PartⅠ Oral drug delivery system Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shap...
PartⅠ Oral drug delivery system Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shape of microsphere were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier-transform infrared spectroscopy (FT-IR). Microspheres containing additives showed more spherical shape than non additive microspheres. In vitro release behavior of microspheres presented at simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The solid dispersion form transformed the drug into an amorphous state and dramatically improved its dissolution rate. These data suggest that the solid dispersion technique is an effective approach for developing the appetite depressant drug products and various pharmaceutical excipients are able to control the release behaviors. Part Ⅱ Local drug delivery system The PLGA microspheres can create an enviroment conductive to promising candidate as an injectable system for tissue engineered application. The purpose of this study was to investigate the condition of emulsion formation and cell adhesion on the microsphere surface. BSA-loaded PLGA microsphere was fabricated using oil-in-water (O/W) and water-in-oil-in-water (W/O/W) solvent evaporation method. Also, sodium alginate was dissolved in water phase for the initial burst control and the lag time improvement caused by PLGA degradation. Morphology of cell attached on the microspheres was studied using scanning electron microscopy (SEM). Cellular proliferation behavior of the human disc cell cultivated with the PLGA microspheres was analyzed using MTT assay. MTT assay revealed that the cells could be attach and proliferate on the PLGA microsphere surface. In this results, BSA-loaded alginate/PLGA microspheres will be used as the injectable system for tissue engineered application. Part III Transdermal drug delivery system Transdermal drug delivery system (TDDS) was drug delivery system that could control drug permeation rate to target organ in accordance with body circulation. This TDDS had many advantages in comparison with conventional oral and IV injection doses. In spite of advantages in TDDS, commercialized drugs such as nitroglycerin for the treatment of angina pectoris, clonidine for hypertension treatment, fentanly for pain management, estradiol-alone or in combination with norethindrone acetate-for the relief of osteoporosis, nicotine as an aid in smoking cessation, and testosterone for the treatment of hypogonadism are just a few. The low drug permeability of the outermost layer of skin, of due to barrier of stratum corneum, was the important reason. Thus, many researches made progress for enhanced drug permeation rate. As a result, the methods using chemical/lipid enhancer, iontophoresis and electrophoresis, ultrasonic or sonophoresis effect were developed. In spite of different mechanism, these methods made enough largely hole to pass in stratum corneum. We designed plane crown/triangle type microneedle system and roll type microneedle system with continuously processing for macromolecular drugs such as vaccine and protein into the body percutaneously. The roll type microneedle system was consisted of 3360 micro-needles and diameter of roll; 1.43 cm. Each needles consisted of width; 2.8 cm, height; 230 um. The plane triangle type microneedle system was consisted of 168 micro-needles and height of each needle was 588 um in area of 2.5 cm x 2.5 cm. The plane crown type microneedle system was consisted of 121 holes in area of 2.5 cm x 2.5 cm, each holes consisted 10 micro-needles and height of each needle was 250 um. We tried to conjugate bufexamac and FITC for calculation of penetration rate of bufexamac, bufexamac linked FITC was made hydrogel and applied on the treated skin surface. Fluorescent spectrophotometer was used to confirm the concentration of FITC linked bufexamac and microscope using fluorescent filter was used to capture the image about location of FITC linked bufexamac in the skin. In the results, we confirmed that permeation rate of bufexamac was increased in the treated skin group by microneedle and was increased by the increasing number treatment of microneedle.
PartⅠ Oral drug delivery system Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shape of microsphere were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier-transform infrared spectroscopy (FT-IR). Microspheres containing additives showed more spherical shape than non additive microspheres. In vitro release behavior of microspheres presented at simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The solid dispersion form transformed the drug into an amorphous state and dramatically improved its dissolution rate. These data suggest that the solid dispersion technique is an effective approach for developing the appetite depressant drug products and various pharmaceutical excipients are able to control the release behaviors. Part Ⅱ Local drug delivery system The PLGA microspheres can create an enviroment conductive to promising candidate as an injectable system for tissue engineered application. The purpose of this study was to investigate the condition of emulsion formation and cell adhesion on the microsphere surface. BSA-loaded PLGA microsphere was fabricated using oil-in-water (O/W) and water-in-oil-in-water (W/O/W) solvent evaporation method. Also, sodium alginate was dissolved in water phase for the initial burst control and the lag time improvement caused by PLGA degradation. Morphology of cell attached on the microspheres was studied using scanning electron microscopy (SEM). Cellular proliferation behavior of the human disc cell cultivated with the PLGA microspheres was analyzed using MTT assay. MTT assay revealed that the cells could be attach and proliferate on the PLGA microsphere surface. In this results, BSA-loaded alginate/PLGA microspheres will be used as the injectable system for tissue engineered application. Part III Transdermal drug delivery system Transdermal drug delivery system (TDDS) was drug delivery system that could control drug permeation rate to target organ in accordance with body circulation. This TDDS had many advantages in comparison with conventional oral and IV injection doses. In spite of advantages in TDDS, commercialized drugs such as nitroglycerin for the treatment of angina pectoris, clonidine for hypertension treatment, fentanly for pain management, estradiol-alone or in combination with norethindrone acetate-for the relief of osteoporosis, nicotine as an aid in smoking cessation, and testosterone for the treatment of hypogonadism are just a few. The low drug permeability of the outermost layer of skin, of due to barrier of stratum corneum, was the important reason. Thus, many researches made progress for enhanced drug permeation rate. As a result, the methods using chemical/lipid enhancer, iontophoresis and electrophoresis, ultrasonic or sonophoresis effect were developed. In spite of different mechanism, these methods made enough largely hole to pass in stratum corneum. We designed plane crown/triangle type microneedle system and roll type microneedle system with continuously processing for macromolecular drugs such as vaccine and protein into the body percutaneously. The roll type microneedle system was consisted of 3360 micro-needles and diameter of roll; 1.43 cm. Each needles consisted of width; 2.8 cm, height; 230 um. The plane triangle type microneedle system was consisted of 168 micro-needles and height of each needle was 588 um in area of 2.5 cm x 2.5 cm. The plane crown type microneedle system was consisted of 121 holes in area of 2.5 cm x 2.5 cm, each holes consisted 10 micro-needles and height of each needle was 250 um. We tried to conjugate bufexamac and FITC for calculation of penetration rate of bufexamac, bufexamac linked FITC was made hydrogel and applied on the treated skin surface. Fluorescent spectrophotometer was used to confirm the concentration of FITC linked bufexamac and microscope using fluorescent filter was used to capture the image about location of FITC linked bufexamac in the skin. In the results, we confirmed that permeation rate of bufexamac was increased in the treated skin group by microneedle and was increased by the increasing number treatment of microneedle.
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#Oral drug delivery system Local drug delivery system Transdermal drug delivery system
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