Solvent Evaporation Method Research Articles

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

A Comparison Study between Green Synthesis of Microwave Irradiation and Solvent Evaporation Methods in The Formation of p-Methoxycinnamic Acid-Succinic Acid Cocrystals

Cocrystal of p-Methoxycinnamate acid-succinic acid has been produced by microwave irradiation and solvent evaporation methods. Cocrystals are formed using succinic acid as the coformer at a molar ratio of 1:1. The formation of cocrystal can be done by solvent evaporation method and microwave radiation method. Physicochemical properties have been studied by FT-IR, DSC, PXRD, and SEM analysis. The solubility test was carried out with pH 6.8 phosphate buffer at a temperature of 25±0.5°C for 5 hours and the dissolution test was carried out with 900 mL pH 6.8 phosphate buffer at a temperature of 37±0.5°C with the speed of 75 rpm using a paddle-type dissolution test apparatus. The solubility of PMCA has increased its solubility in cocrystals by the solvent evaporation method by 1.19 times and by the microwave radiation method by 1.16 times compared to PMCA. The dissolution rate of the cocrystals of the solvent evaporation method increased by 3.50 times and the cocrystals of the microwave radiation method increased by 2.29 times compared to PMCA.

Study of the Effect of Different Additives on the Shelf Life of Microencapsulated Vitamin C

Vitamin C (Vit C) is sensitive to oxidation, so maintaining its stability is the biggest challenge in its preparation and use. The aim of this research was to study the effect of adding various additives on the stability of Vit C microencapsulated in microparticles prepared by solvent evaporation method. The results showed that the system viscosity had an effect on the particle size, encapsulation efficiency EE was affected by PVA, Vit C and polymer concentrations. The additives that have shown a positive effect on EE are sucrose concentration, addition of alginate Na and chitosan. The results also showed that using (sucrose, glucose, cysteine, alginate Na and chitosan) as additives can protect AA in microparticles and increase shelf lives (AA shelf life increased significantly from 15 to 42 days by using sucrose as additive).

Temperature-sensitive fragrance-releasing polymeric microcapsules

This research aimed to control release of fragrance using thermally-actuated microcapsules so that the release rate shows a considerable change at a certain temperature. Accordingly, four different polymers, namely, two grades of poly(methyl methacrylate) having different molecular weight as well as two poly[(methyl methacrylate)–co-(2-ethylhexyl acrylate)] copolymers, which were synthesized in this work, were designated as capsules’ shell. Number-average molecular weight of the copolymers and one of the two used PMMA grades was in the range of 47 to 56 kDa while that of the other PMMA grade was 344 kDa. Furthermore, Tg of the lower molecular weight grade PMMA and the two copolymers was determined as 119.3, 72.2 and 66.3 °C, respectively, using DSC experiments. Subsequently, R-Limonene as a model fragrance, was encapsulated by either of the polymers using solvent evaporation method. Effect of various parameters, including molecular weight and Tg of the shell polymer and concentration of emulsifier, on morphological characteristics of the microcapsules were investigated. Using two microscopic techniques, it was observed that increment of molecular weight of shell polymer enhances microcapsules’ size, shell thickness and porosity. Moreover, elevation of emulsifier concentration to a certain value of 1.5 wt% was shown to lessen size and porosity of microcapsules. The fragrance release profiles were determined and fitted to several mathematical models, proving that at least one more mechanism, in addition to diffusion, is involved in the release, which was attributed to capillary effects in the shell pores. Moreover, a pronounced increase in release rate upon elevation of temperature from 5 to 15 °C was observed for either of the copolymer shells. The effect was ascribed to remarkable strengthening of segmental mobility of the copolymers due to elevation of temperature and can be regarded as a promising way for the fabrication of smart microcapsules capable of thermal controlling fragrance release.

Preparation of mussel-inspired adhesion nanocapsules and their application on cotton fabrics

In this study, a hyperbranched polymer (HBP) with a hydrophobic backbone and hydrophilic adhesive catechol side chains was synthesized through the Michael addition reaction between multi-vinyl monomers with dopamine. Underwater adhesion experiments demonstrated that HBP had rapidly strong adhesion. Using HBP as the wall material and lavender essential oil (LO) as the core material, catechol-hyperbranched nanocapsules (CHNPs) with good adhesion and acidic responsive properties were prepared by solvent evaporation method. Subsequently, ACFs with good wash resistance were prepared by impregnation and further introduction of Fe3+. After 25 washing cycles, the retention rate of LO in CF treated solely with CHNPs solution (CHNPs@CF) was only 9.7 %, whereas the retention rate increased to 17.8 % for CHNPs@CF treated with FeCl3 solution (Fe3+/CHNPs@CF). The persistent adhesion of CHNPs on cotton fabrics (CF) is achieved by hydrogen bonding and Fe3+-catechol coordination bonding. These results confirm the significant potential of CHNPs in aromatic textile applications and it is expected to promote the diversified development of functional textiles.

β-Cyclodextrin and Hyaluronic Acid-Modified Targeted Nanodelivery System for Atherosclerosis Prevention.

Natural products have been widely recognized in clinical treatment because of their low toxicity and high activity. It is worth paying attention to modifying the biopolymer into nanostructures to give natural active ingredients additional targeting effects. In this study, based on the multifunctional modification of β-cyclodextrin (β-CD), a nanoplatform encapsulating the unstable drug (-)-epicatechin gallate (ECG) was designed to deliver to atherosclerotic plaques. Acetalization cyclodextrin (PH-CD), which responds to low-pH environments, and hyaluronic acid cyclodextrin, which targets the CD44 receptor on macrophage membranes, were synthesized from β-CD and hyaluronic acid using acetalization and transesterification, respectively. The resulting dual-carrier nanoparticles (Double-NPs) loaded with ECG were prepared using a solvent evaporation method. The Double-NPs effectively scavenged reactive oxygen species, promoted macrophage migration, inhibited macrophage apoptosis, and suppressed abnormal proliferation and migration of vascular smooth muscle cells. Furthermore, the Double-NPs actively accumulated in atherosclerotic plaques in ApoE-/- mice fed with a high-fat diet, leading to a reduced plaque area, inflammatory infiltration, and plaque instability. Our findings demonstrate that the newly developed ECG nanopreparation represents an effective and safe nanotherapy for diseases such as atherosclerosis.

Formulation and Evaluation of pH-Modulated Amorphous Solid Dispersion-Based Orodispersible Tablets of Cefdinir.

Cefdinir (CEF) is a semi-synthetic third-generation broad-spectrum oral cephalosporin that exhibits poor solubility at lower pH values. Considering this, pH-modulated CEF solid dispersions (ASDs) were produced by solvent evaporation method employing various hydrophilic carriers and alkalizers. Among different carriers, ASDs produced using PEG 6000 with meglumine as alkalizer were found to significantly increase (p < 0.005) the drug solubility (4.50 ± 0.32 mg/mL) in pH 1.2. Fourier transform infrared spectrophotometry confirmed chemical integrity of CEF while differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) indicated CEF was reduced to an amorphous state in ASD8. Antimicrobial assay performed by well diffusion method against Staphylococcus aureus (MTCC96) and Escherichia coli (MTCC118) demonstrated significantly superior (p < 0.001) efficacy of CEFSD compared to CEF. The porous orodispersible tablets (ODTs) of ASD8 (batch F5) were developed by incorporating ammonium bicarbonate as a subliming agent by direct compression, followed by vacuum drying displayed quick disintegration (27.11 ± 1.96 s) that met compendial norms and near-complete dissolution (93.85 ± 1.27%) in 30 min. The ODTs of ASD8 appear to be a promising platform to mitigate the pH-dependent solubility and dissolution issues associated with CEF in challenging physiological pH conditions prevalent in stomach. Thus, ODTs of ASD8 are likely to effectively manage various infections and avoid development of drug-resistant strains, thereby improving the curing rates.

New stable waterborne amorphous polylactic acid/organoclay nanocomposites prepared using emulsification solvent evaporation method

AbstractWater based polylactic acid (PLA)‐surface modified montmorillonite (MMt) nanocomposites as biobased formulations for paper coating were successfully developed using emulsification solvent evaporation method. Electrostatic and steric stabilization mechanisms have contributed to the production of stable emulsions up to 5 months at 23 ± 1°C, revealing strong repulsive forces generated between the nanoparticles as confirmed by zeta potential (ζ) and dynamic light scattering (DLS) analysis. MMt particles were fully encapsulated by PLA as demonstrated by transmission electron microscopy (TEM) micrographs. Meanwhile the film formation process highlighted the importance of emulsifier's type and solubility in the polymer matrix, as no films were obtained when sodium oleate was used alone compared with continuous, homogeneous, and free‐standing films obtained when the combination Tween 80 (80 wt%)—sodium oleate (20 wt%) was used. Scanning electron microscopy (SEM) micrographs of the cross‐section's surfaces showed homogeneous dispersion of the MMt particles with no clusters or agglomerates formed. Thermal analyses using differential scanning calorimetry and thermogravimetric analysis (DSC‐TGA) showed an overall reduction in the glass transition temperature (Tg) and the thermal stability of neat PLA, whoever this reduction was recovered when MMt was added due to the confinement effect. Thickened PLA and PLA/MMt emulsions using 1 wt% xanthan gum showed a non‐Newtonian behavior and shear thinning flow with suitable viscosity values for paper coating applications.Highlights Development of stable PLA/organoclay nanocomposite aqueous dispersions. Steric and electrostatic mechanisms provided excellent stability. Full encapsulation of organoclay platelets in nanometric PLA particles. Formation of free‐standing films from PLA/organoclay emulsions. Thickened PLA/organoclay emulsions using Xanthan gum for paper coatings.

Full colour luminescence tuning including white light from a mixed lanthanide activated metal-organic complex

In an attempt, metal–organic compounds of rare earth ions with 2,6-pyridinedicarboxylic acid (H2pydc) were synthesized and characterized. This paper summarizes the synthesis, characterization, and multicolour luminescence behaviour of a europium and terbium co-doped metal–organic compound (MOC) of formula [Y1.972Eu0.013Tb0.014(pydcH)6]·3H2O, 1 {H2pydc = 2,6-pyridinedicarboxylic acid}. The synthesis was performed by simple solvent evaporation method. We have also synthesized a pure yttrium based compound [Y2(pydcH)6]·3H2O, 1a following a similar procedure. The powder XRD patterns indicated that 1 and 1a were new materials; the patterns being entirely consistent with the simulated XRD pattern generated based on the structure of pure Eu compound determined using the single-crystal XRD. Compound 1 was well characterized by SEM, IR, TGA, EDX, and EDX elemental mapping analysis. Compound 1 showed different colour upon the variation of the excitation wavelength from 260 nm to 385 nm.

Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution.

Lutein is an oxygenated fat-soluble carotenoid and a functional compound with proven health benefits for the human body. Nevertheless, the poor water solubility and low oral bioavailability of lutein greatly limit its application. To address this, we developed an effective approach to enhance the water solubility of lutein through co-amorphous formulation. Specifically, the lutein-sucralose co-amorphous mixture was prepared at a molar ratio of 1:1 using ethanol and water as solvents by employing the solvent evaporation method, followed by solid-state characterization and dissolution testing conducted to assess the properties of the formulation. The X-ray diffraction pattern with an amorphous halo and the differential scanning calorimetry thermogram with no sharp melting peaks confirmed the formation of a binary co-amorphous system. Changes in peak shape, position, and intensity observed in the Fourier transform infrared spectroscopy spectrum revealed intermolecular interactions between lutein and sucralose molecules, while molecular dynamics simulations identified interaction sites between their hydroxyl groups. Additionally, dissolution testing demonstrated better dissolution performance of lutein in the co-amorphous form compared to pure lutein and physical mixture counterparts. Our findings present a novel strategy for improving the water solubility of lutein to make better use of it.

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Background: Aceclofenac (ACF) is a non-steroidal anti-inflammatory drug with potent anti-inflammatory and analgesic properties. ACF is belongs to BCS class II which has poor solubility in water (practically insoluble) and high permeability that leads to a low dissolution rate and reduced bioavailability. Objective: to enhance the solubility and dissolution rate of ACF using the solid dispersion method (SD) by two common techniques which were solvent evaporation (SE) and kneading (Kn) by using different carriers Mannitol, PVP k30, Soluplus®, and Urea in both techniques at 1:1 and 1:5 wight ratio. Methods: The effects of type of carrier and preparation method on solubility and dissolution rate of SD were studied. Solid dispersions were characterized for their, percentage yield, drug content, drug solubility and in-vitro dissolution rate in comparison with pure drug. Results: The best formula is obtained by the Kn formula (F16) which was formulated by the use of ACF: Soluplus®: with a weight ratio of 1:5 which gave a high percentage yield (99.5%), high drug content (99.8± 0.003%) and the best solubility enhancement which was 361 folds compared to pure ACF and faster dissolution rate which was 80% in 10 minutes compared to 20% for pure drug. Conclusion: the solubility and in-vitro dissolution rate of ACF was efficiently improved when prepared by SD techniques, utilizing both solvent evaporation and kneading methods. Furthermore, the kneading method was superior to solvent evaporation method due to the greater enhancement of solubility and dissolution rate obtained by all carriers and ratios with higher improvement by 1:5 ratio, and can be considered a successful and efficient strategy for solubility and in-vitro dissolution rate improvement of hydrophobic drugs.

Formulation and Evaluation of Tablets Using the Solvent Evaporation Method to Increase the Solubility of Lansoprazole

The inability to determine sufficient and repeatable bioavailability and/or desirable pharmacokinetic features in humans is one of the biggest obstacles to the oral administration of new medicines. The solubility and absorption of a medicine determine its bioavailability, which in turn determines its therapeutic efficacy. Achieving the target drug concentration in the systemic circulation and ensuring drug biological activity in humans are both affected by solubility. A stomach ulcer has the potential to rip through the stomach lining, the initial section of the small intestine, and possibly even the lower esophagus. Distinct ulcers form in different parts of the intestines; one forms in the duodenum and one in the stomach. Duodenal ulcers are most commonly characterized by upper abdominal pain at night that subsides after eating. Eating might exacerbate the discomfort from a stomach ulcer. Preparing and assessing the pills will yield optimal outcomes. The active component content is 99.90%, as is the active ingredient release rate. Compared to other formulations, solid dispersion tablets performed better in in-vitro tests (98.85%). The optimized formulation (lansoprazole solid dispersion tablets) outperformed the labeled formulation (conventional lansoprazole tablet) in terms of drug-releasing capacity within 6 hours, outperforming both formulations.

Enhanced anticancer activity of (–)-epigallocatechin-3-gallate (EGCG) encapsulated NPs toward colon cancer cell lines

(–)-Epigallocatechin-3-gallate (EGCG), a bioactive polyphenol of green tea, has chemo-preventive effects against various cancer cells. Nanoparticles (NPs) carrying different ligands are able to specifically interact with their receptors on different cancer cells that can provide effective release of cytotoxic drugs. In the present study, we have prepared EGCG entrapped NPs using PLGA (poly(d,l-lactide-co-glycolide)). Polyethylene glycol (PEG) and folic acid (FA) via double emulsion solvent evaporation (DESE) method obtained PLGA-EGCG (P-E), PLGA-PEG-EGCG (PP-E), and PLGA-PEG-FA-EGCG (PPF-E). Nanoformulations had been characterized with 1H NMR and FT-IR techniques, AFM, and DLS. PPF-E NPs showed an average size of 220 nm. Analysis of zeta potential confirmed the stability of NPs. HCT-116, HT-29, HCT-15, and HEK 293 cells were treated with both the prepared NPs and free EGCG (0–140 μM). Result showed PPF-E NPs had improved delivery, uptake and cell cytotoxicity toward human folic acid receptor-positive (FR+) colorectal cancer (CRC) cells as mainly on HCT-116 compared to HT-29, but not on the folic acid-negative cells (FR−) as HCT-15. PPF-E NPs enhanced intracellular reactive oxygen species (ROS) level in absence of N-acetyl-l-cysteine (NAC), elevated DNA fragmentation level, and increased apoptotic cell death at higher doses compared to other two NPs and free EGCG. In conclusion, PPF-E NPs exerted greater efficacy than PP-E, P-E, and free EGCG in HCT-116 cells.

Hydrophilically-modified poly(ε-caprolactone) with zwitterionic sulfobetaine/tertiary amine and their self-assemblies in water

To achieve hydrophilic modification of poly(ε-caprolactone) (PCL), a series of amphiphilic copolymers, poly(ε-caprolactone)-b-poly(N,N-dimethylaminoethyl methacrylate-co-sulfobetaine methacrylate) (PCDSs), were synthesized with varying sulfobetaine compositions using a three-step synthetic strategy. Firstly, the hydroxyl-terminated polymer, PDMAEMA-OH was synthesized through free radical polymerization using AIBN as an initiator and 2-mercaptoethanol as a chain transfer agent. Subsequently, the block copolymer poly(ε-caprolactone)-b- poly(N,N-dimethylamino ethylmethacrylate) (PCD) was prepared through ring-opening polymerization of PDMAEMA-OH and ε-caprolactone employing Sn(OCt)2 as the catalyst. Finally, zwitterionization of the tertiary amine groups in PCD was achieved by treating it with 1,3-propane sultone (1,3-PS) in THF to obtain the desired PCDSs copolymers. The chemical compositions and the structures of PCDSs were confirmed by 1H nuclear magnetic resonance (1H NMR) spectroscopy and gel permeation chromatography (GPC). Additionally, self-assembly behavior in water was systematically investigated for both PCD and PCDSs copolymers. The results showed that these copolymers could form stable, pH-responsive micelles with diameters less than 150 nm via solvent evaporation method while also exhibiting efficient loading and release capabilities for the anti-tumor drug doxorubicin (DOX). Furthermore, cytotoxicity assay revealed low cell cytotoxicity of PCDS micelles towards L929, HeLa, and MCF-7 cells; however DOX-loaded PCDS micelles (PCDS/DOX), particularly those composed of 47% sulfobetaine content exhibited significant inhibitory effects on HeLa and MCF-7 cells along with enhanced cellular uptake efficiency. These findings highlight that pH-responsive zwitterionic sulfobetaine-based polymeric micelles derived from the PCDSs hold great promise for effective DOX delivery.

Study of the Effect of Preparation and Formulation Factors on the Stability of Vitamin C Microencapsulated by Solvent-Evaporation Method

This research studied the effect of formulation and processing variables on the stability of vitamin C or Ascorbic Acid (AA) encapsulated in Eudragit RS100 microparticles prepared using a solvent evaporation technique. Microparticles ranged in size from 60 to 102 μm and encapsulation efficiencies between 25% and 44% were obtained. Microencapsulation significantly enhanced the stability of AA compared to the free AA in solution. AA shelf life was extended up to 23 days. Increasing AA concentration and using sucrose or Tween 80 in the outer phase further enhanced AA stability. The results suggest that microencapsulation method under the investigated conditions is a promising approach for protecting AA from degradation in aqueous solutions.

Phase Separation‐Induced Electrical Conductivity for Liquid Metal‐Embedded Plastic Hybrid Composites with Metallic Conductivity and Recyclability

AbstractConductive fillers‐embedded plastic polymer hybrid composites are crucial electronic materials in modern technologies owing to their tunable conductive properties, low density, and corrosion resistance. However, the application of traditional rigid inorganic conductive fillers‐embedded plastic composites is constrained by their subpar electrical conductivity and mechanical properties. Consequently, liquid metals (LMs) including gallium and gallium‐based alloys, have recently emerged as the preferred conductive flexible fillers over traditional rigid fillers. This work employs a solvent evaporation method and phase separation‐induced conductivity mechanism. The resulting flexible and electrically conductive LM‐polycarbonate (PC) film circuits demonstrate ultrahigh metallic conductivity, robust mechanical performance, excellent solvent recyclability, and notable processability. The fluidic nature of LMs and the superior mechanical properties of the PC polymer confer high electrical stability and durability to the LM‐PC film circuits under diverse mechanical forces and environmental conditions. The LM‐PC film circuits are exceedingly promising and apt for use as flexible conductors in contemporary electrical applications, including electricity transmission and underwater working.

Endogenous stem cell mobilization and localized immunosuppression synergistically ameliorate DSS-induced Colitis in mice

BackgroundStem cell therapy is a promising alternative for inflammatory diseases and tissue injury treatment. Exogenous delivery of mesenchymal stem cells is associated with instant blood-mediated inflammatory reactions, mechanical stress during administration, and replicative senescence or change in phenotype during long-term culture in vitro. In this study, we aimed to mobilize endogenous hematopoietic stem cells (HSCs) using AMD-3100 and provide local immune suppression using FK506, an immunosuppressive drug, for the treatment of inflammatory bowel diseases.MethodsReactive oxygen species (ROS)-responsive FK506-loaded thioketal microspheres were prepared by emulsification solvent-evaporation method. Thioketal vehicle based FK506 microspheres and AMD3100 were co-administered into male C57BL6/J mice with dextran sulfate sodium (DSS) induced colitis. The effect of FK506-loaded thioketal microspheres in colitis mice were evaluated using disease severity index, myeloperoxidase activity, histology, flow cytometry, and gene expression by qRT-PCR.ResultsThe delivery of AMD-3100 enhanced mobilization of HSCs from the bone marrow into the inflamed colon of mice. Furthermore, targeted oral delivery of FK506 in an inflamed colon inhibited the immune activation in the colon. In the DSS-induced colitis mouse model, the combination of AMD-3100 and FK506-loaded thioketal microspheres ameliorated the disease, decreased immune cell infiltration and activation, and improved body weight, colon length, and epithelial healing process.ConclusionThis study shows that the significant increase in the percentage of mobilized hematopoietic stem cells in the combination therapy of AMD and oral FK506 microspheres may contribute to a synergistic therapeutic effect. Thus, low-dose local delivery of FK506 combined with AMD3100 could be a promising alternative treatment for inflammatory bowel diseases.

Porous PLGA microparticles prepared with nanosized/micronized sugar particles as porogens

The objective of this study was to explore the use of nanosized/micronized sugar particles as porogens for preparing porous poly(lactide-co-glycolide) (PLGA) microparticles by a solid-in-oil-in-water (S/O/W) solvent evaporation method. Porous PLGA microparticles containing dexamethasone were prepared with different nanosized/micronized sugars (sucrose, trehalose and lactose), types of PLGA, and osmogens (NaCl or sucrose) in the external water phase. The microparticles were characterized for morphology, thermal properties, particle size, surface area, encapsulation efficiency and drug release/swelling during release. The addition of nanosized/micronized sugar particles resulted in porous PLGA microparticles with high encapsulation efficiencies. The porosity of the microparticles was caused both by the influx of water into the polymer droplets and the encapsulation and subsequent dissolution of sugar particles during the manufacturing process. The porosity (pore size) of the microparticles and, as a result, the drug release pattern could be well controlled by the particle size and weight fraction of the sugar particles. Because of a larger inner surface area, nanosized sugar particles were more efficient porogen than micronized sugar particles to obtain porous PLGA microparticles with flexible release patterns.

Mesothelin-Mediated Paclitaxel Phase-Shifted Nanodelivery System for Molecular Ultrasound Imaging and Targeted Therapy Potential in Ovarian Cancer

Background: Ovarian cancer presents a substantial risk to women's health and lives, with early detection and treatment proving challenging. Targeted nanodelivery systems are viewed as a promising approach to enhance the effectiveness of ovarian cancer treatment and ultrasonic imaging outcomes. Objective: A phase-shifted nanodelivery system (NPs) loaded with paclitaxel (PTX) and further conjugated with avidin (Ab) was studied, with the goal of investigating the effects of targeted nanodelivery strategies on the in vitro therapeutic efficacy and ultrasonic imaging of ovarian cancer. This study provides a foundation for future in vivo treatments utilizing this approach. Methods: PTX-NPs were prepared using the single water-in-oil (O/W) emulsion solvent evaporation method, with avidin coupling achieved through biotin-avidin affinity. The encapsulation efficiency and release profile of PTX were analyzed using UV spectrophotometry. The phase-shift properties of the Ab-PTX-NPs delivery system were evaluated, and the targeting efficiency, cytotoxicity against SKOV3 cells, and in vivo biosafety of various nanodelivery systems were assessed. Results: The prepared nanodelivery system showed a stable and uniform structure with a good particle size distribution and exhibited favorable release characteristics under ultrasound exposure. In vitro experiments revealed that the nanodelivery system displayed excellent targeting and cytotoxic effects against SKOV3 cells, indicating the potential of the Ab-PTX-NPs delivery system for targeted ovarian cancer therapy. In vivo safety studies demonstrated the high biosafety of the prepared nanodelivery system. Conclusion: A novel nanodelivery system was developed, and the experimental results obtained provide a solid experimental basis for further research on in vivo ultrasound molecular imaging technology, offering new insights into targeted ultrasound molecular imaging and the treatment of ovarian cancer.

Development of 225Ac-doped biocompatible nanoparticles for targeted alpha therapy

Targeted alpha therapy (TAT) relies on chemical affinity or active targeting using radioimmunoconjugates as strategies to deliver α-emitting radionuclides to cancerous tissue. These strategies can be affected by transmetalation of the parent radionuclide by competing ions in vivo and the bond-breaking recoil energy of decay daughters. The retention of α-emitting radionuclides and the dose delivered to cancer cells are influenced by these processes. Encapsulating α-emitting radionuclides within nanoparticles can help overcome many of these challenges. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles are a biodegradable and biocompatible delivery platform that has been used for drug delivery. In this study, PLGA nanoparticles are utilized for encapsulation and retention of actinium-225 ([225Ac]Ac3+). Encapsulation of [225Ac]Ac3+ within PLGA nanoparticles (Zave = 155.3 nm) was achieved by adapting a double-emulsion solvent evaporation method. The encapsulation efficiency was affected by both the solvent conditions and the chelation of [225Ac]Ac3+. Chelation of [225Ac]Ac3+ to a lipophilic 2,9-bis-lactam-1,10-phenanthroline ligand ([225Ac]AcBLPhen) significantly decreased its release (< 2%) and that of its decay daughters (< 50%) from PLGA nanoparticles. PLGA nanoparticles encapsulating [225Ac]AcBLPhen significantly increased the delivery of [225Ac]Ac3+ to murine (E0771) and human (MCF-7 and MDA-MB-231) breast cancer cells with a concomitant increase in cell death over free [225Ac]Ac3+ in solution. These results demonstrate that PLGA nanoparticles have potential as radionuclide delivery platforms for TAT to advance precision radiotherapy for cancer. In addition, this technology offers an alternative use for ligands with poor aqueous solubility, low stability, or low affinity, allowing them to be repurposed for TAT by encapsulation within PLGA nanoparticles.Graphical