Macrophage membrane-functionalized biomimetic Yiqi Huoxue formula nanoparticles improve atherosclerosis by regulating smooth muscle cell phenotypic transition via the KLF4/NF-κB pathway

Development of Wogonin Nanoliposomes Using Box–Behnken Design Optimization: In Vitro Anticancer Activity Evaluation and Cell Cycle Analysis

Targeted Folate-Chitosan Nanoformulations of Quercetin and Coriandrum sativum Reprogram Breast Cancer Hallmarks by Silencing Stemness, Cell Cycle, Angiogenic, and Metastatic Networks

Background/Objectives: This study engineered and evaluated a targeted, folate-functionalized chitosan nanoparticle (CS-FA NP) delivery system to enhance the therapeutic efficacy of standard quercetin and Coriandrum sativum seed extract against breast cancer. Methods: Phytochemical profiling confirmed a 14% crude yield for the methanolic extract, with gas chromatography–mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC) identifying quercetin as the principal bioactive agent. The synthesized CS-FA NPs exhibited a core size of 7–20 nm, an average hydrodynamic diameter of 150–160 nm, a stable zeta potential of −55 mV, and high encapsulation efficiencies (87.2% for quercetin and 80.5% for coriander). Kinetic assessments confirmed a biphasic, diffusion-controlled release matching Higuchi matrix kinetics. Anticancer activity was evaluated in vitro using MTT cytotoxicity, Annexin V-FITC/PI apoptosis analysis, RT-qPCR, and ex vivo rat aortic ring assays, followed by validation in a syngeneic 4T1 mammary tumor mouse model. Results: In vitro, folate-receptor-targeted quercetin nanoparticles (T4) demonstrated superior, selective cytotoxicity, particularly against triple-negative MDA-MB-231 cells, while sparing normal fibroblasts. Annexin V-FITC/PI apoptosis profiling and ex vivo aortic ring assays revealed profound, cell-line-dependent programmed cell death and up to 90% inhibition of microvessel sprout outgrowth. Mechanistically, RT-qPCR verified that nano-formulations induced complete transcriptional silencing of NANOG, MMP-1, VEGFA, TSPAN8, TWIST, EMMPRIN, and CDK1, alongside marked upregulation of P27KIP1 and P21CIP1. In vivo, these nano-formulations successfully improved tumor-associated pathological features, reduced aggressive tumor spindle-cell proliferation, and suppressed elevated serum CA15-3 and arginase biomarkers. Conclusions: Folate-functionalized chitosan nano-formulations significantly enhanced the anticancer efficacy of quercetin and Coriandrum sativum seed extract through improved targeted delivery, potent antiproliferative, anti-angiogenic, and pro-apoptotic activities, together with favorable modulation of multiple molecular pathways associated with breast cancer progression. These findings support their potential as promising targeted nanotherapeutic strategies for breast cancer treatment.

Fabrication and characterization of rutin-loaded liquid crystalline nanoparticles with in vitro anti-inflammatory and antitumor activities

ABSTRACT A rutin-loaded liquid crystalline nanoparticle (R-LCNP) formulation was developed using glyceryl monooleate and Poloxamer 407 by high-pressure homogenization to improve the solubility and biological performance of rutin. The optimized R-LCNP-2 dispersion showed a mean particle size of 176.1 ± 4.5 nm, a polydispersity index (PDI) of 0.211 ± 0.013, and a moderately negative zeta potential of –20.4 ± 1.1 mV, consistent with steric-electrostatic stabilization. The encapsulation efficiency and drug loading were 98.1 ± 1.5% and 2.45 ± 0.04%, respectively, while FTIR, XRD, and DSC analyses indicated molecular dispersion of rutin within the lipid matrix. The formulation showed biphasic diffusion-controlled release and suppressed nitric oxide, TNF-α, and IL-6 more effectively than free rutin in an in vitro LPS-stimulated RAW 264.7 model. R-LCNP-2 also reduced the IC50 values in MCF-7, HeLa, and A549 cells by 3.8–4.5 fold relative to free rutin. These findings support LCNP-based encapsulation as a promising strategy to broaden the functional performance of rutin and justify subsequent in vivo pharmacokinetic and efficacy studies.

A Multifunctional Chitosan-Coated Ciprofloxacin–Luteolin Lipid Nanoplatform for Photodynamic Therapy of Prostatic Cancer

This study developed chitosan (CS)-coated lipid nanoparticles (LNPs) co-loaded with CIP and LUT (CCIPLUTLNPs) as a multifunctional photodynamic therapy (PDT)-enhanced nanoplatform for PCA therapy. The formulations were characterized by particle size, polydispersity index, zeta potential, and encapsulation efficiency. Stability and hemocompatibility were also evaluated. Anticancer activity was assessed in PC-3 cells by measuring cell viability, intracellular reactive oxygen species (ROS) generation under dark and sunlight irradiation, and mitochondrial membrane potential (MMP). In addition, molecular docking was performed against 5α-reductase, androgen receptor (AR), and DNA topoisomerase IIα (TOP2A). Results: The developed LNPs exhibited nanoscale particle size, narrow size distribution, high drug encapsulation efficiency, and a positive surface charge following CS coating. The CS-coated LNPs demonstrated good storage stability and excellent hemocompatibility. Moreover, CCIPLUTLNPs produced the greatest cytotoxicity, enhanced ROS generation, and pronounced mitochondrial membrane depolarization in PC-3 cells. Sunlight irradiation significantly increased ROS production compared with dark conditions, confirming enhanced PDT activity. Molecular docking revealed favorable binding of CIP and LUT to 5α-reductase, AR, and TOP2A, supporting a multitarget anticancer mechanism. Conclusion: CCIPLUTLNPs represent a promising multifunctional nanoplatform that integrates efficient drug delivery, ROS-mediated PDT, and multitarget molecular interactions, offering a potential strategy for improved PCA treatment.

Formulation, Characterization, and Preliminary In Vitro Evaluation of Letrozole Incorporated Eudragit® RS 100 Nanoparticles Using HepG2 Cells.

INTRODUCTION/OBJECTIVE Letrozole (LTZ)-loaded polymeric nanoparticles (PNPs) were formulated with Eudragit® RS100 to investigate their potential as a preliminary drug delivery system for hepatocellular carcinoma (HCC). METHODS Nanoparticles were prepared using the spray-drying technique with a Büchi B-90 Nano Spray Dryer and characterized in terms of morphology, particle size, polydispersity index (PDI), zeta potential, drug loading efficiency, thermal and structural characteristics, in vitro release behavior, and preliminary cytotoxicity. RESULTS SEM analysis demonstrated the formation of predominantly spherical particles with relatively smooth surfaces. The prepared nanoparticles exhibited initial particle sizes ranging between 253 nm and 425 nm, with PDI values of 0.3-0.4 and positive zeta potential values between 36 and 48 mV. Encapsulation efficiency (EE%) and drug loading (DL%) values were determined as 47.9%-56.9% and 9.1%-18.6%, respectively. Thermal and structural analyses indicated the molecular dispersion of LTZ within the polymeric matrix. In vitro release studies conducted at pH 7.4 demonstrated an initial burst release, followed by a sustained drug release profile over 24 h, with cumulative drug release reaching almost 80%. The preliminary cytotoxicity of the formulations was evaluated using the methylthiazolyl-diphenyl-tetrazolium bromide (MTT) assay on human hepatocellular carcinoma (HepG2) and healthy human dermal fibroblast (BJ) cell lines. Free LTZ demonstrated an IC50 value of 142.76 µg/mL against HepG2 cells, whereas the optimized nanoparticle formulation exhibited an IC50 value higher than 121.85 µg/mL. DISCUSSION The obtained results confirmed the successful development of LTZ-loaded polymeric nanoparticles with suitable physicochemical properties, efficient drug encapsulation, and sustained release behavior. The positive surface charge and nanoscale size may support formulation stability. Furthermore, the nanoparticles preserved the cytotoxic activity of LTZ, indicating their potential as an effective drug delivery system. CONCLUSION Overall, the findings suggest that the developed nanoparticles constitute a promising drug delivery system for further investigation in HCC-related therapy. However, additional mechanistic studies and in vivo evaluations are required to comprehensively assess their true therapeutic potential.

Development of Arginine Stearate-Based Solid Lipid Nanoparticles for Enhanced Idebenone Delivery: In Vitro Evaluation on Glioblastoma Model

Glioblastoma (GBM) is the most aggressive primary brain tumor and remains difficult to treat due to its invasive nature, therapeutic resistance, and the presence of the blood–brain barrier (BBB), which represents a major obstacle to effective drug delivery. This study describes the development of biocompatible solid lipid nanoparticles (SLNs) based on a novel arginine stearate derivative for the encapsulation of idebenone, a synthetic antioxidant with potential biological activity. The objective of this work was to design and characterize a lipid-based nanoparticulate system for idebenone delivery and to evaluate its physicochemical properties and preliminary in vitro biological effects. The nanoparticles were characterized by Dynamic Light Scattering (DLS) and Differential Scanning Calorimetry (DSC), and in vitro release profiles were investigated under different pH conditions. Antioxidant activity and cell viability assays were also performed in glioblastoma and non-tumorigenic cell lines. The results indicate successful formulation of idebenone-loaded SLNs with good encapsulation efficiency, maintained antioxidant activity, and promising physical stability over time as monitored by size analysis. The rationale behind the development of arginine stearate-based SLNSs is to optimize the performance of pharmaceutical active ingredients, such as idebenone, versus non-tumorigenic cells. Overall, these findings support the potential of the developed SLNs as a promising delivery system for further in vitro and in vivo investigations.