• Title/Summary/Keyword: drug carriers

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Solubilization of poorly water-soluble drugs using solid dispersions

  • Kim, Tae-Wan;Choi, Choon-Young;Cao, Qing-Ri;Lee, Beom-Jin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.412.2-413
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    • 2002
  • Purpose. To prepare polymer based physical mixtures or solid dispersions containing solubilizing compositions using a spray-dryer. Methods. Lovastatin.simvastatin.aceclofenac and cisapride were selected as poorly water-soluble drugs. Dextrin. poly(vinylalcohol). poly(vinylpyrrolidone)and polyethylene glycol were chosen as solubilizing carriers for solid dispersions. The solid dispersions containing solubilizing compositions without drug were prepared without using organic solvents or tedious changes of formulation compositions. (omitted)

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Synthesis and Characterization of Poly(ethylene glycol) Grafted Polysuccinimide (폴리(에틸렌 글리콜)이 결합된 Polysuccinimide의 합성과 특성)

  • Lim, Nak-Hyun;Lee, Ha-Young;Kim, Moon-Suk;Khang, Gil-Son;Lee, Hai-Bang;Cho, Sun-Hang
    • Polymer(Korea)
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    • v.29 no.1
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    • pp.36-40
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    • 2005
  • Poly(amino acid) derivatives have been widely investigated as a drug carrier in drug delivery system. Particularly,polysuccinimide (PSI) is one of the most promising drug carriers since it possesses suitable physicochemical characteristics for development of macromolecular prodrugs, due to biocompatibility and biodegradability. In this study, we deal with the synthesis of polyaspartamide having various functional groups such as methoxy-poly(ethylene glycol) (MPEG) via ring closing of PSI. PSI was synthesized by polyonensation polymerization of spartic acid. The variety of average molecular weight was confirmed with reacion time and catalyst content to observe the optimum condition of synthesis. MPEG, hydrophilic chain, was bonded to fabricate polymeric micell composed of hydrophilic and hydrophobic polymer. All materials were characterized by 1H-NMR, FT-IR and GPC. In addition, the formation of nanoparticle micelle as drug carrier were also examined. Micelle size was measured by ELS and AFM. The functionalized polysparamide formed nanoparticle micelle whose size ranged from 90 to 130 nm. In conclusion, we prepared polyaspartamide functionalized with PEG examined the possibility as drug carriers.

Preparation, Characterization and Cytotoxicity of Silibinin-Containing Nanoniosomes in T47D Human Breast Carcinoma Cells

  • Amiri, Boshra;Ebrahimi-Far, Meysam;Saffari, Zahra;Akbarzadeh, Azim;Soleimani, Esmaeil;Chiani, Mohsen
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.8
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    • pp.3835-3838
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    • 2016
  • Background: Breast cancer is one of the most frequent cancer types within female populations. Silibinin is a chemotherapeutic agent ative against cancer. Niosomes are biodegradable, biocompatible, safe and effective carriers for drug delivery. Objective:To prepare nanoniosomal silibinin and evaluate its cytotoxicity inthe T-47D breast cancer cell line. Materials and Methods: Niosomes were prepared by reverse phase evaporation of a mixture of span 20, silibinin, PEG-2000 and cholesterol in chloroform and methanol solvent (1:2 v/v). The solvent phase was evaporated using a rotary evaporator and the remaining gel phase was hydrated in phosphate buffer saline. Mean size, size distribution and zeta potential of niosomes were measured with a Zetasizer instrument and then nanoparticles underwent scanning electron microscopy. The drug releasing pattern was evaluated by dialysis and the cytotoxicity of nanoniosomes in T-47D cells was assessed by MTT assay. Results: Particle size, size variation and zeta potential of the niosomal nanoparticles were measured as $178.4{\pm}5.4nm$, $0.38{\pm}0.09$ and $-15.3{\pm}1.3mV$, respectively. The amount of encapsulated drug and the level of drug loading were determined $98.6{\pm}2.7%$ and $22.3{\pm}1.8%$, respectively; released drug was estimated about $18.6{\pm}2.5%$ after 37 hours. The cytotoxic effects of nanoniosome were significantly increased when compared with the free drug. Conclusions: This study finding suggests that silibinin nanoniosomes could serve as a new drug formulation for breast cancer therapy.

A novel hydrogel-dispersed composite membrane of poly(N-isopropylacrylamide) in gelatin matrix and its thermally actuated permeation of 4-acetamidophen

  • Chun, Suk-Won;Kim, Jong-Duk
    • Proceedings of the Membrane Society of Korea Conference
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    • 1995.04a
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    • pp.50-51
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    • 1995
  • The swelling behavior of hyddrogels has been interested in many applications of drug carriers. These gels show reversible swelling changes in response to pH, electric currcnt, and temperature. Among others, the temperature-responsive behavior of poly(N-isopropylacrylanxide) (p(NIPAAm)) was studied, because a lower critical solution temperature(LCST) is in the vicinity of 32$\circ$C, and remarkable temperature-response can be obtained. We propose a novel composite membrane, which is appropriate for transporting drug ingredients above the transition temperature. Our object was to design a high permeation system above the shrinking temperature of p(NIPAAm). The membrane was composed of a matrix polymer and thermosensitive p(NIPAAm) hydrogel. The flux pattern of 4-acctamidophen through membrane in response of temperature was opposite to that of p(NIPAAm) membrane.

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Characterization and Modification of Low Molecular Water-Soluble Chitosan for Pharmaceutical Application

  • Jang, Mi-Kyeong;Nah, Jae-Woon
    • Bulletin of the Korean Chemical Society
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    • v.24 no.9
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    • pp.1303-1307
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    • 2003
  • The low molecular water-soluble chitosan nanoparticles (LMWSC-NPs) were prepared, which was modified with hydrophilic and hydrophobic moieties to evaluate the potential for pharmaceutics application. The synthesis of LMWSC-NPs was identified by FT-IR and $^1H$-NMR spectra. Also, we measured the photon correlation spectroscopy (PCS), transmission electron microscope (TEM) and atomic force microscope (AFM) to investigate the characteristics and morphology of the LMWSC-NPs. At the PCS measurement, the more increase the number of substitutive group, the more decrease the positive charge of LMWSC-NP surface. From the results of TEM and AFM, spherical morphologies were observed, and their sizes were 30-150 nm. Resultantly, LMWSC-NPs prepared in this experiment will be expected as a suitable device for the drug targeting system.

Validation of G-protein beta-3 subunit gene C825T polymorphism as predictor of obesogenic epidemics in overweight/obese Korean children

  • Lee, Yunkyoung;Park, Seong-min;Lee, Myoungsook
    • Journal of Nutrition and Health
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    • v.49 no.4
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    • pp.223-232
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    • 2016
  • Purpose: We investigated the potential interaction between the G-protein beta-3 subunit gene (GNB3) C825T polymorphism, a risk factor for chronic disease in various ethnicities, and obesogenic environments in overweight/obese Korean children. Methods: The present study was conducted as a cross-sectional study using measures of anthropometry, blood pressure (BP), and fasting blood samples as well as 3-day food records. Subjects were recruited from seven elementary schools in an urban district in Seoul, South Korea, between 2007 and 2008. A total of 1,260 children aged 8-9 years were recruited in the study, including 633 boys (50.3%) and 627 girls (49.7%). Results: The allele frequencies of the GNB3 polymorphism were C allele = 49.7% and T allele = 50.3% in subjects. In general, boys with T allele had higher BMI, systolic BP (SBP), and triglycerides, although their energy intake was not significantly different from boys with C allele. In contrast to boys, girls with T allele had lower BMI but higher SBP and energy intake than those with C allele. The girls with T allele had a significantly lower BMI and waist circumference in both the normal weight group and obese group (OB). T allele carriers in both genders had significantly higher TC than C allele carriers in the OB group. At last, girls with T allele in OB appeared to have significantly lower HOMA-IR than those with C allele. Conclusion: Unlike higher risk for negative health outcomes by the GNB3 polymorphism in various ethnicities, GNB3 polymorphism did not influence obesogenic environments in overweight/obese Korean children.

Fabrication of Porous Silk Fibroin Microparticles by Electrohydrodynamic Spraying (전기분사법에 의한 다공성 실크 피브로인 미세입자의 제조)

  • Kim, Moo Kon;Lee, Ki Hoon
    • Polymer(Korea)
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    • v.38 no.1
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    • pp.98-102
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    • 2014
  • Nowadays, silk fibroin receives a lot of attention as novel natural biomaterials due to its excellent biocompatibility and biodegradability. Electrohydrodynamic spraying (EHDS) is one of the method for the preparation of micro or nanoparticles by applying high voltage to the polymer solution. In this research, we fabricated silk fibroin porous microparticles by electrohydrodynamic spraying. Poly(ethylene glycol) (PEG) was added to the fibroin solution to give pores to silk fibroin microparticles. By the addition of PEG, the microparticle size was decreased despite of the decrease in conductivity and the increase of viscosity of the spraying solution. It seems that the immiscibility of silk fibroin and PEG affected much more to the microparticle size than the conductivity and viscosity. Immersing the as-sprayed microparticles into the water removed the phase-separated PEG, and finally, porous silk fibroin microparticles were prepared. The porous silk fibroin microparticles are expected to be applied as drug carriers in drug delivery or cell carriers in tissue engineering.

Rosin Microparticles as Drug Carriers: Influence of Various Solvents on the Formation of Particles and Sustained-release of Indomethacin

  • Lee Chang Moon;Lim Seung;Kim Gwang Yun;Kim Do Man;Kim Dong Woon;Lee Hyun Chul;Lee Ki Young
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.6
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    • pp.476-481
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    • 2004
  • The aim of this study was to formulate a sustained release system for indomethacin (IND) with rosin gum obtained from a pine tree. Rosin microparticles were prepared by a disper­sion and dialysis method without the addition of surfactant. In order to investigate the influence of solvents on the formation of colloidal microparitcles, various solvents like ethanol, DMF, DMAc, and acetone were used. The rosin microparticles containing IND were characterized by X­ray differactometry (XRD) and differential scanning calorimetry (DSC). The morphologies of rosin microparticles observed by scanning electron microscopy (SEM) were spherical. The solvents used to dissolve rosin significantly affected the drug content and drug release rate of IND. The release behaviors of IND from the rosin microparticles were dependent on the drug content and size of the particles. Rosin micorparticles with a higher drug content and of a larger particle size had a slower drug release rate. Also, the IND release rate from the rosin microparticles could be regulated by the rosin content in the microparticles. From these results, rosin microparticles have the potential of being used as a sustained release system of IND.

Surface-attached Solid Dispersion

  • Park, Young-Joon;Oh, Dong-Hoon;Yan, Yi-Dong;Seo, Yoon-Gee;Lee, Sung-Neug;Choi, Han-Gon;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.97-102
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    • 2010
  • A novel surface-attached solid dispersion is designed to improve the solubility and oral bioavailability of poorly water-soluble drugs without crystalline change. Accordingly, it draws increasing interest because of excellent stability and no pollution for accomplishing enhanced solubility and bioavailability, which have recently been highlighted in connection with a number of higher value-added poorly water-soluble drugs. In addition, excellent stability can be attained when the poorly water-soluble drugs are not dissolved but dispersed in water and provide no crystallinity change. This solid dispersion is given by means of attaching the dissolved carriers such as hydrophilic polymer and surfactant to the surface of dispersed drug particles followed by changing the hydrophobic drug to hydrophilic form. The aim of the present review is to outline the preparation, physicochemical property and bioavailability of novel surface-attached solid dispersion with improved solubility and bioavailability of poorly water-soluble drugs without crystalline change.

Pectin Microspheres for Oral Colon Delivery: Preparation Using Spray Drying Method and In Vitro Release of Release of Indomethacin

  • Lee, Chang-Moon;Kim, Dong-Woon;Lee, Hyun-Chul;Lee, Ki-Young
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.3
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    • pp.191-195
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    • 2004
  • Drug delivery systems that are based on pectin have been studied for colon specific delivery using the specific activity of colon microflora. The aim of this study was to design a novel method of manufacturing pectin microspheres without oils and surfactants and to investigate the potential use of the pectin microspheres as an oral colon-specific drug carrier. The pectin microspheres were successfully formed using the spray drying method and crosslinking with calcium chloride. From the crosslinked pectin microspheres, indomethacin (IND) release was more suppressed than its release from non-crosslinked microspheres. In a low pH (pH 1.4) environment, the pectin microspheres released IND at an amount of about 18${\pm}$2% of the total loaded weight for 24 h while the release rate of IND was stimulated at neutral pH (pH 7.4). IND release from the pectin microspheres was increased by the addition of pectinase. The results clearly demonstrate that the pectin microspheres that were prepared by the spray drying and crosslinking methods are potential carriers for colon-specific drug deliveries.