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Formulation and Evaluation of Chitosan/NaCl/Maltodextrin Microparticles as a Saltiness Enhancer: Study on the Optimization of Excipients for the Spray-Drying Process.

ABSTRACT: Spray-dried chitosan/NaCl/maltodextrin microparticles have the potential to be used to enhance saltiness; however, its notable hygroscopicity results in handling and storage problems, thus limiting its application. In the present study, we attempted to introduce maltodextrin, microcrystalline cellulose (MCC), and waxy starch (WS) as excipients into the spray drying formulation of microparticles to reduce the cohesiveness and caking behavior and improve the yield simultaneously by ameliorating the moisture absorption tendency. The prepared microparticles showed a spherical appearance and had particle sizes ranging from 6.29 to 7.64 μm, while the sizes of the NaCl crystals embedded in the microparticles were 0.36 to 1.24 μm. The crystalline reflections of WS and MCC were retained in the microparticles after the spray-drying process. The handling properties were assessed to be acceptable. The formulation with only maltodextrin as the excipient showed a high moisture absorption rate of 2.83 g/100 g·h and a caking strength of 3.27 kg. The addition of MCC and WS significantly reduced the hygroscopic rate and caking strength. The spray-dried products provided better saltiness perception than native NaCl; as such, they may be promising for seasoning dry food products to achieve sodium intake reduction in the food industry.

SUBMITTER: Wang ST

PROVIDER: S-EPMC8706731 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Intranasal delivery has gained prominence since 1990, when the olfactory mucosa was recognized as the window to the brain and the central nervous system (CNS); this has enabled the direct site specific targeting of neurological diseases for the first time. Intranasal delivery is a promising route because general limitations, such as the blood-brain barrier (BBB) are circumvented. In the treatment of multiple sclerosis (MS) or Alzheimer's disease, for example, future treatment prospects include specialized particles as delivery vehicles. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles are well known as promising delivery systems, especially in the area of nose-to-brain (N2B) delivery. Chitosan is also broadly known as a functional additive due to its ability to open tight junctions. In this study, we produced PLGA nanoparticles of different sizes and revealed for the first time their size-time-dependent uptake mechanism into the lamina propria of porcine olfactory mucosa. The intracellular uptake was observed for 80 and 175 nm within only 5 min after application to the epithelium. After 15 min, even 520 nm particles were detected, associated with nuclei. Especially the presence of only 520 nm particles in neuronal fibers is remarkable, implying transcellular and intracellular transport via the olfactory or the trigeminal nerve to the brain and the CNS. Additionally, we developed successfully specialized Nano-in-Micro particles (NiMPs) for the first time via spray drying, consisting of PLGA nanoparticles embedded into chitosan microparticles, characterized by high encapsulation efficiencies up to 51%, reproducible and uniform size distribution, as well as smooth surface. Application of NiMPs accelerated the uptake compared to purely applied PLGA nanoparticles. NiMPs were spread over the whole transverse section of the olfactory mucosa within 15 min. Faster uptake is attributed to additional paracellular transport, which was examined via tight-junction-opening. Furthermore, a separate chitosan penetration gradient of ∼150 µm caused by dissociation from PLGA nanoparticles was observed within 15 min in the lamina propria, which was demonstrated to be proportional to an immunoreactivity gradient of CD14. Due to the beneficial properties of the utilized chitosan-derivative, regarding molecular weight (150-300 kDa), degree of deacetylation (80%), and particle size (0.1-10 µm) we concluded that M2-macrophages herein initiated an anti-inflammatory reaction, which seems to already take place within 15 min following chitosan particle application. In conclusion, we demonstrated the possibility for PLGA nanoparticles, as well as for chitosan NiMPs, to take all three prominent intranasal delivery pathways to the brain and the CNS; namely transcellular, intracellular via neuronal cells, and paracellular transport.

Dataset Information

Formulation and Evaluation of Chitosan/NaCl/Maltodextrin Microparticles as a Saltiness Enhancer: Study on the Optimization of Excipients for the Spray-Drying Process.

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