Search Results (93)

Introduction: Diltiazem hydrochloride (DH) is a calcium channel blocker used in the treatment of hypertension, angina pectoris, and arrhythmias. Its short half-life and frequent dosing requirements limit patient adherence and cause plasma concentration fluctuations. Objective: This review critically examines recent pharmaceutical technologies and formulation strategies for modified-release dosage forms (MRDFs) of diltiazem hydrochloride, emphasizing their impact on pharmacokinetics, clinical performance, and regulatory aspects. Methodology: A structured literature review (2010–2025) was conducted using databases such as PubMed, ScienceDirect, MDPI, and ACS Publications. Studies were selected based on relevance to solid oral MRDFs of DH and their associated manufacturing techniques. Results: Techniques including direct compression, granulation, extrusion–spheronization, spray drying, solvent evaporation, and ionotropic gelation have enabled the development of hydrophilic matrices, coated pellets, microspheres, and osmotic systems. Functional polymers such as HPMC, Eudragit^®, and ethylcellulose play a central role in modulating release kinetics and improving bioavailability. Conclusions: This review not only synthesizes current formulation strategies but also explores reverse engineering of ideal release profiles and the integration of advanced modeling tools such as physiologically based pharmacokinetic (PBPK) modeling and in vitro–in vivo correlation (IVIVC). These approaches support the rational design of personalized, regulatory-compliant DH therapies. Full article

Background/Objectives: Palmitoylethanolamide (PEA) is an endogenous lipid mediator with endocannabinoid-like activity. Despite its therapeutic potential in muscle-related inflammatory disorders, including sarcopenia, its clinical use is limited by poor solubility and bioavailability. To overcome these issues, we developed hybrid nanoparticles combining poly(lactic-co-glycolic acid) (PLGA) and lipids to enhance PEA encapsulation and ok delivery. Methods: PEA-loaded hybrid nanoparticles (PEA-Hyb-np) were produced via a modified single-emulsion solvent evaporation method using stearic acid and Gelucire^® 50/13 as lipid components. Characterization included particle size, morphology, PDI, and zeta potential, as well as DSC, FT-IR, and XRD analyses. For the biological evaluation in a C2C12 myoblasts cell culture, coumarin-6-labeled nanoparticles were employed. Results: PEA-Hyb-np showed mean particle sizes of ~150 nm, with internal lipid–polymer phase separation. This structure enabled high encapsulation efficiency (79%) and drug loading (44.2 mg/g). Drug release in physiological and non-physiological media was enhanced due to drug amorphization, confirmed by DSC, FT-IR, and XRD analyses. Cytocompatibility studies showed no toxicity and improved cell viability compared to unloaded nanoparticles. Cellular uptake studies by confocal microscopy and flow cytometry demonstrated efficient and time-dependent internalization. Conclusions: PEA-Hyb-np represent a promising delivery platform to improve the solubility, bioavailability, and therapeutic efficacy of PEA for muscle-targeted applications. Full article

Superparamagnetic iron oxide nanoparticles (SPIONs) have gained significant attention for Magnetic Fluid Hyperthermia (MFH)-based cancer therapy. However, achieving high heating efficiency under a biologically safe Alternating Magnetic Field (AMF) remains a challenge. This study investigates the synthesis and optimization of SPIONs encapsulated in TPGS-stabilized PLGA nanoparticles (TPS-NPs) using a modified single emulsion solvent evaporation (M-SESE) method. The aim was to achieve efficient magnetic heating under biologically safe AMF conditions while maintaining biocompatibility and colloidal stability, making these magnetic nanoplatforms suitable for MFH-based cancer treatment. TPS-NPs were characterized using various techniques, including Dynamic Light Scattering (DLS), Atomic Force Microscopy (AFM), Transmission Electron Microscopy (TEM), and Superconducting Quantum Interference Device (SQUID) magnetometry, to evaluate their hydrodynamic size (Dh), zeta potential (ζ), encapsulation efficiency, and superparamagnetic properties. Calorimetric MFH studies demonstrated superior heating efficiency, with Specific Absorption Rate (SAR) and Intrinsic Loss Power (ILP) values optimized at an AMF of 4.1 GAm⁻¹s⁻¹, remaining within Hergt’s biological safety limit (~5 GAm⁻¹s⁻¹). These findings suggest that SPION-encapsulated TPS-NPs exhibit enhanced heat induction, making them promising candidates for MFH-based cancer therapy. The study highlights their potential as multifunctional nanoplatforms for magnetic hyperthermia therapy, paving the way for clinical translation in oncology for advanced cancer treatment. Full article

The development of antimicrobial and antioxidant packaging materials is critical for improving food safety and extending shelf life. This study aimed to design and characterize low-density polyethylene (LDPE) and poly(ethylene-co-vinyl acetate) (EVA) films incorporating organically modified montmorillonite (OMt) nanocarriers loaded with carvacrol (C) and thymol (T) essential oil components. The incorporation of carvacrol and thymol into OMt was conducted through an evaporation/adsorption method without the use of organic solvents. In the next step, LDPE, EVA and OMtC or OMtT were melt-compounded in order to obtain films. Characterization of the bioactive nanocarriers and films was performed through X-ray diffraction (XRD), tensile testing, oxygen permeability measurements (OTR) and antioxidant assays. Films LDPE/EVA/OMtC and LDPE/EVA/OMtT showed improved mechanical strength and antioxidant activity, with IC₅₀ values between 0.32 and 0.52 mg/mL. Film with component weight ratio LDPE/EVA/OMtC equal to 80/10/10 also demonstrated enhanced barrier properties and significantly inhibited fungal growth on baguette bread for up to 60 days. These findings highlight the potential of these bioactive films to improve the microbial safety and shelf life of bakery products. Full article

Double-base (DB) propellants, renowned for their superior performance and cost-effectiveness, are extensively utilized in both rocketry and artillery applications. During the 3D printing process of double-base propellants, auxiliary solvents play a crucial role in plasticizing the DB propellant mixtures. Consequently, the printed propellants are prone to significant shrinkage and dimensional instability as a result of solvent evaporation post-printing. To address these challenges, we have innovated a UV-assisted material extrusion 3D printing technique that preserves the intended geometries of the DB propellant. The results of our printing trials indicate that incorporating an energetic UV-curable resin as a modifier into the DB propellant paste is highly effective. Ultimately, we successfully fabricated a porous propellant cylinder featuring a periodic woodpile structure. Additionally, the internal structure, mechanical properties, combustion characteristics, and in-barrel ballistic performance of the printed propellants have been thoroughly characterized. Our findings underscore that the UV-assisted material extrusion additive manufacturing process confers exceptional properties to the DB propellant. Full article

As the demand for sustainable and innovative solutions in food packaging continues to grow, this study endeavors to introduce a comprehensive exploration of novel active materials. Specifically, we focus on characterizing polylactide-poly(ethylene glycol) (PLA/PEG) films filled with olive leaf extract (OLE; Olea europaea) obtained via solvent evaporation. Examined properties include surface structure, thermal degradation and mechanical attributes, as well as antibacterial activity. The results indicated a significant impact of the incorporation of OLE into this polymeric matrix, increasing hydrophobicity, decreasing surface free energy, and enhancing surface roughness, albeit with slight reductions in mechanical properties. Notably, these modified materials exhibited significant bacteriostatic, bactericidal and anti-adhesive activity against both Staphylococcus aureus and Escherichia coli. Consequently, PLA/PEG/OLE films demonstrated considerable potential for advanced food packaging, facilitating interactions between products and their environment. This capability ensures the preservation and extension of food shelf life, safeguards against microbial contamination, and maintains the overall quality, safety, and integrity of the packaged food. These findings suggest potential pathways for developing more sustainable and effective food packaging films. Full article

Emamectin benzoate (EB) is a highly effective broad-spectrum insecticide and acaricide. However, because EB is easily degraded, the conventional formulations of EB are often overapplied. In this study, polylactic acid (PLA)-based microspheres were prepared using the modified solvent evaporation method for the controlled release of EB. The microspheres were optimized to achieve higher EB loading. The effects of process parameters on the properties of microspheres, including encapsulation efficiency (EE), particle size, and pesticide loading, were investigated. Additionally, the controlled release behavior of EB microspheres was compared with that of conventional EB emulsifiable concentrate (EC). Spherical-shaped microspheres were obtained with an EE reaching 90.63 ± 1.90%, and introducing an external aqueous phase into the system can significantly enhance the EE of microspheres by over 30%. FTIR, DSC, and XRD analyses indicate that the preparation process of PLA microspheres was mainly physical encapsulation and had no chemical effect on EB. Notably, the EB microspheres displayed more potent control efficacy compared to commercial formulation EB EC against Plutella xylostella. The corrected mortality for the EB microspheres reached 90.00 ± 5.77% after 21 days of application, whereas the corrected mortality for the EB EC was only 19.23 ± 6.66% after 14 days of application. Our study demonstrates that EB-encapsulated PLA microspheres have strong potential as environmentally friendly control release EB formulations. Full article

Parkinson’s disease (PD) is the second most common neurodegenerative disorder globally that lacks any disease-modifying drug for prevention or treatment. Oxidative stress has been identified as one of the key pathogenic drivers of Parkinson’s disease (PD). Edaravone, an approved free-radical scavenger, has proven to have potential against PD by targeting multiple key pathologies, including oxidative stress, focal mitochondria, and neuroinflammation. However, its bioavailability is potentially restricted due to its poor solubility and short half-life. This study aims to develop a simple and effective drug delivery system for edaravone to enhance its solubility, stability, and bioavailability to improve its neuroprotective efficacy. An MPEG-2000-DSPE-edaravone (MDE) micelle was prepared via solvent evaporation using MPEG-2000-DSPE as a carrier to encapsulate edaravone. The morphology, particle size, zeta potential, chemical structure, and edaravone loading of MDE were evaluated. We then investigated whether such targeted edaravone delivery could provide enhanced neuroprotection. A cell model of PD was established in PC12 cells through exposure to rotenone. The effects of MDE on PC12 cells treated with or without rotenone were evaluated using a cell counting kit-8, calcein acetoxymethyl ester (AM)–propidine iodide (PI) staining, and flow cytometry. Cell migration was evaluated using a wound healing assay. Additionally, the intracellular antioxidant study was performed using an ROS-level-detecting DCFH-DA probe, and the mitochondrial membrane potentials were evaluated using a JC-1 assay. MDE with a drug-loading content of 17.6% and an encapsulation efficiency of 92.8% was successfully prepared. The resultant MDE had a mean particle size of 112.97 ± 5.54 nm with a zeta potential of −42 mV. Cytotoxicity assays confirmed that the MDE (≤200 ug/mL) exhibited promising cytocompatibility with no significant effect on cell viability, cell cycle regulation, or apoptosis levels. Likewise, compared with the free edaravone, no effect on cell migration was noted for MDE. MDE might be able to target edaravone delivery into PC12 cells, increasing the mitochondrial membrane potential and providing a significant local antioxidant effect. The results demonstrated that MPEG-2000-DSPE could be a promising material for enhancing edaravone’s aqueous solubility, stability, and antioxidant effects. MDE could be a potential drug formulation for treating PD and other diseases in which oxidative stress plays a key role in pathogenesis. Full article

Local Khulays clay was modified to prepare polystyrene clay nanocomposite (PCN) coatings on carbon steel. The PCN coatings were added to microcapsules (MCs) loaded with the corrosion inhibitor PCN(MC). The microcapsules were prepared by the encapsulation of rare-earth metal Ce⁺³ ions and isobutyl silanol into polystyrene via the double emulsion solvent evaporation (DESE) technique. From characterization techniques, Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), transmission electron microscopy (TEM), and scanning electron microscopy (SEM) with EDX. SEM and FT-IR confirmed the success of the preparation of the PCN(MC). Nanoindentation tests were performed on the thin-film samples. A significant reduction in both the hardness and the reduced modulus was observed for the PCN film compared to the PS film. Electrochemical impedance spectroscopy (EIS) and electrochemical frequency modulation (EFM) all showed an enhanced protection efficiency (%PE) of 3% PCN(MC) over 3% PCN at high temperatures and at different times. The smart coatings were proven by applying the thermal and the mechanical triggers for the 3% PCN(MC) coating. The mechanism of the release of inhibitors was discussed. The self-healing properties of 3% PCN(MC) were evaluated. The enhanced properties of the developed PCN(MC) coatings make them attractive for potential applications in the oil and other industries. Full article

Mixed matrix lithium adsorbents have attracted much interest for lithium recovery from brine. However, the absence of an interfacial interaction between the inorganic lithium-ion sieves (LISs) and the organic polymer matrix resulted in the poor structural stability and attenuated lithium adsorption efficiency. Here, a novel hollow hemispherical mixed matrix lithium adsorbent (H-LIS) with high interfacial compatibility was constructed based on mussel-bioinspired surface chemistry using a solvent evaporation induced phase transition method. The effects of types of functional modifiers, LIS loading amount, adsorption temperature and pH on their structural stability and lithium adsorption performance were systematically investigated. The optimized H-LIS adsorbent with the LIS loading amount of 50 wt.% possessed the structural merit that the LIS functionally modified by dopamine exposed on both the inner and outer surfaces of the hollow hemispheres. At the best adsorption pH of 12.0, it showed a comparable lithium adsorption capacity of 25.68 mg·g⁻¹ to the powdery LIS within 4 h, favorable adsorption selectivity of Mg/Li and good reusability that could maintain over 90% of lithium adsorption capacity after the LiCl adsorption—0.25 M HCl pickling-DI water cleaning cycling processes for three times. The interfacial interaction mechanism of H-LIS for lithium adsorption was innovatively explored via advanced microcalorimetry technology. It suggested the nature of the Li⁺ adsorption process was exothermic and dopamine modification could reduce the activation energy for lithium adsorption from 15.68 kJ·mol⁻¹ to 13.83 kJ·mol⁻¹ and trigger a faster response to Li⁺ by strengthening the Li⁺-H⁺ exchange rate, which established the thermodynamic relationship between the structure and Li⁺ adsorption performance of H-LIS. This work will provide a technical support for the structural regulation of functional materials for lithium extraction from brine. Full article

Giant unilamellar vesicles (GUVs) are frequently used as membrane models in studies of membrane properties. They are most often produced using the electroformation method. However, there are a number of parameters that can influence the success of the procedure. Some of the most common conditions that have been shown to have a negative effect on GUV electroformation are the presence of high cholesterol (Chol) concentrations, the use of mixtures containing charged lipids, and the solutions with an elevated ionic strength. High Chol concentrations are problematic for the traditional electroformation protocol as it involves the formation of a dry lipid film by complete evaporation of the organic solvent from the lipid mixture. During drying, anhydrous Chol crystals form. They are not involved in the formation of the lipid bilayer, resulting in a lower Chol concentration in the vesicle bilayer compared to the original lipid mixture. Motivated primarily by the issue of artifactual Chol demixing, we have modified the electroformation protocol by incorporating the techniques of rapid solvent exchange (RSE), ultrasonication, plasma cleaning, and spin-coating for reproducible production of GUVs from damp lipid films. Aside from decreasing Chol demixing, we have shown that the method can also be used to produce GUVs from lipid mixtures with charged lipids and in ionic solutions used as internal solutions. A high yield of GUVs was obtained for Chol/1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) samples with mixing ratios ranging from 0 to 2.5. We also succeeded in preparing GUVs from mixtures containing up to 60 mol% of the charged lipid 1-palmitoyl-2-oleoyl-sn-glycero-3-phospho-L-serine (POPS) and in NaCl solutions with low ionic strength (<25 mM). Full article

Compaction pressure can induce an undesirable solid-state polymorphic transition in drugs, fragmentation, loss of coated pellet integrity, and the decreased viability and vitality of microorganisms. Thus, the excipients with increased plasticity can be considered as an option to decrease the undesirable effects of compaction pressure. This study aims to increase the plasticity (to reduce the mean yield pressure; Py) of dried microcrystalline cellulose (MCC) by loading it with a specially selected plasticizer. Diethyl citrate (DEC), water, and glycerol were the considered plasticizers. Computation of solubility parameters was used to predict the miscibility of MCC with plasticizers (possible plasticization effect). Plasticizer-loaded MCC spheres with 5.0 wt.% of water, 5.2 wt.% of DEC, and 4.2 wt.% glycerol were obtained via the solvent method, followed by solvent evaporation. Plasticizer-loaded formulations were characterised by TGA, DSC, pXRD, FTIR, pressure-displacement profiles, and in-die Heckel plots. Py was derived from the in-die Heckel analysis and was used as a plasticity parameter. In comparison with non-plasticized MCC (Py = 136.5 MPa), the plasticity of plasticizer-loaded formulations increased (and Py decreased) from DEC (124.7 MPa) to water (106.6 MPa) and glycerol (99.9 MPa), and that was in full accordance with the predicted miscibility likeliness order based on solubility parameters. Therefore, water and glycerol were able to decrease the Py of non-plasticized MCC spheres by 16.3 and 30.0%, respectively. This feasibility study showed the possibility of modifying the plasticity of MCC by loading it with a specially selected plasticizer. Full article

Hydroxyapatite/polycaprolactone (HA/PCL) composites have been extensively explored in laser powder bed fusion (L-PBF) for bone tissue engineering. However, conventional mechanical mixing methods for preparing composite powders often yield inhomogeneous compositions and suboptimal flowability. In this study, HA/PCL powders were prepared and optimized for L-PBF using the modified emulsion solvent evaporation method. The morphology, flowability and thermal and rheological properties of the powders were systematically investigated, along with the mechanical and biological properties of the fabricated specimens. The HA/PCL powders exhibited spherical morphologies with a homogeneous distribution of HA within the particles. The addition of small amounts of HA (5 wt% and 10 wt%) enhanced the processability and increased the maximum values of the elastic modulus and yield strength of the specimens from 129.8 MPa to 166.2 MPa and 20.2 MPa to 25.1 MPa, respectively, while also improving their biocompatibility. However, excessive addition resulted in compromised sinterability, thereby affecting both mechanical and biological properties. Full article

Unsaturated fatty acids, such as oleic acid (OA) and linoleic acid (LA), are promising antimicrobial and cytostatic agents. We modified OA and LA with thymol (TOA and TLA, respectively) to expand their bioavailability, stability, and possible applications, and encapsulated these derivatives in polymeric nanoparticles (TOA-NPs and TLA-NPs, respectively). Prior to synthesis, we performed mathematical simulations with PASS and ADMETlab 2.0 to predict the biological activity and pharmacokinetics of TOA and TLA. TOA and TLA were synthesized via esterification in the presence of catalysts. Next, we formulated nanoparticles using the single-emulsion solvent evaporation technique. We applied dynamic light scattering, Uv-vis spectroscopy, release studies under gastrointestinal (pH 1.2–6.8) and blood environment simulation conditions (pH 7.4), and in vitro biological activity testing to characterize the nanoparticles. PASS revealed that TOA and TLA have antimicrobial and anticancer therapeutic potential. ADMETlab 2.0 provided a rationale for TOA and TLA encapsulation. The nanoparticles had an average size of 212–227 nm, with a high encapsulation efficiency (71–93%), and released TOA and TLA in a gradual and prolonged mode. TLA-NPs possessed higher antibacterial activity against B. cereus and S. aureus and pronounced cytotoxic activity against MCF-7, K562, and A549 cell lines compared to TOA-NPs. Our findings expand the biomedical application of fatty acids and provide a basis for further in vivo evaluation of designed derivatives and formulations. Full article

Pomegranate (Punica granatum L.) is a widely used fruit in the dietary supplement industry due to its richness in bioactive compounds. In this study, an experimental design was applied to optimize supercritical fluid extraction (SFE) of polar compounds of interest (ellagic acid and punicalagins), known for antioxidant and skin care properties from pomegranate’s pericarp. The effects of temperature, modifier percentage, and water additive percentage added in the modifier were explored through a Box–Behnken design, followed by a study of the extraction kinetics. The results indicated that 40 °C, 20% EtOH:H₂O 80:20 v:v, with an extraction duration of 60 min allowed for the highest recovery of the above-mentioned molecules (19.59 mg/g). Due to solubilization issues encountered by the extract, a screening of cosmetic solvents was carried out to solubilize SFE pomegranate extracts and a composition of Gly:H₂O 80:20 v:v was selected. Furthermore, an integrated SFE pre-formulation process of pomegranate pericarp extract (PPE) was elaborated. This allowed for the recovery of the extracts in cosmetic solvent, avoiding a full evaporation. Finally, the stability of the pre-formulated extracts was evaluated and showed high stability for over 3 months at 5 °C. Full article