• KSBB Journal
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• v.14 no.3
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• pp.297-302
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• 1999

The polymeric matrices coated with poly(DL-lactide) were prepared using chitosan derivatives such as chitosan, chitosan hydrochloride, and sulfonated chitosan for application of drug delivery systems. The drug release study using prednisolone as a model drug was performed in the hydrochloride solution at pH 1.2. The release rate of drug was decreased according to the increased content of matrices. The release rate of prednisolone according to the kinds of polymeric matrices coated were decreased in the order to chitosan, sulfonated chitosan, and chitosan hydrochloride. Drug release rate of polymeric matrices coated with poly(DL-lactide) was not only two times slower than noncoated one, but also the burst effect of initial period of drug release was decreased in comparison with noncoated one. From these results, it was expected that these formulations based on the chitosan derivative matrices coasted with poly(DL-lactide) were acceptable drug delivery devices for a sustained-release dosage form of drug.

• Journal of Pharmaceutical Investigation
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• v.26 no.3
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• pp.187-192
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• 1996

The matrix tablet containing sodium alginate and $CaHPO_4$ can release drugs in a controlled fashion from hydrogel with gelling and swelling due to their interaction as water penetrates the matrices of the tablet. The purpose of this study was to evaluate release characteristics of the matrix tablet varying the amount of sodium alginate, $CaHPO_4$ and other excipients such as chitosan, hydroxypropyl methylcellulose (HPMC) and $Eudragit^{\circledR}$ RS100 in the simulated gastric and intestinal fluid. The practically soluble ibuprofen was used as a model drug. The release profiles of matrix tablet in the gastric fluid as a function of sodium alginate/$CaHPO_4$ ratio was not pronounced because of low solubility of drug and stability of alginate matrices. However, release rate of drug from the matrix tablet in the intestinal fluid was largely changed when sodium alginate/$CaHPO_4$ ratio was increased, suggesting that the ratio of sodium alginate/$CaHPO_4$ was an important factor to control the gelling and swelling of the matrix tablet. The incorporation of other excipients into the matrix tablet also influenced the release rate of drug. The chitosan and HPMC decreased the release rate of drug. No release of drug was occurred when $Eudragit^{\circledR}$ RS100 was added into the tablet. The retarded release of matrix tablet when excipients were added resulted from the hindrance of swelling and gelling of the matrix tablet containing sodium alginate and $CaHPO_4$. The hardness and bulk density of the matrix tablet was not correlated with release rate of drug in the study. From these findings, the ratio of sodium alginate and $CaHPO_4$ in the matrix tablet in addition to incorporation of excipients could be very important to control the release rate of drug in dosage form design.

• Proceedings of the Polymer Society of Korea Conference
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• 2006.10a
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• pp.258-258
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• 2006

Electrospun fibers of poly(vinyl alcohol) (PVA) were successfully prepared and applied as drug carriers for transdermal drug delivery system. Sodium Salicylate (SS) was the model drug and it was incorporated in the PVA fibers by adding 20 % of SS in a PVA solution prior to electrospinning. Electrospinning of SS-containing PVA solution resulted in the formation of beaded fibers. In order to control the rate of SS release and decrease water solubility of PVA, the SS-loaded electrospun PVA mat was cross-linked by either glutaraldehyde or glyoxal vapor. The morphology, thermal behavior, swelling behavior, release characteristic, kinetics of drug release and also toxicity of the cross-linked sample were investigated.

• Journal of Pharmaceutical Investigation
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• v.23 no.4
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• pp.207-211
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• 1993

Reservoir type devices were designed for long-term implantable drug delivery system. The reservoir type device was prepared with the polymethacrylic acid gel coated with polyurethane membrane. Release controlling agent (RCA) were employed to control drug release from devices via generation of micropores in the membranes. The polyurethane membrane functioned as a rate controlling barrier. The drug release pattern of hydrogel demonstrated zero order kinetics. The release rate of drugs could be regulated by varying hydrophobicity/hydrophilicity and content of the RCA, as well as the thickness of the polyurethane membrane. The release of drugs from this system was governed by pore mechanism via simple diffusion and osmotic pressure.

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.

• YAKHAK HOEJI
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• v.45 no.6
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• pp.623-633
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• 2001

Various bupivacaine-loaded microspheres were prepared using poly(d,1-lactide) (PLA) and poly(d,1-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. The effects of process conditions such as drug loading, polymer type and solvent type on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency and yield of PLGA micro- spheres were higher than those of PLA microspheres. The prepared microspheres had an average particle size below 5${\mu}{\textrm}{m}$. The particle size range of microspheres was 1.65~2.24${\mu}{\textrm}{m}$. As a result of SEM, the particle size of PLA microspheres was smaller than that of PLGA microspheres. In morphology studies, microspheres showed a spherical shape and smooth surface in all process conditions. In thermal analysis, bupivacaine-loaded microspheres showed no peaks originating from bupivacaine. This suggested that bupivacaine base was molecular-dispersed in the polymer matrix of microspheres. The release pattern of the drug from microspheres was evaluated for 96 hours. The initial burst release of bupivacaine base decreased with increasing the molecular weight of PLGA, and the drug from microspheres released slowly. In conclusion, bupivacaine-loaded microspheres were successfully prepared from poly(d,1-lactide) and poly (d,1- lactic-co-glycolide) polymers with different molecular weights allowing control of the release rate.

• Applied Chemistry for Engineering
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• v.10 no.2
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• pp.201-205
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• 1999

Hydroxypropylmethylcelluloses (HPMC) are cellulose ethers which may be used as the basis for hydrophilic matrices for controlled release oral delivery and offer the advantages of being non-toxic and relatively inexpensive. In this work, we designed new drug release system using HPMC as matrix, manufactured by direct compression technology and have investigated the effects of the controlling factors on drug release from a swellable hydrophillic delivery system. It was found that the release rate of the drug decreased with increasing the polymer molecular weight and the polymer content in tablets, and was independent of compaction pressure and pH of dissolution fluids. Especially, the ability of the anionic surfactant, sodium laurylsulfate, to retard the release of pseudoephedrine hydrochloride from HPMC was characterised. With increasing the concentration of the sodium laurylsulfate within the matrix, drug release rate decreased. It is believed that, provided the pseudoephedrine hydrochloride and the sodium laurylsulfate are oppositely charged, they will bind together in situ within the HPMC matrix, leading to reduced drug release rates.

• YAKHAK HOEJI
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• v.40 no.4
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• pp.400-410
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• 1996

In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.445-451
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• 2005

As a selective ${\alpha}_{1A}-adrenoreceptor$ antagonist, tamsulosin has been used clinically for urinary obstructed patients with benign prostatic hyperplasia. The single and multi-layered pellets containing tamsulosin hydrochloride were prepared in an effort to control the drug release, avoiding dose-dependent side effects of tamsulosin hydrochloride upon oral administration. The drug release from multi-layered pellets was substantially controlled, compared with single layered pellets. The drug release from coated pellets with single or multi layer was affected by the nature of coating agent, the percentage of coating level and the presence of hydrophilic material in coating layer. In conclusion, the controlled release oral delivery system using multi-layered pellet is very useful for tamsulosin hydrochloride, resulting in improvement of patient compliance and therapeutic drug levels for a longer period of time.

• Bulletin of the Korean Chemical Society
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• v.35 no.5
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• pp.1333-1336
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• 2014

Expanded polytetrafluoroethylene (ePTFE) grafts have been used as vascular access for many patients suffering from end stage renal disease. However, the vascular graft can cause significant clinical problems such as stenosis or thrombosis. For this reason, many studies have been performed to make drug eluting graft, but initial burst is major problem in almost drug eluting systems. Therefore we used biodegradable polymer to reduce initial burst and make sustained drug delivery. The ePTFE grafts were dipped into a paclitaxel-dissolved solution and then PLGA-dissolved solution was passed through the lumen of ePTFE. We analyzed whether the dose of paclitaxel is enough and the loading amount of PLGA on ePTFE graft increases according to the coating solution's concentration. Scanning electron microscope (SEM) images of various concentration of PLGA showed that the porous surface of graft was more packed with PLGA by tetrahydrofuran solution dissolved PLGA. In addition, in vitro release profiles of Ptx-PLGA graft demonstrated that early burst was gradually decreased as increasing the concentration of PLGA. These results suggest that PLGA coating of Ptx loaded graft can retard drug release, it is useful tool to control drug release of medical devices.