Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c02108
Jiangwei Zhao , Yunxiao Dong , Jin Zhu , Jinggang Wang
Biobased polyesters based on 2,5-furandicarboxylic acid show great potential for replacing conventional plastics, but their practical applications are still limited by the inherent brittleness of the materials. A series of high molecular-weight poly(ethylene-diethylene glycol 2,5-furandicarboxylate) (PEDF) copolyesters were synthesized by introducing diethylene glycol, which contained a flexible oxygen ether bond. The thermal stability, mechanical properties, and optical transparency of the PEDF copolyesters improved significantly with the increasing diethylene glycol content. The elongation at break of PED40F can reach 43% which is up to 10.7 folds compared with PEF and maintains a high tensile modulus of 2440 MPa and a tensile strength of 74 MPa, as well as a mass loss of 45.79% after 49 days under CALB enzymatic degradation conditions. In addition, PEDF copolyester has excellent gas barrier properties, with carbon dioxide and oxygen barrier improvement factors (BIFp) 13.0 and 7.3 times higher than those of PET.
{"title":"Highly Tough, Barrier, and Biodegradable Copolyesters Synthesized from Furandicarboxylic Acid","authors":"Jiangwei Zhao , Yunxiao Dong , Jin Zhu , Jinggang Wang","doi":"10.1021/acs.biomac.5c02108","DOIUrl":"10.1021/acs.biomac.5c02108","url":null,"abstract":"<div><div>Biobased polyesters based on 2,5-furandicarboxylic acid show great potential for replacing conventional plastics, but their practical applications are still limited by the inherent brittleness of the materials. A series of high molecular-weight poly(ethylene-diethylene glycol 2,5-furandicarboxylate) (PEDF) copolyesters were synthesized by introducing diethylene glycol, which contained a flexible oxygen ether bond. The thermal stability, mechanical properties, and optical transparency of the PEDF copolyesters improved significantly with the increasing diethylene glycol content. The elongation at break of PED<sub>40</sub>F can reach 43% which is up to 10.7 folds compared with PEF and maintains a high tensile modulus of 2440 MPa and a tensile strength of 74 MPa, as well as a mass loss of 45.79% after 49 days under CALB enzymatic degradation conditions. In addition, PEDF copolyester has excellent gas barrier properties, with carbon dioxide and oxygen barrier improvement factors (BIFp) 13.0 and 7.3 times higher than those of PET.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 835-844"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145877253","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Aggregation-Induced Emission (AIE) is a feature of fluorophores that overcomes the demerits of Aggregation-Caused Quenching (ACQ), which limits the utility of traditional dyes in cancer bioimaging. Tetraphenylethene (TPE) is the prototypical AIEgen among the very few compounds with this property. However, it lacks inherent targeting specificity or therapeutic functions. In an attempt to design an AIE-active, target-specific therapeutic agent, we herein report a quad-functional AIEgen derived from the golden spice – curcumin. The “Golden Spiced AIEgen” was engineered by introducing a phenylboronic acid group into curcumin, imparting pH-responsive and sialic acid-targeting properties. Further integration into self-assembling amphiphilic micelles co-loaded with chemotherapeutics enabled effective loading with extended release. The integrated nanosystem was fully biocompatible with noncancerous cells while effectively killing HepG2 liver cancer cells through sialic acid-mediated AIEgen uptake. It acted synergistically with chemotherapeutic drugs for improved treatment outcomes, and its efficacy was corroborated in hepatocarcinoma in vivo.
{"title":"Design and Synthesis of an Aggregation-Induced Emission-Active Quad-Functional “Curcumin-Spiced Marvel” for Engineering of Sialic Acid-Targeted Nanoplatform for Cancer Therapy","authors":"Twara Kikani , Krutika Patel , Aneri Joshi , Devanshi Gajjar , Sriram Seshadri , Sonal Thakore","doi":"10.1021/acs.biomac.5c02001","DOIUrl":"10.1021/acs.biomac.5c02001","url":null,"abstract":"<div><div>Aggregation-Induced Emission (AIE) is a feature of fluorophores that overcomes the demerits of Aggregation-Caused Quenching (ACQ), which limits the utility of traditional dyes in cancer bioimaging. Tetraphenylethene (TPE) is the prototypical AIEgen among the very few compounds with this property. However, it lacks inherent targeting specificity or therapeutic functions. In an attempt to design an AIE-active, target-specific therapeutic agent, we herein report a quad-functional AIEgen derived from the golden spice – curcumin. The “Golden Spiced AIEgen” was engineered by introducing a phenylboronic acid group into curcumin, imparting pH-responsive and sialic acid-targeting properties. Further integration into self-assembling amphiphilic micelles co-loaded with chemotherapeutics enabled effective loading with extended release. The integrated nanosystem was fully biocompatible with noncancerous cells while effectively killing HepG2 liver cancer cells through sialic acid-mediated AIEgen uptake. It acted synergistically with chemotherapeutic drugs for improved treatment outcomes, and its efficacy was corroborated in hepatocarcinoma <em>in vivo</em>.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 747-763"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145848465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Polypeptide coacervates exhibit remarkable cell membrane permeability for drug delivery, but the precise internalization mechanism is unclear. Here, taking histidine-rich beak derivative protein (HBpep-SR) coacervate as a model, we investigate the interactions of coacervates with ternary lipid raft membranes and mammalian plasma membranes using the Martini 3.0 force field. We show that coacervates preferentially wet the liquid disordered (Ld) phase in a cholesterol-dependent manner with an encapsulation efficiency in the Ld phase of approximately 60%. In rigid, cholesterol-depleted ternary membranes, coacervates fail to induce membrane bending and disperse over time. Conversely, the flexibility of unsaturated lipids in the Ld phase of lipid rafts promotes coacervate wrapping, a process mediated by aromatic rings in polypeptides. Similar trends are observed in plasma membrane systems and other polypeptide coacervate systems. Our findings reveal a universal pathway for coacervate uptake via Ld regions, offering crucial insights for designing coacervates with enhanced cellular internalization.
{"title":"Cholesterol-Rich Membranes Wetting by Polypeptide Coacervate: Pathway and Mechanism via the Liquid-Disordered Phase","authors":"Yiwei Wang, Rongrong Zou, Minghao Wang, Yeqiang Zhou, Yang Liu, Mingming Ding","doi":"10.1021/acs.biomac.5c02341","DOIUrl":"10.1021/acs.biomac.5c02341","url":null,"abstract":"<div><div>Polypeptide coacervates exhibit remarkable cell membrane permeability for drug delivery, but the precise internalization mechanism is unclear. Here, taking histidine-rich beak derivative protein (HBpep-SR) coacervate as a model, we investigate the interactions of coacervates with ternary lipid raft membranes and mammalian plasma membranes using the Martini 3.0 force field. We show that coacervates preferentially wet the liquid disordered (Ld) phase in a cholesterol-dependent manner with an encapsulation efficiency in the Ld phase of approximately 60%. In rigid, cholesterol-depleted ternary membranes, coacervates fail to induce membrane bending and disperse over time. Conversely, the flexibility of unsaturated lipids in the Ld phase of lipid rafts promotes coacervate wrapping, a process mediated by aromatic rings in polypeptides. Similar trends are observed in plasma membrane systems and other polypeptide coacervate systems. Our findings reveal a universal pathway for coacervate uptake via Ld regions, offering crucial insights for designing coacervates with enhanced cellular internalization.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 952-963"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145861367","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c02331
Penghui Wang , Jialing Li , Yingying Yang , Wenjie Zhang , Ji Zhu , Bo Chi
The reconstruction of abdominal wall defects and prevention of postoperative visceral adhesions remain critical clinical challenges in managing abdominal trauma. Here, a highly bioactive macroporous hyaluronic acid hydrogel was firmly integrated onto the upper layer of the poly(vinyl alcohol) hydrogel through dynamic borate ester bonds to construct the biomimetic repair patch (PHA). The anisotropic backbone prepared based on a top-down solvent exchange strategy achieved strong mechanical strength (2.69 MPa), excellent elastic deformation (369.73%), and biomimetic structure of asymmetric porous surfaces with upper (79.62 μm) and lower (0.63 μm) pore sizes. The in vivo abdominal wall defect repair model demonstrated that the asymmetric porous structure of the PHA patch simultaneously enables in situ regeneration of abdominal wall tissues and suppression of visceral adhesions. Therefore, the design of the PHA patch opens a new avenue for developing an integrated biomimetic abdominal wall material, holding significant practical implications for enhancing the clinical treatment efficacy of abdominal wall defects.
{"title":"Anisotropic Janus Hydrogel Patch for Abdominal Wall Regeneration and Postoperative Antiadhesion","authors":"Penghui Wang , Jialing Li , Yingying Yang , Wenjie Zhang , Ji Zhu , Bo Chi","doi":"10.1021/acs.biomac.5c02331","DOIUrl":"10.1021/acs.biomac.5c02331","url":null,"abstract":"<div><div>The reconstruction of abdominal wall defects and prevention of postoperative visceral adhesions remain critical clinical challenges in managing abdominal trauma. Here, a highly bioactive macroporous hyaluronic acid hydrogel was firmly integrated onto the upper layer of the poly(vinyl alcohol) hydrogel through dynamic borate ester bonds to construct the biomimetic repair patch (PHA). The anisotropic backbone prepared based on a top-down solvent exchange strategy achieved strong mechanical strength (2.69 MPa), excellent elastic deformation (369.73%), and biomimetic structure of asymmetric porous surfaces with upper (79.62 μm) and lower (0.63 μm) pore sizes. The <em>in vivo</em> abdominal wall defect repair model demonstrated that the asymmetric porous structure of the PHA patch simultaneously enables <em>in situ</em> regeneration of abdominal wall tissues and suppression of visceral adhesions. Therefore, the design of the PHA patch opens a new avenue for developing an integrated biomimetic abdominal wall material, holding significant practical implications for enhancing the clinical treatment efficacy of abdominal wall defects.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 938-951"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145706826","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c01884
Anna J Boland , Michelle K Greene , Úna M Herron , Michael C Johnston , Peter Smyth , Hideo Yagita , Daniel B Longley , Christopher J Scott
Death receptor 5 (DR5) is a key mediator of the extrinsic apoptotic pathway that is often upregulated in tumors, rendering it an attractive target for cancer therapy. Activation of DR5 requires oligomerization, which can be achieved through multivalent presentation of DR5 ligands on nanoparticles. DR5-targeted nanoparticles can efficiently agonize DR5 to inhibit the growth of human xenografts, although it remains unclear whether these effects would translate to a syngeneic tumor model with an immunocompetent microenvironment. Here, we develop camptothecin-loaded polymeric nanoparticles coated with the murine DR5 antibody MD5–1 and demonstrate their pro-apoptotic effects in murine cell lines in vitro. Moreover, we show that these nanoparticles inhibit the growth of MC38 colorectal allografts in vivo by >90% relative to control nanoparticles. Collectively, our work confirms that the antitumor efficacy of DR5-targeted nanoparticles extends to syngeneic models, paving the way for future studies to explore their impact on tumor immunity and the surrounding microenvironment.
{"title":"Antitumor Activity of Death Receptor 5‑Targeted Camptothecin-Loaded Nanoparticles in Murine Syngeneic Models","authors":"Anna J Boland , Michelle K Greene , Úna M Herron , Michael C Johnston , Peter Smyth , Hideo Yagita , Daniel B Longley , Christopher J Scott","doi":"10.1021/acs.biomac.5c01884","DOIUrl":"10.1021/acs.biomac.5c01884","url":null,"abstract":"<div><div>Death receptor 5 (DR5) is a key mediator of the extrinsic apoptotic pathway that is often upregulated in tumors, rendering it an attractive target for cancer therapy. Activation of DR5 requires oligomerization, which can be achieved through multivalent presentation of DR5 ligands on nanoparticles. DR5-targeted nanoparticles can efficiently agonize DR5 to inhibit the growth of human xenografts, although it remains unclear whether these effects would translate to a syngeneic tumor model with an immunocompetent microenvironment. Here, we develop camptothecin-loaded polymeric nanoparticles coated with the murine DR5 antibody MD5–1 and demonstrate their pro-apoptotic effects in murine cell lines <em>in vitro</em>. Moreover, we show that these nanoparticles inhibit the growth of MC38 colorectal allografts <em>in vivo</em> by >90% relative to control nanoparticles. Collectively, our work confirms that the antitumor efficacy of DR5-targeted nanoparticles extends to syngeneic models, paving the way for future studies to explore their impact on tumor immunity and the surrounding microenvironment.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 662-671"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145720071","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c01953
Zijun Li , Kandasamy Saravanakumar , Lulu Yao , Yunyeong Kim , Jungyu Jo , Sang Yoon Choi , Guijae Yoo , Phil Jun Lee , Soeun Kim , Namki Cho
Cyclopeptides are promising anticancer agents due to their ability to regulate multiple signaling pathways. In this study, a novel cyclopeptide, Asiminatide A (AA), was isolated from Asimina triloba, and a nanodrug delivery system (nDDS) was developed to enhance its efficacy against triple-negative breast cancer (TNBC). High-resolution time-of-flight mass spectrometer (HR-TOF-MS) and 1H/13C NMR analyses identified AA as a cyclic heptapeptide composed of Pro-Val-Phe-Ile-Ser-Ile-Gly. AA was encapsulated into folic-acid-conjugated chitosan nanoparticles (AA-FA-CS NPs), as confirmed by 1H NMR and Fourier-transform infrared spectroscopy (FTIR). The nanoparticles exhibited pH-responsive drug release with enhanced release at pH 5.2. In vitro studies showed that dual pH- and folate receptor-targeted delivery significantly enhanced cytotoxicity in MDA-MB-231 cells via oxidative stress and nuclear damage while maintaining good biocompatibility. In vivo, AA-FA-CS NPs effectively suppressed tumor growth without any evident organ toxicity. These results demonstrate the anticancer potential of AA enabled by nanodelivery.
环肽由于其调节多种信号通路的能力而成为很有前途的抗癌药物。本研究从三叶草中分离出一种新的环肽——亚胺肽a (AA)，并开发了一种纳米给药系统（nDDS）来增强其抗三阴性乳腺癌（TNBC）的疗效。高分辨率飞行时间质谱（HR-TOF-MS）和1H/13C核磁共振分析证实AA是由Pro-Val-Phe-Ile-Ser-Ile-Gly组成的环七肽。通过1H NMR和FTIR对AA- fa - cs纳米粒（AA- fa - cs NPs）进行了包封。纳米颗粒表现出pH响应性的药物释放，在pH 5.2时释放增强。体外研究表明，双重pH和叶酸受体靶向递送可通过氧化应激和核损伤显著增强MDA-MB-231细胞的细胞毒性，同时保持良好的生物相容性。在体内，AA-FA-CS NPs有效抑制肿瘤生长，无明显器官毒性。这些结果证明了纳米递送激活的AA具有抗癌潜力。
{"title":"Enhanced Anticancer Efficacy of Novel Asiminatide A Isolated from Asimina triloba in Triple-Negative Breast Cancer","authors":"Zijun Li , Kandasamy Saravanakumar , Lulu Yao , Yunyeong Kim , Jungyu Jo , Sang Yoon Choi , Guijae Yoo , Phil Jun Lee , Soeun Kim , Namki Cho","doi":"10.1021/acs.biomac.5c01953","DOIUrl":"10.1021/acs.biomac.5c01953","url":null,"abstract":"<div><div>Cyclopeptides are promising anticancer agents due to their ability to regulate multiple signaling pathways. In this study, a novel cyclopeptide, Asiminatide A (AA), was isolated from Asimina triloba, and a nanodrug delivery system (nDDS) was developed to enhance its efficacy against triple-negative breast cancer (TNBC). High-resolution time-of-flight mass spectrometer (HR-TOF-MS) and <sup>1</sup>H/<sup>13</sup>C NMR analyses identified AA as a cyclic heptapeptide composed of Pro-Val-Phe-Ile-Ser-Ile-Gly. AA was encapsulated into folic-acid-conjugated chitosan nanoparticles (AA-FA-CS NPs), as confirmed by <sup>1</sup>H NMR and Fourier-transform infrared spectroscopy (FTIR). The nanoparticles exhibited pH-responsive drug release with enhanced release at pH 5.2. <em>In vitro</em> studies showed that dual pH- and folate receptor-targeted delivery significantly enhanced cytotoxicity in MDA-MB-231 cells via oxidative stress and nuclear damage while maintaining good biocompatibility. <em>In vivo</em>, AA-FA-CS NPs effectively suppressed tumor growth without any evident organ toxicity. These results demonstrate the anticancer potential of AA enabled by nanodelivery.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 702-715"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145848574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c01944
Desoshree Ghosh, Sagar Bag, Priyadarsi De
Enzymes are one of the protagonists present in living organisms, which execute numerous biochemical reactions with ultimate chemo/regioselectivity, specificity, and high turnover number under physiological conditions. Harnessing these advantages, enzyme-responsive materials endow excellent therapeutic efficiency to ameliorate several healthcare adversities. In parallel, polymeric materials have emerged as powerful therapeutic platforms due to their biocompatibility, tunable architectures, enhanced tissue penetration, and ability to form diverse self-assembled nanostructures. Over recent decades, extensive research has focused on developing enzyme-responsive polymers (ERPs) for various healthcare applications. This review article highlights recent (2014–present) advancements in the field of ERPs for anticancer and antibacterial therapies. Furthermore, several underexplored enzymes are showcased with promising potential for innovative ERP design for impactful future biomedical applications. Overall, this review aims to guide readers in predictably leveraging ERPs to address critical biomedical challenges.
{"title":"Enzyme-Responsive Polymeric Materials with Anticancer and Antibacterial Activities","authors":"Desoshree Ghosh, Sagar Bag, Priyadarsi De","doi":"10.1021/acs.biomac.5c01944","DOIUrl":"10.1021/acs.biomac.5c01944","url":null,"abstract":"<div><div>Enzymes are one of the protagonists present in living organisms, which execute numerous biochemical reactions with ultimate chemo/regioselectivity, specificity, and high turnover number under physiological conditions. Harnessing these advantages, enzyme-responsive materials endow excellent therapeutic efficiency to ameliorate several healthcare adversities. In parallel, polymeric materials have emerged as powerful therapeutic platforms due to their biocompatibility, tunable architectures, enhanced tissue penetration, and ability to form diverse self-assembled nanostructures. Over recent decades, extensive research has focused on developing enzyme-responsive polymers (ERPs) for various healthcare applications. This review article highlights recent (2014–present) advancements in the field of ERPs for anticancer and antibacterial therapies. Furthermore, several underexplored enzymes are showcased with promising potential for innovative ERP design for impactful future biomedical applications. Overall, this review aims to guide readers in predictably leveraging ERPs to address critical biomedical challenges.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 16-58"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145808986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c01912
Mengsi Yin, Zijian Qiu, Mengju Xu, Faxin Zhang, Xianglong Wang, Jiaping Zhou, Xiaofu Liang, Weiyu Yan, Ya Yu, Mingyuan Li
Lutein (Lut) and retinol (Ret) exhibit synergistic antioxidant effects yet suffer from poor water solubility and stability. The DPPH assay confirmed that their 1:1 ratio (350 μg/mL each) yielded a high free radical scavenging rate of 86.52 ± 2.24%. Via microfluidic technology, 130 nm Lut/Ret coloaded nanoparticles (L/R-NPs) were successfully prepared with Zein and PVP K30 as carriers; molecular dynamics indicated that van der Waals and electrostatic interactions stabilize their core–shell structure. Embedded in sodium alginate–agarose (SA-Agar) hydrogel beads (L/RNP-GBs) with high encapsulation efficiency (EE), 1:1 L/RNP-GBs had lower rigidity, better elasticity, and reduced dysphagia risk compared to the 1:3 ratio. Crucially, L/RNP-GBs showed pH-responsive release: minimal at pH 1.2, sustained at pH 6.8, enabling intestinal targeting and enhancing bioaccessibility. This “nanoparticle-hydrogel bead” system effectively addresses Lut/Ret delivery challenges, offering a promising strategy for fat-soluble bioactives.
{"title":"pH-Responsive Release Hydrophilic Colloids: Preparation and Characterization of Lutein/Retinol Coloaded Nanoparticles and Their Hydrogel Beads","authors":"Mengsi Yin, Zijian Qiu, Mengju Xu, Faxin Zhang, Xianglong Wang, Jiaping Zhou, Xiaofu Liang, Weiyu Yan, Ya Yu, Mingyuan Li","doi":"10.1021/acs.biomac.5c01912","DOIUrl":"10.1021/acs.biomac.5c01912","url":null,"abstract":"<div><div>Lutein (Lut) and retinol (Ret) exhibit synergistic antioxidant effects yet suffer from poor water solubility and stability. The DPPH assay confirmed that their 1:1 ratio (350 μg/mL each) yielded a high free radical scavenging rate of 86.52 ± 2.24%. Via microfluidic technology, 130 nm Lut/Ret coloaded nanoparticles (L/R-NPs) were successfully prepared with Zein and PVP K30 as carriers; molecular dynamics indicated that van der Waals and electrostatic interactions stabilize their core–shell structure. Embedded in sodium alginate–agarose (SA-Agar) hydrogel beads (L/R<sup>NP</sup>-GBs) with high encapsulation efficiency (EE), 1:1 L/R<sup>NP</sup>-GBs had lower rigidity, better elasticity, and reduced dysphagia risk compared to the 1:3 ratio. Crucially, L/R<sup>NP</sup>-GBs showed pH-responsive release: minimal at pH 1.2, sustained at pH 6.8, enabling intestinal targeting and enhancing bioaccessibility. This “nanoparticle-hydrogel bead” system effectively addresses Lut/Ret delivery challenges, offering a promising strategy for fat-soluble bioactives.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 640-661"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145814651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c01204
Taylor M. Page , Kai Ludwig , Muhammad Shayan Haider , Elisa Quaas , Alexandros Mavroskoufis , Peng Tang , Rui Chen , Jun Feng, Raju Bej , Katharina Achazi , Rainer Haag , Ievgen S. Donskyi
Targeted drug delivery systems that are stimuli-responsive offer great potential for enhancing the therapeutic activity of drugs, decreasing off-target effects, and improving bioavailability. This proof-of-concept study introduces an amphiphilic drug delivery system (DDS) capable of loading hydrophobic cargo. Elevated glutathione (GSH) levels, characteristic of certain types of cancer cells’ microenvironment, degrade the nanostructures and release the cargo. Linear polyglycerol sulfate (LPGS), known for its excellent biocompatibility, is combined with lipoic acid (LA). LA facilitates the formation of cross-linked nanosheet amphiphiles sensitive to reductive conditions. Morphological changes are observed by scanning electron microscopy (SEM), cryogenic transmission electron microscopy (Cryo-TEM), and cryogenic electron tomography (Cryo-ET) upon UV irradiation (hν), creating a stable aggregate for loading hydrophobic cargo and assembling into sheets at elevated concentrations. The resulting material displays controlled release of model dyes under increased levels of GSH, tunable by the polymer size and LPGS:LA acid ratios. This behavior enhances targeted therapy and reduced off-target effects. Further loading with paclitaxel and subsequent release, together with in vitro assays, demonstrates the system’s compatibility with an anticancer drug.
{"title":"Redox-Responsive Self-Assembled Amphiphilic Nanosheets from Polyglycerol Sulfate–Lipoic Acid Copolymers for Targeted Cancer Drug Delivery","authors":"Taylor M. Page , Kai Ludwig , Muhammad Shayan Haider , Elisa Quaas , Alexandros Mavroskoufis , Peng Tang , Rui Chen , Jun Feng, Raju Bej , Katharina Achazi , Rainer Haag , Ievgen S. Donskyi","doi":"10.1021/acs.biomac.5c01204","DOIUrl":"10.1021/acs.biomac.5c01204","url":null,"abstract":"<div><div>Targeted drug delivery systems that are stimuli-responsive offer great potential for enhancing the therapeutic activity of drugs, decreasing off-target effects, and improving bioavailability. This proof-of-concept study introduces an amphiphilic drug delivery system (DDS) capable of loading hydrophobic cargo. Elevated glutathione (GSH) levels, characteristic of certain types of cancer cells’ microenvironment, degrade the nanostructures and release the cargo. Linear polyglycerol sulfate (LPGS), known for its excellent biocompatibility, is combined with lipoic acid (LA). LA facilitates the formation of cross-linked nanosheet amphiphiles sensitive to reductive conditions. Morphological changes are observed by scanning electron microscopy (SEM), cryogenic transmission electron microscopy (Cryo-TEM), and cryogenic electron tomography (Cryo-ET) upon UV irradiation (<em>h</em>ν), creating a stable aggregate for loading hydrophobic cargo and assembling into sheets at elevated concentrations. The resulting material displays controlled release of model dyes under increased levels of GSH, tunable by the polymer size and LPGS:LA acid ratios. This behavior enhances targeted therapy and reduced off-target effects. Further loading with paclitaxel and subsequent release, together with <em>in vitro</em> assays, demonstrates the system’s compatibility with an anticancer drug.</div></div><div><div><span><figure></figure></span></div></div>","PeriodicalId":30,"journal":{"name":"Biomacromolecules","volume":"27 1","pages":"Pages 249-258"},"PeriodicalIF":5.4,"publicationDate":"2026-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145659837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-12DOI: 10.1021/acs.biomac.5c02091
Sarah G. Fisher, Zachary Buck, Margaret J. Karim, Jaime C. Grunlan
Food packaging is critical to prevent food waste, but most of the packaging used today is not sustainable. Paper-based packaging materials offer a renewable option, but exhibit poor resistance to common permeants such as oxygen, grease, and water vapor. In this work, a complex coacervate coating is prepared from two waste biopolymers, gelatin and DNA, and applied to kraft paper to substantially improve its barrier properties. Thermally curing the coating after deposition decreases the water vapor transmission rate and oxygen transmission rate by 83 and 99%, respectively, relative to uncoated paper. This work represents one of the best fully biobased barrier coatings reported for paper and is a promising option for sustainable food packaging.
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