Journal of microencapsulation最新文献

Leflunomide (LEF) is a well-known disease-modifying anti-rheumatic agent (DMARDs) that was approved in 1998 for rheumatoid arthritis (RA) management. It is enzymatically converted into active metabolite teriflunomide (TER) inside the body. LEF and TER possess several pharmacological effects in a variety of diseases including multiple sclerosis, cancer, viral infections and neurobehavioral brain disorders. Despite the aforementioned pharmacological effects exploring these effects in nanomedicine applications has been focused mainly on RA and cancer treatment. This review summarises the main pharmacological, and pharmacokinetic effects of LEF along with highlighting the applications of nanoencapsulation of LEF and its metabolite in different diseases.

Aim: This study was aimed at investigating the cytotoxic effect of a novel combination of doxorubicin (DOX) and nano-formulation of Santolina chamaecyparissus L. essential oil (SCEO-NANO) on hepatic (HepG2) and colon (HT29) cancer cell lines.

Methods: A nano-emulsion was prepared by high-pressure homogenisation, then analysed by zetasizer and Fourier transform infrared spectroscopy. HepG2 and HT29 cells were used in in vitro tests for apoptosis detection.

Results: Formulated droplet size increased in DOX@SCEO-NANO/DOX to 11.54 ± 0.02 with uniform distribution (PDI = 0.13 ± 0.01), when compared with SCEO-NANO (size: 8.91 ± 0.02 nm; PDI = 0.1 ± 0.02). In both cells, DOX@SCEO-NANO/DOX led to a considerable reduction in colony formation. Compared to DOX, apoprotein proteins were overexpressed in HepG2 cells, showing increases of 8.66-fold for caspase-3 and 4.24-fold for the Bax/Bcl-2 ratio. In HT29 cells, ROS-dependent necrosis and apoptosis were seen. Comparing DOX@SCEO-NANO/DOX versus DOX, greater levels of caspase-3 and the Bax/Bcl-2 ratio were observed.

Conclusion: The DOX@SCEO-NANO/DOX formulation showed potential for targeted eradication of colon adenocarcinoma and hepatocellular carcinoma cells.

The current study aimed to evaluate the pharmacokinetics and neuroprotective effect of well-characterised berberine-bovine serum albumin (BBR-BSA) nanoparticles. BBR-BSA nanoparticles were generated by desolvation method. Entrapment efficiency, loading capacity, particle size, polydispersity index, surface morphology, thermal stability, and in-vitro release were estimated. In-vitro pharmacokinetic and tissue distribution were conducted. Their neuroprotection was evaluated against lipopolysaccharides-induced neurodegeneration. BBR-BSA nanoparticles showed satisfactory particle size (202.60 ± 1.20 nm) and entrapment efficiency (57.00 ± 1.56%). Results confirmed the formation of spheroid-thermal stable nanoparticles with a sustained drug release over 48 h. Sublingual and intranasal routes had higher pharmacokinetic plasma profiles than other routes, with C_max values at 0.75 h (444 ± 77.79 and 259 ± 42.41 ng/mL, respectively). BBR and its metabolite distribution in the liver and kidney were higher than in plasma. Intranasal and sublingual treatment improves antioxidants, proinflammatory, amyloidogenic biomarkers, and brain architecture, protecting the brain. In conclusion, neuroinflammation and neurodegeneration may be prevented by intranasal and sublingual BBR-BSA nanoparticles.

Aim(s): This article explores the application of mesalazine-loaded nanoparticles (MLZ-NPs) encapsulated in Abelmoschus esculentus plant polysaccharide-based pellets (MLZ-NPs-Pellets) for ulcerative colitis.

Methods: MLZ-NPs were prepared and evaluated for diameter, PDI, and entrapment efficiency. In-vitro efficacy study was conducted on Caco-2 cells. MLZ-NPs were encapsulated in polysaccharides to form MLZ-NPs-Pellets and characterised for efficacy in animals and targeting efficiency in human volunteers.

Results: Optimised batch of MLZ-NPs were characterised for diameter, PDI, zeta potential and entrapment efficiency which was found to be 145.42 ± 6.75 nm, 0.214 ± 0.049, -31.63 mV and 77.65 ± 2.33(%w/w) respectively. ROS, superoxide and NF-kβ were well controlled in Caco-2 cells when treated with MLZ-NPs. In-vivo data revealed that some parameters (body weight, colon length, lipid peroxidase, and glutathione) recovered significantly in the DSS-induced mice model treated with oral MLZ-NPs-Pellets. Gamma scintigraphy revealed that the formulation can effectively target the colon within 600 min.

Conclusion: MLZ-NPs-Pellets can be effectively used for microbial-triggered colon targeting approach in treating ulcerative colitis.

This article provides a brief description of microcapsule self-healing technique and its potential use in concrete structures. Because concrete is readily available and reasonably priced, it is widely utilised in the building industry globally, despite its susceptibility to the formation of cracks. The longevity and security of concrete buildings are greatly impacted by the existence of cracks and other deterioration occurring during the course of their use. Through the encapsulation of healing material inside microcapsules, which shows rupture upon cracking in cement-based materials, the microcapsule exhibits promise in accomplishing self-healing and increasing durability and strength in the structures. The article first explains the basic ideas behind the science of microcapsule self-healing and then looks at different ways to prepare microcapsules. It also looks into how adding microcapsules affects the basic characteristics of the concrete building. A summary of the efficiency and self-healing mechanisms of microcapsules is also provided.

Aims: This study examines microencapsulation as a method to enhance the stability of natural compounds, which typically suffer from inherent instability under environmental conditions, aiming to extend their application in the pharmaceutical industry.

Methods: We explore and compare various microencapsulation techniques, including spray drying, freeze drying, and coacervation, with a focus on spray drying due to its noted advantages.

Results: The analysis reveals that microencapsulation, especially via spray drying, significantly improves natural compounds' stability, offering varied morphologies, sizes, and efficiencies in encapsulation. These advancements facilitate controlled release, taste modification, protection from degradation, and extended shelf life of pharmaceutical products.

Conclusion: Microencapsulation, particularly through spray drying, presents a viable solution to the instability of natural compounds, broadening their application in pharmaceuticals by enhancing protection and shelf life.

Aim: To construct a novel liposomal drug delivery system co-modified with SP94 and BR2 ligands, encapsulating both the bitter ginseng derivative B21 and doxorubicin (DOX), to achieve superior anti-tumour efficacy and reduced toxic side effects.

Methods: Liposomes were prepared using an organic phase reaction method, with B21 encapsulated in the lipid phase and DOX in the aqueous phase. The liposomes were further modified with SP94 and BR2 peptides. The characterisations, cytotoxicity, and in vitro targeting effects were assessed through various methods including ultraviolet spectrophotometry, high-performance liquid chromatography, nano-size analysis, ultrafiltration centrifugation, dialysis, transmission electron microscopy, flow cytometry, Methylthiazolyldiphenyl-tetrazolium bromide assay, confocal laser scanning microscopy, transwell assay, and tumorsphere assay.

Results: SP94/BR2-B21/DOX-LP liposomes were spherical with an average diameter of 120.87 ± 1.00 nm, a polydispersity index (PDI) of 0.223 ± 0.006, and a surface charge of -23.1 ± 1.27 mV. The encapsulation efficiencies for B21 and DOX were greater than 85% and 97% (mg/mg), respectively. The results indicated that SP94/BR2-B21/DOX-LP exhibited enhanced targeting and cytotoxicity compared to single-ligand modified and unmodified liposomes, with the combined encapsulation of B21 and DOX showing synergistic anti-hepatocarcinogenic effects.

Conclusion: SP94/BR2-B21/DOX-LP liposomes represent a promising targeted drug delivery system for hepatocellular carcinoma, offering improved membrane penetration, enhanced therapeutic efficacy, and reduced systemic toxicity.

Aim: To develop turmeric extract-loaded chitosan microparticles for treating gastrointestinal disorders.

Methods: The microparticles were prepared using a spray-drying process, optimised the characteristics by biomarker loading, and encapsulation efficiency, and assessed for bioactivities related to gastrointestinal diseases.

Results: The optimised microparticles were spherical, with a mean diameter of 2.11 ± 0.34 µm, a SPAN of 4.46 ± 0.68, a zeta potential of +37.6 ± 0.2 mV, loading of 15.7% w/w curcuminoids, 5.4% w/w ar-turmerone, and encapsulation efficiency of 63.26 ± 1.62% w/w curcuminoids and 43.75 ± 1.33% w/w ar-turmerone. Encapsulation of turmeric extract improved release at 6 h by 20 times and mucoadhesion by 3.6 times. The microparticles exhibited high acid-neutralising capacity (1.64 ± 0.34 mEq/g) and inhibited nitric oxide production about twice as effectively as the turmeric extract, while maintaining antioxidant and antibacterial activities.

Conclusion: Encapsulation of turmeric extract in chitosan microparticles effectively enhanced therapeutic potential for gastrointestinal disorders.

This study investigates the synergistic effects of alginate@montmorillonite (Alg@Mt) hybrid microcapsules for enhancing water purification, focusing on improving the encapsulation of hydrophobic contaminants. Alg@Mt microcapsules were prepared through ionotropic gelation. Characterisation was performed using SEM-EDX, FTIR, XRD, and TGA. Encapsulation efficiency (EE), loading capacity (LC), and release behaviour were also examined. Alg@Mt microcapsules effectively removed phenol and its chlorinated derivatives from water. Incorporating Na-Mt improved structural and thermal properties, EE, and LC. Increasing the clay content to 60% (w/w) raised the EE of phenol and its more hydrophobic derivative, 2,4,6-trichlorophenol, from 39.74 ± 3.1% (w/w) and 63.91 ± 2% (w/w) to 60.56 ± 1.6% (w/w) and 82.28 ± 2.3% (w/w), respectively, with more controlled release rates, following Fickian diffusion mechanism. EE increased with phenolic substances hydrophobicity, while LC and release rates were inversely related. This approach is promising for removing hydrophobic contaminants from water.