• Title/Summary/Keyword: Membrane permeability

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Mechanism of Intestinal Transport of an Organic Cation, Tributylmethylammonium in Caco-2 Cell Monolayers

  • Hong Soon-Sun;Moon Sang-Cherl;Shim Chang-Koo
    • Archives of Pharmacal Research
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    • v.29 no.4
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    • pp.318-322
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    • 2006
  • Many quaternary ammonium salts are incompletely absorbed after their oral administration and may also be actively secreted into the intestine. However, the underlying mechanism(s) that control the transport of these cations across the intestinal epithelium is not well understood. In this study, the mechanism of absorption of quaternary ammonium salts was investigated using Caco-2 cell monolayers, a human colon carcinoma cell line. Tributylmethylammonium (TBuMA) was used as a model quaternary ammonium salts. When TBuMA was administrated at a dose of 13.3 imole/kg via iv and oral routes, the AUC values were $783.7{\pm}43.6\;and\;249.1{\pm}28.0{\mu}mole\;min/L$ for iv and oral administration, indicating a lower oral bioavailability of TBuMA $(35.6\%)$. The apparent permeability across Caco-2 monolayers from the basal to the apical side was 1.3 times (p<0.05) greater than that from the apical to the basal side, indicating a net secretion of TBuMA in the intestine. This secretion appeared to be responsible for the low oral bioavailability of the compound, probably mediated by p-gp (p-glycoprotein) located in the apical membrane. In addition, the uptake of TBuMA by the apical membrane showed a $Na^+$ dependency. Thus, TBuMA appears to absorbed via a $Na^+$ dependent carrier and is then secreted via p-gp related carriers.

Study of Superparamagnetic Microneedles containing Iron Oxide Nanoparticles (산화철 나노입자를 함유한 초상자성 마이크로니들에 관한 연구)

  • Lee, Seung-Jun
    • Applied Chemistry for Engineering
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    • v.32 no.5
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    • pp.556-561
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    • 2021
  • Recently, iron oxide nanoparticles have been used as the subject of many studies on drug delivery system (DDS) due to their excellent magnetic properties and biocompatibility in response to external magnetic fields. In this study, hyaluronic acid-superparamagnetic microneedles (HA-SMNs) and carboxy methyl cellulose-superparamagnetic microneedles (CMC-SMNs) containing superparamagnetic iron oxide nanoparticles (SIONs) were prepared with HA and CMC as a matrix materials of MNs (microneedles). Various properties of SMNs were then investigated with scanning electron microscopy (SEM), superconducting quantum interference device-vibrating sample magnetometer (SQUD-VSM), frequency mixing magnetic detection (FMMD), and polymer/bio membrane. The SQUID-VSM measurements showed superparamagnetism of HA-SMNs and CMC-SMNs containing SIONs. The FMMD results demonstrated that the signal intensity changed significantly as the concentration of SIONs increased. In addition, SMNs exhibited the average skin permeability intensities on the bio membrane for HA-SMNs and CMC-SMNs were 92.5 and 98.5%, respectively. These results suggested that SMNs could be utilized as deliver materials for a TDDS and MR molecular imaging.

Performance Analysis for Proposing Proper Construction Method for Joints of Polyurea Waterproofing Membrane Coating (폴리우레아 도막방수재의 이음부 적정 시공안 제안을 위한 성능 분석)

  • Lee, Jung-Hun;Kim, Byoungil
    • Journal of the Korea Institute of Building Construction
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    • v.24 no.1
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    • pp.77-86
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    • 2024
  • In this study, an evaluation was conducted for a total of 16 conditions to suggest an appropriate construction method for the construction joint of polyurea waterproofing membrane coating. It was analyzed that the longer the construction time difference, the higher the rate of water leaks through joints, and it was confirmed that water leaks could be prevented through primer construction. In addition, since the surface of polyurea exposed outdoors for a long period of time is deteriorated and weakened, it was analyzed that polishing the area increases surface damage and affects the formation of the interface. During maintenance construction, it would be desirable to apply a primer before construction, and it is believed that using the same urea-based material will ensure waterproofing stability.

Gas Separation Properties of Polyaniline/Polyimide Blend Membranes (Polyaniline/Polyimide 혼합막의 기체 분리 특성)

  • Lee, Ki-Seob;Kim, Jin-Hwan
    • Applied Chemistry for Engineering
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    • v.18 no.5
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    • pp.483-489
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    • 2007
  • Polyaniline (PANI)/Polyimide (PI) membranes were prepared and the effects of PANI contents and doping on the structural properties and gas separation properties were studied. The polyamic acid (PAA) solution was prepared by the polycondensation reaction of 4,4'-(hexafluoroisopropylidene) diphthalic anhydride (6FDA) and 4,4'-oxydianiline (ODA) in 1-methyl-2-pyrrolydinone (NMP) solvent. The PANI/PI blends were obtained by mixing PAA solution and PANI solution, and were doped with 1 M aqueous HCl solution for 24 h. The structural characterizations of the as-cast and doped membranes were examined by FT-IR, XRD, and TGA. The gas permeation experiments with $H_2$, $CO_2$, $O_2$, $N_2$, and $CH_4$ were carried out by variable pressure method at $30^{\circ}C$ and 5 atm. For all gases tested, the permeability coefficients of the blends decreased with increasing PANI content and the magnitude of permeability was in the order of $H_2$ > $CO_2$ > $O_2$ > $N_2$ > $CH_4$. The permeability for PANI/PI membranes decreased after the doping process while the permselectivity increased. For $H_2/CH_4$ separation, the doped PANI/PI (75/25) membrane has a permselectivity of 991.

Peritoneal Protein Loss in Nephrotic Syndrome on Peritoneal Dialysis (복막 투석 중인 신증후군 환자의 복막을 통한 단백 소실)

  • Ahn, Yo-Han;Jung, Eui-Seok;Lee, Se-Eun;Lee, Hyun-Gyung;Lee, So-Hee;Kang, Hee-Gyung;Ha, Il-Soo;Jung, Hae-Il;Choi, Yong
    • Childhood Kidney Diseases
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    • v.13 no.2
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    • pp.189-196
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    • 2009
  • Purpose : The pathophysiologic mechanism of nephrotic syndrome is not yet known clearly. At least in some cases, certain 'circulating factors' are thought to increase the glomerular protein permeability. Considering the systemic effect of the circulating factor on peritoneal membrane, we evaluated the loss of protein through peritoneal membrane in patients on peritoneal dialysis due to the end stage renal disease (ESRD) caused by steroid resistant nephrotic syndrome (SRNS). Methods : We retrospectively reviewed the medical records of 26 pediatric patients on peritoneal dialysis ensued during the period from 2001 to 2007 at our clinic. Twelve patients had SRNS, while 14 patients had ESRD caused by the congenital anomalies of urinary system. Results : While the other parameters including nPNA indicating the adequacy of protein intake were similar between the two groups, serum albumin was lower in SRNS patients than the non-SRNS patients ($3.7{\pm}0.3$ g/dL vs. $4.0{\pm}0.4$ g/dL, P=0.021). Peritoneal protein loss was higher in SRNS patients than in non-SRNS patients ($3,044.4{\pm}837.6\;mg/m^2$/day vs. $1,791.6{\pm}1,244.0\;mg/m^2$/day, P=0.007). The protein permeability of the peritoneal membrane measured by the ratio of total protein concentration in dialysate to plasma was twice as high in SRNS patients as the non-SRNS ($1.06{\pm}0.46%$ vs. $0.58{\pm}0.43%$, P=0.010). After 1 year, peritoneal protein loss increased in both patient groups, but to a significantly greater degree in non-SRNS patient (P=0.023). Conclusion : The results of our study support the notion that in nephrotic syndrome there are some 'circulating factors' with the systemic effect. Since the greater protein loss through peritoneal membrane in SRNS was confirmed in this study, more meticulous nutritional support and close monitoring on the nutrition are required in these patients.

Anti-angiogenic, Anti-inflammatory and Anti-nociceptive Activities of Vanillin in ICR Mice

  • Lim, Eun-Ju;Kang, Hyun-Jung;Jung, Hyun-Joo;Song, Yun-Seon;Lim, Chang-Jin;Park, Eun-Hee
    • Biomolecules & Therapeutics
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    • v.16 no.2
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    • pp.132-136
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    • 2008
  • The current study aimed to assess some novel pharmacological activities of vanillin. Vanillin inhibited the chick chorioallantoic membrane (CAM) angiogenesis. Vanillin had anti-inflammatory activity using the acetic acid-induced permeability model in mice. Anti-nociceptive activity of vanillin was shown using the acetic acid-induced writhing test in mice. Vanillin inhibited production of nitric oxide (NO) and induction of inducible nitric oxide synthase (iNOS) but not cyclooxygenase-2 (COX-2) in the lipopolysaccharide (LPS)-activated RAW264.7 macrophages. Vanillin decreased the level of iNOS mRNA in the LPS-activated macrophages. Taken together, these results suggest that vanillin can have anti-angiogenic, anti-inflammatory and anti-nociceptive activities in ICR Mice.

Studies on the Requirements of $Ca^{++}$ for Cell Division and $Ca^{++}$ Permeability of Plasma Membrane of Fast Dividing Mouse Embryo Cells. (세포분열이 왕성한 생쥐 배세포에서 세포분열에 대한 $Ca^{++}$의 요구와 세포막투과성에 대한 연구)

  • Bae, In-Ha;Park, Ji-Hye
    • Clinical and Experimental Reproductive Medicine
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    • v.14 no.2
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    • pp.93-100
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    • 1987
  • To determine the effect of calcium on the preimplantational development of mouse two-cell embryo, the various concentrations of calcium were added into the culture media and the rate of blastocyst formation was observed. Also, to examine the effect of trifluoperazine, an inhibitor of calmodulin which is involved in the several intracellular calcium functions, embryos were cultured for 48 hours at the various concentrations of this inhibitor. An additional 24 hour culture was done to examine the effect of this drug on the transformation from morula to blastocyst. The results are as following ; 1. About 1.71mM of extracellular calcium is adequate for blastocyst formation and the higher concentrations of calcium (3.43mM and 8.55mM) do not affect on the blastocyst formation and the degenerating rate. 2. Trifluoperazine $100{\mu}M$ presents the inhibitory effect on the blastocyst formation while $1{\mu}M$ and $10{\mu}M$ do not so. 3. After an additional 24 hour culture, there is transformation of morula to blastocyst and the degenerating rate of embryo is increased all together.

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Preliminary Imaging Analysis for Enhanced Intestinal Uptake of Non-soluble Polystyrene Microspheres in the Presence of Oleic Acid using Rat Intestine

  • Tran, Huyen Thi Thanh;Tran, Phuong Ha Lien;Tran, Thao Truong-Dinh;Lee, Kyung-Ho;Lee, Beom-Jin
    • Journal of Pharmaceutical Investigation
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    • v.39 no.3
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    • pp.155-159
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    • 2009
  • In vitro intestinal uptake of non-soluble polystyrene microspheres (NPMS) was visualized with and without oleic acid using a fluorescence microscopy. Fluorescent polystyrene latex microspheres with 1${\mu}$m larger size were used as models for nonspecifically absorbed nonbiodegradable particulates. The NPMS could not penetrate the enterocytes but a few NPMS could be penetrated via Peyer's patches. When the oleic acid was mixed with NPMS, the transporting efficiency of NPMS through enterocytes as well as Peyer's patches was significantly enhanced. The modification of the intestinal membrane permeability and surface feature of the NPMS in the presence of oleic acid might be a clue to the transport of NSPM although the detailed mechanism is still under investigation.

Self-Nanoemulsifying Drug Delivery System of Lutein: Physicochemical Properties and Effect on Bioavailability of Warfarin

  • Yoo, Juno;Baskaran, Rengarajan;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.21 no.2
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    • pp.173-179
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    • 2013
  • Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

Fabrication of Fluorinated Polymeric Membranes and Their Noble Gas Separation Properties (불소 표면 개질 고분자 분리막의 제조와 노블가스 분리특성)

  • Kim, Gi-Bum;Yoon, Kuk-Ro
    • Applied Chemistry for Engineering
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    • v.21 no.4
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    • pp.475-478
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    • 2010
  • Fluorinated polymeric membranes were prepared by direct surface modification of PDMS with fluorine gas ($50{\sim}2000\;{\mu}mol/mol$ in nitrogen). The formed fluorinated polymeric membranes were characterized by FT-IR spectroscopy, GC (Gas chromatography), atomic force microscopy, and scanning electron microscopy. Direct fluorination resulted in the change of permeability and selectivity of various gases (pure gases such as $CO_2$, $O_2$, $N_2$, $C_2H_4$, mixture of He, Ne, Kr, Xe) through PDMS membranes. Fluorination resulted in the maximum 50% increase of selectivity through PDMS membrane.