Solvent Evaporation Research Articles

Formulation and Evaluation of Lamotrigine Spherules with Robust Gelation Technique

Many freshly created high-potential medications have low water solubility, which is a challenge in formulation development. The study aimed to improve the solubility of Lamotrigine, a weakly soluble medication classified as BCS class II, by solid dispersion techniques. Lamotrigine solid dispersion was created using the solvent evaporation method, and the formulation was assessed using stability tests, Fourier transform infrared spectroscopy (FTIR), and physical properties. Preformulation investigations yielded satisfactory results, therefore pellets were formed and evaluated. Solid dispersion had a different pharmacokinetic profile than pure medication, which could be attributable to Lamotrigine's faster dissolution rate from solid dispersion

Highly crystalline poly-3-hexylthiophene particles prepared from Pickering emulsions stabilized by alkylamine functionalized graphene quantum dots

Pickering emulsions have received much attention due to their high emulsions stability and ability to form functional emulsions compared to conventional emulsions. The stability of Pickering emulsions is dependent on the geometry and wettability of the particle type emulsifiers, which affect the detachment energy at the interface. Therefore, surface property control of the particle is essential. The graphene quantum dots (GQDs) functionalized with octylamine (C8), dodecylamine (C12), and hexadecylamine (C16) were synthesized and the stability of oil-in-water type Pickering emulsions compared. The detachment energies of the Pickering emulsifiers were calculated by measuring their wettability. Crystalline poly-3-hexylthiopene nanoparticles (P3HT NPs) were synthesized from the Pickering emulsion with C12-GQDs. Among the three GQDs, the C12-GQDs formed the most stable Pickering emulsions at the water-CHCl3 interface because of an appropriate balance between the water and oil phases due to the highest detachment energy. High-crystalline P3HT NPs can be synthesized from the Pickering emulsion with C12-GQDs due to the slower solvent evaporation and enhanced stability.

Fe nanoparticle-functionalized ordered mesoporous carbon with tailored mesostructures and their applications in magnetic removal of Ag(i)

Abstract Fe nanoparticle-functionalized ordered mesoporous carbon (Fe0/OMC) was synthesized using triblock copolymers as templates and through solvent evaporation self-assembly, followed by a carbothermal reduction. Fe0/OMC had three microstructures of two-dimensional hexagonal (space group, p6mm, Fe0/OMC-1), body centered cubic (Im3̄m, Fe0/OMC-2), and face centered cubic (Fm3̄m, Fe0/OMC-3) which were controlled by simply adjusting the template. All Fe0/OMC displayed paramagnetic characteristics, with a maximum saturation magnetization of 50.1 emu·g−1. This high magnetization is advantageous for the swift extraction of the adsorbent from the solution following the adsorption process. Fe0/OMC was used as an adsorbent for the removal of silver ions (Ag(i)) from aqueous solutions, and the adsorption capacity of Fe0/OMC-1 was enhanced by the functionalization of Fe0. Adsorption property of Fe0/OMC-1 was significantly higher than that of Fe0/OMC-2 and Fe0/OMC-3, indicating that the long and straight ordered pore channels were more favorable for adsorption, and the adsorption capacity of Ag(i) on Fe0/OMC-1 was 233 mg·g−1. The adsorption process exhibited conformity with both the pseudo-second-order kinetic model and the Freundlich model, suggesting that the dominant mechanism of adsorption involved multilayer adsorption on heterogeneous surfaces.

Preparation of Microsponge Drug Delivery System (MSDDS) Followed by a Scale-Up Approach.

In 1987, Won invented the solid-phase porous microsphere (MS), which stores bioactive compounds in many interconnected voids. Spherical particles (5-300 μm), MS, may form clusters of smaller spheres, resulting in many benefits. The current investigation focussed on gel-encased formulation, which can be suitable for dermal usage. First, quasi-emulsion (w/o/w) solvent evaporation was used to prepare 5-fluorouracil (5 FU) MS particles. The final product was characterized (SEM shows porous structure, FTIR and DSC showed drug compatibility with excipients, and gel formulation is shear-thinning) and further scaled up using the 8-fold method. Furthermore, CCD (Central Composite Design) was implemented to obtain the optimized results. After optimizing the conditions, including the polymer (600 mg, ethyl cellulose (EC), eudragit RS 100 (ERS)), stirring speed (1197 rpm), and surfactant concentration (2% w/v), we achieved the following results: optimal yield (63%), mean particle size (152 µm), drug entrapment efficiency (76%), and cumulative drug release (74.24% within 8 h). These findings are promising for industrial applications and align with the objectives outlined in UN Sustainable Development Goals 3, 9, and 17, as well as the goals of the G20 initiative.

Development of optimized resveratrol/piperine-loaded phytosomal nanocomplex for isoproterenol-induced myocardial infarction treatment

Cardiovascular disease is a significant and ever-growing concern, causing high morbidity and mortality worldwide. Conventional therapy is often very precarious and requires long-term usage. Several phytochemicals, including Resveratrol (RSV) and Piperine (PIP), possess significant cardioprotection and may be restrained in clinical settings due to inadequate pharmacokinetic properties. Therefore, this study strives to develop an optimized RSV phytosomes (RSVP) and RSV phytosomes co-loaded with PIP (RPP) via solvent evaporation method using Box-Behnken design to enhance the pharmacokinetic properties in isoproterenol-induced myocardial infarction (MI). The optimized particle size (20.976 ± 0.39 and 176.53 ± 0.88 nm), zeta potential (−33.33 ± 1.5 and −48.7 ± 1.6 mV), drug content (84.57 ± 0.9 and 87.16 ± 0.6%), and %EE (70.56 ± 0.7 and 67.60 ± 0.57%) of the prepared RSVP and RPP, respectively demonstrated enhanced solubility and control release in diffusion media. The oral administration of optimized RSVP and RPP in myocardial infarction-induced rats exhibited significant (p < 0.001) improvement in heart rate, ECG, biomarker, anti-oxidant levels, and no inflammation than pure RSV. The pharmacokinetic assessment on healthy Wistar rats exhibited prolonged circulation (>24 h) of RSVP and RPP compared to free drug/s. The enhanced ability of RSVP and RPP to penetrate bio-membranes and enter the systemic circulation renders them a more promising strategy for mitigating MI.

Construction of recombinant Omp25 or EipB protein loaded PLGA nanovaccines for Brucellosis protection

Safe and effective vaccine candidates are needed to address the limitations of existing vaccines against Brucellosis, a disease responsible for substantial economic losses in livestock. The present study aimed to encapsulate recombinant Omp25 and EipB proteins, knowledged antigen properties, into PLGA nanoparticles, characterize synthesized nanoparticles with different methods, and assessed their in vitro/in vivo immunostimulatory activities to develop new vaccine candidates. The recombinant Omp25 and EipB proteins produced with recombinant DNA technology were encapsulated into PLGA nanoparticles by double emulsion solvent evaporation technique. The nanoparticles were characterized using FE-SEM, Zeta-sizer, and FT-IR instruments to determine size, morphology, zeta potentials, and polydispersity index values, as well as to analyze functional groups chemically. Additionally, the release profiles and encapsulation efficiencies were assessed using UV–Vis spectroscopy. After loading with recombinant proteins, O-NPs reached sizes of 221.2 ± 5.21 nm, while E-NPs reached sizes of 274.4 ± 9.51 nm. The cumulative release rates of the antigens, monitored until the end of day 14, were determined to be 90.39% for O-NPs and 56.1% for E-NPs. Following the assessment of the in vitro cytotoxicity and immunostimulatory effects of both proteins and nanoparticles on the J774 murine macrophage cells, in vivo immunization experiments were conducted using concentrations of 16 µg ml−1 for each protein. Both free antigens and antigen-containing nanoparticles excessively induced humoral immunity by increasing produced Brucella-specific IgG antibody levels for 3 times in contrast to control. Furthermore, it was also demonstrated that vaccine candidates stimulated Th1-mediated cellular immunity as well since they significantly raised IFN-gamma and IL-12 cytokine levels in murine splenocytes rather than IL-4 following to immunization. Additionally, the vaccine candidates conferred higher than 90% protection from the infection according to challenge results. Our findings reveal that PLGA nanoparticles constructed with the encapsulation of recombinant Omp25 or EipB proteins possess great potential to trigger Brucella-specific humoral and cellular immune response.

Dynamic Ion Gels from the Complex Coacervation of Oppositely Charged Poly(ionic liquid)s.

A cationic poly(ionic liquid) (PIL) with pendent butyl imidazolium cations and free bis(trifluoromethylsulfonyl)imide (TFSI) anions and an anionic PIL with pendent TFSI anions and free 1-butyl-3-methylimidazolium cations are synthesized by postpolymerization chemical modification and reversible addition-fragmentation chain-transfer radical copolymerization, respectively. Upon mixing solutions of these two PILs in acetone with stoichiometric amounts of ion pairs, ionic exchanges induce coacervation and, after solvent evaporation, lead to the formation of a dynamic ion gel (DIG) and the concomitant release of free [1-methyl-3-butyl imidazolium]TFSI ionic liquid (IL). A comparison of thermal (Tg), ion conducting (σDC), and viscoelastic (elastic moduli (G')) properties for DIGs and their parent polyelectrolytes, as well as extracted and IL-doped DIGs, demonstrates the formation of ionic cross-links and the ability to easily produce polymer electrolytes with enhanced ionic conductivity (σDC up to 4.5 × 10-5 S cm-1 at 30 °C) and higher elastic moduli (G' up to 4 kPa at 25 °C and 1 rad s-1), making them highly desirable in many electrochemical applications, including supercapacitors, soft robotics, electrochromic devices, sensors, and solar cells.

Solid self-nanoemulsifying drug delivery systems of nimodipine: development and evaluation

BackgroundThis study aimed to formulate solid self-nanoemulsifying drug delivery systems (SNEDDS) for nimodipine (NIM). The selection of Cremophor RH 40, Lipoxol 300, and PEG 400 as oil, surfactant, and co-surfactant was based on solubility and self-emulsification assessments. A ternary phase diagram determined the optimal oil to Smix (surfactant/co-surfactant) ratio (40:60). By utilizing liquid SNEDDS (NIM-SNEDDS) as an adsorbate and chitosan EDTA microparticles, developed through spray drying (SD-CHEM) and solvent evaporation (SE-CHEM) as adsorbents, the solid SNEDDS were created (NIM-SD-SSNEDDS and NIM-SE-SSNEDDS, respectively).ResultsBoth solid formulations exhibited favourable drug loading (NIM-SD-SSNEDDS = 79.67 ± 2.97%, NIM-SE-SSNEDDS = 77.76 ± 4.29%), excellent flowability, and drug amorphization as per XRD and DSC analysis. Scanning electron microscopy revealed smoothening and filling of adsorbent surfaces by adsorbate (with size range NIM-SD-SSNEDDS = 10–15 μm, NIM-SE-SSNEDDS = 20–25 μm). FTIR confirmed no interaction of drug and excipients. Stability studies demonstrated the physical and thermodynamic stability of reconstituted nanoemulsions with droplet size, PDI, zeta potential, emulsification time, % transmittance and cloud temperature for NIM-SD-SSNEDDS as 247.1 nm, PDI 0.620, 1.353 mV, 38–41 s, 94.64%, 54 °C and for NIM-SE-SSNEDDS as 399.6 nm, PDI 0.821, 1.351 mV, 40–48 s, 92.96%, 49 °C, respectively. FE-SEM images showed globules formed with small sizes, and there was no coalescence evidence, implying the reconstituted nanoemulsions' stability. In vitro dissolution studies revealed a fourfold increase in drug dissolution for NIM-SD-SSNEDDS (84.43%) and NIM-SE-SSNEDDS (76.68%) compared to pure drug (28%). Ex vivo permeation studies indicated almost similar profiles for NIM-SD-SSNEDDS (22.61%) and NIM-SE-SSNEDDS (21.93%) compared to NIM-SNEDDS (25.02%).ConclusionNIM-SD-SSNEDDS exhibited superior performance compared to NIM-SE-SSNEDDS, highlighting the efficacy of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These results suggest enhanced dissolution and permeation for nimodipine in both the solid SNEDDS.

Development of Albendazole Nanodispersion for the Effective Treatment of Helminthiasis

Albendazole is a drug used to treat parasitic worm infections. ALB results in the tegument and intestinal cells of the worm undergoing degenerative changes, which ultimately lead the parasite to become immobile and die. The purpose of the study was to improve the solubility and effectiveness of an ALB-loaded solid nano dispersion for the effective treatment of helminthiasis.ALBFs were generated by a solvent evaporation procedure involving PVPK30 and carbopol, which may improve the stability of controlled drug release rates. The newly found ALBFs are more soluble than pure albendazole and have a better bioavailability. ALBFs allow for the optimization of therapeutic efficacy while lowering potential side effects and modulating enzymatic resistance, degradation, and drug release rate. Thus, the created ALBFs demonstrated successful helminthiasis treatment with lower dose frequency.

Lithium iodide transport in double gyroid nanochannels formed by zwitterion‐containing solid polymer electrolytes

AbstractThe fabrication of nanostructured block copolymer (BCP) films endowed with lithium ion‐conducting gyroid (GYR) nanochannels is an appealing solution to build solid polymer electrolytes (SPEs) that combines high ionic conductivity (IC) with suitable mechanical properties. However, the formation of a well‐developed GYR structure remains challenging to achieve from the self‐assembly of polyelectrolyte BCP chains. To overcome this issue, large ion conducting gyroid grains were produced within freestanding polystyrene‐block‐poly(2‐vinylpyridine)‐block‐poly(ethylene oxide) (PS‐b‐P2VP‐b‐PEO) films by combining a solvent vapor annealing (SVA) treatment with an infiltration process. Here, the SVA treatment enabled the manufacture of SPEs entirely composed of a GYR structure while the infiltration process allowed for the incorporation of an appropriate Li salt (i.e., lithium iodoacetate, LiIAc) within the 3D‐interconected nanochannels via a Menshutkin reaction. By using this SVA‐Infiltration strategy, it has been demonstrated that the creation of ion conducting GYR nanochannels enhances the ion transportation capacity of pyridine‐containing SPEs since substantially lower ICs were measured from analog PS‐b‐P2VP‐b‐PEO/LiIAc films having a nominally disordered as‐cast state. Remarkably, zwitterionic pyridinium‐based moieties formed inside the interpenetrated nanochannels enable an efficient migration of Li+ and I3− species, leading to an IC as high as 10−4 S cm−1 at 70°C.

Pharmaceutical Properties of the Phloretin-4,4'-Bipyridine Cocrystal: Structure Analysis, Drug Release Profile, and Antioxidant Activity Research.

To improve the water solubility of phloretin, we synthesized the Phl-4B cocrystal using the solvent evaporation method. Various analytical techniques including powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), 1HNMR, and single-crystal X-ray diffraction (SCXRD) were employed to evaluate the crystal thermodynamics and structure. The results of PXRD and SCXRD showed that it was a new cocrystal crystallized in the P-1 space group of the triclinic system. Thermal analysis confirmed the purity of the Phl-4B cocrystal. The equilibrium solubility of the Phl-4B cocrystal in pH 1.2 was improved. In vitro simulated digestion experiments indicated that the release of the Phl-4B cocrystal followed Fick diffusion. The stability activity of phloretin after pharmaceutical cocrystallization was improved. The antioxidant of the Phl-4B cocrystal was better than that of pure Phl.

Recent Progress in Solid-State Room Temperature Afterglow Based on Pure Organic Small Molecules.

Organic room temperature afterglow (ORTA) can be categorized into two key mechanisms: continuous thermally activated delayed fluorescence (TADF) and room-temperature phosphorescence (RTP), both of which involve a triplet excited state. However, triplet excited states are easily quenched by non-radiative transitions due to oxygen and molecular vibrations. Solid-phase systems provide a conducive environment for triplet excitons due to constrained molecular motion and limited oxygen permeation within closely packed molecules. The stimulated triplet state tends to release energy through radiative transitions. Despite numerous reports on RTP in solid-phase systems in recent years, the complexity of these systems precludes the formulation of a universal theory to elucidate the underlying principles. Several strategies for achieving ORTA luminescence in the solid phase have been developed, encompassing crystallization, polymer host-guest doping, and small molecule host-guest doping. Many of these systems exhibit luminescent responses to various physical stimuli, including light stimulation, mechanical stimuli, and solvent vapor exposure. The appearance of these intriguing luminescent phenomena in solid-phase systems underscores their significant potential applications in areas such as light sensing, biological imaging, and information security.

Auranofin-loaded PLGA nanoparticles alleviate cognitive deficit induced by streptozotocin in rats model: modulation of oxidative stress, neuroinflammatory markers, and neurotransmitters.

Alzheimer's disease remains an unsolved neurological puzzle with no cure. Current therapies offer only symptomatic relief, hindered by limited uptake through the blood-brain barrier. Auranofin, an FDA-approved compound, exhibits potent antioxidative and anti-inflammatory properties targeting brain disorders. Yet, its oral bioavailability challenge prompts the exploration of nanoformulation-based solutions enhancing blood-brain barrier penetrability. The study aimed to investigate the neuroprotective potential of auranofin nanoparticles in streptozotocin-induced AD rats. Auranofin-containing polylactic-co-glycolic acid nanoparticles were formulated by the multiple emulsion solvent evaporation method. Characterization was done by determining entrapment efficiency, particle size distribution, surface charge, and morphology. An in vivo study was performed by administering streptozotocin (3mg/kg/i.c.v., days 1 and 3), auranofin (5 and 10mg/kg), auranofin nanoparticles (2.5 and 5mg/kg), and donepezil (2mg/kg) for 14days orally. Behavioral deficits were evaluated using the open field test, Morris water maze, objective recognition test, change in oxidative stress levels, and AD markers in the brain. Following the decapitation of the rats, the brains were excised to isolate the hippocampus. Subsequent analyses included the quantification of biochemical and neuroinflammatory markers, as well as the assessment of neurotransmitter levels. The characterization of auranofin nanoparticles showed an entrapment efficiency of 98%, an average particle size of 101.5 ± 10.3nm, a surface charge of 27.5 ± 5.10mV, and a polydispersity index of 0.438 ± 0.12. In vivo, administration of auranofin and auranofin nanoparticles significantly reversed streptozotocin-induced cognitive deficits, biochemical alteration, neuroinflammatory markers, and neurotransmitter levels. The present finding suggests that auranofin nanoparticles have more significant neuroprotective potential than auranofin alone. The therapeutic efficacy may be attributed to its antioxidant and anti-inflammatory properties, as well as its positive neuromodulatory effects. Therefore, our findings suggest that it could be a promising candidate for Alzheimer's disease therapy.

Melt-extruded biocompatible surgical sutures loaded with microspheres designed for wound healing

Sutures are commonly used in surgical procedures and have immense potential for direct drug delivery into the wound site. However, incorporating active pharmaceutical ingredients into the sutures has always been challenging as their mechanical strength deteriorates. This study proposes a new method to produce microspheres-embedded surgical sutures that offer adequate mechanical properties for effective wound healing applications. The study used curcumin, a bioactive compound found in turmeric, as a model drug due to its anti-inflammatory, antioxidant, and anti-bacterial properties, which make it an ideal candidate for a surgical suture drug delivery system. Curcumin-loaded microspheres were produced using the emulsion solvent evaporation method with polyvinyl alcohol (PVA) as the aqueous phase. The microspheres’ particle sizes, drug loading (DL) capacity, and encapsulation efficiency (EE) were investigated. Microspheres were melt-extruded with polycaprolactone and polyethylene glycol via a 3D bioplotter, followed by a drawing process to optimise the mechanical strength. The sutures’ thermal, physiochemical, and mechanical properties were investigated, and the drug delivery and biocompatibility were evaluated. The results showed that increasing the aqueous phase concentration resulted in smaller particle sizes and improved DL capacity and EE. However, if PVA was used at 3% w/v or below, it prevented aggregate formation after lyophilisation, and the average particle size was found to be 34.32 ± 12.82 μm. The sutures produced with the addition of microspheres had a diameter of 0.38 ± 0.02 mm, a smooth surface, minimal tissue drag, and proper tensile strength. Furthermore, due to the encapsulated drug-polymer structure, the sutures exhibited a prolonged and sustained drug release of up to 14 d. Microsphere-loaded sutures demonstrated non-toxicity and accelerated wound healing in the in vitro studies. We anticipate that the microsphere-loaded sutures will serve as an excellent biomedical device for facilitating wound healing.

Synthesis and structural characterization of supramolecular cocrystals of [(4-cyano-1-methylpyridinium)2-(18-crown-6)] diiodide

Abstract This study focuses on synthesizing and characterizing supramolecular cocrystals derived from 4-cyano-1-methylpyridinium iodide and 18-crown-6. The synthesis employed a solvent evaporation technique, followed by a thorough structural analysis utilizing XRD methods. The compound’s purity is confirmed by powder XRD analysis, while single-crystal XRD confirms its triclinic system packing with a centrosymmetric space group ( P 1 ‾ $P\overline{1}$ ). The findings unveiled the emergence of unique cocrystals characterized by distinct molecular configurations supported by hydrogen bonding and ion-dipole interactions. Through diffuse reflectance spectral measurements, the direct band gap energy was assessed at 2.36 eV. Thermogravimetric analysis was utilized to evaluate the thermal properties of the compound across varying temperatures. The compound’s elemental composition and surface morphology were analyzed through investigations using EDS and SEM.

In Situ Transformation of an Amorphous Supramolecular Coating to a Hydrogen-Bonded Organic Framework Membrane to Trigger Selective Gas Permeation.

We introduce a "solution-processing-transformation" strategy, deploying solvent vapor as scaffolds, to fabricate high-quality hydrogen-bonded organic framework (HOF) membranes. This strategy can overcome the mismatch in processing conditions and crystal growth thermodynamics faced during the facile solution processing of the membrane. The procedure includes the vapor-trigged in situ transformation of dense amorphous supramolecules to crystalline HOF-16, with HOF-11 as the transient state. The mechanism involves a vapor-activated dissolution-precipitation equilibrium shifting and hydrogen bonding-guided molecule rearrangement, elucidated through combined experimental and theoretical analysis. Upon removal of the molecular scaffolds, the resulting HOF-16 membranes showcase significant improvement in hydrogen separation performance over their amorphous counterparts and previously reported HOF membranes. The method's broad applicability is evidenced by successfully extending it to other substrates and HOF structures. This study provides a fundamental understanding of guest-induced ordered supramolecular assembly and paves the way for the advanced manufacture of high-performance HOF membranes for gas separation processes.

In Situ Transformation of an Amorphous Supramolecular Coating to a Hydrogen‐Bonded Organic Framework Membrane to Trigger Selective Gas Permeation

AbstractWe introduce a “solution‐processing‐transformation” strategy, deploying solvent vapor as scaffolds, to fabricate high‐quality hydrogen‐bonded organic framework (HOF) membranes. This strategy can overcome the mismatch in processing conditions and crystal growth thermodynamics faced during the facile solution processing of the membrane. The procedure includes the vapor‐trigged in situ transformation of dense amorphous supramolecules to crystalline HOF‐16, with HOF‐11 as the transient state. The mechanism involves a vapor‐activated dissolution‐precipitation equilibrium shifting and hydrogen bonding‐guided molecule rearrangement, elucidated through combined experimental and theoretical analysis. Upon removal of the molecular scaffolds, the resulting HOF‐16 membranes showcase significant improvement in hydrogen separation performance over their amorphous counterparts and previously reported HOF membranes. The method's broad applicability is evidenced by successfully extending it to other substrates and HOF structures. This study provides a fundamental understanding of guest‐induced ordered supramolecular assembly and paves the way for the advanced manufacture of high‐performance HOF membranes for gas separation processes.

Preparation and Evaluation of Berberine-Excipient Complexes in Enhancing the Dissolution Rate of Berberine Incorporated into Pellet Formulations

Berberine is used in the treatment of metabolic syndrome and its low solubility and very poor oral bioavailability of berberine was one of the primary hurdles for its market approval. This study aimed to improve the solubility and bioavailability of berberine by preparing pellet formulations containing drug-excipient complex (obtained by solid dispersion). Berberine-excipient solid dispersion complexes were obtained with different ratios by the solvent evaporation method. The maximum saturation solubility test was performed as a key factor for choosing the optimal complex for the drug-excipient. The properties of these complexes were investigated by FTIR, DSC, XRD and dissolution tests. The obtained pellets were evaluated and compared in terms of pelletization efficiency, particle size, mechanical strength, sphericity and drug release profile in simulated media of gastric and intestine. Solid-state analysis showed complex formation between the drug and excipients used in solid dispersion. The optimal berberine-phospholipid complex showed a 2-fold increase and the optimal berberine-gelucire and berberine-citric acid complexes showed more than a 3-fold increase in the solubility of berberine compared to pure berberine powder. The evaluation of pellets from each of the optimal complexes showed that the rate and amount of drug released from all pellet formulations in the simulated gastric medium were significantly lower than in the intestine medium. The results of this study showed that the use of berberine-citric acid or berberine-gelucire complex could be considered a promising technique to increase the saturation solubility and improve the release characteristics of berberine from the pellet formulation.Graphical

Low-cost method to reduce interlayer voids in material extrusion: in situ layer-by-layer solvent treatment

Material extrusion (MEX) is worldwide known as one of the most flexible additive manufacturing (AM) technologies for the fabrication of complex polymeric structures. However, the extremely high geometrical freedom has a price to pay: the presence of interlayer voids between consecutive extruded layers is the main backwards of MEX technology. Interlayer voids make 3D printed parts weaker (poor mechanical properties) compared to polymeric components fabricated by means of counterpart processes (i.e., injection molding). The present research work introduces a novel approach for the reduction of voids based on the layer-by-layer application of solvent vapor during the fabrication process, to smooth every single deposited layer. In this way, the new extruded layer has a greater area to bond with the previously extruded layer, resulting in an overall reduction of the porosity. The proposed approach is cost-effective, and it is based on the stop and go method enabled by MEX technologies: the fabrication process is paused after every layer, and when the solvent treatment is performed, the 3D printing process is resumed. The effectiveness of the layer-by-layer solvent vapor approach was evaluated, thereby resulting in a great reduction of the void density and average void area of 96%, and 79% respectively, and an increase of the wetting factor of 34%. Such findings pave the way for the exploitation of the proposed approach for the fabrication of complex structures with a reduced number of voids to be employed as structural components.

Enhanced antimicrobial potency and stability of juglone/β-cyclodextrin inclusion complexes: a comparative study of formulation methods

Juglone (5-hydroxy-1,4-naphthoquinone), a natural antifungal and antibacterial agent derived from walnut trees, possesses significant therapeutic potential limited by its low water solubility and instability in varying pH and temperature conditions This study aims to address these limitations by enhancing juglone’s solubility, stability, and antimicrobial efficacy through the formation of inclusion complexes with β-cyclodextrin (β-CD). Employing methods such as co-precipitation, freeze-drying, and solvent evaporation, we synthesized these complexes and confirmed their formation using UV–vis, and FT-IR spectroscopy. The obtained optimum complex was characterized using SEM to reveal its structural properties, while NMR analysis showed significant chemical shift changes, indicative of complex formation between juglone and β-CD; additionally, XRD analysis confirmed the amorphous nature of the J-β-CD3-4 inclusion complex, providing direct evidence for its formation. Our findings reveal a notable enhancement in the pH and thermal stability of juglone within the β-CD inclusion complex, in comparison to its free form. Moreover, the antimicrobial activity of the juglone-β-CD complex surpassed that of juglone alone. The increased water solubility of juglone in the inclusion complex contributed to its enhanced antimicrobial activity. The inhibition zone diameters of J-β-CD3-4 inclusion complex against E. coli, S. aureus, and C. albicans were 7, 22, and 8.5 mm, respectively, relatively higher than juglone. Remarkably, in the broth microdluation method, the MIC and MBC values of the inclusion complex were determined to be much lower than those of free juglone, a significant fourfold decrease for S. aureus, and C. albicans and twofold for E. coli. These results underscore the potential of juglone-β-CD complexation in extending the applicability of juglone, especially in sectors such as food preservation, agriculture, and pharmaceuticals, where enhanced stability and efficacy of natural antimicrobial agents are crucial.