• Archives of Pharmacal Research
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• v.27 no.7
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• pp.763-768
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• 2004

To investigate the feasibility of developing a new quercetin transdermal system, a preformulation study was carried out. Therefore, the effects of vehicles and pressure-sensitive adhesives (PSA) on the in vitro permeation of quercetin across dorsal hairless mouse skin were studied. Among vehicles used, propylene glycol monocaprylate (PGMC) and propylene glycol mono-laurate were found to have relatively high permeation flux from solution formulation (i.e., the permeation fluxes were 17.25$\pm$1.96 and 9.60$\pm$3.87 $\mu\textrm{g}$/$\textrm{cm}^2$/h, respectively). The release rate from PSA formulations followed a matrix-controlled diffusion model and was mainly affected by the amount of PSA and drug loaded. The overall permeation fluxes from PSA formulations were less than 0.30 $\mu\textrm{g}$/$\textrm{cm}^2$/h, which were significantly lower compared to those obtained from solution formulations. The lower permeation fluxes may be due to the decrease of solubility and diffusivity of quercetin in the PSA layer, considering the fact that the highest flux of 0.26 $\mu\textrm{g}$/$\textrm{cm}^2$/h was obtained with the addition of 0.2％ butylated hydroxyanisole in PGMC-diethyl-ene glycol monoethyl ether co-solvents (80-85 ： 15-20, v/v). Taken together, these observations indicate that improvement in the solubility and diffusivity of quercetin is necessary to realize fully the clinically applicable transdermal delivery system for the drug.

• Carbon letters
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• v.13 no.3
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• pp.173-177
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• 2012

A drug delivery system (DDS) was prepared with a temperature and pH-responsive hydrogel. Poly(vinyl alcohol) (PVA)/poly(acrylic acid) (PAAc)/poly(N-isopropylacrylamide) (PNIPAAm)/multi-walled carbon nanotube (MWCNT) nanocomposites were prepared by radical polymerization for the temperature and pH-responsive hydrogels. MWCNTs were employed to improve both the thermal conductivity and mechanical properties of the PVA/PAAc/PNIPAAm/MWCNT nanocomposite hydrogels. Various amounts of MWCNTs (0, 0.5, 1 and 3 wt%) were added to the nanocomposite hydrogels. PVA/PAAc/PNIPAAm/MWCNT nanocomposite hydrogels were characterized with a scanning electron microscope. The mechanical properties were measured with a universal testing machine. Swelling and releasing properties of nanocomposite hydrogels were investigated at various temperatures and pHs. Temperature and pH-responsive release behavior was found to be dependent on the content of MWCNTs in nanocomposite hydrogels.

• Archives of Pharmacal Research
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• v.24 no.1
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• pp.69-73
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• 2001

Biodegradable hydrogels based on glycidyl methacrylate dextran (CMD) and dimethacrylate poly(ethylene glycol) (DMP) were proposed for colon-specific drug delivery. GMD was synthesized by coupling of glycidyl methacylate with dextran in the presence of 4-(N, N-dimethylamino)pyridine (DMAP) using dimethylsulfoxide as a solvent. Methacrylate-terminated poly (ethylene glycol) (PEG) macromer was prepared by the reaction of PEG with methacryloyl chloride. CMD/DMP hydrogels were prepared by radical polymerization of phosphate buffer solution (0.1 M, pH 7.4) of GMD and DMP using ammonium peroxydisulfate (APS) and UV as initiating system. The synthetic GMD, DMP and GMD/DMP hydrogels were characterized by fourier transform infrared (FT-lR) spectroscopy. The FITC-albumin loaded hydrogels were prepared by adding FITC-albumin solution before UV irradiation. Swelling capacity of GMD/DMP hydrogels was controlled not only by molecular weight of dextran, but also by incorporation ratio of DMP Degradation of the hydrogels has been studied in vitro with dextranase. FITC-albumin release from the GMD/DMP hydrogels was affected by molecular weight of nextran and the presence of dextranase in the release medium.

• Journal of Pharmaceutical Investigation
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• v.38 no.6
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• pp.381-385
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• 2008

Isosorbide dinitrate is an oral assiatant therapy agent of angina pectoris, myocardial infarction and congestive heart failure. The objective of this study was to formulate sustained release containing isosorbide dinitrate and assess their formulation variables. Pellets were prepared by fluid bed process and consist of drug layer and membrane layer. The pellets were coated with ethylcellulose along with $5{\sim}15%$ of plasticizer such as triacetin and diethyl butylrate. In vitro evaluation study was performed by comparative dissolution test between test and reference isosorbide dinitrate preparation. We could prepare sustained pellets of isosorbide dinitrate by fluid bed process which were reduced process time and had high content. The pellet coated with 1% ethylcellulose and triacetin(l5%) had a similar dissolution behavior compare to reference isosorbide dinitrate preparation controlling initial dissolution and those of dissolution at 30 min were 17.25 and 17.09%, respectively. Difference factor and similarity factor were $0{\sim}15$ and $50{\sim}100$ and there was no significant difference in bioequivalence between formulations. It might be concluded that our sustained release pellet of isosorbide dinitrate could be an alternatively delivery system to reference drug preparation.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1333-1338
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• 2013

Chitosan-based nanoparticles (CSNP) were prepared through ionic cross-linking and gelation of chitosan (CS) by tripolyphosphate (TPP). CS properties such as molecular weight, and preparation conditions were screened and the resulting nanoparticles were examined by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The obtained particles were consistently spherical with an overall diameter of approximately $107{\pm}20$ nm. They were successfully used as a carrier for Zidovudine, an anti-human immunodeficiency virus (HIV) which, to our knowledge, is novel. The encapsulation ability, loading capacity, and controlled release behavior for these CSNP was evaluated. Results indicated that their intrinsic properties were strongly affected by properties inherent to CS such as molecular weight, and by the preparation condition, such as cross-linking density, which depends on the concentration of the cross-linker. In vitro release tests for the entrapped zidovudine showed that the CNNP provided a continuous release that can last upwards 20 h.

• Bulletin of the Korean Chemical Society
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• v.28 no.3
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• pp.397-402
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• 2007

Restenosis after percutaneous coronary intervention (PCI) continues to be a serious problem in clinical cardiology. To solve this problem, drug eluting stents (DES) with antiproliferative agents have been developed. Variable local drug delivery systems in the context of stenting require the development of stent manufacture, drug pharmacology and coating technology. We have worked on a system that integrates electrophoretic deposition (EPD) technology with the polymeric nanoparticles in DES for local drug delivery and a controlled release system. The surface morphology and drug loading amount of DES by EPD have been investigated under different operational conditions, such as operation time, voltage and the composition of media. We prepared poly-D,L-lactide-co-glycolic acid (PLGA) nanoparticles embedded with curcumin, which was done by a modified spontaneous emulsification method and used polyacrylic acid (PAA) as a surfactant because its carboxylic group contribute negative charge to the surface of CPNPs (?53.5 ± 5.8 mV). In the process of ‘trial and error' endeavors, we found that it is easy to control the drug loading amount deposited onto the stent while keeping uniform surface morphology. Accordingly, stent coating by EPD has a wide application to the modification of DES using various kinds of nanoparticles and drugs.

• Journal of environmental and Sanitary engineering
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• v.20 no.2 s.56
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• pp.33-38
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• 2005

Chitosan is a dietary fiber because of a linear polysaccharide composed of $\beta-(1{\rightarrow}4)$-linked 2-amino-2-deoxy-D-glucopyranose. In this study, control release system of vitamin C has been estimated in chitosan molecular network as a vitamin C carrier of controlled release. The amount of released vitamin C were decreased in higher amount of chitosan concentration. Especially, vitamin C were slowly released from chitosan solution in dialysis membrane when compared with vitamin C solution alone in dialysis membrane. These result assumed that chitosan driving force is dependent on chitosan molecular weight and cationic property of amino group with anionic property of vitamin C.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.488-494
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• 2000

Cerebellar granule and glial cells prepared from 7 day-old rat pups were used to investigate the effects of sub-acute nicotine exposure on the glutamatergic nervous system. These cells were exposed to nicotine in various concentrations for 2 to 10 days in situ. Nicotine-exposure did not result in any changes in cerebellar granule and glial cell viability at concentrations of up to 500 $\mu\textrm{M}$. In cerebellar granule cells, the basal extracellular levels of glutamate, aspartate and glycine were enhanced in the nicotine-exposed granule cells. In addition, the responses of N-methyl-D-aspartate (NMDA)-induced glutamate release were enhanced at low NMDA concentrations in the nicotine-exposed granule cells. However, this decreased at higher NMDA concentrations. The glutaminase activity was increased after nicotine exposure. In cerebellar glial cells, glutamate uptake in the nicotine-exposed glial cells were either increased at low nicotine exposure levels or decreased at higher levels. The inhibition of glutamate uptake by L-trans-pyrollidine-2,4-dicarboxylic acid (PDC) was lower in glial cells exposed to 50 $\mu\textrm{M}$ nicotine. Glutamine synthetase activity was lower in glial cells exposed to 100 or 500 $\mu\textrm{M}$ of nicotine. These results indicate that the properties of cerebellar granule and glial cells may alter after subacute nicotine exposure. Furthermore, they suggest that nicotine exposure during development may modulate glutamatergic nervous activity.

• Archives of Pharmacal Research
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• v.26 no.8
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• pp.644-648
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• 2003

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

• Macromolecular Research
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• v.8 no.6
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• pp.253-260
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• 2000

Biodegradable wafers were prepared with poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV;5, 10, and 15 mole% for 3-hydroxyvalerate) by simple heat pressing method for the sustained release of antibiotic agent, gentamicin sulfate (GS) to investigate the possibility of the treatment for osteomyelitis. The effects of hydroxyvalerate (HV) content, thickness of wafers, various types of additives such as sodium dodecyl sulfate (SDS), microcrystalline cellulose, polyvinylpyrrolidone, and hydroxypropylcellulose (HPC), and different initial drug loading ratio on the release profile have been investigated. In vitro release studies showed that different release patterns and rates could be achieved by simply modifying factors in the preparation conditions. PHBV wafers with 3 mm thickness, 10% of GS initial loading, 15% of HV content and addition of 5% of SDS and HPC were free from initial burst and a near-zero-order sustained release was observed for over 30 days. It might be suggested that the mechanisms of G5 release may be more predominant simple dissolution and diffusion of GS than erosion of PHBV in our system.