• Title/Summary/Keyword: Poly (/-lactic acid)

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Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery

  • Choi, Yeon-Soon;Joo, Jae-Ryang;Hong, Areum;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.867-872
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    • 2011
  • For the prolonged delivery and sustained release rates of low molecular weight drugs, poly(lactic-co-glycolic acid) (PLGA) microparticles containing the drug SKL-2020 have been investigated. On increasing polyvinyl alcohol (PVA) concentration (from 0.2% to 5%), the size of microparticles decreased (from $48.02{\mu}m$ to $10.63{\mu}m$) and more uniform size distribution was noticeable due to the powerful emulsifying ability of PVA. A higher drug loading (from 5% to 20%) caused a larger concentration gradient between 2 phases at the polymer precipitation step; this resulted in decreased encapsulation efficiency (from 34.19% to 25.67%) and a greater initial burst (from 61.71% to 70.05%). SKL-2020-loaded PLGA microparticles prepared with different fabrication conditions exhibited unique release patterns of SKL-2020. High PVA concentration and high drug loading led to an initial burst effect by rapid drug diffusion through the polymer matrix. Since PLGA microparticles enabled the slow release of SKL-2020 over 1 week in vitro and in vivo, more convenient and comfortable treatment could be facilitated with less frequent administration. It is feasible to design a release profile by mixing microparticles that were prepared with different fabrication conditions. By this method, the initial burst could be repressed properly and drug release rate could decrease.

Biocompatibility of two experimental scaffolds for regenerative endodontics

  • Leong, Dephne Jack Xin;Setzer, Frank C.;Trope, Martin;Karabucak, Bekir
    • Restorative Dentistry and Endodontics
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    • v.41 no.2
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    • pp.98-105
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    • 2016
  • Objectives: The biocompatibility of two experimental scaffolds for potential use in revascularization or pulp regeneration was evaluated. Materials and Methods: One resilient lyophilized collagen scaffold (COLL), releasing metronidazole and clindamycin, was compared to an experimental injectable poly(lactic-co-glycolic) acid scaffold (PLGA), releasing clindamycin. Human dental pulp stem cells (hDPSCs) were seeded at densities of $1.0{\times}10^4$, $2.5{\times}10^4$, and $5.0{\times}10^4$. The cells were investigated by light microscopy (cell morphology), MTT assay (cell proliferation) and a cytokine (IL-8) ELISA test (biocompatibility). Results: Under microscope, the morphology of cells coincubated for 7 days with the scaffolds appeared healthy with COLL. Cells in contact with PLGA showed signs of degeneration and apoptosis. MTT assay showed that at $5.0{\times}10^4$ hDPSCs, COLL demonstrated significantly higher cell proliferation rates than cells in media only (control, p < 0.01) or cells co-incubated with PLGA (p < 0.01). In ELISA test, no significant differences were observed between cells with media only and COLL at 1, 3, and 6 days. Cells incubated with PLGA expressed significantly higher IL-8 than the control at all time points (p < 0.01) and compared to COLL after 1 and 3 days (p < 0.01). Conclusions: The COLL showed superior biocompatibility and thus may be suitable for endodontic regeneration purposes.

A Study on the Fabrication and Comparison of the Phantom for Computed Tomography Image Quality Measurements Using Three-Dimensions Printing Technology (삼차원 프린팅 기술을 이용한 전산화단층영상 품질 측정용 팬텀 제작 및 비교 연구)

  • Yoon, Myeong-Seong;Hong, Soon-Min;Heo, Yeong-Cheol;Han, Dong-Kyoon
    • Journal of radiological science and technology
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    • v.41 no.6
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    • pp.595-602
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    • 2018
  • Quality control (QC) of Computed Tomography (CT) devices is based on image quality measurement on AAPM CT phantom which is a standard phantom. Although it is possible to control the accuracy of the CT apparatus, it is expensive and has a disadvantage of low penetration rate. Therefore, in this study, we make image quality measurement phantom at low cost using FFF (Fused Filament Fabrication) type three-dimensional printer and try to analyze the usefulness, compare it with existing standard phantom. To print a phantom, We used three-dimensional printer of the FFF system and PLA (Poly Lactic Acid, density: $1.24g/cm^3$) filament, and the CT device of 64 MDCT (Aquilion CX, Toshiba, Japan). In addition, we printed a phantom using three-dimensional printer after design using various tool based on existing standard phantom. For image quality evaluation, AAPM CT phantom and self-generated phantom were measured 10 times for each block. The measured data were analyzed for significance using the Mannwhiteney U-test of SPSS (Version 22.0, SPSS, Chicago, IL, USA). As a result of the analysis, phantom fabricated with three-dimensional printer and standard phantom showed no significant difference (p>0.05). Furthermore, we confirmed that image quality measurement performance of a phantom using three-dimensional printer is similar to the existing standard phantom. In conclusion, we confirmed the possibility of low cost phantom fabrication using three dimensional printer.

Antiproliferative Effects of Free and Encapsulated Hypericum Perforatum L. Extract and Its Potential Interaction with Doxorubicin for Esophageal Squamous Cell Carcinoma

  • Amjadi, Issa;Mohajeri, Mohammad;Borisov, Andrei;Hosseini, Motahare-Sadat
    • Journal of Pharmacopuncture
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    • v.22 no.2
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    • pp.102-108
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    • 2019
  • Objectives: Esophageal squamous cell carcinoma (ESCC) is considered as a deadly medical condition that affects a growing number of people worldwide. Targeted therapy of ESCC has been suggested recently and required extensive research. With cyclin D1 as a therapeutic target, the present study aimed at evaluating the anticancer effects of doxorubicin (Dox) or Hypericum perforatum L. (HP) extract encapsulated in poly(lactic-co-glycolic acid) (PLGA) nanoparticles on the ESCC cell line KYSE30. Methods: Nanoparticles were prepared using double emulsion method. Cytotoxicity assay was carried out to measure the anti-proliferation activity of Dox-loaded (Dox NPs) and HP-loaded nanoparticles (HP NPs) against both cancer and normal cell lines. The mRNA gene expression of cyclin D1 was evaluated to validate the cytotoxicity studies at molecular level. Results: Free drugs and nanoparticles significantly inhibited KYSE30 cells by 55-73% and slightly affected normal cells up to 29%. The IC50 of Dox NPs and HP NPs was ~ 0.04-0.06 mg/mL and ~ 0.6-0.7 mg/mL, respectively. Significant decrease occurred in cyclin D1 expression by Dox NPs and HP NPs (P < 0.05). Exposure of KYSE-30 cells to combined treatments including both Dox and HP extract significantly increased the level of cyclin D1 expression as compared to those with individual treatments (P < 0.05). Conclusion: Dox NPs and HP NPs can successfully and specifically target ESCC cells through downregulation of cyclin D1. The simultaneous use of Dox and HP extract should be avoided for the treatment of ESCC.

Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells

  • Tran, Phuong;Nguyen, Thu Nhan;Lee, Yeseul;Tran, Phan Nhan;Park, Jeong-Sook
    • The Korean Journal of Physiology and Pharmacology
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    • v.25 no.5
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    • pp.479-488
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    • 2021
  • This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC50 values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

Induction of Peptide-specific CTL Activity and Inhibition of Tumor Growth Following Immunization with Nanoparticles Coated with Tumor Peptide-MHC-I Complexes

  • Sang-Hyun Kim;Ha-Eun Park;Seong-Un Jeong;Jun-Hyeok Moon;Young-Ran Lee;Jeong-Ki Kim;Hyunseok Kong;Chan-Su Park;Chong-Kil Lee
    • IMMUNE NETWORK
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    • v.21 no.6
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    • pp.44.1-44.15
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    • 2021
  • Tumor peptides associated with MHC class I molecules or their synthetic variants have attracted great attention for their potential use as vaccines to induce tumor-specific CTLs. However, the outcome of clinical trials of peptide-based tumor vaccines has been disappointing. There are various reasons for this lack of success, such as difficulties in delivering the peptides specifically to professional Ag-presenting cells, short peptide half-life in vivo, and limited peptide immunogenicity. We report here a novel peptide vaccination strategy that efficiently induces peptide-specific CTLs. Nanoparticles (NPs) were fabricated from a biodegradable polymer, poly(D,L-lactic-co-glycolic acid), attached to H-2Kb molecules, and then the natural peptide epitopes associated with the H-2Kb molecules were exchanged with a model tumor peptide, SIINFEKL (OVA257-268). These NPs were efficiently phagocytosed by immature dendritic cells (DCs), inducing DC maturation and activation. In addition, the DCs that phagocytosed SIINFEKL-pulsed NPs potently activated SIINFEKL-H2Kb complex-specific CD8+ T cells via cross-presentation of SIINFEKL. In vivo studies showed that intravenous administration of SIINFEKL-pulsed NPs effectively generated SIINFEKL-specific CD8+ T cells in both normal and tumor-bearing mice. Furthermore, intravenous administration of SIINFEKL-pulsed NPs into EG7.OVA tumor-bearing mice almost completely inhibited the tumor growth. These results demonstrate that vaccination with polymeric NPs coated with tumor peptide-MHC-I complexes is a novel strategy for efficient induction of tumor-specific CTLs.

A Study of Drug Content and Cell Cytotoxicity of Paclitaxel-eluting Stents Coated with Various Biopolymer (다양한 생체고분자로 코팅된 Paclitaxel Eluting Stent의 약물함량과 세포독성 연구)

  • Kim, Dong-Gon;Shin, Il-Gyun;Kim, Gi-Han;Kim, Seong-Hyeon;Lee, Ju-Ho;Ki, Byoyng-Yun;Nah, Jae-Woon;Suh, Tae-Suk;Kim, Sang-Ho
    • Progress in Medical Physics
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    • v.20 no.3
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    • pp.125-131
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    • 2009
  • In this study, the paclitaxel eluting stent (PES) was prepared by coating a biliary stent with paclitaxel using various biopolymer such as poly (vinyl acetate) (PVAc), poly (lactic-co-glycolic acid) (PLGA), Silicone rubber for restenosis prevention in gastrointestinal disease by a dip-coating method. Drug contents of PES were increased as surface area of stent, concentration and molecular weight of coating polymer increase. In $^1H-NMR$ specta, we know that drug did not change by confirming specific peaks of paclitaxel in PES. As shown in SEM image, PES prepared using various biopolymer is coated clearly and regularly except Silicone rubber coating polymer. In in vitro cell cytotoxicity test, bare stent showed low cytotoxic effect against CT-26 colon carcinoma cell line on 3 day. However, PES coated with PLGA 502H showed the highest cytotoxicity because PLGA 502H is biodegradable polymer and has less molecular weight than other coating polymer. These results suggest that PES coated various biopolymer can be prevented restenosis in gastrointestinal disease.

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Study on Characteristics of PLA/PBAT Composite Film with Various Chain Extenders (고분자 사슬연장제를 이용한 폴리유산 / 폴리부틸렌 아디페이트테레프탈레이트 복합필름의 제조 및 특성 분석)

  • Kim, Sun-jong;Cho, Hyun-seung;Lee, Jae-hwan;You, Myung-je;Um, Yoo-Jun;Park, Su-il
    • KOREAN JOURNAL OF PACKAGING SCIENCE & TECHNOLOGY
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    • v.23 no.2
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    • pp.61-66
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    • 2017
  • Poly lactic acid(PLA) and poly butylene adipate-co-terephthalate(PBAT) film was prepared using a twin extruder. PLA (25%) and PBAT (75%) were mixed with various ratio of chain extenders, such as $Joncryl^{(R)}$ and hexamethylene diisocyanate(HDI) to improve the mechanical and thermal properties of produced bio composite films. Tensile strengths of films were steadily increased with increasing ratio of chain extender. The tensile strength of control films was about 25 MPa, and the tensile strength of films with combined chain extenders was above 40 MPa. The films with $Joncryl^{(R)}$ resulted in improved tensile strength, while the film with HDI alone showed improved percent elongation at break. By adding chain extenders into PLA/PBAT resin, the cold crystallization temperature (Tcc) and decomposition temperature (Td) of the produced bio composite films increased. It revealed that the addition of two types of chain extenders was efficient way to get PLA/PBAT film with improved strength and elongation.

Application of PLA/PBAT Composite Films Containing Calcined Oyster Shell Powder for Antimicrobial Packaging (소성 처리된 굴 패각을 활용한 PLA/PBAT 복합필름의 항균 포장재 적용 연구)

  • Yena Oh;Kitae Park;Jongchul Seo
    • KOREAN JOURNAL OF PACKAGING SCIENCE & TECHNOLOGY
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    • v.29 no.2
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    • pp.79-86
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    • 2023
  • In this study, poly(lactic acid) (PLA) and Poly(butylene-adipate-co-terephthalate) (PBAT) composite films containing calcined oyster shell powder (OSP) were evaluated for the applicability of antimicrobial packaging. PLA/PBAT-OSP composite films were prepared using twin-screw extruder. The OSP composite was incorporated into PLA/PBAT blend with different ratios (0, 1, 3, 5 and 10%) and the effect of OSP in the PLA/PBAT matrix was evaluated. The PLA/PBAT-OSP composite films were evaluated for properties using FT-IR, SEM, TGA, DSC, UTM, UV-vis, and Contact angle, as well as antimicrobial property was examined according to ISO 22196 - Antimicrobial Plastic Test. As OSP was added, it showed high antimicrobial activities for both Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. On the other hand, it was found that mechanical properties decreased as OSP was added. For the application of PLA/PBAT-OSP composite films as an antimicrobial packaging material, it is necessary to improve the dispersibility of OSP in the PLA/PBAT composite films and their physical properties at the same time.

Angiogenic Responce to Transmyocardial Mechanical Reveascularization(TMMR) with Polymer Myocardial Stent (고분자 중합체 심근 스템트를 이용한 기계적 경심근 혈류재건술의 혈관생성 반응)

  • Choi, Ho;Lee, Cheol-Joo;Moon, Kwang-Deok;Kim, Young-Jin;Kang, Joon-Kyu;Hong, Jun-Wha;Jee, Kyung-Soo;Han, Man-Jung;Cho, Sang-Ho
    • Journal of Chest Surgery
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    • v.33 no.6
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    • pp.494-501
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    • 2000
  • Background: Transmyocardial laser revascularization(TMLR) for revascularizing ischemic myocardium in patients was originally based on the assumption that laser channels remain their patency much longer. But recent studies show that laser channels did not remain open and that TMLR could achieve treatment benefits without long-term channel patency. The angiongencesis is currently thought to be induced by non-specific inflammatory response to mechanical tissue injury. This study is to evaluate hypothesis that various transmyocaridal mechanical revascularization(TMMR) may induce the angiogenic responses similar to that seen with TMLR, and transmyocaridal polymer stent revascularization(TMSR), the polymer stent in the myocardial tissue is hydrolyzed in 2 weeks, may enhance the non-specific inflammatory reaction resulting angiogenesis. Furthermore, polymer myocaridal stent channels remain long-term patency. Material and Method: Eight domestic pigs underwent ligation of the proximal circumflex artery, and 2 weeks later they were randomized to undergo transmycardial acupunctural revascularization (TMPR, Group I) of the left lateral wall with 18-G needle(n=2), to undergo transmyocardial (TMDR, Group II) with industrial 2mm steel drill(n=2), to undergo transmyocardial polymer stent revascularization (TMSR, Group III) after drilling the infarcted myocardium(n=2), the stent is poly(lactic acid-co-glycolic acid), which is self-degradated in the myocardium, and to a control group the ischemic zone was unterated(n=2). All the pigs were sacrificed after 4 weeks TMMR. Sections from the ischemic zone were submitted for vascular endothelial growth factor (VEGF) ELISA and histology. Result: There were makedly increase in the VEGF immunoassay in the ischemic zone of the TMMR group compared to the ischemic zone of the control group(control: each 30.85 and 43.15pg/mg protein, TMPR: each 44.14 and 68.61 pg/mg protein, TMDR: each 65.92 and 78.65 pg/mg protein, TMSR: each 177.39 and 168.87 pg/mg protein). TMSR channels caused greatest VEGF expression than channels made by other group and the polymer stent channels remained vacuole after 4 weeks. Conclusion: Transmyocardial polymer stent revascularization promoted the most angiogenci response by the VEGF immunoassay, although our study did not show the statistical significancy. The channels remained but the flow patency was not verified. Transmyocardial polymer stent revascularization (TMSR) is desirable in future experimental trials and in view of the significant cost implications comparable to that of laser.

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