Punch sticking is a common phenomenon in tablet manufacturing, often leading to tablet defects and compromise product quality. A thorough understanding of the sticking mechanism is essential to optimize the tablet production process. The aim of this study was to investigate the influence of formulations and punch properties on sticking. Seven model active pharmaceutical ingredients (APIs) (i.e., ibuprofen, aspirin, paracetamol, metronidazole, diltiazem, diclofenac, and cefuroxime) with various melting points and particle sizes were used to evaluate their propensity for sticking. The APIs stuck to punch were extracted and quantified using UV spectroscopy. The impact of fillers (i.e., microcrystalline cellulose, lactose monohydrate, dicalcium phosphate, pregelatinized starch, cellactose) and lubricants (i.e., magnesium stearate, stearic acid, aerosil, talc) were investigated. Additionally, the role of punch cup geometry (i.e., flat, standard concave, and deep concave) and punch materials was also investigated to determine their influence on sticking behaviour. Experimental results showed that the APIs with either a high melting point or small particle size have a lower tendency to stick. The differential scan calorimetry plots and X-ray diffraction graphs revealed changes in the crystalline structure due to compaction, which increased the tendency to stick. The excipients and API particle size influencede the degree of sticking. Chromium nitride-coated punches did not eliminate potential sticking at low compaction speeds. The flat-face punch demonstrated a higher sticking tendency than the concave punch. The factors contributing to sticking during tablet manufacturing were either ingredient properties, tableting parameters or both. Formulations containing MCC as a filler and utilizing deep concave punch were found to significantly reduce sticking tendencies compared to those with dicalcium phosphate filler and flat-faced punches.

Background/Objectives: Vitexin and isovitexin are bioactive flavonoids with promising pharmacological effects; however, they have poor bioavailability. Microencapsulation with biodegradable polymers is a promising strategy for improving their stability, bioavailability, and biocompatibility. This study aimed to optimize the formulation parameters to obtain microspheres with desired properties in terms of size, loading ratio, and vitexin–isovitexin release. Methods: Microspheres were prepared using alginate as the core matrix and a chitosan outer layer. A Design of Experiment approach using response surface methodology was employed. The hypoglycemic effects of the obtained microspheres were evaluated. Results: The formulation using 1.17% low-viscosity alginate, 7.60% calcium chloride, 5.78% Tween 80, and 5.00% Span 80 resulted in microspheres with optimal mean size (10.78 µm), high loading ratio (22.45%) and encapsulation efficiency (68.92%). The in vitro release of vitexin–isovitexin from microspheres was completed within 24 h in controlled manner. The microspheres were found to be non-toxic in vivo and exhibited hypoglycemic effects after 21 days at doses equivalent to 30 and 60 mg/kg of vitexin–isovitexin. The potential mechanisms might involve increasing the size of Islets of Langerhans and improving pancreatic β-cell function and insulin resistance, as observed in alloxan-induced diabetic mice. Conclusions: This work successfully developed alginate–chitosan-based microspheres for the controlled release of vitexin–isovitexin while maintaining their bioactivities.

Background/Objectives: Vitexin and isovitexin are bioactive flavonoids with promising pharmacological effects; however, they have poor bioavailability. Microencapsulation with biodegradable polymers is promising strategy for improving their stability, bioavailability, and biocompatibility. This study aimed to optimize the formulation parameters to obtain microspheres with desired properties in terms of size, loading ratio, and vitexin-isovitexin release. Methods: Microspheres were prepared using alginate as core matrix and a chitosan outer layer. Design of experiments approach using response surface methodology was employed. The hypoglycemic effects of obtained microspheres were evaluated. Results: The formulation using 1.17% low-viscosity alginate, 7.60% calcium chloride, 5.78% Tween 80, and 5.00% Span 80 resulted in microspheres with optimal mean size (10.78 µm), high loading ratio (22.45%) and encapsulation efficiency (68.92%). The in vitro release of vitexin-isovitexin from microspheres was completed within 24 hours in controlled manner. The microspheres were found to be non-toxic in vivo and exhibited hypoglycemic effects after 21 days at doses equivalent to 30 and 60 mg/kg of vitexin-isovitexin. These effects were attributed to increasing in the size of Islets of Langerhans, improving in pancreatic β-cell function and insulin resistance, as observed in alloxan-induced diabetic mices. Conclusions: This work successfully developed alginate-chitosan-based microspheres for the controlled release of vitexin-isovitexin while maintaining their bioactivities.

Context: In Chinese medicine, and Ayurvedic, Andrographis paniculata is traditionally employed as a remedy for colds and influenza, particularly to alleviate fever linked with infectious illnesses like upper respiratory infections (URIs). Aims: To determine the potential anti-infective mechanisms of A. paniculata on upper respiratory infections through network pharmacology and docking modeling. Methods: Initially, active chemical constituents of A. paniculata were identified using the Traditional Chinese Medicine Systems Pharmacology database. Subsequently, the target genes of these active ingredients were determined by the UniProtKB database, while target genes related to upper respiratory infections were identified through the GeneCards database. The compound-target network of AP was constructed by the Cytoscape. The protein-protein interaction network was generated using the STRING database. Further analysis was conducted through the DAVID database, integrating Gene Ontology and KEGG pathway enrichment analyses. Results: Twenty-two active components of A. paniculata and highlighted key pathways such as the TNF signaling pathway, IL-17 signaling pathway, and human cytomegalovirus infection are potentially crucial for URIs treatment. Additionally, target genes of A. paniculata, including TNF, IL6, AKT1, TP53, CXCL8, CASP3, and PTGS2, were identified as significant in regulating these biological processes and pathways. Conclusions: This study provides valuable insights into the mechanism of A. paniculata in treating URIs, laying the groundwork for further research in this area.

Biodegradable BPMO@DTX (B@D) nanoparticles were successfully synthesized, exhibiting potent anticancer activity while mitigating the systemic toxicity of docetaxel (DTX). To advance the development of an injectable B@D nanoformulation, an accurate and robust method for DTX quantification was required. High-performance liquid chromatography (HPLC) was employed, with sample preparation based on a biodegradation technique, Glutathione (GSH-induced degradation), which was selected as the optimized procedure. Ultrasonication was evaluated only during the method development stage as a comparative approach. Key parameters—including solvent type, sample-to-solvent ratio, and biodegradation time—were optimized, and the method was validated according to International Conference on Harmonization Q2(R2) guidelines. The optimized HPLC conditions comprised a mobile phase of acetonitrile:water (60:40, v/v), PDA detection at 230 nm, a Gemini 5 μm C18 (250 × 4.6 mm) column, 30°C temperature, 1.2 ml/minute flow rate, and 20 μl injection volume, all meeting validation requirements. Ultrasonication resulted in only ~30% DTX recovery, rendering it unsuitable for quantification. In contrast, the biodegradation method—incubating B@D with 20 mM GSH for 48 hours, followed by dichloromethane extraction (1:5 ratio, 5 minutes, 6,000 rpm, repeated five times)—achieved >99% recovery. This validated method provides a reliable analytical tool for DTX quantification in B@D formulations, supporting further pharmaceutical development.