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Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease with a very poor prognosis. Its treatment is hindered by a lack of new therapeutic alternatives and the existence of the blood–brain barrier (BBB), which restricts the access of drugs commonly used in ALS, such as riluzole, to the brain. To overcome these limitations and increase brain targeting, riluzole-loaded nanostructured lipid carriers (NLC) were prepared and functionalized with lactoferrin (Lf), facilitating transport across the BBB by interacting with Lf receptors expressed in the brain endothelium. NLC were characterized with respect to their physicochemical properties (size, zeta potential, polydispersity index) as well as their stability, encapsulation efficiency, morphology, in vitro release profile, and biocompatibility. Moreover, crystallinity and melting behavior were assessed by DSC and PXRD. Nanoparticles exhibited initial mean diameters between 180 and 220 nm and a polydispersity index below 0.3, indicating a narrow size distribution. NLC remained stable over at least 3 months. Riluzole encapsulation efficiency was very high, around 94–98%. FTIR and protein quantification studies confirmed the conjugation of Lf on the surface of the nanocarriers, with TEM images showing that the functionalized NLC presented a smooth surface and uniform spherical shape. An MTT assay revealed that the nanocarriers developed in this study did not cause a substantial reduction in the viability of NSC-34 and hCMEC/D3 cells at a riluzole concentration up to 10 μM, being therefore biocompatible. The results suggest that Lf-functionalized NLC are a suitable and promising delivery system to target riluzole to the brain.

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

Chitosan/montmorillonite nanocomposite films were prepared by the solvent evaporation method to immobilize the drug ibuprofen (IBU) and delay its release in a medium that simulates the environment of the gastrointestinal tract. The effects of montmorillonite, at different mass proportions (10, 20, and 50%), on the morphological and physical properties of the films were studied. The samples were characterized by X-ray diffraction (XRD), Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), degree of swelling, drug encapsulation, and drug release efficiency. According to the XRD it was evidenced that the incorporation of montmorillonite to chitosan led to the formation of nanocomposites of ordered morphology. The infrared spectra confirmed the good interaction between montmorillonite and chitosan by the formation of nanocomposites. This fact, which favored the imprisonment of the IBU, reduced the diffusion coefficient in the studied systems. The micrographs comproved the formation of dense and uniform films. The controlled release profile, especially for the nanocomposite with 10% clay mass, showed a slow drug release rate. The incorporation of montmorillonite at different proportions produced different morphologies, with good encapsulation efficiency and an adequate profile for the controlled release of the drug.

Background: Development of antivenom or antidote requires the repetition of immunization of large animals, such as horses and goats, which ultimately releases the IgG immunoglobulin produced in the serum specimen. As snake venom involves a variety of proteins and enzymes getting administered into the animal, this process can inflict significant harm to the animal, therefore choosing carriers that can deliver the least amount of venom could be a safer option for animal immunization Objective: In this research, nanoliposomes were used to encapsulate venom as a protected cargo for immunization. We used two distinct liposomal formulations to entrap the venom: 1,2-distearoyl-sn-glycero-3-phosphocholine, 1,2-distearoyl-sn-glycero-3-phospho-(1′-rac-glycerol) associated with cholesterol in one formulation and dimethyldioctadecylamonium (Bromide salt) paired with cholesterol in the other. Method: Liposomal formulations prepared by solvent evaporation method and the venom was encapsulated in liposomes and evaluated for size and zeta potential. Meanwhile, encapsulation efficiency, venom release percentage, and phospholipase activity have all been analyzed. Results: The findings revealed that dimethyldioctadecylamonium (Bromide salt) combined with cholesterol had the highest encapsulation efficiency. In this formulation, the venom release rate had a steady-state profile. The lack of phospholipase activity in this formulation may be due to a bromide group in the liposomal structure that could be useful for immunization. Conclusion: Liposomal formulations, which do not have the active site of the snake venom enzymes, could be used for venom encapsulation.

In this work, the lactoferrin (LF) was glycosylated by dextran (molecular weight 10, 40, and 70 kDa, LF 10K, LF 40K, and LF 70K) via Maillard reaction as a stabilizer to establish zein/glycosylated LF nanoparticles and encapsulate 7,8-dihydroxyflavone (7,8-DHF). Three zein/glycosylated LF nanoparticles (79.27–87.24 nm) with low turbidity (<0.220) and polydispersity index (PDI) (<0.230) were successfully established by hydrophobic interactions and hydrogen bonding. Compared with zein/LF nanoparticles, zein/glycosylated LF nanoparticles further increased stability to ionic strength (0–500 mM NaCl) at low pH conditions. Zein/glycosylated LF nanoparticles had nanoscale spherical shape and glycosylated LF changed surface morphology of zein nanoparticles. Besides, encapsulated 7,8-DHF exhibited an amorphous state inside zein/glycosylated LF nanoparticles. Most importantly, zein/glycosylated LF nanoparticles had good water redispersibility, high encapsulation efficiency (above 98.50%), favorable storage stability, and bioaccessibility for 7,8-DHF, particularly LF 40K. Collectively, the above research provides a theoretical reference for the application of zein-based delivery systems.

Recently, researchers are involved in finding a cure for fibrotic disorders, which is an acute disease. Along with an ideal drug, a superlative carrier is required for developing a sustainable...

Research background. Gallic acid is a polyphenol presenting antioxidant and antitumor activities, however its use as a nutraceutical or drug is hindered by its low bioavailability. Zein is a natural protein found in corn and has been applied as nanoparticle for drug carrier. In this study, zein nanoparticles were obtained and stabilized with polyethylene glycol (PEG) as gallic acid carriers. Experimental approach. Nanoparticles were obtained by the liquid-liquid method and characterized in terms of mean size, polydispersity index, zeta potential, morphology, solid-state interactions, and encapsulation efficiency/drug loading. The stability of nanoparticles was evaluated in simulated gastrointestinal fluids and food simulants, and the antioxidant activity was determined by the scavenging of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. Results and conclusions. Zein nanoparticles containing gallic acid were obtained and stabilized only in the presence of PEG. The optimal conditions originated nanoparticles with mean size <200 nm, low polydispersity index (<0.25) and negative zeta potential (20 mV). The gallic acid encapsulation efficiency was about 40 %, drug loading about 5 %, and the compound was encapsulated in an amorphous state. FTIR did not identify chemical interactions after gallic acid nanoencapsulation. Zein nanoparticles were more susceptible to release the gallic acid in gastric than intestinal simulated medium, however more than 50 % of drug content was protected from premature release. In food simulants, the gallic acid release from nanoparticles was prolonged and sustained. Moreover, the nanoencapsulation did not reduce the antioxidant activity of gallic acid. Novelty and scientific contribution. The results show the importance of PEG on the formation and properties of zein nanoparticles obtained by the liquid-liquid dispersion method. This study indicates PEG-stabilized zein nanoparticles are potential carriers for gallic acid delivery by the oral route to take advantage of its antioxidant properties and be applied both in the pharmaceutical and food industry.

Abstract This study aimed to improve the anticancer activity of letrozole through a niosomal formulation. Optimized niosomal formulation of letrozole was achieved by response surface methodology (RSM). The niosomes were well-characterized by several methods. The anticancer activity and its mechanism were studied in MCF-7 and MDA-MB-231 breast cancer cells. The release of the drug from the niosomes was according to the Kors Meyer-Peppa kinetic model. The niosomes were stable with high encapsulation efficiency. Significant higher anticancer activity and more induction of apoptosis were obtained for niosomal letrozole. Results indicated that niosomes could be a promising drug carrier for delivery of letrozole to breast cancer cells.

The aim of this research was evaluated the effect of type and ratio of coating materials on characteristics of betacyanin extract microencapsulated by freeze drying. The combination was consisted of maltodextrin+gum arabic (MD+GA), maltodextrin+carboxymethyl cellulose (MD+CMC), maltodextrin+carrageenan (MD+C), and maltodextrin (MD) with ratio 3:1 and 4:1 (w/v) to the extract. Betacyanin microcapsules was analyzed for its characteristics, including encapsulation efficiency and microstructure. The result showed type and ratio of coating materials significantly influenced moisture content, color, and bulk density of the microcapsules (p<0,05). MD+GA coating material had the highest value of encapsulation efficiency (99.41 %). Microstructure analysis of the microcapsules showed it had amorphous shape. Betacyanin microcapsules from red dragon peel was potential to be natural food colorant.