• 제목/요약/키워드: Polymeric micelle

검색결과 42건 처리시간 0.021초

Drug Release from Thermo-Responsive Self-assembled Polymeric Micelles Composed of Cholic Acid and Poly(N-isopropylacrylamide)

  • Kim, In-Sook;Jeong, Young-Il;Lee, Yun-Ho;Kim, Sung-Ho
    • Archives of Pharmacal Research
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    • 제23권4호
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    • pp.367-373
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    • 2000
  • Cholic acid, conjugated with amine-terminated poly(W-isopropylacrylamide) (abbreviated as CA/ATPNIPAAm), was synthesized by a N, N'-dicyclohexyl carbodiimide (DCC)-mediated coupling reaction. Self-assembled CA/ATPNIPAAm micelles were prepared by a diafiltration method in aqueous media. The CA/ATPNIPAAm micelles exhibited a lower critical solution temperature (LCST) at $31.5^{\circ}C$. Micelle sizes measured by photon correlation spectroscopy (PCS) were approximately 31.6 $\times$$\times$ 5.8 nm. The CA/ATPNIPAAm micelles were spherical and their thermal size transition was observed by transmission electron microscope (TEM). A fluorescence probe technique was used for determining the micelle formation behavior of CA/ATPNIPAAm in aqueous solutions using Pyrene as a hydrophobic Probe. The critical micelle concentration (CMC) was evaluated as $8.9{\times}0^{-2}$ g/L. A drug release study was performed using indomethacin (IN) as a hydrophobic model drug. The release kinetics of IN from the CA/ATPNIPAAm micelles revealed a thermo-sensitivity by the unique character of poly(N-isopropylacrylamide) i.e. the release rate was higher at $25^{\circ}C$ than at $37^{\circ}C$.

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고분자 분산제를 이용한 Core-shell 수성 감압점착제 (Waterborne Core-shell Pressure Sensitive Adhesive (PSA) Based on Polymeric Nano-dispersant)

  • 이진경;진인주
    • 접착 및 계면
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    • 제17권3호
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    • pp.89-95
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    • 2016
  • 유연한 식품포장필름에 사용되고 있는 드라이 라미네이션용 유성접착제를 대체하기 위해, 고분자 분산제를 사용하여 유화하는 방법으로 수성 감압점착제를 친환경적으로 설계하였다. 유화중합에서 널리 사용하는 저분자량의 계면활성제는 물성의 변수로 작용해 왔다. 본 연구에서는 먼저 용액중합으로 polymeric nano-dispersant (PND)를 제조하고, 이 PND 입자들의 분산제를 micelle seed로 이용하여 core-shell grafted acrylic 점착제를 합성하였다. 이때 입자의 바깥층(shell)과 입자내층(core)의 $T_g$를 달리하여 얇은 필름의 점착조건인 초기접착력과 유지력의 균형을 이루도록 설계하였다. 최적화된 시험군 합성 점착제의 물성을 국내외 제조사에서 개발된 연구시료들과 비교분석하여, 점착제로서의 물성을 검토하였다. 물성 비교 결과, 본 연구에서 설계 합성한 저분자량의 계면활성제를 대체 사용한 고분자 나노분산제 기반 core-shell 점착제가 연포장에 적합한 점착물성을 나타냄을 확인하였다.

고분자형 계면활성제가 마이셀 촉진 한외여과법에 의한 1-나프틸 아민의 제거에 미치는 영향 (Effect of Polymeric Surfactant on the Separation of 1-Naphthylamine by Micellar Enhanced Ultrafiltration Membranes)

  • Youngkook Choi;Soobok Lee;Minok Koo;Yutaka Ishigami;Toshio Kajiuchi
    • 멤브레인
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    • 제7권3호
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    • pp.131-135
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    • 1997
  • 신규 고분자형 계면활성제($\alpha$-allyl-$\omega$-methoxy polyoxyethylene and maleic anhydride block copolymer)를 사용하는 고분자형 마이셀 촉진 한외여과법을 제안하였다. 제거용질로서는 염료의 중간체이며 발암성 물질인 1-나프틸 아민을 사용하였다. 고분자형 마이셀의 촉진효과는 중공사형 폴리아크리로니트릴 막(분획 분자량 6,000, 표면적 0.017$m^2$)을 사용하여 조사하였다. 플럭스의 선형의존성은 0.6kg/${cm}^2$까지 유지되었고, 점차 압력증가에 따라 플럭스 증가율은 감소하였다. 고분자형 마이셀을 첨가하지 않은 상태에서의 제거율은 2mM의 용질에 대하여 0.19, 2 wt.%의 고분자를 첨가한 상태에서의 제거율은 0.96이었다 고분자형 마이셀 내부로의 가용화가 분리효율을 5배 촉진시킨 것을 확인하였다.

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Poly(benzyl-L-histidine)-b-Poly(ethylene glycol) Micelle Engineered for Tumor Acidic pH-Targeting, in vitro Evaluation

  • Lee, Eun-Seong;Youn, Yu-Seok
    • Bulletin of the Korean Chemical Society
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    • 제29권8호
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    • pp.1539-1544
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    • 2008
  • A polymeric micelle, based on the poly(benzyl-L-histidine)-b-poly(ethylene glycol) (polyBz-His-b-PEG) diblock copolymer, was designed as a tumor-specific targeting carrier. The micelles (particle size: 67-80 nm, critical micelle concentration (CMC); 2-3 $\mu$g/mL) were formed from the diafilteration method at pH 7.4, as a result of self-assembly of the polyBz-His block at the core and PEG block on the shell. Removing benzyl (Bz) group from polyBz-His block provided pH-sensitivity of the micellar core; the micelles were physically destabilized in the pH range of pH 7.4-5.5, depending on the content of the His group free from Bz group. The ionization of His group at a slightly acidic pH promoted the deformation of the interior core. These pHdependent physical changes of the micelles provide the mechanism for pH-triggering anticancer drug (e.g., doxorubicin: DOX) release from the micelle in response to the tumor’s extracellular pH range (pH 7.2-6.5).

Preparation of Polymeric Self-Assembly and Its Application to Biomaterials

  • Cho, Chong-Su;Park, In-Kyu;Nah, Jae-Woon;Toshihiro Akaike
    • Macromolecular Research
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    • 제11권1호
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    • pp.2-8
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    • 2003
  • The self-assembly of polymers can lead to supramolecular systems and is related to the their functions of material and life sciences. In this article, self-assembly of Langmuir-Blodgett (LB) films, polymer micelles, and polymeric nanoparticles, and their biomedical applications are described. LB surfaces with a well-ordered and layered structure adhered more cells including platelet, hepatocyte, and fibroblast than the cast surfaces with microphase-separated domains. Extensive morphologic changes were observed in LB surface-adhered cells compared to the cast films. Amphiphilic block copolymers, consisting of poly(${\gamma}$-benzyl L-glutamate) (PBLG) as the hydrophobic part and poly(ethylene oxide) (PEO) [or poly(N-isopropylacrylamide) (PNIPAAm)] as the hydrophilic one, can self-assemble in water to form nanoparticles presumed to be composed of the hydrophilic shell and hydrophobic core. The release characteristics of hydrophobic drugs from these polymeric nanoparticles were dependent on the drug loading contents and chain length of the hydrophobic part of the copolymers. Achiral hydrophobic merocyanine dyes (MDs) were self-assembled in copolymeric nanoparticles, which provided a chiral microenvironment as red-shifted aggregates, and the circular dichroism (CD) of MD was induced in the self-assembled copolymeric nanoparticles.

Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

  • Hong, Sun-Mi;Jeon, Sang-Ok;Seo, Jo-Eun;Chun, Kyeung-Hwa;Oh, Dong-Ho;Choi, Young Wook;Lee, Do Ik;Jeong, Seong Hoon;Kang, Jae Seon;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • 제35권11호
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    • pp.3188-3194
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    • 2014
  • Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

실리마린의 용출개선 및 흰쥐에서의 생체이용률 평가 (Improved Dissolution Characteristics of Silymarin and Their Bioavailability in Rats)

  • 김정훈;장선우;권종원;김원배;최영욱
    • Journal of Pharmaceutical Investigation
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    • 제33권1호
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    • pp.61-65
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    • 2003
  • Silybin is the main component of Cardus marianus extracts originated from Silybum marianum and has a hepato-protective effect. It is a water-insoluble compound and poorly absorbed from the gastrointestinal tract, resulting in very low oral bioavailability(BA). Polymeric mixed-micelle precursor formulation was made to enhance the dissolution rate of silybin, showing the results of pH-independent release profile with increased dissolution. Oral BA of different preparations in rats was evaluated, revealing that the new formulation showed increased BA more than 2-fold and 4-fold compared to the marketed product and Cardus marianus extracts itself, respectively.

Ultra pH-Sensitive Polymeric Nanosystems for Tumor Targeting and chemotherapy

  • Lee, Eun-Seong;Na, Kun;Bae, You-Han
    • 한국고분자학회:학술대회논문집
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    • 한국고분자학회 2006년도 IUPAC International Symposium on Advanced Polymers for Emerging Technologies
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    • pp.56-57
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    • 2006
  • The ultra pH-sensitive polymeric mixed micelles based on poly(L-histidine) chemistry and constructed from block copolymers containing polyHis, present four functionalities as decreasing pH: ligand exposure at pH 7.0, micelle destabilization below pH 6.8, enhanced DOX release and endosomal membrane disruption. The first functionality is expected to endow tumor pH specificity to nonspecific ligands and the rest ones may help to treat solid tumors that are hard-to-treat by conventional chemotherapy (resistant tumors). The concept was proven in vitro studies and in vivo model.

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Synthesis and Characterization of Poly(alkyl $\alpha$, L-glutamate-co-ethylene oxide)

  • Kim, Gunwoo;Kim, Jin-Yeol;Daewon Sohn;Lee, Youngil
    • Macromolecular Research
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    • 제10권1호
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    • pp.49-52
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    • 2002
  • Rod-coil amphiphilic block copolymers, PALG-PEOs, poly(alkyl $\alpha$, L-glutamate-co-ethylene oxide)s, were successfully synthesized in three steps: 1) esterification of L-glutamic acid, 2) synthesis of ${\gamma}$-alkyl L-gultamate N-carboxyanhydride, and 3) polymerization of NCA monomers. These molecules form polymeric micelles with the hydrophobic core and hydrophilic corona in aqueous solution, which were characterized by light scattering and static fluorescence measurement.