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用于调节肠道微生物群的口腔速崩片的功能与安全性概况及研发

Functional and Safety Profile of and Development of Oral Fast-Disintegrating Tablets for Gut Microbiota Modulation.

作者信息

Giordani Barbara, Monti Federica, Corazza Elisa, Gasperini Sofia, Parolin Carola, Abruzzo Angela, Foschi Claudio, Marangoni Antonella, Lenzi Monia, Luppi Barbara, Vitali Beatrice

机构信息

Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, 40127 Bologna, Italy.

Section of Microbiology, Department of Medical and Surgical Sciences, Alma Mater Studiorum, University of Bologna, 40127 Bologna, Italy.

出版信息

Pharmaceutics. 2025 Aug 1;17(8):1011. doi: 10.3390/pharmaceutics17081011.

Abstract

: Early gut colonization by bifidobacteria, occurring more favorably in vaginally born infants than in those delivered via C-section, is crucial for maintaining overall health. The study investigated the health-promoting properties of BC17 both as viable cells and as postbiotics (i.e., cell-free supernatant and heat-killed cells), with the purpose of developing oral formulations to support intestinal health. : The safety, effects on the adhesion of bifidobacteria and enteropathogens to intestinal cells, and anti-inflammatory properties of BC17 viable cells and postbiotics were evaluated. Fast-disintegrating tablets were formulated by freeze-drying cell-free supernatant in combination with heat-killed or viable cells alongside maltodextrins. : The formulations were shown to be non-genotoxic and compatible with intestinal cell lines (Caco-2 and HT-29). BC17 viable cells survived in co-culture with intestinal cells up to 48 h and exhibited moderate adhesion to the cell lines. Notably, both BC17 viable cells and postbiotics enhanced the adhesion of beneficial bifidobacteria to Caco-2 cells by up to 250%, while reducing enteropathogens adhesion by 40-70%. Moreover, they exerted significant anti-inflammatory effects, reducing nitric oxide production in macrophages by 40-50% and protecting intestinal cells from SDS-induced damage. The formulations allowed administration of at least 10 BC17 cells in infants and adults through easy and rapid dispersion in milk or water, or directly in the oral cavity without chewing, and preserved their functional properties for up to 3 months of storage. : BC17 viable cells and postbiotics, as well as fast-disintegrating tablets, showed promising functional and safety profiles. Although further in vivo validation is needed, this approach represents a compelling strategy for promoting gut health.

摘要

双歧杆菌早期在肠道内定殖,这在经阴道分娩的婴儿中比剖宫产出生的婴儿中更易发生,对维持整体健康至关重要。该研究调查了BC17作为活细胞和后生元(即无细胞上清液和热灭活细胞)的健康促进特性,目的是开发支持肠道健康的口服制剂。评估了BC17活细胞和后生元的安全性、对双歧杆菌和肠道病原体与肠道细胞粘附的影响以及抗炎特性。通过将无细胞上清液与热灭活或活细胞以及麦芽糊精冻干来制备速崩片。这些制剂被证明无基因毒性且与肠道细胞系(Caco-2和HT-29)兼容。BC17活细胞与肠道细胞共培养48小时仍能存活,并对细胞系表现出适度的粘附。值得注意的是,BC17活细胞和后生元都能使有益双歧杆菌对Caco-2细胞的粘附增加高达250%,同时使肠道病原体的粘附减少40-70%。此外,它们发挥了显著的抗炎作用,使巨噬细胞中一氧化氮的产生减少40-50%,并保护肠道细胞免受SDS诱导的损伤。这些制剂通过在牛奶或水中轻松快速分散,或直接在口腔中无需咀嚼,可使婴儿和成人摄入至少10个BC17细胞,并在储存长达3个月的时间内保持其功能特性。BC17活细胞和后生元以及速崩片显示出有前景的功能和安全性概况。尽管还需要进一步的体内验证,但这种方法代表了一种促进肠道健康的引人注目的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acbd/12389607/0dad66c87ce8/pharmaceutics-17-01011-g003.jpg

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