Targeted phenylboronic acid-rosuvastatin based nanoconstructs: A novel therapeutic avenue for treatment of colorectal cancer.

Theaflavin-3,3’ -Digallate Encapsulated βββββ -Chitosan Nanoparticles for the Prevention of Chemotherapy-Induced Toxicity: Mechanisms, Therapeutic Potential, and Future Perspectives

Development and in vitro evaluation of glycyrrhetinic acid and alpha-lipoic acid co-loaded nanophytosomes: a strategy to mitigate cisplatin-induced hepatocellular damage.

Cisplatin (CDDP) remains a cornerstone chemotherapeutic agent; however, its clinical use is limited by dose-dependent systemic toxicities, particularly hepatotoxicity mediated by oxidative stress, mitochondrial dysfunction, and inflammatory signaling. Glycyrrhetinic acid (GA) and α-lipoic acid (ALA) provide complementary hepatoprotective mechanisms. Nevertheless, both compounds suffer from poor aqueous solubility, high crystallinity, and limited bioavailability. To address these biopharmaceutical limitations, a dual-drug nanophytosome (GALP) was engineered using a crystalline-to-amorphous phase transition strategy to enhance dissolution, loading efficiency, and hepatocellular delivery. GALP nanophytosomes were prepared via solvent evaporation using Soy Phospholipid (SPC). The optimized formulation exhibited a mean particle size of 93.3 ± 1.99 nm, a narrow polydispersity index, and a negative zeta potential  -33.7 ± 0.28 mV). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses confirmed the complete elimination of GA and ALA crystalline peaks, demonstrating successful amorphization within the phospholipid matrix. Functionally, pretreatment with GALP significantly reduced CDDP-induced cytotoxicity in an optimized HepG2/LX-2 co-culture model, restoring overall cell viability to approximately 78%, which was statistically superior to the free drug combinations (P < 0.05). The engineered GALP platform addresses the shared biopharmaceutical limitations of GA and ALA, offering a physicochemical profile (sub-100 nm diameter and negative surface charge) well-suited for future in vivo pharmacokinetic and liver distribution studies.

Green synthesis of Artemisia argyi-mediated CuFe2O4 nanoparticles: Experimental and theoretical insights into anticancer activity.

Cancer remains the second leading cause of death worldwide, and two inherent challenges in conventional therapies, indiscriminate toxicity and development of drug resistance by cancer cells, have increased the demand for novel therapeutic means. In this study, copper ferrite (CuFe2O4) nanoparticles were synthesized using an aqueous leaf extract of Artemisia argyi through a green, eco-friendly route. The synthesized nanoparticles were characterized by XRD, SEM-EDX, and FTIR to reveal their crystalline spinel structure, spherical morphology, and functional group composition. The average crystallite size was 15.25 ± 6.48 nm. Cytotoxic potential of the particles was assessed using three different cell lines, MCF-7 (breast), A549 (lung), and L929, (normal fibroblast). MTT assays revealed a dose- and time-dependent reduction in cancer cell viability. Highest sensitivity was demonstrated by MCF-7 cells. Exposure to the particles also appeared to have caused changes in the expression levels of some of the key genes involved in cell survival: Caspase-3 and BAX, for which a meaningful increase was observed, while the amount of BCL-2 decreased. Such an activity pattern suggested apoptosis as the primary pathway in cell death. Flow cytometry results further unraveled the role of late apoptosis in MCF-7 cells. Importantly, the nanoparticles showed lower cytotoxicity toward L929 cells, indicating a degree of selectivity for cancer cells. These findings demonstrate promising in vitro anticancer activity of CuFe2O4 nanoparticles. Gibbs free energy changes of the complexes formed by some of the Artemisia argyi molecules and copper ferrite nanoparticles were investigated using the Gaussian software package in B3LYP, HF, and M06-2x method at 6-31 + + g(d,p) basis set. The activities of four of the molecules, having very high negative Gibbs free energies, against breast and lung cancer proteins were compared.

Cabazitaxel and camptothecin co-loaded in pH-sensitive transferrin-targeted, PEGylated cholesterol-based poly(amidoamine) dendrimers as a synergistic combination for prostate cancer.

The clinical utility of combining cabazitaxel (CBZ) and camptothecin (CPT) for advanced prostate cancer is hindered by emerging drug resistance and the absence of optimized nanocarriers for co-delivery. We investigated the potential of novel Tf-targeted nanocarriers to encapsulate CBZ and CPT, aiming to selectively augment their synergistic anti-cancer activity within in vitro prostate cancer models. Our findings demonstrate a robust synergistic interaction between CBZ and CPT (with a growth inhibition percentage of 87.42% and a combination index of 0.12) in PC3-Luc cells at CBZ:CPT molar ratio of 1:8. Transferrin-bearing PEGylated cholesterol-based poly(amidoamine) dendrimers were successfully synthesized and observed their assembly at a threshold aggregation concentration of around 10 µg/mL. CBZ was encapsulated with 88.35% efficiency and over 70% of the payload released under acidic tumor conditions (pH 5.5-6.4). When fluorescent CBZ was mixed with CPT and delivered by Tf-targeted PPSSCH, its cellular uptake among PC3-Luc, DU145, and LNCaP cells enhanced by 16.50-, 17.20-, and 21.18-times, respectively. Encapsulation of the CBZ/CPT combination using optimized synergistic ratio within transferrin-functionalized, PEGylated cholesterol-based poly(amidoamine) dendrimers significantly potentiated the antiproliferative activity of CBZ by 3.93-, 4.72-, and 5.06-fold in these three cell lines, respectively. These promising in vitro findings support further preclinical (in vivo) evaluation of transferrin-targeted PEGylated cholesterol-based PAMAM dendrimers for CBZ-CPT co-delivery.

Theaflavin-3,3′-Digallate Encapsulated β-Chitosan Nanoparticles for the Prevention of Chemotherapy-Induced Toxicity: Mechanisms, Therapeutic Potential, and Future Perspectives

Chemotherapy remains a cornerstone of cancer management; however, its clinical effectiveness is often compromised by severe systemic toxicity that limits therapeutic dosing and adversely affects patent quality of life. In recent years, natural polyphenols have gained attention as adjunctive agents capable of mitigating chemotherapy induced adverse effects. Among these, theaflavin-3’,3’-digallate (TFDG), a major bioactive constituent of black tea, exhibits potent antioxidant, anti-inflammatory, and antitumour activities. Despite its therapeutic promise, the clinical translation of TFDG is hindered by poor aqueous solubility, low bioavailability, and rapid metabolic degradation. Nanotechnology based delivery systems, particularly biopolymeric carriers such as chitosan nanoparticles (CS-NPs), offer a viable strategy to overcome these limitations. Chitosan based nanoparticles provide enhanced stability, controlled release, improved cellular uptake, and favourable biocompatibility, making them suitable vehicles for polyphenol delivery. This review critically summarizes current knowledge on the chemical characteristics and biological functions of TFDG, recent advances in chitosan nanoparticle formulations, and their combined potential to act as a biological shield against chemotherapy-induced toxicity. The integration of TFDG with CS-NPs represents a promising nanotherapeutic approach to improve treatment tolerance with preserving anticancer efficacy.

Research progress of gambogic acid-loaded nanoformulations in tumor therapy

Gambogic acid (GA), a natural xanthone derived from Garcinia plants, exhibits potent broad-spectrum antitumor activity through multiple mechanisms, including apoptosis induction, cell cycle arrest, angiogenesis inhibition, and ferroptosis/pyroptosis triggering. However, its clinical translation is severely hampered by poor water solubility, low bioavailability, rapid metabolism, short half-life, and significant off-target toxicity. Nanotechnology offers a promising solution to overcome these limitations. Nanoparticle-based delivery systems can enhance GA's solubility, extend its circulation time, improve tumor targeting via passive (enhanced permeability and retention effect) or active (ligand-mediated) strategies, and reduce systemic side effects. This review systematically evaluates recent advances in GA-loaded nanoformulations for cancer therapy, covering diverse nanocarrier types (lipid-based, polymeric, inorganic, biomimetic, and metal-coordinated systems), design strategies to address GA's application bottlenecks (e.g., solubilization, long-circulation, smart-responsive release, active targeting), and their therapeutic efficacy in various tumor models. Furthermore, emerging combination therapies integrating GA with chemotherapy, photothermal therapy, or immunotherapy are discussed. The goal is to provide a comprehensive reference for leveraging nanomedicine to unlock the full clinical potential of GA.