• Title/Summary/Keyword: drug release system

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Skin Permeability of piroxicam Gel by Phonophoretic Transdermal Drug Delivery (음파영동 경피약물수송에 의한 Piroxicam Gel의 경피투과)

  • Choi Suk-Joo;Oh Myung-Hwa;Kim Tae-Youl
    • The Journal of Korean Physical Therapy
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    • v.14 no.4
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    • pp.147-162
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    • 2002
  • Transdermal permeation enhancer has been used to increased skin absorption. External control of drug release and skin absorption can also be achieved by iontophoresis or phonophoresis. However, because several problems with iontophoresis are that it has a risk to skin damage because of the change of pH and the increase of current density in applying it and that it can be applied only in the form of water solution, This study is to enhance drug permeation via skin following application of ultrasound. For this goal, in gel containing piroxicam, the degree of skin permeation in vitro and anti-inflammatory effect in in vivo were investigated. Permeation study using hairless mouse skin was performed at 37 $^{\circ}C$ using buffer saline as the receptor solution. The amount of piroxicam were quantified using a HPLC system consisting of solvent delivery system. Following adoption of ultrasound 1 MHZ, it showed relatively high permeation rate where it was compared with non treated by ultrasound. The influence of duty cycle having an effect on skin permeation rate was slight higher in the case of using pulsed mode. Skin permeation increase attended by intensity of ultrasound, the permeation of trice was accelerated at 2.0 W/$cm^{2}$ than 1.0 W/$cm^{2}$. The skin permeation of piroxicam was substantially influenced by ultrasound. Anti-inflammatory effects were determined using carrageenan-induced paw swelling method in SD rat. Paw swelling tests showed that pulsed phonophoresis group was more effective than control group and only gel application group. The conclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory effect in vivo.

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Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS) (자가미세유화를 통한 아토르바스타틴 칼슘의 난용성 개선)

  • Lee, Jun-Hee;Choi, Myoung-Kyu;Kim, Yun-Tae;Kim, Myoung-Jin;Oh, Jae-Min;Park, Jung-Soo;Mo, Jong-Hyun;Kim, Moon-Suk;Khang, Gil-Son;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.37 no.6
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    • pp.339-347
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    • 2007
  • SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

Preparation of Gemcitabine-Loaded PLLA/Gemcitabine-PLLA Microparticles Using Supercritical Fluid and Their Release Characteristics (초임계 유체를 이용한 젬시타빈 함유 PLLA/젬시타빈-PLLA 미립자의 제조 및 방출 특성)

  • Hong, Jin-Hee;Lim, Giobin;Ryu, Jong-Hoon
    • KSBB Journal
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    • v.29 no.6
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    • pp.405-413
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    • 2014
  • In this study, gemcitabine (Gem)-Poly(L-lactic acid) (PLLA) conjugates were synthesized through an amide linkage reaction. Then, the microparticles of Gem-PLLA/PLLA blends containing gemcitabine were prepared using a supercritical fluid process, called aerosol solvent extraction system (ASES). Gemcitabine-loaded Gem-PLLA/PLLA microparticles obtained from the ASES process showed a spherical shape. The amount of gemcitabine released after 30 day incubation in a phosphate buffer solution of pH 7.4 was about 90% of the total amount of gemcitabine present in the product.

Simvastatin loaded porous poly(lactide-co-glycolide)(PLGA) microspheres as delivery systems strategies for injuring tissue and invitro study

  • Bao, Trinh-Quang;Kim, Yang-Hee;Lee, Byong-Taek
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2009.11a
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    • pp.38.2-38.2
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    • 2009
  • Regeration of natural tissuesor to create biological substitutes for defective or lost tissues and organs through the use of cells. In addition to cells and their porous, drugs are required to promote tissue regeneration. Therefore, the present studies were prepared using simvastatim loaded porous poly(lactide-co-glycolide) (PLGA) by double emulsion solvent evaporation water-in-oil-in-water technique (W/O/W) as drug delivery system strategies for injuring tissue. The resulting microspheres were evaluated for morphology, particle size, encapsulation efficiency, degradation of PLGA microspheres in vitro drug release and in vitro cell viability. Scanning electronic microscopic (SEM) showed that the porosities of the particles was changed by experimental conditions and cultured cells were attached well on porous microspheres surface. The X-ray diffraction (XRD) and differential scanning calometry (DSC) analysis indicate thatsimvastatim was highly dipersed in the microsphere at amorphousstate.

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Targeting of Drugs Especially by Liposomes (담체(膽體)를 이용(利用)한 약물(藥物)의 표적조직집중기법(標的組織集中技法) -리포솜을 중심(中心)으로-)

  • Shim, Chang-Koo;Lee, Jun-Ho
    • Journal of Pharmaceutical Investigation
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    • v.13 no.4
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    • pp.153-172
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    • 1983
  • The use of carrier systems for the delivery of drugs to areas in the body in need of pharmacological intervention is now the subject of intense research in many laboratories. Because of its obvious advantages (e.g. protection of drugs from hostile environments, facilitated target penetration and avoidance of side effects), drug delivery is expected to ease the pressure and expense of new drug development by making better use of drugs in existence. Generally, carrier-mediated delivery has been envisaged either as direct transport of drugs to a biological target by a carrier that will associate with it selectively, or as release of drugs from a carrier circulating in the blood or immobilized in tissues, at rates compatible with optimal action. One system that has attracted considerable attention is the use of liposomes as carriers of pharmacologically active agents. 154 references were reviewed with special emphasis on the targeting of drugs by use of liposomes in this respect. Recent advances in the other carrier systems and in methods for the preparation of liposomes were also reviewed briefly.

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Facile and Rapid Glycosylation Monitoring of Therapeutic Antibodies Through Intact Protein Analysis

  • Oh, Myung Jin;Seo, Nari;Seo, JungA;Kim, Ga Hyeon;An, Hyun Joo
    • Mass Spectrometry Letters
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    • v.12 no.3
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    • pp.85-92
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    • 2021
  • The therapeutic antibody drug market has experienced explosive growth as mAbs become the main therapeutic modality for a variety of diseases. Characterization of glycosylation that directly affects the efficacy and safety of therapeutic monoclonal antibodies (mAbs) is critical for therapeutics development, bioprocess system optimization, lot release, and comparability evaluation. The LC/MS approach has been widely used to structurally characterize mAbs, and recently attempts have been made to obtain comprehensive information on the primary structure and post-translational modifications (PTMs) of mAbs through intact protein analysis. In this study, we performed state-of-the-art LC/MS based intact protein analysis to readily identify and characterize glycoforms of various mAbs. Different glycoforms of mAbs produced in different expression cell lines including CHO, SP2/0 and HEK cells were monitored and compared. In addition, the comparability of protein molecular weight, glycoform pattern, and relative abundances of glycoforms between the commercialized trastuzumab biosimilar and the original product was determined in detail using the given platform. Intact mAb analysis allowed us to gain insight into the overall mAb structure, including the complexity and diversity of glycosylation. Furthermore, our analytical platform with high reproducibility is expected to be widely used for biopharmaceutical characterization required at all stages of drug development and manufacturing.

Preparation and Characterization of Cellulose Nanocrystals Reinforced Poly (vinyl alcohol) Based Hydrogels for Drug Delivery System (약물 전달 시스템 적용을 위한 셀룰로오스 나노크리스탈(CNCs) 강화 Poly(vinyl alcohol) 기반 하이드로겔의 제조 및 특성)

  • CHO, Hyejung;YOO, Won-Jae;AHN, Jinsoo;CHUN, Sang-Jin;LEE, Sun-Young;GWON, Jaegyoung
    • Journal of the Korean Wood Science and Technology
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    • v.48 no.4
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    • pp.431-449
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    • 2020
  • Structural property of most hydrogels is soft, resulting in low mechanical performance that limits their usage in the biomedical applications. For overcoming the drawback, cellulose nanocrystals (CNCs) were adopted in this study. Effects of CNCs on characteristics and drug delivery performance of poly (vinyl alcohol) based hydrogels were explored. FT-IR results showed that the fabricated hydrogels had semi-IPN (semi-interpenetrating polymer network) by formation of acetal and aldehyde bridge. Water absorption and swelling ratio decreased with increasing CNCs content, and the hydrogels with CNCs showed better viscoelastic performance than the without CNCs. Also, CNCs mostly improved the ability of the hydrogel to absorb the drug and the sustainability of the drug release. These results demonstrated that incorporating CNCs into the hydrogel systems can be a good alternative to improve drug delivery performance and mechanical property of the hydrogels.

In Vitro Study of Transdermal Delivery System for Caffein in Slim Patch Type (Slim Patch Type을 이용한 카페인의 경피흡수에 관한 연구)

  • Kim, Jung-Soo;Kwon, Dong-Hwan;Lim, Do-Hyeong;Kim, Gu-Seo;Kang, Chin-Yang
    • Journal of Pharmaceutical Investigation
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    • v.36 no.2
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    • pp.97-102
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    • 2006
  • The aim of this study was to investigate the feasibility and optimize permeability of slim patch type as a transdermal delivery system of caffein. Slim patch type was formulated and tested in modified Franz diffusion cell across cellulose membrane and hairless mouse skin in pH 5.8 phosphate buffer solution (PBS). The effect of $Pharmsolv^{\circledR}$ and drug concentration on permeation at four model, 1,2% $Pharmsolv^{\circledR}$ with $0.12\;mg/cm^2$ caffein and 0.12, $1.2\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR}$ through hairless mouse skin was studied in vitro. The release of caffein from slim patch with various loading was fitted by the Higuchi's diffusion equation. The result showed that chemical $Pharmsolv^{\circledR}$ produced a large and significant increase of permeation. The effect of 2% $Pharmsolv^{\circledR}$ on permeation of caffein was greater about 10-fold greater than 1% $Pharmsolv^{\circledR}$ in first 60 minutes. The effect of drug concentration, however, was lower than that produced by chemical $Pharmsolv^{\circledR}$. Within the tested system, the most efficient combination for caffein slim patch type was $0.12\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR},$ although $1.2\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR}$ showed highest amounts permeation, because permeated percentages were significantly lower about $1/4{\sim}1/5$ times.

Preparation and Stability Evaluation of Docetaxel-Loaded Oral Liposome

  • Chon, Chong-Run;Kim, Hyun-Mi;Lee, Pung-Sok;Oh, Eui-Chaul;Lee, Ma-Se
    • Journal of Pharmaceutical Investigation
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    • v.40 no.2
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    • pp.85-90
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    • 2010
  • Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.

Application of Molecular Diagnostics Technology in the Development of a Companion Diagnostics for Malignant Solid Tumors (악성 고형암의 항암제 동반진단 기술에서 분자진단기술의 적용)

  • Kim, Jin-Hee
    • The Journal of the Korea Contents Association
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    • v.19 no.3
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    • pp.365-374
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    • 2019
  • Unlike benign tumors, malignant tumors are capable of metastasis, easy to relapse, poor survival, and low quality of life. In Korea, here is a tendency to treat the tumors collectively according to the General Principles of Cancer Chemotherapy(GPCC) of the Health Insurance Review & Assessment Service (HIRA). But recently, companion diagnostics(CDx) is recommended rather than unilateral medication because biomarker-based molecular diagnostics is possible to predict the drug response of patients before drug treatment. Not only domestic but also overseas Food and Drug Administratio (FDA) recommends the development of the CDx system at the stage of drug development to ensure the responsiveness and safety of medicines. In this study, I focused on the necessity of CDx development direction as well as CDx development status through literature review. Furthermore I also discussed CDx types according to the molecular diagnostic technology such as immunohistochemistry (IHC), polymerase chain reaction (PCR), in situ hybridization (ISH), and next-generation sequencing (NGS) not only in the approved CDx but also in the developing one by US FDA. And I suggested the technology issue of CDx development process such as a selection of molecular diagnostics at the time of release, a clear understanding of the CDx mechanism, and a convergence of drug with CDx development. The necessity of social insurance system also was proposed for CDx development.