Search Results (32)

Background/Objectives: Enteric coating protects active pharmaceutical ingredients from gastric degradation, but conventional tablets may present swallowing difficulties in geriatric and pediatric patients. Hence, this study intended to develop pH-responsive multiparticulates, formulated into orally disintegrating tablets (ODTs), for targeted intestinal drug delivery in individuals with dysphagia. Methods: Multiparticulates were developed via sequential seal coating, drug layering, sub-coating, and enteric coating on inert cores using a fluidized bed coater (Pam Glatt, India; bottom spray). Selected enteric-coated batches were directly compressed into ODTs using microcrystalline cellulose (Avicel PH102) and mannitol (Pearlitol SD 160) as fillers, with Explotab^®, Ac-Di-Sol^®, or crospovidone M^® as superdisintegrants. Results: Multiparticulates exhibited mean diameters of 197.671–529.511 μm and span values of 0.603–0.838. Span value < 1, indicating a narrow size distribution. Electron microscopy confirmed the spherical morphology of Batches 7a and b. Enteric-coated batches (5b, 6, 7a, 7b) released ≤10% of the drug in 0.1 N HCl at 2 h. Optimized formulation ODT 7b released 7.904% of the drug under gastric conditions and 79.749% in phosphate buffer (pH 6.8) within 2.5 h, following first-order drug release kinetics. ODT 7b demonstrated hardness (2.538 ± 0.144 kg/cm²), wetting time (11.17 ± 1.051 s), friability (0.712%), and drug content (99.81 ± 1.01%) within acceptable limits. Conclusions: The pH-dependent multiparticulates provided sustained intestinal drug release and, when incorporated into ODTs, yielded a dosage form with a rapid wetting time and acceptable mechanical properties. This dosage form can offer a promising approach for improving compliance and therapeutic efficacy in patients with swallowing difficulties (dysphagia). Full article

Aeromonas hydrophila (A. hydrophila) is responsible for causing abdominal dropsy, swimming abnormalities, skin ulcerations, and pale gills in fish. Vaccination is an essential strategy for disease prevention in aquaculture. This study evaluated the efficacy of an oral vaccine against A. hydrophila in Ctenopharyngodon idella (C. idella). The vaccine was formulated as feed-based monovalent pellets, incorporating or spraying formalin-killed A. hydrophila on/into commercial feed with 30% crude protein. Mineral and fish oils were used as adjuvants at 10% of the feed. Prior to the trial, the experimental feed groups were subjected to quality and safety tests. Grass carp fingerlings (20 ± 5 g) were divided into seven groups (n = 20 per group): sprayed vaccinated feed with fish oil (SVFF), incorporated vaccinated feed with fish oil (IVFF), sprayed vaccinated feed with mineral oil (SVFM), incorporated vaccinated feed with mineral oil (IVFM), sprayed vaccinated feed (SVF), incorporated vaccinated feed (IVF), and a control group. Feed was provided at 3% of body weight for 60 days. Immunomodulation was investigated through lysozyme activity, antibody titers, and immunoglobulin M (IgM). The IVFF group showed significantly enhanced immunity and growth performance, with an 87% protection rate, 13% mortality, and the highest relative percentage survival (83%) following intraperitoneal A. hydrophila (6.8 × 10⁹ CFU/mL) challenge. Histological analysis indicated minimal pathological changes in the IVFF group compared to controls. Fish oil as an adjuvant enhanced immunity without adverse health effects. Overall, this study demonstrated that feed-based monovalent vaccines effectively improve immune responses and provide protection against A. hydrophila in C. idella. Full article

Honey bees and other pollinators are key to functioning natural and managed ecosystems. However, their health is threatened by many factors, including pesticides. Spraying fungicides during flowering of fruit trees is widespread even though it directly exposes pollinators to these fungicides. Here, we report a series of experiments designed to understand how the combination of propiconazole and carbendazim, marketed in China as Chunmanchun^®, affects honey bee health. With an acute oral toxicity of 23.8 μg a.i./bee over 24 h in the laboratory, we considered the acute mortality risk from normal Chunmanchun^® applications as relatively low. However, our comprehensive studies revealed other diverse effects: Chunmanchun^® reduced memory after classic conditioning by approximately 25% and altered the activity of protective enzymes and the composition of the honey bees’ gut microbiota. Specifically, the genus Lactobacillus was decreased by ~13%, and Bartonella and Snodgrassella were increased by ~10% and ~7.5%, respectively. The gut metabolome was also disrupted in diverse ways, possibly as a functional consequence of the microbiome changes. Thus, we demonstrated numerous sublethal effects of the combination of propiconazole and carbendazim, which adds to the growing evidence that agrochemicals and fungicides in particular can harm pollinator health in subtle ways that are not captured in simple mortality assays. Full article

Tannic acid (TA) possesses antioxidant, anticancer, and antibacterial properties. However, its pH sensitivity, protein cross-linking properties, and susceptibility to oxidation restrict its application. To address these challenges, W/O/W multiple emulsified TA microcapsules were developed using soybean protein isolate (SPI) as the natural wall material emulsifier through a two-step emulsification and spray drying process. The encapsulation efficiency of the obtained TA microcapsules was 87.6%, and TA’s thermal stability was significantly improved. TA microcapsules effectively reduced the acidity and irritability of TA, eliminated protein flocculation, and enhanced biocompatibility. Notably, the cell viability of the TA microcapsule (>94%) was significantly higher than free TA (65.6%). The storage stability test revealed that the microcapsules maintained structural integrity, with a retention rate of 96% after 10 days of storage. In vitro release studies of TA microcapsules demonstrated a sustained-release effect within 24 h. Simulated digestion studies further elucidated the protective effect of microcapsules on TA during gastric digestion. These multi-structured microcapsules based on SPI effectively address the limitations associated with TA utilization and enhance its potential for dual oral/transdermal administration in biomedical and cosmetic applications. Full article

Respiratory diseases have presented a remarkable challenge during modern history, contributing to important pandemics. The scientific community has focused its efforts on developing vaccines and blocking the transmission of viruses through the respiratory tract. In this study, we propose the use of stable silver nanoparticles (AgNPs) functionalized with tannic acid (TA) and sodium citrate (SC) as a nasal spray disinfectant (NSD). The non-ionic ethoxylated surfactant Tween 80 (T80) was added to enhance the wetting effect on nasal and oral tissues following spray application. We analyzed the physicochemical properties of the AgNPs and the NSD, including zeta potential, polarity, morphology, composition, particle size, and distribution. The results indicated spherical AgNPs ranging from 3 to 5 nm, stabilized by TA-SC. The addition of T80 resulted in particles with negative polarity, high stability, and improved coverage area. Furthermore, the colloidal stability was monitored over one year, showing no signs of degradation or precipitation. Interestingly, the interaction between the capped AgNP complex, the spike protein, and ACE2 was studied by molecular docking, indicating a strong and thermodynamically favorable complex interaction. These findings hold promise for the development of potential inhibitors, antagonist receptors, Ag-complex agonists (as observed here), and drug development for viral protection. Full article

Probiotics are an essential dietary supplement for intestinal flora balance, inhibition of pathogenic bacteria and immune regulation. However, probiotic inactivation during gastrointestinal transportation remains a big challenge for oral administration. Hence, oral delivery systems (ODSs) based on polysaccharides have been constructed to protect probiotics from harsh environments. Cellulose, chitosan, alginate and their derivates have been used to form a protective layer for probiotics. This review summarizes the superiority and application of polysaccharides in forming protective layers for probiotics. Meanwhile, ODS processes including extrusion, emulsion and spray drying are also summarized. The preparation technique mechanism, the microparticle formation process and especially the role polysaccharides serve in the preparation process are overviewed. Lastly, the need for cell viability retention during the dehydration and construction of core-shell ODS microparticles is emphasized in this review. Full article

The present study compared vacuum drum drying (VDD) and conventional spray drying (SD) for solidifying crystalline ABT-199 nanosuspensions into redispersible oral drug products. The aim was to optimize formulation compositions and process conditions to maintain nanoparticle size after tablet redispersion. The impact of drug load (22%, 33%, 44%) and type of drying protectant (mannitol, mannitol/trehalose mix (1:1), trehalose) on redispersibility and material powder properties were investigated. Moreover, compression analysis was performed assessing the influence of compaction pressure on primary nanocrystal redispersibility and tablet disintegration. Higher drug loads and lower drying protectant levels resulted in particle growth, confirming a drug load dependence on redispersibility behavior. Notably, all drying protectants showed similar protection properties at properly chosen drying process parameters (T_g-dependent), except when VDD was used for mannitol formulations. Differences between the applied drying processes were observed in terms of downstream processing and tabletability: mannitol-containing formulations solidified via VDD showed an improved processability compared to formulations with trehalose. In conclusion, VDD is a promising drying technique that offers advantageous downstream processability compared to SD and represents an attractive novel processing technology for the pharmaceutical industry. As demonstrated in the present study, VDD combines higher yields with a leaner manufacturing process flow. The improved bulk properties provide enhanced tabletability and enable direct compression. Full article

Alginate is a natural biopolymer widely studied for pharmaceutical applications due to its biocompatibility, low toxicity, and mild gelation abilities. This review summarizes recent advances in alginate-based encapsulation systems for targeted drug delivery. Alginate formulations like microparticles, nanoparticles, microgels, and composites fabricated by methods including ionic gelation, emulsification, spray drying, and freeze drying enable tailored drug loading, enhanced stability, and sustained release kinetics. Alginate microspheres prepared by spray drying or ionic gelation provide gastric protection and colon-targeted release of orally delivered drugs. Alginate nanoparticles exhibit enhanced cellular uptake and tumor-targeting capabilities through the enhanced permeation and retention effect. Crosslinked alginate microgels allow high drug loading and controlled release profiles. Composite alginate gels with cellulose, chitosan, or inorganic nanomaterials display improved mechanical properties, mucoadhesion, and tunable release kinetics. Alginate-based wound dressings containing antimicrobial nanoparticles promote healing of burns and chronic wounds through sustained topical delivery. Although alginate is well-established as a pharmaceutical excipient, more extensive in vivo testing is needed to assess clinical safety and efficacy of emerging formulations prior to human trials. Future opportunities include engineered systems combining stimuli-responsiveness, active targeting, and diagnostic capabilities. In summary, this review discusses recent advances in alginate encapsulation techniques for oral, transdermal, and intravenous delivery, with an emphasis on approaches enabling targeted and sustained drug release for enhanced therapeutic outcomes. Full article

Graft-versus-host disease (GvHD) is a common and severe complication following allogeneic hematopoietic stem cell transplantation (HSCT). Its prevention and treatment is a major challenge. Ferulic acid (FA) has anti-inflammatory and antioxidant properties that could be attractive in this setting. Our aim was to evaluate a bioactive ingredient derived from wheat bran (WB), selected for its high concentration of FA, in a murine model of GvHD. The ingredient was obtained via a bioprocess involving hydrolysis and spray-drying. GvHD was induced via HSCT between MHC-mismatched mouse strains. FA treatment was administered orally. Survival and disease scores (weight loss, hunching, activity, fur texture, and skin integrity, each scored between 0 and 2 depending on disease severity) were recorded daily, histological evaluation was performed at the end of the experiment, and serum inflammatory cytokines were analyzed on days 9 and 28. Treatment with FA did not protect GvHD mice from death, nor did it diminish GvHD scores. However, histological analysis showed that ulcers with large areas of inflammatory cells, vessels, and keratin were less common in skin samples from FA-treated mice. Areas of intense inflammatory response were also seen in fewer small intestine samples from treated mice. In addition, a slight decrease in INF-γ and TNF-α expression was observed in the serum of treated mice on day 28. The results showed some local effect of the ingredient intervention, but that the dose used may not be sufficient to control or reduce the inflammatory response at the systemic level in mice with GvHD. Higher dosages of FA may have an impact when evaluating the immunomodulatory capabilities of the hydrolyzed WB ingredient. Thus, further experiments and the use of technological strategies that enrich the ingredients in soluble ferulic acid to improve its efficacy in this setting are warranted. Full article

The degradation of anthraquinones extracted from aloe vera plants can be prevented by encapsulating them in casein micelles (CMs). The oral, gastric, and intestinal digestion behavior of spray-dried microcapsules of casein micelles loaded with aloe vera-extracted anthraquinone powder (CMAQP), freeze-dried powder (CMFDP), and whole-leaf aloe vera gel (CMWLAG) obtained through ultrasonication was investigated. The results found that CMAQP and CMFDP dissolved slowly and coagulated into large curds during gastric digestion, improving the retention of anthraquinones in the digestive tract. In contrast, CMWLAG structure was destroyed and increased amounts of anthraquinones were released during oral and gastric digestion phases, indicating increased amounts of surface anthraquinones instead of the encapsulation of anthraquinones in the interior of CMs. The strong hydrophobic interactions protected anthraquinones within the core of CM for CMAQP and delayed diffusion. However, during SIF digestion, both CMAQP and CMFDP released significant amounts of anthraquinones, although CMAQP showed a much more controlled release for both aloin and aloe-emodin over SIF digestion time. The release behavior of anthraquinones from CM microcapsules was a function of the type of anthraquinone that was used to encapsulate. The present study provides insight into the release behavior of loaded bioactive compounds using food-grade CMs as the wall material during in vitro digestion and highlights the importance of the type of bioactive component form that will be encapsulated. Full article

Actinidia arguta leaves have gained notoriety over the past years due to their rich bioactive composition with human pro-healthy effects, particularly in relation to antioxidants. Nevertheless, antioxidants are well known for their chemical instability, making it necessary to develop suitable delivery systems, such as microparticles, to provide protection and ensure a controlled release. The aim of this work was to produce polymeric particles of A. arguta leaves extract by spray-drying that may improve the oral mucositis condition. Microparticles were characterized by size, shape, antioxidant/antiradical activities, swelling capacity, moisture content, and effect on oral cells (TR146 and HSC-3) viability, with the aim to assess their potential application in this oral condition. The results attested the microparticles’ spherical morphology and production yields of 41.43% and 36.40%, respectively, for empty and A. arguta leaves extract microparticles. The A. arguta leaves extract microparticles obtained the highest phenolic content (19.29 mg GAE/g) and antioxidant/antiradical activities (FRAP = 81.72 µmol FSE/g; DPPH = 4.90 mg TE/g), being perceived as an increase in moisture content and swelling capacity. No differences were observed between empty and loaded microparticles through FTIR analysis. Furthermore, the exposure to HSC-3 and TR146 did not lead to a viability decrease, attesting their safety for oral administration. Overall, these results highlight the significant potential of A. arguta leaves extract microparticles for applications in the pharmaceutical and nutraceutical industries. Full article

The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) virus has been causing the COVID-19 pandemic since December 2019, with over 600 million infected persons worldwide and over six million deaths. We investigated the anti-viral effects of polyphenolic green tea ingredients and the synthetic resveratrol analogue 3,3′,4,4′,5,5′-hexahydroxy-trans-stilbene (HHS), a compound with antioxidant, antitumor and anti-HIV properties. In the TCID₅₀ assay, four out of nine green tea constituents showed minor to modest cell protective effects, whereas HHS demonstrated the highest reduction (1103-fold) of the TCID₅₀, indicating pronounced inhibition of virus replication. HHS was also a highly effective inhibitor of SARS-CoV-2 proliferation in VeroE6 cells with an IC₅₀ value of 31.1 µM. HSS also inhibited the binding of the receptor-binding domain (RBD) of the spike protein to the human angiotensin-converting enzyme 2 (ACE2) receptor (RBD-ACE2) binding with 29% at 100 µM and with 9.2% at 50 µM indicating that the SARS-CoV-2 inhibitory effect might at least in part be attributed to the inhibition of virus binding to ACE2. Based on the chemical similarity to other polyphenols, the oral bioavailability of HHS is likely also very low, resulting in blood levels far below the inhibitory concentration of EGCG against SARS-CoV-2 observed in vitro. However, administration of HHS topically as a nose or throat spray would increase concentrations several-fold above the minimal inhibitory concentration (MIC) in the mucosa and might reduce virus load when administered soon after infection. Due to these promising tissue culture results, further preclinical and clinical studies are warranted to develop HHS as an additional treatment option for SARS-CoV-2 infection to complement vaccines, which is and will be the main pillar to combat the COVID-19 pandemic. Full article

Streptococcosis and aeromonasis inflicted by Streptococcus iniae and Aeromonas hydrophila, respectively, have affected tilapia industries worldwide. In this study, we investigated antibody responses and explored the mechanisms of protection rendered by an oral bivalent vaccine in red tilapia following challenges with S. iniae and A. hydrophila. The results of specific IgM antibody response revealed that the IgM titers against S. iniae and A. hydrophila in the bivalent incorporated (BI) vaccine group were significantly higher (p < 0.05) than those in the bivalent spray (BS) vaccine fish and unvaccinated control fish throughout the experiment. Real-time qPCR results also showed that the gene expression of CD4, MHC-I, MHC-II, IgT, C-type lysozyme, IL-1β, TNF-α, and TGF-β remained significantly higher (p < 0.05) than that of the controls between 24 and 72 h post-infection (hpi) in both mucosal (hindgut) and systemic (spleen and head–kidney) organs of BI vaccinated fish. Furthermore, the highest relative expression of the TGF-β, C-type lysozyme, and IgT genes in the BI vaccinated group was observed in the challenged fish’s spleen (8.8-fold), head kidney (4.4-fold), and hindgut (19.7-fold) tissues, respectively. The present study suggests that the bivalent incorporated (BI) vaccine could effectively improve the immune function and activate both humoral and cell-mediated immunities in vaccinated red tilapia following the bacterial challenges. Full article