Articles published on Poor Solubility
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- New
- Research Article
- 10.1039/d5mh02076j
- Feb 4, 2026
- Materials horizons
- Kang Wang + 9 more
Achieving scarless healing combined with skin appendage regeneration remains an extremely challenging task in the treatment of skin wounds. Vitamin A derivatives have shown great potential for follicle neogenesis and scarless repair but suffer from poor solubility, instability, photosensitivity, and toxicity in wound healing processes. Here, we present a multifunctional bioadhesive hydrogel system that integrates polydopamine (PDA) nanoparticles with vitamin A derivatives to promote functional skin regeneration. The PDA nanoparticles stabilized and enabled pH-responsive release of vitamin A derivatives, while simultaneously providing reactive oxygen species (ROS) scavenging and antioxidant protection. Embedded within an imine-crosslinked adhesive hydrogel network, this platform achieved strong tissue adhesion, sustained drug delivery, and favorable immune microenvironment modulation. In vivo, using both rat burn wounds and rabbit hypertrophic scar models, the optimized formulation accelerated wound closure, rebalanced collagen deposition, suppressed myofibroblast activation, and markedly prevented pathological fibrosis. Strikingly, it also induced robust de novo hair follicle formation, indicating true functional tissue restoration. Transcriptomic and immunofluorescence analyses further revealed downregulation of pro-fibrotic and inflammatory pathways alongside activation of regenerative signaling, including M2 macrophage polarization and suppression of the M1 phenotype in treated wounds. This study introduces an early vitamin A-based nanocomposite hydrogel with dual anti-scarring and regenerative functions, offering a promising strategy for advanced wound care.
- New
- Research Article
- 10.1039/d5tb02141c
- Feb 4, 2026
- Journal of materials chemistry. B
- Amene Navaser + 1 more
Targeted modulation of enzyme activity offers a promising strategy for both elucidating catalytic mechanisms and developing novel therapeutics. In this study Zn2+ ions were introduced as an effective competitive inhibitor of fumarase, a pivotal enzyme in the citric acid cycle. Zn2+ binding significantly alters the Michaelis constant (Km) for both L-malate and fumarate, with a pronounced preference for inhibiting the reverse reaction (L-malate to fumarate), a direction relevant to redox homeostasis and anaplerotic flux. A major limitation of the clinical application of many metal-based inhibitors is their poor water solubility. To overcome this challenge and introduce a new class of enzyme inhibitors, zinc-modified carbon quantum dots (Zn-CQDs) were synthesized. Owing to their polar surface, Zn-CQDs interact more effectively with the enzyme, which increases the local concentration of Zn2+ ions at the active site. As a result, these nanomaterials exhibit enhanced water solubility and significantly greater inhibitory potency compared to free Zn2+ ions. Biophysical and kinetic analyses confirmed the competitive inhibition mechanism and demonstrated that Zn-CQDs interact with the enzyme without perturbing its secondary structure. Notably, both Zn2+ ions and Zn-CQDs preferentially inhibited the reverse reaction of fumarase, offering precise control over fumarase activity. Molecular docking and MD simulations elucidated the plausible binding site of Zn2+ within the active site. It was found that Zn2+ interacts with Glu340, a residue previously shown to be involved in binding fumarase inhibitors. These findings establish Zn-CQDs as a novel class of water-soluble fumarase inhibitors, distinguished by their facile synthesis, tunable solubility, and selective inhibition profile. This work highlights the potential of zinc-based nanomaterials in enzyme regulation, offering a powerful alternative to existing inhibitors and developing targeted redox-sensitive therapeutic strategies.
- New
- Research Article
- 10.1021/acs.langmuir.5c05751
- Feb 3, 2026
- Langmuir : the ACS journal of surfaces and colloids
- Shixi Li + 8 more
To address the limitations of conventional fluorescent probes, including aggregation-caused quenching (ACQ) and poor water solubility, an intelligent nanoprobe (LPNPs@SA) with tumor microenvironment responsiveness and aggregation-induced emission (AIE) properties was developed. This nanoprobe enables sequential, reversible, and highly sensitive detection of Cu2+ and S2-. The AIE-active fluorophore salicylaldehyde azine (SA) was designed and synthesized, exhibiting intense emission in aggregated states but poor stability under non-neutral pH conditions. To overcome this limitation, SA was encapsulated into lipid-polymer hybrid nanoparticles (LPNPs) via self-assembly using an amphiphilic copolymer (C16-SS-PEG/DMMA), polycaprolactone (PCL), and phosphatidylcholine (PC). The resulting LPNPs@SA nanoprobe possessed favorable storage stability, broad pH tolerance, effective surface charge conversion, and good hemocompatibility, with a hemolysis rate below 5%. In terms of sensing performance, the nanoprobe showed selective fluorescence quenching ("turn-off" mode) toward Cu2+. Stern-Volmer analysis revealed a quenching constant (Ksv) of 2.9 × 105 L/mol. Further fluorescence titration and Job's plot analyses confirmed a 1:1 binding stoichiometry between the nanoprobe and Cu2+, with an association constant (Ka) of 2.2 × 104 L/mol. The detection limit (LOD) for Cu2+ was determined to be 1.2 μmol/L, demonstrating high sensitivity. Remarkably, upon introducing S2- into the copper-loaded nanoprobe system, substantial fluorescence recovery was observed, yielding a distinct "turn-on" signal for S2- detection. In summary, this work presents a biocompatible nanoprobe with excellent optical properties that functions as an effective reversible fluorescence-switching platform. It offers a promising analytical tool for dynamically monitoring Cu2+ and S2- in biological environments, facilitating studies of related pathological processes and potential diagnostic applications.
- New
- Research Article
- 10.1016/j.foodres.2025.118070
- Feb 1, 2026
- Food research international (Ottawa, Ont.)
- Junlin Ge + 7 more
Enhancing the functional properties of egg yolk through post-treatments following short-term fermentation for application in powdered oils.
- New
- Research Article
- 10.1002/cbdv.202502609
- Feb 1, 2026
- Chemistry & biodiversity
- Zeba Usmani + 6 more
The skin functions as the body's primary defensive barrier, safeguarding internal organs from environmental, physical, and chemical insults. Among all malignancies, skin cancer remains the most frequently diagnosed worldwide, particularly affecting individuals with lighter skin. It primarily includes basal cell carcinoma and squamous cell carcinoma, which originate from keratinocytes, and melanoma, originating from melanocytes and exhibiting greater metastatic potential. Skin cancer results from uncontrolled proliferation of abnormal cells caused by ultraviolet (UV) radiation-induced DNA damage, oxidative stress, and mutations in tumor suppressor genes. Although conventional treatments such as chemotherapy, radiotherapy, surgery, and phototherapies are widely employed, their efficacy is often limited by poor selectivity, systemic toxicity, and drug resistance. Therefore, novel, targeted, and biocompatible therapeutic strategies are urgently needed. Phytochemicals, derived from medicinal plants, have shown promising anticancer potential due to their antioxidant, anti-inflammatory, and proapoptotic activities. However, their clinical translation is restricted by poor solubility, low stability, and limited bioavailability. This review provides a distinctive perspective by integrating the therapeutic relevance of phytochemicals with advances in nanotechnology-based delivery systems for skin cancer management. It outlines disease pathophysiology, conventional therapies, and the synergistic role of nanocarriers such as liposomes, niosomes, and nanostructured lipid carriers in enhancing phytochemical delivery, improving penetration, and overcoming multidrug resistance. The review also discusses current research challenges and future directions, highlighting how phytochemical-nanotechnology hybrid systems can offer targeted, effective, and safer approaches for managing skin cancer.
- New
- Research Article
- 10.1016/j.intimp.2025.116071
- Feb 1, 2026
- International immunopharmacology
- Donghui Li + 6 more
Cationic stearic acid-chitosan micelles enhance intranasal antigen delivery and mucosal immunity.
- New
- Research Article
- 10.1016/j.jconrel.2025.114474
- Feb 1, 2026
- Journal of controlled release : official journal of the Controlled Release Society
- Zi-Xi Wang + 4 more
Smart photo-enabled micelles for cancer therapy: Mechanisms, challenges, and innovations.
- New
- Research Article
- 10.1016/j.bioadv.2025.214480
- Feb 1, 2026
- Biomaterials advances
- Xiaolong Chen + 6 more
α-Cyclodextrin mediated 3D printed ceramic/polymer composite scaffolds for immunomodulation and osteogenesis in bone defect repair.
- New
- Research Article
1
- 10.1016/j.bioadv.2025.214513
- Feb 1, 2026
- Biomaterials advances
- Zhidong Lin + 10 more
Smart responsive injectable hydrogel loaded with icariin inhibits ferroptosis and promotes nucleus pulposus repair in intervertebral disc degeneration.
- New
- Research Article
1
- 10.1016/j.bmcl.2025.130442
- Feb 1, 2026
- Bioorganic & medicinal chemistry letters
- Yong Wang + 7 more
Late-stage functionalization of Cycloastragenol and anti-inflammatory study.
- New
- Research Article
- 10.1016/j.bioorg.2025.109434
- Feb 1, 2026
- Bioorganic chemistry
- Bin Li + 6 more
Synthesis of Andrographolide glycosides and evaluation of their antibacterial activity in vitro and in vivo.
- New
- Research Article
- 10.1016/j.ejps.2025.107397
- Feb 1, 2026
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
- Simon Hoang Dinh + 7 more
Synthesis, in vitro characterization and biopharmaceutical evaluation of a novel phosphate prodrug of sorafenib.
- New
- Research Article
- 10.1016/j.foodres.2025.118121
- Feb 1, 2026
- Food research international (Ottawa, Ont.)
- Huan Liu + 6 more
Convenient fabrication of shellac-chitosan composite nanoparticles by antisolvent precipitation for efficiently stabilizing Pickering emulsions and encapsulating peppermint essential oil.
- New
- Research Article
- 10.1016/j.ejpb.2026.115007
- Feb 1, 2026
- European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
- Ruirui Liu + 6 more
Two-birds-one-stone, microfluidic producing DES/W microemulsions to solubilize quercetin and penetrate intestinal mucosa for enhanced oral bioavailability.
- New
- Research Article
- 10.1016/j.foodres.2025.118133
- Feb 1, 2026
- Food research international (Ottawa, Ont.)
- Huizhen Xing + 6 more
Rice bran protein-based self-propelled nanomotors for targeted delivery of dihydroquercetin: A food-grade nano-system for anti-atherosclerosis.
- New
- Research Article
- 10.1186/s13568-026-02014-8
- Feb 1, 2026
- AMB Express
- Bohan Yang + 6 more
Epigallocatechin gallate (EGCG), the predominant catechin in green tea, has limited application due to its poor water solubility and instability. To address these issues, this study utilized recombinant sucrose phosphorylase to catalyze the glucosylation of EGCG, successfully synthesizing (-)-epigallocatechin gallate 4',4″-O-α-D-diglucopyranoside (EGCG-2G). The process was optimized using response surface methodology, achieving a 97.46% conversion rate of EGCG. EGCG-2G was purified to ≥ 99% purity by semi-preparative liquid chromatography. It exhibited approximately 124-fold higher water solubility than EGCG and demonstrated significantly enhanced stability under thermal and acidic conditions (50°C, pH = 5), with an 84.82% and 35.36% improvement over EGCG and commercial (-)-epigallocatechin-3-gallate-4'-O-α-D-glucoside (EGCG-1G), respectively. Furthermore, EGCG-2G displayed notable antioxidant, anti-inflammatory, and anti-melanogenic activities. It effectively scavenged intracellular and extracellular free radicals, reduced inflammatory cytokine levels, and inhibited melanin synthesis. Molecular docking and gene expression analyses suggested that its anti-melanogenic effect might be associated with the MC1R/cAMP/MITF signaling pathway.
- New
- Research Article
- 10.1002/slct.202506790
- Jan 31, 2026
- ChemistrySelect
- Xiaohan Fang + 4 more
ABSTRACT Neonicotinoid is one of the most important insecticides family that acts on the nervous system of insects. However, the detrimental effects of neonicotinoids on non‐target organisms, highlighted the urgent need for the development of novel alternatives. Herein, an AI‐driven identified coumarin insecticidal lead compound from our previous study was further optimized. The target compounds A16 and A18 showed 67.8% and 62.5% insecticidal activity against Aphis craccivora at 100 mg/L, respectively. Docking binding mode analysis demonstrated that A16 and A18 cannot form the water‐bridged hydrogen bond, which may explain the less desirable activity of the compounds. The electrostatic and hydrophobic potential surfaces both revealed the weaker positive electrostatic distribution and relatively poor aqueous solubility resulted in the limited insecticidal potency. In summary, this work provides valuable insights into the structure–activity relationships of coumarin‐based neonicotinoids and advances the development of novel neonicotinoid insecticides.
- New
- Research Article
- 10.1111/1750-3841.70894
- Jan 31, 2026
- Journal of food science
- Jian Ma + 7 more
Astaxanthin (AST) has been widely studied for its potential antioxidant and anti-inflammatory effects; however, its application is limited by poor water solubility and low bioavailability. To address this, zein and chito-oligosaccharides composite nanoparticles (ZCNps) were constructed using antisolvent precipitation for efficient AST delivery. At a zein to COS mass ratio of 10:1, AST-loaded ZCNps (ZCANps) achieved an encapsulation efficiency of 81.23% and drug loading of 4.18 mg/g. Structural characterization confirmed that AST was successfully encapsulated in an amorphous state, stabilized by hydrophobic interactions and hydrogen bonding. ZCANps demonstrated stability under a wide range of conditions, including pH levels of 2-8, NaCl concentrations of up to 50 mmol/L, temperatures of up to 80°C, and storage for 8 weeks at 4°C. Additionally, ZCANps provided 62% UV-light protection for AST. Compared to free AST, the encapsulated form showed significantly enhanced antioxidant activity and bioaccessibility. These results highlight ZCNps as a delivery system for improving the stability, bioavailability, and functional properties of AST in food applications.
- New
- Research Article
- 10.1002/pca.70052
- Jan 29, 2026
- Phytochemical analysis : PCA
- Mohammed Burhan Uddin + 8 more
Corosolic acid (CRS) is a naturally occurring pentacyclic triterpenoid primarily isolated from Lagerstroemia speciosa and other medicinal plants and has attracted growing interest because of its promising anticancer properties. This review provides a comprehensive synthesis of the botanical sources, biopharmaceutical characteristics, molecular mechanisms of action, toxicological profile, and clinical evidence associated with CRS. A comprehensive literature search was conducted across major scientific databases, including PubMed, Google Scholar, Web of Science, ScienceDirect, SpringerLink, and Wiley Online, covering studies published up to April 2025. Peer-reviewed articles investigating the anticancer activity, pharmacology, toxicity, pharmacokinetics, and clinical relevance of CRS were included. Preclinical evidence demonstrates that CRS exerts broad-spectrum anticancer activity by inducing apoptosis, autophagy, ferroptosis, and cytotoxicity, while inhibiting tumor cell proliferation, metastasis, and survival signaling pathways, including PI3K/Akt/mTOR, NF-κB, STAT3, and YAP/TAZ. Emerging data also highlight its immunomodulatory role, particularly through suppression of Th17-mediated inflammatory responses, which may further contribute to its antitumor effects. Toxicological evaluations indicate that CRS possesses a favorable safety profile at therapeutic doses; however, its clinical translation is hindered by poor aqueous solubility and limited oral bioavailability. Recent advances in formulation strategies and structural modification approaches show potential for overcoming these limitations. Overall, this review integrates current knowledge, identifies critical research gaps, and emphasizes the need for well-designed clinical trials to establish CRS as a viable multitarget anticancer agent.
- New
- Research Article
- 10.1021/acsabm.5c01270
- Jan 28, 2026
- ACS applied bio materials
- Mojdeh Mirshafiei + 7 more
Hepatocellular carcinoma (HCC) remains one of the leading causes of cancer-related mortality. Sorafenib is the current first-line oral therapy; however, its therapeutic efficacy is limited by poor aqueous solubility, low bioavailability, and gastrointestinal instability. This study aimed to develop a pH-responsive nano-in-microparticle delivery system using a single-step droplet-based microfluidic process to protect sorafenib in the gastric environment and achieve controlled release for enhanced oral chemotherapy. Sorafenib-loaded ZIF-8 nanoparticles (SZ NPs) were synthesized and characterized by scanning electron microscopy (SEM), Fourier-transform infrared (FTIR) spectroscopy, Energy-dispersive X-ray (EDX) spectroscopy, and X-ray diffraction (XRD), exhibiting a mean diameter of about 72 nm and a drug encapsulation efficiency of 76%. These SZ NPs were subsequently encapsulated in alginate to form pH-responsive nano-in-microparticles. Computational fluid dynamics (CFD) simulations were conducted to optimize flow dynamics and droplet formation within the microfluidic channels, and particle morphology and uniformity were assessed via bright-field microscopy, fluorescence microscopy, and SEM. The resulting nano-in-microparticles exhibited spherical morphology with hydrodynamic sizes ranging from 76 to 113 μm, depending on the flow rate ratio, demonstrating uniform SZ NP dispersion. Drug release studies in simulated gastric and intestinal fluids revealed that the nano-in-microparticles prevented premature drug release in acidic simulated gastric fluid (pH < 5.7), while facilitating a controlled and sustained release profile under simulated intestinal conditions (pH 7.4) over 24 h. Cytotoxicity assays against HepG2 liver cancer cells showed significant anticancer efficacy compared to free sorafenib. These findings highlight the potential of this pH-responsive platform as an effective oral delivery strategy for HCC therapy.