RSC Pharmaceutics最新文献

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Systematic antimicrobial, biofilm, free radical inhibition and tyrosinase inhibition assessments of efficient green silver nanoparticles from the aqueous root extract of Cyphostemma adenocaule (CA) 绿银纳米粒子的抗菌、生物膜抑制、自由基抑制和酪氨酸酶抑制研究
RSC Pharmaceutics Pub Date : 2024-11-22 DOI: 10.1039/D4PM00173G
Kamalakkannan Kaliappan, Pradeep Nagarajan, Jayaprakash Jayabalan, Hemalatha Pushparaj, Selvaraja Elumalai, Baranidharan Paramanathan, Vijayabaskaran Manickam, Huyn Tae Jang and Ganesh Mani
{"title":"Systematic antimicrobial, biofilm, free radical inhibition and tyrosinase inhibition assessments of efficient green silver nanoparticles from the aqueous root extract of Cyphostemma adenocaule (CA)","authors":"Kamalakkannan Kaliappan, Pradeep Nagarajan, Jayaprakash Jayabalan, Hemalatha Pushparaj, Selvaraja Elumalai, Baranidharan Paramanathan, Vijayabaskaran Manickam, Huyn Tae Jang and Ganesh Mani","doi":"10.1039/D4PM00173G","DOIUrl":"https://doi.org/10.1039/D4PM00173G","url":null,"abstract":"<p >A novel, fast and optimized etiquette for the production of silver nanoparticles using the root extract of <em>Cyphostemma adenocaule</em> (<em>CA</em>) is reported in our study. This plant is known to possess many natural terpenes, glycosides and sterols, which can reduce AgNO<small><sub>3</sub></small> solution. Typical physiochemical analyses like UV-spectroscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM), powder X-ray diffraction (XRD), and Fourier transformed infrared spectroscopy (FTIR) were used to characterize and confirm the synthesis of the produced nanoparticles. The XRD and TEM analyses validated that the obtained particles were spherical shaped with the average size of 18 nm. The CA–AgNPs depicted excellent anti-bacterial activity against the studied gram (+ve) and (−ve) microorganisms and showed a very good <em>S. aureus</em> biofilm in a dose-dependent response (a maximum inhibition of 88% at a 125 μg mL<small><sup>−1</sup></small> dose). Further results proved its ability to neutralize ABTS free radicals (96.5% neutralization was noted at a 200 μg mL<small><sup>−1</sup></small> dose with the IC<small><sub>50</sub></small> value of 48.62 μg mL<small><sup>−1</sup></small>) and mushroom tyrosinase enzyme (tyrosinase is the enzyme responsible for hyperpigmentation) inhibition from 34.25% ± 3.68% to 90.90% ± 3.45%, with the highest activity at 100 μg mL<small><sup>−1</sup></small>. The above results indicate the potential of silver nanoparticles as antibacterial and antioxidant agents and tyrosinase inhibitors in the food, cosmetics and medicinal industries.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 147-162"},"PeriodicalIF":0.0,"publicationDate":"2024-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00173g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994247","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
Herceptin-conjugated plasmonic gold nanocapsules for targeted NIR-II photothermal therapy† 靶向NIR-II光热治疗的赫赛汀偶联等离子体金纳米胶囊
RSC Pharmaceutics Pub Date : 2024-11-21 DOI: 10.1039/D4PM00244J
Prem Singh, Ankita Sarkar, Nivedita Mukherjee and Amit Jaiswal
{"title":"Herceptin-conjugated plasmonic gold nanocapsules for targeted NIR-II photothermal therapy†","authors":"Prem Singh, Ankita Sarkar, Nivedita Mukherjee and Amit Jaiswal","doi":"10.1039/D4PM00244J","DOIUrl":"https://doi.org/10.1039/D4PM00244J","url":null,"abstract":"<p >In recent years, researchers have extensively studied nanomaterials for plasmonic photothermal therapy (PPTT), with most of the research focused on those active in the near-infrared I (NIR I) window (<em>λ</em> = 650–950 nm). However, there is growing interest in developing nanomaterials that are active in the near-infrared II (NIR II) region (<em>λ</em> = 950–1300 nm) due to the better penetrability and higher tolerance limit of NIR II light by human skin. In this study, the potential of gold nanocapsules (Au Ncap) with a rattle-like structure, consisting of a solid gold bead core and a porous, thin, rod-shaped gold shell was investigated for PPTT. Specifically, the targeted <em>in vitro</em> photothermal activity of Herceptin-conjugated gold nanocapsules that are active in both the NIR I and II regions are explored towards the Her2 positive SK-BR-3 breast cancer cell line. The conjugation of SH-PEG and Herceptin molecules on the surface of gold nanocapsules was validated through a detailed X-ray photoemission spectroscopy (XPS) analysis. The Au Ncap exhibited high photothermal conversion efficiency of 38.6% and <em>in vitro</em> PPTT results showed its excellent cytotoxicity against the SK-BR-3 cell line leading to apoptotic cell death. These findings suggest that this nanostructure can serve as an efficient photothermal agent in the NIR II region showing excellent PPTT activity at a low laser power density of 0.5 W cm<small><sup>−2</sup></small>.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 124-134"},"PeriodicalIF":0.0,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00244j?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994246","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
Controlling the solid-state and particle properties of a fixed-dose combination co-amorphous system by spray drying† 用喷雾干燥法控制固定剂量组合共晶体系的固态和颗粒特性
RSC Pharmaceutics Pub Date : 2024-11-20 DOI: 10.1039/D4PM00257A
Alice Parkes, Ahmad Ziaee and Emmet O'Reilly
{"title":"Controlling the solid-state and particle properties of a fixed-dose combination co-amorphous system by spray drying†","authors":"Alice Parkes, Ahmad Ziaee and Emmet O'Reilly","doi":"10.1039/D4PM00257A","DOIUrl":"https://doi.org/10.1039/D4PM00257A","url":null,"abstract":"<p >Controlling the solid-state stability of co-amorphous drug delivery systems has been an ongoing challenge in the pharmaceutical field to date. The main route to stabilise co-amorphous systems is to increase excipient load either in the co-amorphous formulation or <em>via</em> an additional excipient, creating a ternary amorphous system. Increasing excipient load in a formulation can have disadvantages such as producing large oral dosage forms. In this work, the impact of spray drying process parameters on the formation and short-term stability of a drug–drug co-amorphous mixture in the absence of any excipients is investigated. A 9-point design of experiments (DoE) was conducted to assess the impact of atomising gas flowrate and feed flowrate on the co-amorphous formation and stability. It was found that when the outlet temperature was fixed at 50 °C, the atomising gas flowrate had a more significant effect on the physical stability of the co-amorphous mixture than the feed flowrate. Monitoring the stability of formulations at accelerated stability conditions (40 °C per 75% relative humidity) showed that the co-amorphous systems produced at higher atomising gas flowrates, with smaller droplet sizes and subsequent particle sizes, exhibited a higher stability than those produced at lower atomising gas flowrates. Co-amorphous systems produced at the higher atomising gas flowrates remained stable for the 3-month stability testing period demonstrating that the co-amorphous physical stability can be controlled by optimising the spray drying process. The results presented in this study have significant implications for producing co-amorphous drug delivery systems with a high physical stability without the addition of excipients by spray drying.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 102-113"},"PeriodicalIF":0.0,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00257a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994244","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
Increased thermal stability and retained antibacterial properties in a sulbactam and amantadine salt: towards effective antibacterial–antiviral combination therapies† 舒巴坦和金刚烷胺盐中增加的热稳定性和保留的抗菌特性:朝向有效的抗菌抗病毒联合疗法†
RSC Pharmaceutics Pub Date : 2024-11-19 DOI: 10.1039/D4PM00247D
Josephine Bicknell, Ivan Bondarenko, Alice Colatrella, Elani J. Cabrera-Vega, Jesus Daniel Loya, Delbert S. Botes, Jay L. Mellies and Gonzalo Campillo-Alvarado
{"title":"Increased thermal stability and retained antibacterial properties in a sulbactam and amantadine salt: towards effective antibacterial–antiviral combination therapies†","authors":"Josephine Bicknell, Ivan Bondarenko, Alice Colatrella, Elani J. Cabrera-Vega, Jesus Daniel Loya, Delbert S. Botes, Jay L. Mellies and Gonzalo Campillo-Alvarado","doi":"10.1039/D4PM00247D","DOIUrl":"https://doi.org/10.1039/D4PM00247D","url":null,"abstract":"<p >We describe the formation of a multidrug salt comprising sulbactam (SUL, β-lactamase inhibitor) and amantadine (AMNH, antiviral). Physicochemical investigation of the <strong>SUL·AMNH</strong> salt revealed enhanced thermal stability compared to pristine starting materials. <em>In vitro</em> studies found that salt formation in <strong>SUL·AMNH</strong> does not disrupt antibacterial activity against model organisms <em>Escherichia coli</em> and <em>Staphylococcus epidermidis</em>. To our knowledge, we show the first β-lactamase inhibitor-antiviral salt where both components have been approved by the U.S. Food and Drug Administration (FDA), and the first multicomponent solid containing SUL. We envisage our strategy could inspire the design of multicomponent solids for antimicrobial combination therapies.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 958-962"},"PeriodicalIF":0.0,"publicationDate":"2024-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00247d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798234","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
Nano–bio interactions and drug delivery using soft nanoparticles: a new paradigm in pharmaceutical cargo release 纳米生物相互作用和使用软纳米颗粒的药物递送:药物货物释放的新范例
RSC Pharmaceutics Pub Date : 2024-11-15 DOI: 10.1039/D4PM00170B
Rohini Singh, Fei Rui Long, Anjali Saini, Natali Joma, Abhirup Basu, Morteza Mahmoudi, Hojatollah Vali and Ashok Kakkar
{"title":"Nano–bio interactions and drug delivery using soft nanoparticles: a new paradigm in pharmaceutical cargo release","authors":"Rohini Singh, Fei Rui Long, Anjali Saini, Natali Joma, Abhirup Basu, Morteza Mahmoudi, Hojatollah Vali and Ashok Kakkar","doi":"10.1039/D4PM00170B","DOIUrl":"https://doi.org/10.1039/D4PM00170B","url":null,"abstract":"<p >The bilateral relationship between nanomaterials and biological systems can play a significant role in therapeutic interventions and diagnostics. The nanomaterials may lose their synthetic identity after encountering biological fluids (<em>e.g.</em>, serum or plasma), and it might lead to unintended outcomes in real-time applications. Despite advances in nanomedicine, clinical translation and overall patient survival using nanoformulations have largely remained elusive. The layer of biomolecules formed around nanoparticles (NPs), often referred to as protein-corona (PC), can impact their physicochemical properties, including size, surface charge/chemistry, chemical composition, solubility, <em>etc</em>. Recently, a few mechanistic evaluations have demonstrated that the formation of a corona layer on nanoparticles can also have a consequential effect on the release profiles of polymeric soft NPs. To evaluate their therapeutic efficacy and resolve discrepancies that exist between <em>in vitro</em> and <em>in vivo</em> results, transition of NPs from their native to the corona-coupled state and its impact on unloading of their cargo need to be understood. Here, we highlight (i) how inherent properties of polymer precursors can affect PC build-up on soft NPs and its impact on cargo-release kinetics and (ii) limitations of existing methods in analyzing PC in complex systems, with emphasis on the impact nano–bio interactions have on the soft nanoparticle-based drug delivery domain.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 44-58"},"PeriodicalIF":0.0,"publicationDate":"2024-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00170b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994219","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 novel solid formulation of a rivaroxaban eutectic using a hot melt extruder with improved thermal stability and dissolution profile† 一种新型的利伐沙班共晶固体配方,采用热熔挤出机,具有更好的热稳定性和溶解谱†
RSC Pharmaceutics Pub Date : 2024-11-14 DOI: 10.1039/D4PM00253A
Parth S. Shaligram, Ranjitsinh Pawar, Nagabhushan Shet and Rajesh G. Gonnade
{"title":"A novel solid formulation of a rivaroxaban eutectic using a hot melt extruder with improved thermal stability and dissolution profile†","authors":"Parth S. Shaligram, Ranjitsinh Pawar, Nagabhushan Shet and Rajesh G. Gonnade","doi":"10.1039/D4PM00253A","DOIUrl":"https://doi.org/10.1039/D4PM00253A","url":null,"abstract":"<p >The current work aims to enhance the solubility, dissolution rate and stability of the poorly water-soluble drug rivaroxaban (RXB) by preparing an amorphous solid dispersion (ASD) of its eutectic with mandelic acid (MA) as an acidic coformer. Eutectics generally have lower melting points compared to their constituents. Hence, they can be used to lower the processing temperature of the drug to prevent its thermal degradation under a hot melt extruder (HME). Six eutectics of RXB were prepared with various carboxylic acid coformers. The eutectic of RXB and MA (1 : 4, mol/mol), which had the lowest melting point, was selected for the HME process. A hydrophilic polymeric matrix was used to prepare the ASD of the selected eutectic. The resultant extruded filament was further subjected to solubility and dissolution studies. We could load up to 25% RXB–MA eutectic in the polymer matrix to yield a complete ASD of RXB–MA at a lower processing temperature of 110 °C. The ASD of the RXB–MA eutectic showed three times the drug release compared to pure RXB. The RXB–MA (1 : 4) eutectic lowered the HME process temperature, further enhancing the thermal stability, solubility and dissolution rate of RXB. The solubility and dissolution rate enhancement might favourably impact the drug's bioavailability.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 114-123"},"PeriodicalIF":0.0,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00253a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994245","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
Navigating rheumatoid arthritis: insights into ligand-anchored nanoparticle strategies for anti-inflammatory therapy and relief 导航类风湿性关节炎:洞察配体锚定纳米颗粒策略抗炎治疗和缓解
RSC Pharmaceutics Pub Date : 2024-11-08 DOI: 10.1039/D4PM00133H
Shriya Karmarkar, Trinette Fernandes, Zainab Choonia, Sankalp Gharat and Sujata Sawarkar
{"title":"Navigating rheumatoid arthritis: insights into ligand-anchored nanoparticle strategies for anti-inflammatory therapy and relief","authors":"Shriya Karmarkar, Trinette Fernandes, Zainab Choonia, Sankalp Gharat and Sujata Sawarkar","doi":"10.1039/D4PM00133H","DOIUrl":"https://doi.org/10.1039/D4PM00133H","url":null,"abstract":"<p >Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease that primarily affects the synovial joints, causing substantial physical impairment, socioeconomic challenges and, in severe cases, death. Symptoms often appear between the ages of 35 and 60, with varying severity caused by periods of remission and exacerbation. In addition, children under the age of 16 might develop juvenile rheumatoid arthritis (JRA). According to a 2021 CDC poll, the World Health Organization estimates that 14 million people worldwide suffer with RA, with 0.92% of India's adult population afflicted. Non-steroidal anti-inflammatory drugs (NSAIDs), synthetic disease-modifying anti-rheumatic drugs (sDMARDs), and biological DMARDs are among the current therapeutic interventions. However, these therapies frequently exhibit limitations such as systemic side effects, short biological half-lives, erratic absorption, and frequent dosing regimens. Recent advances in ligand-based nanotechnology have introduced ligands such as folic acid and sialic acid that improve the targeted delivery when conjugated with nanoparticles. This approach has demonstrated efficacy in improving therapeutic outcomes while alleviating the side effects associated with conventional drug delivery systems. This review highlights the key molecular targets in RA, including T cells, B cells, and TNF-α, while exploring novel ligand-based active targeting strategies as innovative therapeutic avenues. Furthermore, it gives in-depth insights into critical molecular targets and their corresponding ligands, emphasizing the rising importance of ligand-based nanotechnology in the development of targeted drug therapy for autoimmune illnesses such as RA. The findings show the potential for these technologies to revolutionize RA therapy by improving medication specificity and reducing side effects <em>via</em> precise novel targeting mechanisms.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 19-43"},"PeriodicalIF":0.0,"publicationDate":"2024-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00133h?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994218","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
On-demand release of encapsulated ZnO nanoparticles and chemotherapeutics for drug delivery applications† 按需释放封装ZnO纳米颗粒和化疗药物递送应用。
RSC Pharmaceutics Pub Date : 2024-11-06 DOI: 10.1039/D4PM00189C
Josh E. Eixenberger, Catherine B. Anders, Rebecca Hermann, Katelyn Wada, Kongara M. Reddy, Raquel J. Montenegro-Brown, Daniel Fologea and Denise G. Wingett
{"title":"On-demand release of encapsulated ZnO nanoparticles and chemotherapeutics for drug delivery applications†","authors":"Josh E. Eixenberger, Catherine B. Anders, Rebecca Hermann, Katelyn Wada, Kongara M. Reddy, Raquel J. Montenegro-Brown, Daniel Fologea and Denise G. Wingett","doi":"10.1039/D4PM00189C","DOIUrl":"10.1039/D4PM00189C","url":null,"abstract":"<p >Nanomedicines offer high promise for the treatment of various diseases, and numerous novel approaches using nanomaterials have been developed over the years. In this report, we introduce a new strategy utilizing ZnO nanoparticles (nZnO) to trigger the rapid release of lipid-encapsulated therapeutics upon photo-irradiation with UV light (365 nm). <em>In vitro</em> studies demonstrate that encapsulation of nZnO effectively eliminates the cytotoxicity of nZnO, but this can be re-established upon release from the lipid coating. Using 5(6)-carboxyfluorescein as a model for hydrophilic drug loading, we show the ability to co-load drugs with nZnO into liposomes. Kinetic studies reveal the ability to release the majority of the dye within 60 minutes post-photo-irradiation and provide insights into factors that impact release kinetics. To further explore this, Jurkat T cell leukemia and T47D breast cancer cells were treated with co-encapsulated nZnO and the hydrophobic cancer drug paclitaxel. These studies revealed enhanced toxicity of the triggered release groups with an extreme difference noted in the viability profiles of the T47D breast cancer cell model. Taken together, these studies indicate that this system of co-encapsulating nZnO and chemotherapeutic drugs has the potential to minimize systemic toxicity, by controlling therapeutic release, while allowing for the localized selective destruction of cancer.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 82-93"},"PeriodicalIF":0.0,"publicationDate":"2024-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11650639/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142866908","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
From burst to controlled release: using hydrogel crosslinking chemistry to tune release of micro-crystalline active pharmaceutical ingredients† 从爆发到控释:利用水凝胶交联化学调节微晶活性药物成分的释放
RSC Pharmaceutics Pub Date : 2024-11-05 DOI: 10.1039/D4PM00186A
Purnima N. Manghnani, Arif Z. Nelson, Kelvin Wong, Yi Wei Lee, Saif A. Khan and Patrick S. Doyle
{"title":"From burst to controlled release: using hydrogel crosslinking chemistry to tune release of micro-crystalline active pharmaceutical ingredients†","authors":"Purnima N. Manghnani, Arif Z. Nelson, Kelvin Wong, Yi Wei Lee, Saif A. Khan and Patrick S. Doyle","doi":"10.1039/D4PM00186A","DOIUrl":"https://doi.org/10.1039/D4PM00186A","url":null,"abstract":"<p >Hydrogels have been widely studied as substrates for drug delivery and tissue engineering owing to their biocompatibility and ability to swell in aqueous media. Encapsulation of lipophilic active pharmaceutical ingredients (API) as crystalline micro-/nanoparticles within hydrogel formulations has shown promise for improving their bioavailability and achieving high drug load. Despite the size reduction of the API within the hydrogel mesh, the bioavailability of these formulations is largely governed by the inherent ability of the hydrogel polymer backbone to release the API. In this work, Michael addition-based Polyethylene glycol (PEG) hydrogels are developed for micro-crystalline fenofibrate (Fen) encapsulation. Using a parallelized step emulsification device, API nanoemulsion (NE) loaded micro-hydrogels are fabricated and subsequently subjected to anti-solvent extraction for API crystallization. The bi-molecular nature of the Michael addition reaction provides modular incorporation of crosslinking functional groups leading to precise temporal control over hydrogel degradation, thereby offering a sensitive handle on the release of micro-crystalline fenofibrate. By merely changing the chemical identity of the hydrogel cross-link, complete Fen release could be tuned from 4 hours to 10 days. Furthermore, the interaction of crystallizing Fen and PEG within the micro-hydrogel environment led to eutectic formation. This unique feature offered a second handle on the Fen release from the composite micro-hydrogels.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 1","pages":" 94-101"},"PeriodicalIF":0.0,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00186a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994222","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
Effect of fluorine substituents in 4-(1-benzyl-1H-benzo[d]imidazol-2-yl)thiazole for the study of antiparasitic treatment of cysticercosis on a Taenia crassiceps model† 4-(1-苄基- 1h -苯并[d]咪唑-2-基)噻唑中氟取代基对猪带绦虫模型抗寄生虫治疗囊虫病的影响
RSC Pharmaceutics Pub Date : 2024-11-01 DOI: 10.1039/D4PM00210E
Monserrath I. Rodríguez-Mora, Raúl Colorado-Peralta, Viviana Reyes-Márquez, Marco A. García-Eleno, Erick Cuevas-Yáñez, Jesús R. Parra-Unda, Abraham Landa and David Morales-Morales
{"title":"Effect of fluorine substituents in 4-(1-benzyl-1H-benzo[d]imidazol-2-yl)thiazole for the study of antiparasitic treatment of cysticercosis on a Taenia crassiceps model†","authors":"Monserrath I. Rodríguez-Mora, Raúl Colorado-Peralta, Viviana Reyes-Márquez, Marco A. García-Eleno, Erick Cuevas-Yáñez, Jesús R. Parra-Unda, Abraham Landa and David Morales-Morales","doi":"10.1039/D4PM00210E","DOIUrl":"https://doi.org/10.1039/D4PM00210E","url":null,"abstract":"<p >This work details the synthesis of five <em>N</em>-benzylated derivatives of thiabendazoles (<strong>L1–L5</strong>), four of which were previously unreported in the literature (<strong>L2–L5</strong>). The compounds were characterised using a comprehensive array of spectroscopic (FT-IR, <small><sup>1</sup></small>H, <small><sup>13</sup></small>C{1H}, and <small><sup>19</sup></small>F{1H} NMR), spectrometric (MS-EI+) and diffractometric (SC-DRX) techniques. To evaluate the effect of increased fluorine substituents in the <em>N</em>-benzyl fragment, we conducted a parasitotoxic activity assay, testing the compounds at various concentrations of unhatched <em>Taenia crassiceps</em> cysticerci. The inclusion of the <em>N</em>-benzyl fragment and the increase in fluorine substituents led to an enhancement in the lipophilicity of thiabendazoles.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 5","pages":" 1055-1065"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00210e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142798217","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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