RSC Pharmaceutics最新文献

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Comparative analysis of drug release kinetics in polyethylene oxide and xanthan gum matrices with various excipients 不同赋形剂在聚氧乙烯和黄原胶基质中的药物释放动力学比较分析
RSC Pharmaceutics Pub Date : 2024-12-23 DOI: 10.1039/D4PM00296B
Haja Muhamad, Nihad Mawla, Saedah Dereiah, Adam Ward, James Williamson and Kofi Asare-Addo
{"title":"Comparative analysis of drug release kinetics in polyethylene oxide and xanthan gum matrices with various excipients","authors":"Haja Muhamad, Nihad Mawla, Saedah Dereiah, Adam Ward, James Williamson and Kofi Asare-Addo","doi":"10.1039/D4PM00296B","DOIUrl":"https://doi.org/10.1039/D4PM00296B","url":null,"abstract":"<p >This study aimed to investigate the effect of various pharmaceutical excipients on the drug release kinetics of extended-release formulations composed of polyethylene oxide (PEO) and xanthan gum (XG), using propranolol hydrochloride (PPN) as the model drug. The formulations contained different ratios (1 : 3, 1 : 1, and 3 : 1 w/w) of PEO or XG to either lactose, dibasic calcium phosphate (DCP), or microcrystalline cellulose (MCC). Compaction analysis revealed that formulations that contain higher excipient content exhibit increased porosity and decreased hardness values. Contact angle measurements indicated that formulations with higher excipient content, particularly with lactose, displayed lower contact angles, which is indicative of increased hydrophilicity. After the <em>in vitro</em> dissolution studies were conducted, the dissolution efficiency (DE), mean dissolution time (MDT), mean dissolution rate (MDR), and similarity factors (<em>f</em><small><sub>2</sub></small>) were analysed. The findings showed that a higher amount of lactose in both PEO and XG formulations resulted in faster drug release, with the PEO : lactose 1 : 3 ratio achieving the highest DE (64 ± 8%) and the shortest MDT (77 ± 10 min). Similarly, the XG : lactose 1 : 3 ratio exhibited the highest DE (61 ± 2%) and fastest MDR (0.20 ± 0.01% min<small><sup>−1</sup></small>), although the effect was less pronounced compared to PEO formulations. The kinetic analysis showed that most PEO formulations followed the Peppas model, indicating non-Fickian transport driven by both diffusion and polymer erosion mechanisms. However, most of the XG formulations followed the Higuchi model. The similarity factors (<em>f</em><small><sub>2</sub></small>) revealed the influence of excipient type and ratio on the dissolution profiles. Formulations containing a higher amount of MCC displayed higher similarity with the pure polymer profiles. These results give important insights into how excipients can be used to optimise polymeric matrices to regulate drug release in extended-release formulations.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 303-317"},"PeriodicalIF":0.0,"publicationDate":"2024-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00296b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638122","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
Strategies for beating the bitter taste of pharmaceutical formulations towards better therapeutic outcomes 战胜药物配方的苦味以获得更好治疗效果的策略
RSC Pharmaceutics Pub Date : 2024-12-18 DOI: 10.1039/D4PM00191E
Lohare Rahul Sanjay, Makka Krupali Ashokbhai, Shubham Ghatole, Subhadeep Roy, Kardile Punam Kashinath and Santanu Kaity
{"title":"Strategies for beating the bitter taste of pharmaceutical formulations towards better therapeutic outcomes","authors":"Lohare Rahul Sanjay, Makka Krupali Ashokbhai, Shubham Ghatole, Subhadeep Roy, Kardile Punam Kashinath and Santanu Kaity","doi":"10.1039/D4PM00191E","DOIUrl":"https://doi.org/10.1039/D4PM00191E","url":null,"abstract":"<p >Oral drug delivery remains the most favored method of administration due to its convenience and patient compliance. However, the unpleasant taste of certain medications often leads to poor acceptance, particularly among pediatric and geriatric patients. To address this issue, taste-masking (TM) technologies have emerged as effective solutions for improving the palatability of oral drugs. This review provides an overview of the key features of TM technologies, including the properties of materials used, their mechanisms, and applications in drug delivery. Typically, TM materials work by complexing or encapsulating drug molecules to prevent direct interaction with taste receptors, thus mitigating unpleasant flavors and enhancing the overall sensory experience. The review explores a range of materials—both synthetic and natural—and various TM technologies designed to mask bitter taste. Additionally, it discusses the latest methods for assessing the effectiveness of TM and the current regulatory landscape surrounding the use of these technologies in drug delivery.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 59-81"},"PeriodicalIF":0.0,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00191e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994220","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
Injectable sustained-release hydrogel for high-concentration antibody delivery† 可注射的缓释水凝胶用于高浓度抗体递送†
RSC Pharmaceutics Pub Date : 2024-12-18 DOI: 10.1039/D4PM00290C
Talia Zheng and Patrick S. Doyle
{"title":"Injectable sustained-release hydrogel for high-concentration antibody delivery†","authors":"Talia Zheng and Patrick S. Doyle","doi":"10.1039/D4PM00290C","DOIUrl":"https://doi.org/10.1039/D4PM00290C","url":null,"abstract":"<p >There is an increasing interest in subcutaneous (SC) delivery as an alternative to the traditional intravenous (IV) for immunotherapies and other advanced therapies. High-concentration formulations of antibodies are needed to meet the limited-volume requirements of subcutaneous SC delivery. Despite this need, there remain challenges in delivering stable and injectable antibodies in these high concentrations. Hydrogel encapsulation of amorphous solid antibodies has been proven to improve the stability and injectability of high-concentration antibody formulations. However, the antibody is quickly released from the hydrogel due to the material's porosity, leading to rapid, uncontrolled drug release kinetics undesirable for the drug's efficacy and safety. In this paper, we propose a dual-network composite hydrogel which leverages interactions between the two polymer networks to achieve controlled release of the antibody. We load the solid form of the antibody at high concentrations within alginate hydrogel microparticles which are then suspended in thermogelling methylcellulose solution to formulate the <em>in situ</em> gelling composite hydrogel. By facile chemical modification of the alginate to tune the microparticles’ gel properties and alginate–methylcellulose interactions, we demonstrate how the composite system can delay release of the drug in a tunable manner and achieve a near-zero order release profile for improved therapeutic efficacy. We show acceptable injectability properties of the composite hydrogel at high antibody concentrations, highlighting the functionalities of dualnetwork encapsulation. We imagine this composite system to be applicable for the sustained delivery of various therapeutic protein forms, especially for high-loading SC formulations.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 186-196"},"PeriodicalIF":0.0,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00290c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994217","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
Design and evaluation of solid self-nanoemulsifying drug delivery systems of cyclosporine developed with a superior adsorbent base† 具有优良吸附碱†的环孢素固体自纳米乳化给药系统的设计与评价
RSC Pharmaceutics Pub Date : 2024-12-11 DOI: 10.1039/D4PM00198B
Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla
{"title":"Design and evaluation of solid self-nanoemulsifying drug delivery systems of cyclosporine developed with a superior adsorbent base†","authors":"Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla","doi":"10.1039/D4PM00198B","DOIUrl":"https://doi.org/10.1039/D4PM00198B","url":null,"abstract":"<p >Cyclosporine (CYC) is a drug that belongs to the BCS class II category. This study was designed to develop novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for cyclosporine (CYC), using chitosan–EDTA microparticles. Such microparticles are known to exhibit superior adsorbent characteristics and were prepared by two different methods <em>viz</em>. spray drying (SD-CHEM) and solvent evaporation (SE-CHEM). Capmul® GMS-50K, Labrafac, and PEG 400 were chosen as the oil, surfactant, and co-surfactant, respectively. The cyclosporine liquid self-nanoemulsifying drug delivery system (CYC-L-SNEDDS) was developed with an optimal oil to <em>S</em><small><sub>mix</sub></small> (surfactant : co-surfactant) ratio of 40 : 60, determined through a pseudo ternary phase diagram. The novel S-SNEDDS were developed by adsorbing CYC-L-SNEDDS onto the chitosan–EDTA microparticles, resulting in CYC-SD-S-SNEDDS and CYC-SE-S-SNEDDS. Both formulations exhibited favorable drug loading, with 81.184 ± 4.191% for CYC-SD-S-SNEDDS and 56.426 ± 5.471% for CYC-SE-S-SNEDDS. XRD and DSC confirmed drug amorphization, while SEM revealed a smooth, well-distributed adsorbate on the adsorbent surfaces, with particle sizes of 5–8 μm for CYC-SD-S-SNEDDS and 10–12 μm for CYC-SE-S-SNEDDS. When tested for stability, the developed formulations exhibited excellent physical and thermodynamic stability. The globule size for CYC-SD-S-SNEDDS was 138.7 ± 4.14 nm, with a PDI of 0.613 ± 0.004, while CYC-SE-S-SNEDDS had a globule size of 166.9 ± 4.04 nm and a PDI of 0.579 ± 0.003. The results of <em>in vitro</em> dissolution studies revealed that there was a fourfold increase in drug dissolution for CYC-SD-S-SNEDDS (80.03%) and CYC-SE-S-SNEDDS (72.26%) when compared to the pure cyclosporine (19.8%). A similar pattern was observed in <em>ex vivo</em> permeation studies where CYC-SD-S-SNEDDS showed 39.34% release and CYC-SE-S-SNEDDS exhibited 28.31% release as compared to CYC-L-SNEDDS (41.46%). Furthermore, CYC-SD-S-SNEDDS outperformed CYC-SE-S-SNEDDS, indicating the superiority of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These findings suggest enhanced dissolution and permeation for cyclosporine in S-SNEDDS.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 318-332"},"PeriodicalIF":0.0,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00198b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638123","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
Preparation and characterization of efavirenz cocrystal-encapsulated pronanoliposomes for antiretroviral therapy with improved bioavailability† 用于抗逆转录病毒治疗的依非韦伦共晶包封原脂质体的制备和表征及其生物利用度的提高
RSC Pharmaceutics Pub Date : 2024-12-06 DOI: 10.1039/D4PM00215F
Sucheta Sarkar, Arijit Prosad Roy, Sanchita Mitra, Gouranga Nandi, Ranabir Sahu, Tarun Kumar Dua and Paramita Paul
{"title":"Preparation and characterization of efavirenz cocrystal-encapsulated pronanoliposomes for antiretroviral therapy with improved bioavailability†","authors":"Sucheta Sarkar, Arijit Prosad Roy, Sanchita Mitra, Gouranga Nandi, Ranabir Sahu, Tarun Kumar Dua and Paramita Paul","doi":"10.1039/D4PM00215F","DOIUrl":"https://doi.org/10.1039/D4PM00215F","url":null,"abstract":"<p >The present research work aims to improve the bioavailability of the antiretroviral drug efavirenz (EFV) using pharmaceutical cocrystallization technique. EFV is a potential antiretroviral drug that exhibits extremely poor water solubility and poor oral bioavailability and falls under the BCS-II category. EFV and <small>L</small>-proline were selected in a 1 : 1 equimolar ratio to formulate efavirenz proline co-crystals, and a facile method was adopted to prepare co-crystals of EFV. The formation of a new solid phase was confirmed through advanced techniques such as Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and powder X-ray diffraction (pXRD) analysis, and solubility study was conducted utilising UV visible spectroscopy. Proliposomal vesicles containing EFV or EFV cocrystals were prepared using thin film hydration methods with few modifications. The vesicle size in dispersion, zeta potential, surface morphology, drug loading and <em>in vitro</em> drug release were assessed. Co-crystallization increased the solubility of EFV up to 3 fold, and the liposomes were found to release the drug in a sustained manner. The optimized formulation was found to have a substantial amount of EFV loading (32.70%) and entrapment efficiency (99.28%) with a narrow range of size distribution. The liposomes containing the pure drug showed 72% release of the drug in 72 h, whereas the liposomes containing co-crystals showed 99.98% release of the drug in 72 h. This was due to the presence of <small>L</small>-proline in association with EFV, which led to an enhancement in the polarity of hydrophobic EFV, thus increasing its dissolution in drug release media. The present work reports a cost-effective method for the enhancement of drug solubility, providing sustained drug release from liposome and thereby improving the oral bioavailability of the antiviral agent EFV.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 342-352"},"PeriodicalIF":0.0,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00215f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638126","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-action antimicrobial surface coatings: methylene blue and quaternary ammonium cation conjugated silica nanoparticles† 双作用抗菌表面涂层:亚甲基蓝和季铵离子共轭二氧化硅纳米颗粒†
RSC Pharmaceutics Pub Date : 2024-12-04 DOI: 10.1039/D4PM00278D
Haritha Kirla, Juliana Hamzah, Zhong-Tao Jiang and David J. Henry
{"title":"Dual-action antimicrobial surface coatings: methylene blue and quaternary ammonium cation conjugated silica nanoparticles†","authors":"Haritha Kirla, Juliana Hamzah, Zhong-Tao Jiang and David J. Henry","doi":"10.1039/D4PM00278D","DOIUrl":"https://doi.org/10.1039/D4PM00278D","url":null,"abstract":"<p >The increasing prevalence of healthcare-associated infections from multidrug-resistant bacteria presents a growing challenge due to their high transmissibility, and resistance to traditional antimicrobial strategies. In this study, we introduce an innovative dual-mode antibacterial strategy through the development of novel surface coatings on glass substrates, offering a proof-of-concept solution for enhanced infection control. Our approach uniquely combines the light-active methylene blue silane (MBS1) dye with the potent antimicrobial compound dimethyloctadecyl[3-(trimethoxysilyl)propyl] ammonium chloride (QAS) into silica nanoparticles (SNPs) to create multifunctional antibacterial surface coatings. The distinct use of silane-functionalized MB and QA enables strong covalent bonding with silica nanoparticles, while the robust silane chemistry ensures durable adhesion of SNPs to the glass substrates. While MBS1–SNP coatings generated highly hydrophilic (CA = 28°), light-active surfaces, combination of QAS (QA–MBS1–SNP) coating enhanced surface hydrophobicity (CA = 90°) without compromising photokilling efficiency. The antibacterial efficacy of these coatings was rigorously tested against the Gram-negative bacterium <em>Escherichia coli</em>. The synergistic action of MB and QA demonstrated exceptional photokilling performance achieving &gt;99.999% (&gt;5-log reduction) bactericidal activity under white light (∼500 lux, ∼0.0732 mW cm<small><sup>−2</sup></small>) and effectively inhibited biofilm formation by up to 80%. The demonstrated efficacy of these coatings highlights their potential for transformative applications in healthcare settings, providing a robust, multifaceted approach to infection control.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 163-177"},"PeriodicalIF":0.0,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00278d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994215","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
Efficient development of high drug loaded posaconazole tablets enabled by amorphous solid dispersion 非晶态固体分散体高效制备高载泊沙康唑片
RSC Pharmaceutics Pub Date : 2024-12-04 DOI: 10.1039/D4PM00301B
Tianyi Xiang, Sichen Song, Ronald A. Siegel and Changquan Calvin Sun
{"title":"Efficient development of high drug loaded posaconazole tablets enabled by amorphous solid dispersion","authors":"Tianyi Xiang, Sichen Song, Ronald A. Siegel and Changquan Calvin Sun","doi":"10.1039/D4PM00301B","DOIUrl":"https://doi.org/10.1039/D4PM00301B","url":null,"abstract":"<p >Determining the upper limits of drug loading in amorphous solid dispersion (ASD) with sufficient physical stability and release performance is critical for developing ASD-enabled tablets for poorly soluble drugs. Recent studies have highlighted the utility of the polymer overlap concentration, <em>c</em>*, in maintaining the physical stability of ASD formulations. The present work demonstrates the feasibility of effectively developing high drug loaded ASD tablets using the <em>c</em>* concept as a guide, with posaconazole as the model drug. By incorporating various material sparing formulation technologies, a record high 50% POS loaded tablet with adequate manufacturability and satisfactory dissolution performance was developed using 1.5 g of POS within 14 days. Physical stabilities of the ASD and tablet were maintained for at least 6 months under ambient conditions and 1 month at 40 °C.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 178-185"},"PeriodicalIF":0.0,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00301b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994216","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 characterization of a gallic acid-infused topical emulgel for enhanced wound management: formulation and in vitro optimization 一种没食子酸注入局部凝胶的开发和特性,用于增强伤口管理:配方和体外优化
RSC Pharmaceutics Pub Date : 2024-12-03 DOI: 10.1039/D4PM00297K
Sourav Dhandhi, Yeshna, Vishal, Monika, Samrat Chauhan, Monika Singh, Rahul Pratap Singh and Vikas Jhawat
{"title":"Development and characterization of a gallic acid-infused topical emulgel for enhanced wound management: formulation and in vitro optimization","authors":"Sourav Dhandhi, Yeshna, Vishal, Monika, Samrat Chauhan, Monika Singh, Rahul Pratap Singh and Vikas Jhawat","doi":"10.1039/D4PM00297K","DOIUrl":"https://doi.org/10.1039/D4PM00297K","url":null,"abstract":"<p >This study aimed to develop and characterize a topical emulgel for wound management, combining gallic acid with skin-permeable excipients and optimized the gelation process for consistency and stability, ensuring ease of application and prolonged drug release. The emulgel was analyzed for physicochemical properties, including rheological and texture analysis, which assessed gel strength, viscosity, spreadability, and adherence. Drug release was evaluated using <em>in vitro</em> models under varying conditions to determine the optimal formulation for sustained delivery. Anti-inflammatory efficacy was also tested, revealing the gel's potential to reduce inflammation and wound symptoms. Key metrics showed spreadability ranged from 7.6 to 9.4 cm, viscosity from 3100 to 5230 cps, drug content from 81% to 94%, and cumulative drug release from 55% to 85%. These findings support the potential of topical emulgels for enhanced wound care through localized drug delivery, better patient compliance, and minimized systemic effects.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 333-341"},"PeriodicalIF":0.0,"publicationDate":"2024-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00297k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638124","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
Microfluidics-generated PLA nanoparticles: impact of purification method on macrophage interactions, anti-inflammatory effects, biodistribution, and protein corona formation 微流体生成的聚乳酸纳米颗粒:纯化方法对巨噬细胞相互作用、抗炎作用、生物分布和蛋白冠形成的影响
RSC Pharmaceutics Pub Date : 2024-11-26 DOI: 10.1039/D4PM00233D
Jacob R. Shaw, Radha Vaidya, Fanny Xu, Shruti Dharmaraj and Ryan M. Pearson
{"title":"Microfluidics-generated PLA nanoparticles: impact of purification method on macrophage interactions, anti-inflammatory effects, biodistribution, and protein corona formation","authors":"Jacob R. Shaw, Radha Vaidya, Fanny Xu, Shruti Dharmaraj and Ryan M. Pearson","doi":"10.1039/D4PM00233D","DOIUrl":"10.1039/D4PM00233D","url":null,"abstract":"<p >Polymeric nanoparticles (NPs) are traditionally formulated using batch methodologies that are poorly scalable and require time consuming, hands-on purification procedures. Here, we prepared poly(lactic acid) (PLA)-based polymeric NPs using a scalable microfluidics-based method and systematically investigated the impact of purification method (centrifugation <em>versus</em> tangential flow filtration (TFF)) to remove poly(vinyl alcohol) (PVA) on macrophage uptake, anti-inflammatory effects, biodistribution, and protein corona formation. TFF purification demonstrated significantly higher recovery of NPs compared to the centrifugation method, with little-to-no aggregation observed. PVA removal efficiency was superior with centrifugation, although TFF was comparable. NP cellular association, <em>in vitro</em> anti-inflammatory activity, and <em>in vivo</em> biodistribution studies suggested purification method-dependent alterations, which were correlated with protein corona profiles. This study underscores the potential of TFF, combined with microfluidics, as an efficient and high-yield purification method for NPs, and reveals the need for extensive confirmation of NP biological activity alongside physicochemical properties when developing NP therapeutics at-scale.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 135-146"},"PeriodicalIF":0.0,"publicationDate":"2024-11-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11615567/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142804232","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
Heparin sodium enriched gelatin/polycaprolactone based multi-layer nanofibrous scaffold for accelerated wound healing in diabetes 富肝素钠明胶/聚己内酯多层纳米纤维支架加速糖尿病伤口愈合
RSC Pharmaceutics Pub Date : 2024-11-25 DOI: 10.1039/D4PM00130C
Madhukiran R. Dhondale, Manjit Manjit, Abhishek Jha, Manish Kumar, Kanchan Bharti, Dinesh Kumar and Brahmeshwar Mishra
{"title":"Heparin sodium enriched gelatin/polycaprolactone based multi-layer nanofibrous scaffold for accelerated wound healing in diabetes","authors":"Madhukiran R. Dhondale, Manjit Manjit, Abhishek Jha, Manish Kumar, Kanchan Bharti, Dinesh Kumar and Brahmeshwar Mishra","doi":"10.1039/D4PM00130C","DOIUrl":"https://doi.org/10.1039/D4PM00130C","url":null,"abstract":"<p >Multilayered nanofibrous scaffolds (MNSs) obtained by electrospinning have gained widespread attention owing to their control over the delivery of drugs. However, polymer and drug solubility issues in common solvent systems still limit their applications. The present work employed acetic acid : water : ethyl acetate (4 : 4 : 2 v/v/v) as a common solvent system for dissolving gelatin and heparin sodium (HS). A GL 20% w/v solution showing optimum viscosity and conductivity, and high encapsulation (89.2 ± 2.13%) was selected. Additionally, TPGS-1000 incorporated in GL reduced the surface tension for better electrospinning and additional free-radical scavenging activity (∼6 fold of blank nanofibers). The central layer was surrounded by upper and lower PCL–GL layers to control the release of the hydrophilic drug (HS). The electrospun PCL : GL layer sustained the release for ∼24 hours. The developed multilayered nanofibrous scaffolds showed accelerated wound healing in a diabetic rat model. Histological analysis of the wound confirmed the accelerated re-epithelialization and reduced inflammatory response. Laser Doppler flowmetry further showed a significant improvement in the blood flow at the wound site at day 14 and day 21, revealing neovascularization. Therefore, the developed multilayered nanofibrous scaffolds provided a plausible method for fabricating regenerative scaffolds for drug delivery and diabetic wound healing.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 1021-1032"},"PeriodicalIF":0.0,"publicationDate":"2024-11-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00130c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798214","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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