RSC Pharmaceutics最新文献

筛选
英文 中文
Rapid plasma membrane reorganisation and endocytosis in HER2 breast cancer cells incubated with trastuzumab decorated polymer nanoparticles 用曲妥珠单抗修饰的聚合物纳米颗粒培养HER2乳腺癌细胞的快速质膜重组和内吞作用
RSC Pharmaceutics Pub Date : 2026-02-10 DOI: 10.1039/D5PM00168D
Carwyn S. Hughes, Saeed Tayeb, Duncan Muir, Anthony J. Hayes, Peter Watson and Arwyn T. Jones
{"title":"Rapid plasma membrane reorganisation and endocytosis in HER2 breast cancer cells incubated with trastuzumab decorated polymer nanoparticles","authors":"Carwyn S. Hughes, Saeed Tayeb, Duncan Muir, Anthony J. Hayes, Peter Watson and Arwyn T. Jones","doi":"10.1039/D5PM00168D","DOIUrl":"https://doi.org/10.1039/D5PM00168D","url":null,"abstract":"<p >Knowledge on HER2+ breast cancer biology has informed drug design leading to targeted therapies giving improved clinical outcomes. Drug resistance and disease relapse, however still drive a continuous need for more efficacious and reliable therapeutics. Nanoparticles (NPs) as HER2 targeting nanomedicines offer new hope for selective targeting of HER2 within and beyond solid tumours, together with concomitant delivery of therapeutic cargo. For initial preclinical characterisation, studies on NP endocytosis and drug delivery are often performed in HER2+ breast cancer cell models, but information on initial NP-HER2 dynamics at the plasma membrane and how this impacts endocytic uptake and delivery efficiency is largely missing. Here using polymer poly(lactic-<em>co</em>-glycolide) acid NPs decorated with different valencies of the HER2 targeting monoclonal antibody trastuzumab, we have designed approaches to immediately study the impact of NP-HER2 targeting on high and low HER2 expressing breast cancer cell models. Using resonant scanning confocal imaging of live cell plasma membrane dynamics, we show in very high detail and within 10 minutes of cell exposure of the receptor to the NPs, extensive blebbing and ruffling of the plasma membrane, manifesting before much longer uptake of the NPs into the cell interior. Plasma membrane reorganisation was rapidly reversible, with cells reaching baseline morphology in 30 minutes. Our findings were confirmed at the ultrastructural level by scanning electron microscopy in cells fixed within 10 and 30 minutes of exposure to the NPs. Endocytic traffic of the NPs was in part directed to lysosomes and we discover a relationship between antibody valency and the ability of the NPs to deliver the chemotherapeutic agent doxorubicin to mediate cell death. Knowledge gained from these studies offers new approaches to study NP-cell dynamics in different NP-receptor settings and how receptor targeting influences plasma membrane organisation, endocytosis and delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 390-400"},"PeriodicalIF":0.0,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00168d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558603","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
Lung physiologically based pharmacokinetic modelling to predict sublingual buprenorphine kinetics following oral inhalation 基于肺生理学的药代动力学模型预测口服丁丙诺啡舌下动力学
RSC Pharmaceutics Pub Date : 2026-02-03 DOI: 10.1039/D5PM00266D
Tobechi Brendan Nnanna, Daniel Okwudili Nnamani, Elias Bestman Adikwu and Chisom Anthony Nnanna
{"title":"Lung physiologically based pharmacokinetic modelling to predict sublingual buprenorphine kinetics following oral inhalation","authors":"Tobechi Brendan Nnanna, Daniel Okwudili Nnamani, Elias Bestman Adikwu and Chisom Anthony Nnanna","doi":"10.1039/D5PM00266D","DOIUrl":"https://doi.org/10.1039/D5PM00266D","url":null,"abstract":"<p >The pulmonary system embodies a heterogeneous yet highly efficient interface for xenobiotic uptake, offering unique translational opportunities for pharmacokinetic modelling. The sublingual route is widely exploited to deliver buprenorphine, a lipophilic partial μ-opioid receptor agonist, while circumventing gastrointestinal degradation and hepatic first-pass metabolism; however, the pharmacokinetics of buprenorphine are marked by pronounced nonlinearity and variability driven by mucosal residence time, dissolution, and involuntary swallowing. In the absence of a native sublingual absorption module within the Open Systems Pharmacology (OSP) ecosystem, this study investigated whether a mechanistically constrained inhalation physiologically based pharmacokinetic (PBPK) framework could serve as a defensible surrogate to recover sublingual buprenorphine kinetics. A human inhalation PBPK model incorporating a 24-generation lung architecture was implemented in MoBi and PK-Sim, integrating morphometric and physiological descriptors with the physicochemical parameters of buprenorphine. Particle deposition was deliberately biased toward the extrathoracic and proximal tracheobronchial regions by selecting reported metered-dose inhaler particle sizes (MMAD ≈ 7.5 µm), thereby emulating sublingual mucosal exposure. The model explicitly resolved particle deposition, epithelial lining fluid dissolution, permeability-limited epithelial transfer, mucociliary clearance–driven swallowing, and systemic distribution, preserving the causal structure. Systemic disposition was described using a two-compartment model, with key parameters estimated through Monte Carlo optimisation. Model performance was evaluated against single-ascending-dose clinical data (2–24 mg) and further verified using independent studies of sublingual tablets and solutions. Across all dose levels (2–24 mg), predicted <em>C</em><small><sub>max</sub></small> and AUC metrics were recovered within predefined two-fold acceptance limits, with prediction accuracies generally ranging from 73% to 138% for AUC and 81% to 103% for <em>C</em><small><sub>max</sub></small>. The model robustly reproduced early exposure and peak timing while systematically underpredicting the terminal half-life, consistent with the structural constraints of the systemic disposition model and the absence of explicit mucosal depot or enterohepatic recirculation processes. Sensitivity analysis identified particle dissolution dynamics and mucociliary clearance kinetics as dominant drivers of exposure. In conclusion, this work demonstrates that an open-source inhalation PBPK framework can mechanistically and quantitatively approximate sublingual buprenorphine pharmacokinetics. The approach provides a transparent, extensible surrogate for sublingual absorption, supporting translational modelling and hypothesis generation when route-specific modules are unavailable.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 585-603"},"PeriodicalIF":0.0,"publicationDate":"2026-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00266d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558504","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
Overcoming stromal barriers in pancreatic cancer via size-engineered carrier-free nano-prodrugs 通过尺寸工程的无载体纳米前药克服胰腺癌的间质屏障
RSC Pharmaceutics Pub Date : 2026-01-30 DOI: 10.1039/D5PM00364D
Mengheng Yang, Ryuju Suzuki, Yoshitaka Koseki, Shuto Kodera, Ken Saijo, Hisato Kawakami, Keita Tanita, Sanjay Kumar, Kouki Oka and Hitoshi Kasai
{"title":"Overcoming stromal barriers in pancreatic cancer via size-engineered carrier-free nano-prodrugs","authors":"Mengheng Yang, Ryuju Suzuki, Yoshitaka Koseki, Shuto Kodera, Ken Saijo, Hisato Kawakami, Keita Tanita, Sanjay Kumar, Kouki Oka and Hitoshi Kasai","doi":"10.1039/D5PM00364D","DOIUrl":"https://doi.org/10.1039/D5PM00364D","url":null,"abstract":"<p >Pancreatic cancer remains a major therapeutic challenge due to its dense desmoplastic stroma, which limits drug penetration and reduces chemotherapy efficacy. Here, we report a carrier-free nanoprodrug (CFNPG) based on SNC4DC, a homodimeric prodrug of SN-38, enabling controlled SN-38 release in pancreatic cancer cells. Using a precisely controlled reprecipitation method, we generated stable CFNPGs with tunable particle sizes down to ∼30 nm, resulting in enhanced tissue penetration. These nanoparticles exhibited high drug loading, absence of carrier-associated toxicity, potent antitumor activity, and minimal systemic side effects in an orthotopic pancreatic cancer model, providing a physiologically relevant assessment of drug delivery. Our findings demonstrate that precise size engineering of carrier-free nanoprodrugs can significantly improve tissue penetration and therapeutic efficacy, providing a clinically translatable strategy for pancreatic cancer therapy.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 694-700"},"PeriodicalIF":0.0,"publicationDate":"2026-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00364d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011768","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 product development: rapid optimization and scale-up of PBAE-based siRNA delivery via DoE-guided microfluidics QbD产品开发:通过doe引导的微流体快速优化和扩大基于pbae的siRNA递送。
RSC Pharmaceutics Pub Date : 2026-01-30 DOI: 10.1039/D5PM00379B
Adrian P. E. Kromer, Laetitia J. M. Eller, David C. Jürgens and Olivia M. Merkel
{"title":"QbD product development: rapid optimization and scale-up of PBAE-based siRNA delivery via DoE-guided microfluidics","authors":"Adrian P. E. Kromer, Laetitia J. M. Eller, David C. Jürgens and Olivia M. Merkel","doi":"10.1039/D5PM00379B","DOIUrl":"10.1039/D5PM00379B","url":null,"abstract":"<p >Poly(β-amino ester) (PBAE)-based nanoparticles have emerged as promising carriers for RNA delivery, yet clear design rules linking formulation parameters to performance are still lacking. In this study, a Quality by Design (QbD)-guided and Design of Experiments (DoE)-driven approach was combined with high-throughput microfluidics to rapidly identify formulations with favorable physicochemical properties and consistent critical quality attributes (CQAs). Response Surface Modeling revealed that high total flow rates (TFR ≥ 10), nitrogen to phosphorus (N/P) ratios ≥10, and a Flow Rate Ratio (FRR) of 1 : 3 (buffer : ethanol) led to the formation of smaller, more stable particles. Among the polymers tested, a polymer candidate with a balanced composition of hydrophobic and hydrophilic side chains demonstrated optimal intraparticle stability and gene silencing performance. Notably, transfection efficiency depended strongly on formulation parameters beyond polymer type and N/P ratio, with flow rate ratio emerging as a key driver of gene knockdown kinetics. The lead formulation achieved ∼95% gene knockdown even after two weeks of storage at 4 °C. Scale-up production of the lead candidate confirmed the transferability of optimized Critical Process Parameters (CPPs) and preserved CQA profiles, validating the robustness of the design space. This study establishes a robust and scalable QbD-guided workflow for the development of microfluidically manufactured siRNA nanoparticles, enabling rapid optimization, reliable scale-up, and clinically relevant performance.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 379-389"},"PeriodicalIF":0.0,"publicationDate":"2026-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12926864/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147286966","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
A bioinspired, pH-responsive microsphere matrix of cold-water extracted Colocasia esculenta mucilage and alginate: a new approach for sustained oral delivery of tramadol 一个生物启发,ph响应微球基质的冷水提取土芋泥和海藻酸盐:持续口服递送曲马多的新方法
RSC Pharmaceutics Pub Date : 2026-01-28 DOI: 10.1039/D5PM00263J
Shazia Noureen, Sobia Noreen, Fozia Batool, Shazia Akram Ghumman, Sara Hasan, Samina Aslam and Nisar Ahmed
{"title":"A bioinspired, pH-responsive microsphere matrix of cold-water extracted Colocasia esculenta mucilage and alginate: a new approach for sustained oral delivery of tramadol","authors":"Shazia Noureen, Sobia Noreen, Fozia Batool, Shazia Akram Ghumman, Sara Hasan, Samina Aslam and Nisar Ahmed","doi":"10.1039/D5PM00263J","DOIUrl":"https://doi.org/10.1039/D5PM00263J","url":null,"abstract":"<p >Natural polymers derived from plant mucilages are increasingly explored as release-modifying agents in advanced drug delivery systems. This study presents an innovative approach utilizing cold-water extraction and ethanol precipitation to obtain <em>Colocasia esculenta</em> mucilage (CEM), which was then used to fabricate Tramadol hydrochloride-loaded microspheres <em>via</em> ionic gelation. A three-level, two-factor central composite design was employed to optimize a cross-linked CEM–alginate matrix, using polymer concentrations as independent variables, and particle size and encapsulation efficiency as response parameters. The optimized formulation exhibited stable, spherical microspheres with pH-responsive swelling and degradation behavior, high encapsulation efficiency (90.10%), and an average particle size of 726 μm. Characterization by FTIR, DSC, and XRD confirmed drug–polymer compatibility, while SEM analysis revealed a rough, wrinkled surface with fine pores. <em>In vitro</em> studies demonstrated pH-dependent drug release, achieving 67.30% release over 12 hours. <em>In vivo</em> evaluations in rabbits confirmed the formulation's safety, improved bioavailability, and prolonged gastrointestinal residence time. These results highlight the potential of cold-extracted CEM–alginate microspheres as a biocompatible, pH-responsive platform for sustained oral delivery of Tramadol. Furthermore, the simplicity and reproducibility of the ionic gelation method indicate good potential for formulation scalability, and future studies may explore the applicability of this CEM–alginate platform for other therapeutic agents requiring sustained oral delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 423-440"},"PeriodicalIF":0.0,"publicationDate":"2026-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00263j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558582","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
Advanced mechanisms of polymer-based drug delivery systems for clinical applications 用于临床应用的聚合物基给药系统的先进机制
RSC Pharmaceutics Pub Date : 2026-01-28 DOI: 10.1039/D5PM00242G
Barakat Olamide Ishola, Khandoker Asiqur Rahaman, Shaikh Abdur Razzak, Md Mahamudul Hasan Rumon, Md Salman Shakil and Shihab Uddin
{"title":"Advanced mechanisms of polymer-based drug delivery systems for clinical applications","authors":"Barakat Olamide Ishola, Khandoker Asiqur Rahaman, Shaikh Abdur Razzak, Md Mahamudul Hasan Rumon, Md Salman Shakil and Shihab Uddin","doi":"10.1039/D5PM00242G","DOIUrl":"https://doi.org/10.1039/D5PM00242G","url":null,"abstract":"<p >Polymer-based drug delivery technologies have revolutionized modern therapeutics by enabling controlled, sustained, and targeted drug release. These systems employ diverse natural and synthetic polymers that engage with biological environments to exert therapeutic effects. The history of polymeric drug delivery systems, their classification, formulation techniques, mechanisms of action, and diverse applications across various disease conditions are essential for future advancements. Polymer chemistry has led to the development of stimuli-responsive polymers that release drugs in response to external triggers, such as pH, temperature, electricity, light, or ultrasound. Moreover, 3D printing technologies are increasingly employed to develop more complex, multifunctional, layered, polymer-based drug delivery systems. While polymer-based technologies have demonstrated remarkable potential in drug delivery, challenges like scalability, biocompatibility, and regulatory compliance persist. Interdisciplinary collaboration and multifaceted strategies can advance targeted treatments for life-threatening diseases and enhance quality of life through tissue regeneration.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 331-360"},"PeriodicalIF":0.0,"publicationDate":"2026-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00242g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558600","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
Self-nanoemulsifying drug delivery systems (SNEDDS) for treating neglected tropical diseases: affordable and scalable pathways for global health impact 用于治疗被忽视热带病的自纳米乳化药物输送系统:可负担和可扩展的全球卫生影响途径
RSC Pharmaceutics Pub Date : 2026-01-27 DOI: 10.1039/D5PM00343A
João Paulo Figueiró Longo and Josué de Moraes
{"title":"Self-nanoemulsifying drug delivery systems (SNEDDS) for treating neglected tropical diseases: affordable and scalable pathways for global health impact","authors":"João Paulo Figueiró Longo and Josué de Moraes","doi":"10.1039/D5PM00343A","DOIUrl":"https://doi.org/10.1039/D5PM00343A","url":null,"abstract":"<p >Nanomaterials present promising avenues for advancing global health, particularly in addressing neglected tropical diseases (NTDs). Affecting over a billion people, NTDs suffer from limited treatment options, often relying on drugs with poor solubility and bioavailability. This challenge is compounded by increasing drug resistance and difficulties in administering treatments effectively. This situation underscores a critical gap in pharmaceutical innovation, influenced more by market forces than by scientific limitations. The prohibitive costs and high failure rates of traditional drug development render standard innovation pathways economically impractical for neglected tropical diseases. Moreover, regulatory frameworks and intellectual property rights often hinder the development of affordable treatments for neglected tropical diseases. Nanotechnology, specifically self-nanoemulsifying drug delivery systems (SNEDDS), offers a scalable solution to overcome solubility and bioavailability barriers. By spontaneously forming emulsions in gastrointestinal fluids, SNEDDS eliminate complex manufacturing needs, as seen with successful clinical examples like ritonavir and cyclosporine. Leveraging these cost-effective, orally compatible platforms allows for the repurposing of existing drugs. Integrating such streamlined nanotechnologies into global health programs is essential to close the therapeutic gap in resource-limited settings.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 374-378"},"PeriodicalIF":0.0,"publicationDate":"2026-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00343a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558602","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
Advanced bispecific antibody design and inhaled biologics; emerging strategies for asthma 先进的双特异性抗体设计和吸入生物制剂;针对哮喘的新策略
RSC Pharmaceutics Pub Date : 2026-01-22 DOI: 10.1039/D5PM00230C
Zeina Kassem, Jenny K. W. Lam and Hanieh Khalili
{"title":"Advanced bispecific antibody design and inhaled biologics; emerging strategies for asthma","authors":"Zeina Kassem, Jenny K. W. Lam and Hanieh Khalili","doi":"10.1039/D5PM00230C","DOIUrl":"https://doi.org/10.1039/D5PM00230C","url":null,"abstract":"<p >Asthma is a chronic inflammatory respiratory disease affecting over 300 million individuals worldwide. While current therapies, including inhaled corticosteroids and monoclonal antibodies, have significantly improved management of Type 2 (T2)-high asthma, treatment options for T2-low, steroid-resistant, and severe asthma remain limited. Recent advances in biologic therapeutics have introduced bispecific antibodies (bsAbs) as a promising next-generation strategy. BsAbs are engineered to simultaneously target two distinct inflammatory pathways, offering broader immunomodulatory effects and the potential to improve disease control in heterogeneous asthma phenotypes. Concurrently, pulmonary delivery systems such as nebulisers, dry powder inhalers (DPIs) and soft mist inhalers (SMIs) have emerged as attractive non-invasive alternatives to injections for biologic administration, providing localised treatment directly to the lungs, reduced systemic side effects, and enhanced patient adherence. This review examines the immunological basis of asthma endotypes, evaluates current monoclonal antibody therapies and their limitations, and explores the design, mechanisms, and clinical progress of bispecific antibodies in the treatment of asthma. Additionally, we analyse the feasibility and challenges of inhaled biologic delivery, including formulation strategies and device optimisation. We conclude by highlighting future research priorities, including the development of inhalable bsAbs for T2-low asthma and the need for scalable, stable, and patient-friendly formulations. This dual-focused approach, combining novel antibody engineering with targeted delivery, represents a critical step towards personalised, effective asthma care.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 630-644"},"PeriodicalIF":0.0,"publicationDate":"2026-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00230c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011762","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
Polymeric nano-in-microparticles for pulmonary delivery of remdesivir against SARS-CoV-2 用于肺部递送抗SARS-CoV-2瑞德西韦的聚合纳米微粒
RSC Pharmaceutics Pub Date : 2026-01-21 DOI: 10.1039/D5PM00269A
Alison Tatiana Madrid Sani, Brenno da Cunha Lima, Beatriz Moreira Rodrigues, Michelle Alvares Sarcinelli, Marcelo Henrique da Cunha Chaves, Helvécio Vinícius Antunes Rocha, Natália Neto Pereira Cerize, Maria Helena Ambrosio Zanin, Juliana Terzi Maricato, Valker Araujo Feitosa and Carlota de Oliveira Rangel-Yagui
{"title":"Polymeric nano-in-microparticles for pulmonary delivery of remdesivir against SARS-CoV-2","authors":"Alison Tatiana Madrid Sani, Brenno da Cunha Lima, Beatriz Moreira Rodrigues, Michelle Alvares Sarcinelli, Marcelo Henrique da Cunha Chaves, Helvécio Vinícius Antunes Rocha, Natália Neto Pereira Cerize, Maria Helena Ambrosio Zanin, Juliana Terzi Maricato, Valker Araujo Feitosa and Carlota de Oliveira Rangel-Yagui","doi":"10.1039/D5PM00269A","DOIUrl":"https://doi.org/10.1039/D5PM00269A","url":null,"abstract":"<p >The COVID-19 pandemic underscored the urgent need for advanced drug delivery systems to enhance the safety and efficacy of existing antiviral therapies. This study presents an inhalable powder formulation of remdesivir (RDV) using polymeric nano-in-microparticles for pulmonary administration. RDV was nanoencapsulated in a polycaprolactone (PCL) matrix <em>via</em> emulsion–diffusion–solvent evaporation and stabilized with DPPC and Pluronic F127, resulting in nanoparticles (RDV-PCL-NP) of 184 ± 11 nm and 87% encapsulation efficiency. Cytotoxicity assays in Vero E6 cells confirmed the RDV-PCL-NP safety at therapeutic concentrations, with a marked reduction in the SARS-CoV-2 viral load at 5 µM RDV. The nanoparticles were spray dried with lactose, yielding a dry powder (RDV-PCL-MP) with 63% process yield. Physicochemical characterization (SEM, FTIR, DRX, DSC/TGA, laser diffraction) confirmed uniform particle size and stability (1–5 µm) of the RDV-PCL-MP inhalable powder. <em>In vitro</em> lung deposition studies showed 40% fine fraction and 39% respirable fraction. These findings support the potential of RDV-loaded nano-in-microparticles as a scalable pulmonary delivery platform to improve COVID-19 treatment.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 552-563"},"PeriodicalIF":0.0,"publicationDate":"2026-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00269a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147558535","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
Development and evaluation of fenticonazole nitrate-loaded, fucoidan-coated lecithin–chitosan nanoparticles for the treatment of vaginitis 硝酸唑负载、岩藻糖苷包被卵磷脂-壳聚糖纳米颗粒治疗阴道炎的研制与评价
RSC Pharmaceutics Pub Date : 2026-01-16 DOI: 10.1039/D5PM00345H
Valamla Bhavana, Padakanti Sandeep Chary, Urati Anuradha, Kishan Kumar Parida, Nitin Pal Kalia and Neelesh Kumar Mehra
{"title":"Development and evaluation of fenticonazole nitrate-loaded, fucoidan-coated lecithin–chitosan nanoparticles for the treatment of vaginitis","authors":"Valamla Bhavana, Padakanti Sandeep Chary, Urati Anuradha, Kishan Kumar Parida, Nitin Pal Kalia and Neelesh Kumar Mehra","doi":"10.1039/D5PM00345H","DOIUrl":"https://doi.org/10.1039/D5PM00345H","url":null,"abstract":"<p >In this investigation, self-assembling fenticonazole-loaded lecithin–chitosan nanoparticles (FZNP) with cationic zeta potential were altered by coating them with an anionic fucoidan polymer (Fu-FZNP) through an ionic gelation method to overcome the vaginal mucosal barrier. FZNP and Fu-FZNP possessed particle sizes of 129.20 ± 0.25 nm and 227.10 ± 1.54 nm, polydispersity indexes of 0.21 ± 0.00 and 0.26 ± 0.01, and zeta potentials of 30.96 ± 1.15 mV and −26.75 ± 0.3 mV, respectively. The entrapment efficiency and drug loading were 65.47% ± 2.32% and 11.69% ± 0.414% for FZNP and 71.13% ± 5.74% and 7.41% ± 0.60% for Fu-FZNP, respectively. The nanoparticles exhibited spherical and smooth morphology under TEM imaging. An excised goat vagina was used for the <em>ex vivo</em> permeation studies, which showed drug permeations of 61.74% ± 2.07% for FZNP and 72.11% ± 1.4% for Fu-FZNP. FZNP and Fu-FZNP demonstrated antibacterial and antifungal properties against <em>Staphylococcus aureus</em> and <em>Candida albicans</em>, respectively, <em>in vitro</em>. Therefore, FZN and Fu-FZNP may be developed further for the safe, practical, and efficient treatment of mixed vaginal infections.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 726-737"},"PeriodicalIF":0.0,"publicationDate":"2026-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2026/pm/d5pm00345h?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148011771","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
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书