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Formulation Development Research Papers - 2026-01-18
18/01/2026
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Liposomes, as nanoscale drug delivery systems, have demonstrated significant advantages in cancer therapy owing to their excellent biocompatibility, controllable drug release properties, and high versatility for chemical and structural modification. However, the clinical translation of conventional liposomal formulations remains confronted with multiple challenges, including limited targeting efficiency largely dependent on the enhanced permeability and retention (EPR) effect, restricted circulation time in vivo, and difficulties in maintaining manufacturing consistency and formulation stability. In recent years, functionalization strategies such as surface modification, ligand conjugation, multistage targeting, and biomimetic camouflage have led to substantial progress in improving drug biodistribution, enhancing tumor accumulation, and reducing systemic toxicity. Meanwhile, the development of novel biodegradable or ionizable lipids has provided additional opportunities to improve the clinical applicability of liposomal systems. This review systematically summarizes the classification of liposomes, drug-loading mechanisms, current clinical applications, and targeted functional delivery strategies, and discusses their future prospects in precision cancer therapy, providing a theoretical framework for the clinical translation of liposomal nanomedicines and the development of next-generation drug delivery systems.
Dapagliflozin (DAPA), a selective SGLT2 inhibitor approved for type 2 diabetes, shows emerging potential for repurposing in oncology due to its anti-inflammatory and antiproliferative properties. However, its poor solubility and rapid systemic clearance limit its therapeutic utility in cancer treatment. Here, we report the development of an oral novel gravity-induced nano hydrogel mass system encapsulating DAPA using sodium alginate (SA) and polyvinyl alcohol (PVA) nanoparticles (DAPA-PVA-SA-NPs). The formulation exhibited enhanced solubility (1.8-fold increase), high encapsulation efficiency (88.37%), and sustained release in simulated gastrointestinal conditions. In vitro studies demonstrated improved cytotoxicity against HCT-116 colorectal cancer cells and significant downregulation of oncogenic and inflammatory markers (KRAS, IL-6, TGF-β, TNF-α). In vivo pharmacokinetic evaluation in rats showed delayed Tmax, extended half-life, and a 7% increase in AUC, indicating prolonged systemic exposure with modest AUC improvement. This delivery platform improves oral exposure in rats, shows in vitro activity in HCT-116 cells and supporting further exploratory evaluation for repurposing DAPA in colorectal cancer, pending confirmation in additional models.
Noise pollution poses a major threat to public health and urban sustainability, necessitating effective and environmentally compatible acoustic solutions. Here we report a high-performance hybrid absorber that integrates a natural-fiber micro-perforated panel (MPP) fabricated from alkali-treated flax and rice husks with an optimized polyurethane-fibrogranule (PU-FG) composite backing reinforced by the same renewable fillers. Using response surface methodology based on central composite design, we systematically optimized composite formulation, panel porosity, and air-gap geometry to achieve superior broadband absorption. The resulting system, a 1.61% porosity MPP, 28.5 mm front air gap, 40 mm PU-FG backing, and a 30 mm rear air gap, achieves a sound absorption average (SAA) of 0.82 and a noise reduction coefficient (NRC) of 0.85 across the frequency range 100-2500 Hz. This configuration provides effective broadband absorption through the combined action of Helmholtz resonance from the MPP and visco-thermal losses in the porous backing. Morphological analysis via field-emission scanning electron microscopy confirms hierarchical pore structures enhancing tortuosity and interfacial adhesion. By substantially increasing the renewable content of both the MPP and the porous backing, this lightweight, high-efficiency hybrid offers a practical and scalable pathway toward more sustainable noise-control materials for architectural, transportation, and urban applications.
The functionality of lipid nanoparticles (LNPs) as delivery systems in mRNA-based therapeutics is intricately linked to the protonation behavior of their aminolipid components. This study employs large-scale constant-pH molecular dynamics (CpHMD) simulations to decode the environment-dependent pK a ${\rm pK}{\text{a}}$ of aminolipids in the Comirnaty lipid formulation, providing a detailed view of their pH-dependent structural dynamics. Our results reveal a significant shift in the apparent pK a ${\rm pK}{\text{a}}$ of the aminolipid ALC-0315, from an intrinsic value of 9.3 in water to 4.9 within the LNP environment. This shift arises from the interplay between lipid reorganization and local electrostatic interactions, resulting in distinct protonation states across the LNP core and surface. At low pH, protonated aminolipids dominate the LNP surface, promoting efficient mRNA encapsulation, whereas at neutral pH, deprotonated aminolipids migrate to the hydrophobic core, driving structural stabilization. Notably, the localized pK a ${\rm pK}{\text{a}}$ of aminolipids varies significantly with their position, decreasing from near-surface regions (7 to 8) to the hydrophobic core ( ≤ $\le$ 4). These findings elucidate the molecular mechanisms underpinning LNP phase transitions and highlight the key role of pK a ${\rm pK}{\text{a}}$ shifts for the design of aminolipids and for optimizing LNP compositions for enhanced therapeutic delivery. This study bridges experimental observations with molecular-level insights, advancing the rational development of next-generation lipid-based nanocarriers.
Frequent emergence of respiratory viruses with pandemic potential, like severe acute respiratory syndrome coronavirus 2 or influenza, underscores the need for broad-spectrum prophylaxis. Existing vaccines show reduced efficacy against newly emerged variants, and the ongoing risk of new outbreaks highlights the importance of alternative strategies to prevent infection and viral transmission. As respiratory viruses primarily enter through the nose, formulations targeting the nasal epithelium are attractive candidates to neutralize pathogens and thus prevent or minimize infection. Enoxaparin, a low-molecular-weight heparin (LMWH) widely used as an anticoagulant, also exhibits antiviral and anti-inflammatory properties. We found that in highly differentiated human nasal and upper respiratory tract 3D models, enoxaparin inhibited influenza A/H3N2 and B/Victoria infection, reduced release of proinflammatory cytokines and chemokines, and mitigated epithelial damage caused by infection. Our study highlights the LMWH inhibitory effect on respiratory viruses. When applied to mucosal entry sites, LMWH shows promise as prophylactic and valuable alternative to traditional antiviral approaches.
