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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
Editor in Chief :
Volume & Issues
Volume 40, Issue 6 - Dec 2010
Volume 40, Issue 5 - Oct 2010
Volume 40, Issue 4 - Aug 2010
Volume 40, Issue 3 - Jun 2010
Volume 40, Issue spc - May 2010
Volume 40, Issue 2 - Apr 2010
Volume 40, Issue 1 - Feb 2010
Selecting the target year
In vitro Nasal Cell Culture Systems for Drug Transport Studies
Cho, Hyun-Jong ; Termsarasab, Ubonvan ; Kim, Jung-Sun ; Kim, Dae-Duk ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 321~332
DOI : 10.4333/KPS.2010.40.6.321
Growing interest in the nasal route as a drug delivery system calls for a reliable in vitro model which is crucial for efficiently evaluating drug transport through the nasal cells. Various in vitro cell culture systems has thus been developed to displace the ex vivo excised nasal tissue and in vivo animal models. Due to species difference, results from animal studies are not sufficient for estimating the drug absorption kinetics in humans. However, the difficulty in obtaining reliable human tissue source limits the use of primary culture of human nasal epithelial cells. This shortage of human nasal tissue has therefore prompted studies on the "passage" culture of nasal epithelial cells. A serially passaged primary human nasal epithelial cell monolayer system developed by the air-liquid interface (ALI) culture is known to promote the differentiation of cilia and mucin gene and maintain high TEER values. Recent studies on the in vitro nasal cell culture systems for drug transport studies are reviewed in this article.
Preparation and Characterization of Genetically Engineered Mesenchymal Stem Cell Aggregates for Regenerative Medicine
Kim, Sun-Hwa ; Moon, Hyung-Ho ; Chung, Bong-Genn ; Choi, Dong-Hoon ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 333~337
DOI : 10.4333/KPS.2010.40.6.333
Combining cell- and gene-based therapy is a promising therapeutic strategy in regenerative medicine. The aim of this study was to develop genetically modified mesenchymal stem cell (MSC) aggregates using a poly(ethylene glycol) (PEG) hydrogel micro-well array technique. Stable PEG hydrogel micro-well arrays with diameters of 200 to
were fabricated and used to generate genetically engineered MSC aggregates. Rat bone marrow-derived MSCs were transfected with a green fluorescent protein (GFP) plasmid as a reporter gene, and aggregated by culturing in the PEG hydrogel micro-well arrays. The resultant cell aggregates had a mean diameter of less than
, and maintained the mesenchymal phenotype even after genetic modification and cell aggregation. Transplantation of MSC aggregates that are genetically modified to express therapeutic or cell-survival genes may be a potential therapeutic approach for regenerative medicine.
Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)
Cho, Young-Dae ; Park, Young-Joon ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 339~345
DOI : 10.4333/KPS.2010.40.6.339
Fenofibrate has been used for many years to lower cholesterol levels and its pharmacokinetic profile is well understood. However, due to its low solubility in water, it has low bioavailability after oral administration. In order to improve the dissolution rate, fenofibrate was formulated into a self-microemulsifying drug delivery systems (SMEDDS). We used pseudo-ternary phase diagrams to evaluate the area of microemulsification, and an in vitro dissolution test was used to investigate the dissolution rate of fenofibrate. The optimized formulation for in vitro dissolution assessment consisted of Lauroglycol FCC (60%), Solutol HS 15 (27%), and Transcutol-P (13%). The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was about 130 nm. The dissolution rate of fenofibrate from SMEDDS was significantly higher than that of the reference tablet. Our studies suggested that the fenofibrate containing SMEDDS composition can effectively increase the solubility and oral bioavailability of poorly water-soluble drugs.
Determination of Physicochemical Properties and Pharmacokinetic Profiles of Soybean Extracts
Jung, Hyun-Chan ; You, Sung-Kyun ; Kwon, Sun-Kyu ; Hwang, Ji-Sook ; Cho, Cheong-Weon ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 347~351
DOI : 10.4333/KPS.2010.40.6.347
Isoflavones have received much attention because of their health-related and clinical benefits such as estrogenic and anti-oxidative activities as well as triggering of natural killer cell activity. However, there are few publications reporting the pharmacokinetic profiles together with physicochemical properties of main isoflavones. Therefore, the pharmacokinetic parameters of main aglycones, daidzein, glycitein and genistein after oral administration of soybean extracts were investigated and the physicochemical properties of soybean extracts were characterized. It was observed that angle of repose was
and tap density, bulk density and porosity were 10.12, 4.3 and
and the mean
of daidzein, glycitein and genistein was
, respectively. Cell viability was 60% at a concentration of 10 mg/mL. Taken together, it was suggested that isoflavones were contained in the soybean products and had an antioxidant activity and this study would be the basis to control the quality of soybean products and study of the bioequivalence between soybean products in future.
Preparation and Characterization of Bovine Serum Albumin-loaded Cationic Liposomes: Effect of Hydration Phase
Park, Se-Jin ; Jeong, Ui-Hyeon ; Lee, Ji-Woo ; Park, Jeong-Sook ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 353~356
DOI : 10.4333/KPS.2010.40.6.353
Although liposomes have been applied as drug delivery systems in various fields, the usage was limited due to the low encapsulation efficiency compared to other carrier systems. Here, cationic liposomes were prepared by mixing 1,2-dioleoyl-3-trimethylammoniopropane (DOTAP) as a cationic lipid, 1,2-dioleoyl-sn-glycerol-phosphoethanolamine (DOPE) and cholesterol (CH), and the liposomes were hydrated by varying the aqueous phases such as phosphate-buffered saline (PBS), 5% dextrose, and 10% sucrose in order to improve the encapsulation efficiency of bovine serum albumin (BSA). The particle size and zeta potential were determined by dynamic light scattering method and in vitro release patterns were investigated by spectrophotometry. Particle size and zeta potential of liposomes were varied depending on the ratio of DOTAP/DOPE/CH in range of 270-350 nm and 0.8-9.7 mV, respectively. Moreover, the addition of polyethylene glycol (PEG) improved the encapsulation efficiency from 37% to 43% as well as reduced particle sizes of liposomes while the liposomes were hydrated in PBS. When the liposomes were hydrated with 10% sucrose, the encapsulation efficiency of BSA was higher than any other groups. Whereas PBS was used as hydration solution, lower encapsulation efficiency was obtained compared with other groups. More than 60% of BSA was released from the liposomes hydrated with 10% sucrose; thereafter another 20% of BSA was released. Therefore, release pattern of BSA from cationic liposomes was extended release in this study. From the results, cationic liposomes dispersed in 10% sucrose would be potential carrier with high encapsulation efficiency.
Complexation of Adiponectin-encoding Plasmid DNA with Rosiglitazone-loaded Cationic Liposomes
Davaa, Enkhzaya ; Jeong, Ui-Hyeon ; Shin, Baek-Ki ; Choi, Soon-Gil ; Myung, Chang-Seon ; Park, Jeong-Sook ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 357~362
DOI : 10.4333/KPS.2010.40.6.357
To enhance therapeutic effects of insulin-sensitizing adipokine, ADN gene and potent agonists, rosiglitazone for the
, cationic liposomes as non-viral vectors were formulated. The particle size and zeta potential of drug loaded and unloaded cationic liposomes were investigated. The complex formation between cationic liposomes and negatively charged plasmid DNA was confirmed and the protection from DNase was observed. In vitro transfection was investigated in HepG2, HeLa, and HEK293 cells by mRNA expression of ADN. Encapsulation efficacy of rosiglitazone-loaded liposomes was determined by UV detection. Particle sizes of cationic liposomes were in the range of 110-170 nm and those of rosiglitazone-loaded cationic liposomes were in the range of 130-180 nm, respectively. Gel retardation of complexes indicated that the complex was formed at weight ratios of cationic lipid to plasmid DNA higher than 20:1. Both complexes protected plasmid DNA from DNase either drug free or drug loading. Encapsulation efficiency of rosiglitazone-loaded emulsion was increased by drug dose. The mRNA expression levels of ADN were dose-dependently increased in cells transfected with plasmid DNA. Therefore, cationic liposomes could be potential co-delivery system for drug and gene.
Optimization of Experimental Conditions for In vitro P-glycoprotein Assay Using LLC-GA5 Cells
Ahn, A-Ra ; Oh, Ju-Hee ; Lee, Joo-Hyun ; Lee, Young-Joo ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 363~366
DOI : 10.4333/KPS.2010.40.6.363
Identification of compounds that function as P-glycoprotein (P-gp) substrates or inhibitors can facilitate the selection and optimization of new drug candidates. The purpose of this study is to optimize the experimental conditions for in vitro P-gp assay using LLC-GA5 cells, which is a well-known transformant cell line derived by transfecting LLC-PK1 with human MDR1. The amount of rhodamine123 transported by the LLC-GA5 and LLC-PK1 cells was evaluated under the following experimental conditions: 3 different types of transport media, colchicine pretreatment or nontreatment of the cells in the culture media, and with and without poly-L-lysine coating of the culture plates. The assay sensitivity was found to considerably differ depending on the diluents used in the transport media. P-gp-mediated transport in LLC-GA5 cells was most clearly characterized in the Hanks' balanced salt solution based transport media. The sensitivity of P-gp-mediated transport was not changed by colchicine pretreatment or poly-L-lysine coating of the culture plates.
Investigation of Degradation Mechanism of Rabeprazole with Solid State Pharmaceutical Excipients
Ren, Shan ; Tran, Thao Truong-Dinh ; Tran, Phuong Ha-Lien ; Rhee, Yun-Seok ; Lee, Beom-Jin ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 367~372
DOI : 10.4333/KPS.2010.40.6.367
Rabeprazole sodium (RPN) is known to be very unstable at acidic condition or some acidic pharmaceutical excipients such as acrylic acid polymer (carbomer 934) with carboxylic acids. Thus, degradation mechanism of binary blends of rabeprazole with pharmaceutical excipients in a solid state without using solvents at three different ratios (3:1, 1:1 and 1:3) was investigated using Fourier transform infrad (FTIR) spectroscopy. Alkalizer (MgO), neutral hydroxypropymethylcellulose (HPMC 4000) were also tested for comparison. The binary blends were stored under accelerated conditions (
/75% relative humidity) for two weeks. The concentration of thioether rabeprazole from the binary blends with acidic carbomer 934 increased as the rabeprazole concentration decreased. In addition, the degradation half-life of rabeprazole as well as the relative peak area ratios obtained from FTIR spectra of S=O stretching at
decreased consistently as the fraction of carbomer 934 increased due to its sensitivity between the basic benzimidazole nitrogen and carboxylic acid group of carbomer 934. The physical appearance also turned into strong brown color in the presence of carbomer 934. In contrast, there were no significant changes in the degradation kinetics of rabeprazole with MgO and HPMC 4000 in a solid state. This present study demonstrated that the solid-state compatibility test with the aid of HPLC chromatographic and FTIR spectral analyses could offer a valuable methodology to select suitable pharmaceutical excipients and to elucidate the degradation mechanism of RPN for drug formulations at the early formulation stages.
Enhanced Occlusiveness of Nanostructured Lipid Carrier (NLC)-based Carbogel as a Skin Moisturizing Vehicle
Choi, Woo-Sik ; Cho, Hye-In ; Lee, Hyun-Young ; Lee, Seo-Hyun ; Choi, Young-Wook ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 373~378
DOI : 10.4333/KPS.2010.40.6.373
In order to develop a topical preparation which has a high occlusive property with skin moisturization, nano-structured lipid carrier (NLC) systems along with solid lipid nanoparticle (SLN) were designed. Various NLC dispersions were successfully formulated with Compritol 888 ATO as a solid lipid, Labrafil M 1944 CS as an oil, and Tween 80 as a surfactant. The increase of oil content (5 to 50%) led to the decrease in the occlusion factor in the order of SLN > NLC-5 > NLC-15 = NLC-30 > NLC-50. Particle size of lipid particulates was in the range of 100 to 160 nm. NLC-based carbogels were prepared by the employment of humectants such as urea, glycerin, and Tinocare GL to carbomer gel. NLC-30 gel formulations containing 4 or 8 % of lipid particles showed improved occlusive effect in vitro, compared to NLC-free gel base. Even though NLC-free gel base revealed comparable occlusion effect by itself, the occlusion factor of 4 % NLC-30 gel was about 2-fold higher than that of NLC-free gel base.
Long-acting Recombinant Human Granulocyte Colony Stimulating Factor (rhG-CSF) with a Trimer-Structured Polyethylene Glycol
Jo, Yeong-Woo ; Lee, Mee-Yong ; Choi, Yun-Kyu ; Lee, Sung-Hee ; Kang, Soo-Hyoung ; Na, Kun ; Youn, Yu-Seok ; Choi, Eung-Chil ;
Journal of Pharmaceutical Investigation, volume 40, issue 6, 2010, Pages 379~386
DOI : 10.4333/KPS.2010.40.6.379
Mono PEGylated rhG-CSF (PEG-G-CSF) prepared by utilizing unique PEG was purified and characterized by cation-exchange chromatography. A unique, trimer-structured PEG was chosen for PEGylation of rhG-CSF among various PEG moieties. The in-vitro bioactivity, stability, and pharmacokinetics of mono-PEG-G-CSF were examined and compared to those of native rhG-CSF. Mono PEG-G-CSF exhibited reduced in-vitro bioactivity to native rhG-CSF but showed an excellent in-vivo bioactivity and stability. Furthermore, it showed markedly reduced clearance in rats, thereby increasing the biological half-life by about 4.5-fold compared to that of native rhG-CSF. The results suggest that this unique, trimer-structured 23 kDa PEG can provide advantages to improve the bioactivity of therapeutic proteins in clinical use.