{"title":"nor-MC3 and nor-KC2: cationic ionizable lipids for the delivery of therapeutic nucleic acids","authors":"Deaglan Arnold, Nagavenkata Durga Prasad Atmuri, Fariba Saadati, Ardalan Nabi, Daniel Z. Kurek, Anthony Tam, Taniya Adak, Dominik Witzigmann, Glenn Sammis, Pieter R. Cullis, Jayesh Kulkarni and Marco A. Ciufolini","doi":"10.1039/D5PM00350D","DOIUrl":"https://doi.org/10.1039/D5PM00350D","url":null,"abstract":"<p > <em>nor</em>-MC3 and <em>nor</em>-KC2, analogues of D-Lin-MC3-DMA (cationic ionizable lipid in Onpattro®) and D-Lin-KC2-DMA (valuable research tool) wherein C<small><sub>17</sub></small> lipophilic chains replace C<small><sub>18</sub></small> ones, are at least as efficacious as the originals, but more economical and safer to produce.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 654-658"},"PeriodicalIF":0.0,"publicationDate":"2026-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00350d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011764","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Advancing sustainability through digitalization: from drug development to patient care 通过数字化推进可持续发展:从药物开发到患者护理
RSC Pharmaceutics Pub Date : 2026-02-19 DOI: 10.1039/D5PM00342C
Remo Eugster and Paola Luciani
{"title":"Advancing sustainability through digitalization: from drug development to patient care","authors":"Remo Eugster and Paola Luciani","doi":"10.1039/D5PM00342C","DOIUrl":"https://doi.org/10.1039/D5PM00342C","url":null,"abstract":"<p >Digitalization is transforming the pharmaceutical industry, offering innovative solutions to enhance sustainability across the pharmaceutical value chain. From drug discovery to patient care, digital tools such as artificial intelligence (AI), machine learning (ML), blockchain, and digital twins optimize processes, reduce resource use, and mitigate environmental and social impacts. In drug discovery, AI accelerates and optimizes research while green chemistry initiatives prevent toxic waste. During manufacturing, predictive maintenance and quality control boost efficiency, and digital tools ensure secure, traceable distribution and enhance supply chain transparency. Within clinical care, AI-driven personalized medicine improves patient outcomes and reduces inefficiencies, while digital health records, diagnostics, and therapies promote healthcare equity and expand access. Collectively, these innovations align the industry with global sustainability goals, advancing a pharmaceutical ecosystem that is more efficient, environmentally responsible, and socially just. Yet challenges in energy demand, data equity, and regulatory adaptation must be addressed to tap into the full potential of a digital transformation.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 361-373"},"PeriodicalIF":0.0,"publicationDate":"2026-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00342c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Redesigning valproic acid therapy in pregnancy: intranasal liposomes for targeted maternal treatment 妊娠期丙戊酸治疗的重新设计:鼻内脂质体用于孕妇的靶向治疗
RSC Pharmaceutics Pub Date : 2026-02-17 DOI: 10.1039/D5PM00329F
Bruna Corradetti, Luigi C. Zangari, Francesco Mainardi, Tamara Pezzotta, Richard H. Finnell and Francesca Taraballi
{"title":"Redesigning valproic acid therapy in pregnancy: intranasal liposomes for targeted maternal treatment","authors":"Bruna Corradetti, Luigi C. Zangari, Francesco Mainardi, Tamara Pezzotta, Richard H. Finnell and Francesca Taraballi","doi":"10.1039/D5PM00329F","DOIUrl":"https://doi.org/10.1039/D5PM00329F","url":null,"abstract":"<p >Valproic acid (VPA) is a potent antiseizure medication and mood stabilizer, yet its teratogenicity severely limits safe use during pregnancy. Despite guidelines advising against VPA use in women of reproductive age, it remains indispensable for certain drug-resistant epilepsies, highlighting the urgent need for safer and more targeted delivery strategies. Intranasal (IN) administration <em>via</em> nanocarriers represents a promising approach to enhance brain uptake while minimizing systemic exposure and placental transfer. In this review, we evaluate the scientific rationale and translational potential of IN nanoformulations of VPA specifically designed for use during pregnancy. We discuss strategies to engineer nanocarriers that achieve effective maternal brain delivery while reducing fetal risk, and we analyze preclinical data on biodistribution, placental passage, and therapeutic efficacy. Importantly, we highlight how gestational changes in maternal physiology and placental architecture can inform the rational design of pregnancy-adapted nanocarriers. By integrating insights from nanotechnology, pharmacology, and maternal-fetal medicine, this review outlines a paradigm shift from drug avoidance to precision delivery that maximizes reproductive safety. This strategy not only addresses the unmet need for safer VPA use in pregnancy, but also establishes a versatile framework for broader applications of nanomedicine in neurological and systemic disorders in women of childbearing age.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 615-629"},"PeriodicalIF":0.0,"publicationDate":"2026-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00329f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011751","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dual centrifugation – a novel perspective on lipid nanoparticle formulation development 双重离心-在脂质纳米颗粒配方发展的新视角
RSC Pharmaceutics Pub Date : 2026-02-16 DOI: 10.1039/D5PM00287G
Valentin Bender, Leon Fuchs, Monika Köll-Weber, Jan Lembeck, Laurine Kaul, Regine Süss and Ulrich Massing
{"title":"Dual centrifugation – a novel perspective on lipid nanoparticle formulation development","authors":"Valentin Bender, Leon Fuchs, Monika Köll-Weber, Jan Lembeck, Laurine Kaul, Regine Süss and Ulrich Massing","doi":"10.1039/D5PM00287G","DOIUrl":"https://doi.org/10.1039/D5PM00287G","url":null,"abstract":"<p >The application of therapeutic RNAs, such as miRNAs, siRNAs, and mRNAs, has emerged as a promising therapeutic approach for treating diseases like cancer. Lipid nanoparticles (LNPs) are widely used for RNA delivery, typically produced using microfluidic mixing systems (MMS). However, MMS manufacturing is rather complex, time-consuming, and cost intensive. Dual centrifugation (DC), an in-vial homogenization technique, offers a straightforward, fast, and efficient alternative for preparing nanoscale lipid formulations, including LNPs. This study focuses on downscaling a DC-based LNP production method to enable 1 mg batch sizes, greatly reducing reagent consumption and allowing high-throughput research. Using a Design-of-Experiment (DoE) approach, key process parameters (lipid concentration, bead amount, and homogenization time) were optimized for small batches of LNPs formulated with cationic or ionizable lipids (DODMA, SM-102, ALC-0315). The optimized process was then applied to produce mRNA- and miRNA-loaded LNPs, which were evaluated for size, size distribution, encapsulation efficiency, and <em>in vitro</em> transfection performance. This work introduces DC as a novel and cost-efficient method for producing small-batch size LNPs, with satisfactory size characteristics and <em>in vitro</em> performance.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 711-725"},"PeriodicalIF":0.0,"publicationDate":"2026-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00287g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fucoidan/bis-MPA-based dendrimer nanoparticles with intrinsic anti-angiogenic activity for oncology applications 具有内在抗血管生成活性的岩藻聚糖/双mpa基树状聚合物纳米颗粒在肿瘤学中的应用
RSC Pharmaceutics Pub Date : 2026-02-12 DOI: 10.1039/D5PM00362H
Filipe Olim, Ana Duarte, Ana Rute Neves, Irene Rodriguez-Clemente, Joel T. Kidgell, Barbara C. Wimmer, Valentín Ceña and Helena Tomás
{"title":"Fucoidan/bis-MPA-based dendrimer nanoparticles with intrinsic anti-angiogenic activity for oncology applications","authors":"Filipe Olim, Ana Duarte, Ana Rute Neves, Irene Rodriguez-Clemente, Joel T. Kidgell, Barbara C. Wimmer, Valentín Ceña and Helena Tomás","doi":"10.1039/D5PM00362H","DOIUrl":"https://doi.org/10.1039/D5PM00362H","url":null,"abstract":"<p >Nanoparticles with intrinsic anti-angiogenic activity hold strong promise in cancer nanomedicine, as they can both help suppress metastasis and deliver therapeutics, offering a dual strategy for addressing the disease. In this study, fucoidans from <em>F. vesiculosus</em> and <em>U. pinnatifida</em> with two different molecular weights (<em>M</em><small><sub>W</sub></small>) of each were initially screened for <em>in vitro</em> anti-angiogenic potential using the tube formation assay with HUVEC cells. The higher <em>M</em><small><sub>W</sub></small> fucoidans, which represent native <em>M</em><small><sub>W</sub></small> fucoidan, exhibited greater anti-angiogenic activity and were subsequently combined with 2,2-bis(hydroxymethyl)propionic acid (bis-MPA)-based dendrimers (generation 2) at different fucoidan/dendrimer (F/D) mass ratios to form self-assembled nanoparticles through electrostatic interactions. Optimisation yielded two nanoparticle types with positive (F/D = 1 : 2) and negative (F/D = 2 : 1) zeta potentials, which were characterised for their physicochemical properties, including hydrodynamic diameter, zeta potential, chemical composition (FTIR), and morphology (TEM). These nanoparticles presented a near-spherical shape, were cytocompatible, and did not cause haemolysis. Positively charged nanoparticles showed stronger anti-angiogenic activity than negatively charged ones. Since the dendrimers alone were also anti-angiogenic, the overall effect likely results from the combined contribution of both components, with nanoparticle assembly potentially playing a role. Overall, these findings highlight the potential of fucoidan/dendrimer nanoparticles as multifunctional platforms for cancer nanomedicine, by targeting angiogenesis and potentially serving as drug or gene delivery systems.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 574-584"},"PeriodicalIF":0.0,"publicationDate":"2026-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00362h?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558503","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Reformulating lumefantrine as Flash NanoPrecipitated particles and the impact of incorporation into milk-based formulations on drug solubilisation during digestion 将氨苯曲明重新配制为闪速纳米沉淀颗粒,并将其掺入乳基配方中对消化过程中药物溶解的影响
RSC Pharmaceutics Pub Date : 2026-02-11 DOI: 10.1039/D5PM00294J
Malinda Salim, Kurt D. Ristroph, Thomas Eason, Gisela Ramirez, Andrew J. Clulow, Robert K. Prud'homme and Ben J. Boyd
{"title":"Reformulating lumefantrine as Flash NanoPrecipitated particles and the impact of incorporation into milk-based formulations on drug solubilisation during digestion","authors":"Malinda Salim, Kurt D. Ristroph, Thomas Eason, Gisela Ramirez, Andrew J. Clulow, Robert K. Prud'homme and Ben J. Boyd","doi":"10.1039/D5PM00294J","DOIUrl":"https://doi.org/10.1039/D5PM00294J","url":null,"abstract":"<p >Lumefantrine and artemether are currently used as one of the first line therapies for treatment of uncomplicated malaria. However, commercially-available lumefantrine/artemether tablets often result in poor and variable oral bioavailability due to low aqueous solubility of the drugs. To circumvent these issues, consumption of food containing lipids with the lumefantrine/artemether tablet(s) is recommended to increase exposure of the drugs, which brings high variability to the systemic drug exposure. In this study, we investigated the potential use of infant formula as a milk-based lipid formulation to improve the solubilisation of lumefantrine/artemether with controlled fat content, both as a formulation for the two drug substances as well as when co-dosed with lumefantrine after re-formulation into nanoparticles. Time-resolved synchrotron small angle X-ray scattering (SAXS) was used to probe the solubilisation behaviour of the drugs and high-performance liquid chromatography (HPLC) was used to quantify the amount of drugs dissolved during digestion. Findings from these studies suggest that the solubility of artemether in undigested and digested infant formula was greater than 5 fold relative to lumefantrine and that 5 g of fat was not sufficient to completely solubilise a 120 mg lumefantrine dose. When formulated as nanoparticles, there was evidence of slight lumefantrine crystallisation when the highly amorphous drug powder was added to infant formula but digestion did not appear to significantly affect the presence of crystalline lumefantrine. These findings suggest a potential reduced food effect for lumefantrine nanoparticles compared to the crystalline counterpart, further highlighting that lumefantrine nanoparticles may be orally administered in both fasted and fed conditions.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 564-573"},"PeriodicalIF":0.0,"publicationDate":"2026-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00294j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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