Protocol-Dependent Effects on Colloidal Characterization and Drug Loading/Release Analysis of Thermosensitive PNIPAM-co-COOH Microgels

Computational and Experimental Approaches for HPMCAS-Based Solid Dispersions of Abiraterone Acetate: Formulation, Characterization, and Biopharmaceutical Enhancement Evaluation.

OBJECTIVE To enhance the solubility, dissolution rate, and permeability of poorly water-soluble drug Abiraterone Acetate (ABA) by developing solid dispersions using hydroxypropyl methylcellulose acetate succinate (HPMCAS-LF). SIGNIFICANCE Enhancing the biopharmaceutical performance of ABA is crucial due to its extremely poor solubility and dissolution characteristics. The present study demonstrates that HPMCAS-LF-based solid dispersion effectively improves the physicochemical performance of ABA through enhanced solubility, dissolution, and in vitro drug diffusion. METHODS Molecular dynamics (MD) simulations were conducted over 100 ns to evaluate the stability and structural behavior of the ABA-HPMCAS-LF complex, with analyses including root mean square deviation (RMSD), radius of gyration and solvent-accessible surface area . Binding free energy was measured using MM-GBSA calculations. Solid dispersions were prepared using co-grinding and solvent assisted cogrinding techniques and characterized by FTIR, PXRD, thermal analysis (TGA/DTG-DTA), SEM, and solid-state13C NMR. Solubility, in vitro dissolution, in vitro drug diffusion, hygroscopicity, and anticancer activity were assessed. RESULTS The ABA-HPMCAS-LF complex exhibited dynamic stability, with RMSD stabilization at 6-7 Å and a binding free energy of -33.45 kcal/mol, indicating strong van der Waals, lipophilic, and Coulombic interactions. Solid dispersions demonstrated a 1.07 to 16.72-fold increase in solubility compared to pure ABA, and in vitro release enhanced drug dissolution across different media. Diffusion increased by 6.36-fold in simulated gastric fluid (SGF 1.2) and 2.55-fold in phosphate buffer (pH 6.8) relative to pure ABA. CONCLUSION The solid dispersion of ABA with HPMCAS-LF significantly improved solubility, dissolution, and diffusion, highlighting its potential for enhanced oral bioavailability and improved therapeutic outcomes.

Design and Optimization of Transethosomal Drug Delivery Systems for Ritonavir: Comparative Evaluation, Characterization, and Release Kinetics

The present study focused on the characterization and microencapsulation of Eperisone hydrochloride to develop sustained release formulations. The drug’s melting point was determined using the capillary method (183.0 ± 0.6 °C) and validated by DSC (183.5 °C), confirming its thermal stability and purity. FTIR analysis established drug identity and compatibility with Amberchrom resins, with characteristic peaks observed for functional groups such as N–H, C–H, C=C, C–N, and C–O, and no evidence of chemical interaction in drug–resin complexes. Microencapsulation was performed using the O/O method, yielding high drug content recovery (49.00–49.58 mg) and encapsulation efficiencies above 98%, demonstrating reproducibility and minimal drug loss. Particle size analysis showed uniformity across formulations (198.5–206.5 µm), ensuring consistent release behavior. The extent of coating varied from 4.8% to 20.6%, directly influencing drug release rates. In vitro release studies revealed that higher polymer concentration (20% Eudragit RS100) and PEG 400 plasticizer slowed drug release, while increased rotation speed (1500 rpm) enhanced release due to thinner coatings. Kinetic modeling indicated that most formulations followed zero order kinetics, while others aligned with Korsmeyer–Peppas or first order models, confirming diffusion controlled mechanisms. Among all formulations, F4 (20% Eudragit RS100, 10% PEG 400, 500 rpm) exhibited the most controlled release profile, consistent with sustained release objectives. Overall, the study demonstrated that formulation parameters significantly affect drug release, and F4 was identified as the optimal batch for achieving effective sustained delivery of Eperisone hydrochloride

Assembly mechanism-instructed precision nanocarriers: Esox lucius apoferritin for hydrophilic or hydrophobic drug loading and smart release.

Ferritin (Fn) nanocages offer significant potential as drug delivery vehicles due to their biocompatibility, well-defined structure, and inherent targeting capabilities. In this study, we isolated Fn from the liver of Esox lucius and prepared its apo-form (apo-Fn) to engineer its reversible disassembly/reassembly for drug encapsulation. We demonstrated that apo-Fn undergoes controlled disassembly under mild acidic conditions (pH 2.0-4.0) or 4 M urea, and efficiently reassembles upon neutralization or urea removal. Thermal treatment below 55 °C also facilitated reversible structural transitions. Based on these properties, three loading strategies were developed. The temperature-gradient method was optimal for hydrophilic drugs (doxorubicin and phenytoin), while the urea-gradient method achieved 42.18% encapsulation for hydrophobic paclitaxel. The resulting formulations showed uniform size, colloidal stability, and minimal leakage at pH 7.4, but exhibited rapid release at acidic pH 5.0. Furthermore, apo-Fn showed high biocompatibility (> 90% cell viability) and exerted intrinsic anti-inflammatory effects by modulating macrophage polarization. This study highlights piscine apo-Fn as a promising platform for targeted drug delivery.

Linking interfacial behavior to thermo-diffusive cisplatin release in biopolymeric nanogels.

Cisplatin-loaded biopolymeric nanogels are promising carriers for sustained anticancer drug delivery; however, establishing physically interpretable links between formulation structure, transport behavior, and temperature-dependent release remains challenging. Here, mucilage-alginate-coated chitosan (MACC) nanogels were developed and evaluated using an integrated framework combining empirical kinetic analysis, mechanistic thermo-diffusive modeling, and complementary interfacial characterization. Basil seed mucilage was incorporated as a hydrophilic shell modifier to tune nanogel physicochemical behavior and release performance. The optimized MACC₂ formulation showed stable core-shell morphology, an average particle size of 75 ± 12 nm, and an encapsulation efficiency of 46.85%. In vitro assays demonstrated high compatibility with normal fibroblast cells and dose-dependent inhibition of MCF-7 breast cancer cells, supporting controlled cisplatin delivery. Drug release in PBS (pH 7.4) followed a biphasic profile with an initial burst stage and a sustained diffusion-dominated regime. Temperature-dependent studies at 35-39 °C showed accelerated release, with effective diffusion coefficients increasing from 2.0 × 10-21 to 3.6 × 10-21 m2 s-1, while Arrhenius analysis supported thermally activated transport within the hydrated polymeric matrix. Empirical kinetic modeling further indicated predominantly diffusion-controlled release with secondary polymer-relaxation contributions. Air-water interfacial tensiometry showed reduced interfacial activity for mucilage-containing nanogels, consistent with increased aqueous affinity and formulation-dependent physicochemical behavior. These measurements were interpreted as complementary descriptors rather than direct evidence of hydration or bulk diffusion. Overall, this integrated empirical-mechanistic-interfacial framework provides a physically interpretable approach for analyzing thermo-diffusive cisplatin transport in hydrated biopolymeric nanogels.

Thermosensitive In-Situ Nanoemulsion Gel for Sustained Drug Release of Lidocaine and Prilocaine: Design, Optimization, and Characterization

Polymeric Nanogels for Selenite Delivery and Release in Foliar Biofortification: Experimental and Theoretical Insights into Polymer–Ion Interactions

This work reports an integrated experimental and theoretical study of polymeric nanogels as tunable colloidal platforms for selenite binding and controlled ion delivery. Three formulations (N600, N3000, and Nmix) form stable colloidal dispersions (120–260 nm) with structure and interfacial properties governed by polymer architecture and network composition. Performance is evaluated under foliar application in Eruca sativa as a proof-of-concept system, showing enhanced selenium uptake and reduced phytotoxicity compared to free selenite. N600 exhibits the most balanced behavior, combining moderate binding strength, efficient ion release, and high compatibility. Multitechnique characterization and density functional theory (DFT) calculations reveal that selenite interaction with the polymer network is governed by coupled polymer–ion interactions, proton-transfer equilibria, and solvation effects. At pH 5.5, where HSeO3– predominates, binding is dynamic and reversible, enabling polymer-mediated selenium delivery. N3000 and Nmix show stronger stabilization via proton-transfer-assisted interactions, whereas N600 is dominated by weaker electrostatic association, consistent with polymer protonation state and pKa-dependent behavior. The results demonstrate that the balance between ion stabilization and mobility governs binding and release behavior. This study provides molecular-level insight into polymer–ion systems and establishes design principles for tunable colloidal platforms for controlled ion delivery.