• 제목/요약/키워드: Gastrointestinal stability

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Microbiome-Linked Crosstalk in the Gastrointestinal Exposome towards Host Health and Disease

  • Moon, Yuseok
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • 제19권4호
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    • pp.221-228
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    • 2016
  • The gastrointestinal exposome represents the integration of all xenobiotic components and host-derived endogenous components affecting the host health, disease progression and ultimately clinical outcomes during the lifespan. The human gut microbiome as a dynamic exposome of commensalism continuously interacts with other exogenous exposome as well as host sentineling components including the immune and neuroendocrine circuit. The composition and diversity of the microbiome are established on the basis of the luminal environment (physical, chemical and biological exposome) and host surveillance at each part of the gastrointestinal lining. Whereas the chemical exposome derived from nutrients and other xenobiotics can influence the dynamics of microbiome community (the stability, diversity, or resilience), the microbiomes reciprocally alter the bioavailability and activities of the chemical exposome in the mucosa. In particular, xenobiotic metabolites by the gut microbial enzymes can be either beneficial or detrimental to the host health although xenobiotics can alter the composition and diversity of the gut microbiome. The integration of the mucosal crosstalk in the exposome determines the fate of microbiome community and host response to the etiologic factors of disease. Therefore, the network between microbiome and other mucosal exposome would provide new insights into the clinical intervention against the mucosal or systemic disorders via regulation of the gut-associated immunological, metabolic, or neuroendocrine system.

파클리탁셀을 함유한 지질나노입자의 제조와 인공 소화액에서의 안정성 평가 (Preparation of Lipid Nanoparticles Containing Paclitaxel and their in vitro Gastrointestinal Stability)

  • 김은혜;이정은;임덕휘;정석현;성하수;박은석;신병철
    • Journal of Pharmaceutical Investigation
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    • 제38권2호
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    • pp.127-134
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    • 2008
  • Peroral administration is the most convenient one for the administration of pharmaceutically active compounds. Most of poorly water-soluble drugs administered via the oral route, however, remain poorly available due to their precipitation in the gastrointestinal (GI) tract and low permeability through intestinal mucosa. In this study, one of drug delivery carriers, lipid nanoparticles (LNPs) were designed in order to reduce side effects and improve solubility and stability in GI tract of the poorly water soluble drugs. However, plain LNPs are generally unstable in the GI tract and susceptible to the action of acids, bile salts and enzymes. Accordingly, the surface of LNPs was modified with polyethylene glycol (PEG) for the purpose of improving solubility and GI stability of paclitaxel (PTX) in vitro. PEG-modified LNPs containing PTX was prepared by spontaneous emulsification and solvent evaporation (SESE) method and characterized for mean particle diameter, entrapping efficiency, zeta potential value and in vitro GI stability. Mean particle diameter and zeta potential value of PEG-modified LNP containing PTX showed approximately 86.9 nm and -22.9 mV, respectively. PTX entrapping efficiency was about 70.5% determined by UV/VIS spectrophotometer. Futhermore, change of particle diameter of PTX-loaded PEG-LNPs in simulated GI fluids and bile fluid was evaluated as a criteria of GI stability. Particle diameter of PTX-loaded PEG-LNPs were preserved under 200 nm for 6 hrs in simulated GI fluids and bile fluid at $37^{\circ}C$ when DSPE-mPEG2000 was added to formulation of LNPs above 4 mole ratio. As a result, PEG-modified LNPs improved stability of plain LNPs that would aggregate in simulated GI fluids and bile solution. These results indicate that LNPs modified with biocompatible and nontoxic polymer such as PEG might be useful for enhancement of GI stability of poorly water-soluble drugs and they might affect PTX absorption affirmatively in gastrointestinal mucosa.

신문사 근로자들의 스트레스와 건강상태에 관한 연구 (A Study on the Stress and the Health Status of Newspaper Employees)

  • 김진희
    • 한국직업건강간호학회지
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    • 제10권1호
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    • pp.41-54
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    • 2001
  • This study was designed to assess the relationship between occupational stress and health status in a study group of 197 workers employed in four newspaper publishing companies, using a self-adminstrative questionnaire. The types of occupation of them were reporters(79), clerical workers(54), and engineers (64). The studies on workers' health have been focused mainly on the physical, chemical, and biological diseases in our country. Therefore, the study of mental health, especially of occupational stress, is to be carried out. I consider stress as a factor having an effect on the health status of the newspaper employees, who have been well known to have high stress due to time pressures. I expect that this research will be helpful not only for understanding of health status by occupation, but also for making clear the issues that have been raised continuously from the previous researches. The results of this study are as follows; 1. The mean values of stress by occupation were statistically significant; the reporters had the highest stress symptom scores, and the engineers had the lowest levels of stress. The mean values of stress symptoms were higher in the workers who had long working hours. 2. The health status by occupation showed significant differences in gastrointestinal systems and in depression. The clerical workers were healthier than the engineers in gastrointestinal systems, and the reporters were more depressed than the engineers in depression. 3. The health status by the general characteristics, there was a statistical significance as for a gender, marital status, and absenteeism in the gastrointestinal systems. The men, the married, and the workers who had not been absent were more healthy. Only absenteeism had an effect on the problems in optical-dermal systems and in oro-fecal systems. Gender, marital status, absenteeism, and working hours were related with health status : the men. the married, the workers who had not been absent, and the workers who had longer working hours were more healthy. In mental stability, gender had a significant effect : the men were more healthy than the women. In general condition, the men, the older, the married, and the workers who had not been absent were more healthy. 4. Stress level had an effect on the health status in the respiratory systems, optical-dermal systems, oro-fecal system, depression, mental stability, general condition, and health condition. The workers who perceived more stress had more problems in their health status. 5. In the results of the multiple regression analyses, age in the respiratory systems, absenteeism in the optical-dermal systems, occupation and absenteeism in the gastrointestinal systems and in the oro-fecal systems, gender in depression and in mental stability, gender, age, absenteeism, and working hours in the general condition, absenteeism in the health condition had an effect on the health status of the workers.

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Synthesis and In-vitro Evaluation of N4-Amino Acid Derivatives of Cytarabine for Improving the Oral Delivery of Cytarabine

  • Jin, Ming-Ji;Hong, Joon-Hee;Han, Hyo-Kyung
    • Journal of Pharmaceutical Investigation
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    • 제38권4호
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    • pp.255-259
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    • 2008
  • The present study aimed to investigate the in-vitro characteristics of N4-amino acid derivatives of cytarabine for the oral delivery of cytarabine. After the synthesis of L-Ile-cytarabine, L-Leu-cytarabine and L-Arg-cytarabine, the gastrointestinal stability of each prodrug was examined using artificial gastric juice and intestinal fluids. The cellular uptake characteristics of prodrugs were also examined in Caco-2 cells. While L-Ile-cytarabine and L-Leu-cytarabine appeared to be stable in all the tested biological media during 4-hr incubation, L-Arg-cytarabine was rapidly disappeared within 5 min. Accordingly, the cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine was significantly higher than that of its parent drug, cytarabine in Caco-2 cells but the cellular uptake of L-Arg-cytarabine was similar to that from its parent drug. The cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine appeared to be saturable as drug concentration increased from 0.4 to 4 mM. Collectively, L-Ile-cytarabine and L-Leu-cytarabine could be promising candidates to improve the oral absorption of cytarabine via a saturable transport pathway.

Characterization of Antimicrobial Substance Producing Lactococcus sp. HM58 Isolated from Gastrointestinal Track of Flounder

  • Jeong Hyun-Mi;Yum Do-Young;Lee Jung-Ki;Choi Mi-Young;Kim Jin-Man
    • Fisheries and Aquatic Sciences
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    • 제6권1호
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    • pp.27-33
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    • 2003
  • A lactic acid bacterium showing antimicrobial activity against fish pathogen was isolated from gastrointestinal tract of flounder for the purpose of use as an aquaculture probiotics. From the analysis of morphological and physiological characteristics, the isolated strain was named as Lactococcus sp. HM58. Antimicrobial substance (AMS) from Lactococcus sp. HM58 showed strong growth inhibitory activity against Streptococcus sp., which is a fish pathogenic bacterium. AMS was presumed a proteinaceous compound with stability in heat and wide pH range from 2 to 10. It was started to produce in exponential growth phase and was not produced any more in stationary phase. It showed comparatively broad antimicrobial spectrum against most of gram positive bacteria used for this study. About $84\%$ of Lactococcus sp. HM58 was able to survive in the artificial gastric juice though it was low to the extent in the artificial bile juice. In the sensitivity test for various antibiotics, this strain was highly sensitive for doxycycline, erythromycin, amoxicillin clavu1anic acid and ampicillin.

Microencapsulation of Live Probiotic Bacteria

  • Islam, Mohammad Ariful;Yun, Cheol-Heui;Choi, Yun-Jaie;Cho, Chong-Su
    • Journal of Microbiology and Biotechnology
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    • 제20권10호
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    • pp.1367-1377
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    • 2010
  • Scientific research regarding the use of live bacterial cells for therapeutic purposes has been rapidly growing over the years and has generated considerable interest to scientists and health professionals. Probiotics are defined as essential live microorganisms that, when administered in adequate amounts, confer a health benefit on the host. Owing to their considerable beneficial health effects, these microorganisms are increasingly incorporated into dairy products; however, many reports have demonstrated their poor survival and stability. Their survival in the gastrointestinal tract is also questionable. To overcome these problems, microencapsulation techniques are currently receiving considerable attention. This review describes the importance of live probiotic bacterial microencapsulation using an alginate microparticulate system and presents the potentiality of various coating polymers such as chitosan and polylysine for improving the stability of this microencapsulation.

Assessment of allergenicity of genetically modified foods (GMOs)

  • Lee, Jung-Hyun;Yoon, Won-Ki;Han, Sang-Bae;Yun, Si-On;Park, Sun-Hong;Lee, Hyun-Ju;Yoon, Pyung-Seop;Moon, Jae-Sun;Kim, Hyung-Chin;Kim, Hwan-Mook
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.267.1-267.1
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    • 2002
  • The potential allergenicity of the transgene products in genetically modified organisms (GMOs). has been an important issue. As a part of the risk assessment of GMOs. we investigated the physicochemical stability and the immunogenicity of food allergens to determine their allergenicity. We have systematically evaluated the stability of food allergens in the gastrointestinal tract by using simple models of gastric (Stimulated gastric fluid) and intestinal (Stimulated intestinal fluid) digestion. (omitted)

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사이클로스포린을 함유한 고형 지질미립구의 제조와 평가 (Preparation and Evaluation of Solid lipid Microspheres Containing Cyclosporine A)

  • 양수근;박준상;최영욱
    • 약학회지
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    • 제39권5호
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    • pp.487-494
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    • 1995
  • Solid lipid microspheres (SLMs) were prepared using various lipids and solidifying agents, in order to enhance the gastrointestinal absorption of Cyclosporine A (Cs A) which is a practically water-insoluble drug with low systemic bioavailability. Egg lecithin and HCO-60 (polyoxyethylated 60 mol, hydrogenated castor oil) were used as lipids. Stearic acid and stearyl alcohol were used as solidifying agents. Emulsion concentrates containing Cs A were prepared by mixing the melted lipid and solidifying agent with water, employing bile salts as a cosurfactant. SLMs were obtained by dispersing the warm emulsion concentrate in cold distilled water under mechanical stirring, followed by freeze drying. Physical characteristics of each SLM were investigated by particle size analysis, optical microscopy and scanning electron microscopy. Mean particle size of SLMs was in the range of 30 to 40.mu.m. The SLMs were in good appearance with spherical shape before freeze drying, but were deformed partially after freeze drying. Drug loading efficiencies of SLMs were observed as high as 80 to 90% in average. The systemic bioavailability of Cs A from different SLM formula was investigated in rats following oral administration. Cs A in whole blood was extracted and assayed by HPLC. SLMs revealed the higher bioavailabilities than the standard formula based on the marketed product. SLMs might have several advantages over standard formula for enhanced gastrointestinal absorption, controlled release properties, high loading capacity of the water-insoluble drug, and feasibility of solid dosage forms with better stability in storage.

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Anti-aging potential of fish collagen hydrolysates subjected to simulated gastrointestinal digestion and Caco-2 cell permeation

  • Je, Hyun Jeong;Han, Yoo Kyung;Lee, Hyeon Gyu;Bae, In Young
    • Journal of Applied Biological Chemistry
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    • 제62권1호
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    • pp.101-107
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    • 2019
  • The objectives of this study were to evaluate the anti-aging effects and investigate the effect of simulated gastrointestinal (GI) digestion on the anti-aging properties and intestinal permeation of the potential fish collagen hydrolysates (FCH). Therefore, procollagen synthesis, matrix metalloproteinase-1 (MMP-1) production, and Caco-2 cell permeability were analyzed before and after in vitro digestion for FCHs, low-molecular weight fractions (<1 kDa), and high molecular weight fractions (>1 kDa). After being subjected to GI digestion, the level of MMP-1 inhibition was maintained, although the procollagen production was significantly (>20%) lower with all samples. Also, the digested FCHs and their <1 kDa fraction yielded 9.1 and 13.8% increased peptide transport, respectively, compared to undigested samples. Based on the effective intestinal permeation and high digestive enzyme stability, the <1 kDa fraction of FCHs is a potential bioactive material suitable for anti-aging applications in the food and cosmetics industries.

Effects of Chitosan Coating for Liposomes as an Oral Carrier

  • Lee, Chang-Moon;Kim, Dong-Woon;Lee, Ki-Young
    • 대한의생명과학회지
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    • 제17권3호
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    • pp.211-216
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    • 2011
  • The chitosan-coated liposomes (chitosomes) were designed to improve the stability in the gastrointestinal (GI) tract and to enhance the efficacy for oral drug delivery of liposomes. The phosphatic acid (PA)-incorporated anionic liposomes were surface-coated with water soluble chitosan (WSC) by electro-ionic interaction. The shape of the chitosomes observed by transmission electron microscopy (TEM) was spherical in all the formulations and the coating layer by WSC could be founded through TEM images. The mean size and the zeta potential values of the chitosomes increased significantly with depending on the content of WSC added for coating the liposomes. The stability of the chitosomes in the GI tract was confirmed through the change of relative turbidity of the liposomal suspension. The plain liposomes (plasomes) suspension without adding WSC clearly showed the change of relatively turbidity in simulated gastric fluid (SGF), while the change degree of turbidity of the chitosomes in the SGF decreased as increasing of WSC content added for coating liposome. In the 5-CF release study from the plasomes and chitosomes, the plasomes released >90% of the initial 5-CF content at 4 h of release measurement. In contrast, the chitosomes released below 40% of initial content of 5-CF. In conclusion, these results indicate that the chitosomes can be used as a potential carrier for effective oral drug delivery.