High-performance liquid chromatography (HPLC) is a widely used analytical technique in pharmaceutical research, but its application to ionizable drug-like compounds requires optimization. This study aims to enhance the determination of Abraham solvation parameters in pharmaceuticals by refining HPLC methodologies. The research focuses on optimizing HPLC for ionizable compounds, minimizing column usage while maintaining accuracy, evaluating the role of hydrogen-bond (H-bond) descriptors in drug characterization, overcoming adaptation challenges, and improving quantitative structure-activity relationship (QSAR) modeling. A quantitative methodology was employed, with experimental HPLC analysis conducted on 62 pharmaceutical molecules. Results indicate that optimized HPLC parameters effectively accommodate ionizable compounds, while advanced materials and techniques allow for column minimization without compromising accuracy. H-bond descriptors significantly impact drug characterization, and novel approaches are required to adapt HPLC methods for complex drug matrices. Furthermore, optimized solvation parameters enhance QSAR modeling, contributing to better predictive capabilities in pharmaceutical research. These findings highlight the potential of refined HPLC methods in drug discovery and analysis.
The development of an advanced dual-responsive drug delivery system is critical in addressing the limitations of conventional cancer treatments, such as non-specific adverse effects and poor targeting. This study explores the use of gold-coated superparamagnetic iron oxide nanoparticles (Au-SPIONs) integrated with chitosan microspheres for the targeted delivery of small interfering RNA (siRNA) to breast cancer sites. The formulation's performance is assessed by examining encapsulation efficiency, drug loading capacity, release kinetics, and dual-responsive characteristics under both pH and magnetic stimuli. Experimental analysis demonstrates that Au-SPIONs significantly enhance siRNA encapsulation, medium molecular weight chitosan optimizes drug loading, and controlled crosslinker concentration regulates sustained release. The dual-responsive nature of the system provides enhanced targeting precision compared to traditional delivery systems. These findings suggest that this innovative formulation holds promise for improving the efficacy of siRNA-based breast cancer therapies, although further clinical studies are necessary to validate its real-world applicability.
The development of high-concentration human immune globulin suspension formulations requires a deep understanding of formulation strategies, injectability challenges, and colloidal stability. This study investigates the impact of spray drying, excipient-induced protein saturation, concentration-injection force relationships, viscosity behavior, and clinical implications of non-Newtonian suspensions. A quantitative research methodology was employed, analyzing independent variables such as spray drying conditions, excipient concentrations, and formulation parameters against dependent variables including particle size distribution, protein solubility, injection force, and viscosity. The results demonstrate that optimized spray drying significantly improves particle size uniformity, pharmaceutical excipients enhance protein solubility while maintaining stability, higher concentration suspensions require greater injection force, viscosity increases with concentration affecting injectability, and formulation strategies can mitigate injectability challenges to enhance clinical viability. The findings contribute to improved formulation techniques for injectable high-viscosity suspensions, addressing gaps in drug delivery and biopharmaceutical manufacturing. Future research should explore long-term stability, forced degradation, and regulatory considerations for clinical translation.
The miscibility of Nifedipine/Polyvinylpyrrolidone (NIF/PVP) amorphous solid dispersions (ASDs) is crucial for predicting crystallization resistance and stability. This study evaluates the effectiveness of rheological and solid-state nuclear magnetic resonance (ssNMR) methods for determining miscibility at different temperatures. Specifically, it examines whether rheological methods are reliable at high temperatures (175°C) and ssNMR at low temperatures (-20°C), their consistency in results, the impact of molecular weight on miscibility, and the implications for stability prediction. Experimental data confirm that rheological analysis provides accurate miscibility assessment at elevated temperatures, while ssNMR is precise at lower temperatures. The findings demonstrate consistency between these methods, establish molecular weight as a significant factor in miscibility determination, and highlight the importance of accurate miscibility measurement for predicting ASD stability. These insights contribute to improving methodologies for evaluating ASD stability, addressing existing research gaps, and enhancing pharmaceutical formulation strategies.
Tacrolimus, an immunosuppressive drug with a narrow therapeutic index, exhibits significant pharmacokinetic variability influenced by its crystallinity. This study investigates the impact of drug crystallinity on key pharmacokinetic parameters, including maximum concentration (Cmax) and area under the curve (AUC), through a randomized, single-dose, four-treatment, four-period, four-way crossover study. Findings demonstrate that increased crystallinity leads to higher Cmax and lower AUC, presenting challenges in achieving bioequivalence with reference listed drugs (RLD). The study further explores the mechanistic underpinnings, indicating that solubility and dissolution rate modifications mediate these pharmacokinetic changes. Clinical implications suggest that crystallinity variability necessitates tailored formulation strategies to ensure therapeutic efficacy and consistent drug exposure. The results emphasize the need for stringent crystallinity control in tacrolimus formulations to optimize pharmacokinetic performance and improve clinical outcomes.