• Journal of Pharmaceutical Investigation
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• 제32권3호
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• pp.199-207
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• 2002

In order to develop a sustained release formulation of bovine somatotropin (BST), which has been used to increase the body weight of oxen or the milk production of dairy cows, poly(D,L-lactide-co-glyceride)(PLGA) microspheres were made by W/O/W multiple emulsification method and solvent extraction method. Physical properties including particle size, drug entrapment, drug release, protein denaturation, and in vivo body weight increase in rats were characterized. The size of the microspheres was increased as the molecular weight of PLGA increased. When Span 65 and stearic acid during preparation were added, the size was decreased but the amount of surface protein was increased, resulting in a high loading efficiency, with fast release of BST from the microspheres. Aggregation or fragmentation of BST by SDS-PAGE during microsphere preparation and drug release study was not observed. Body weight of Sprague-Dawley's male rats was significantly increased after subcutaneous administrations of BST-loaded PLGA microspheres. There was a good correlation between in vivo weight gain and in vitro release rate of microspheres. PLGA microspheres with a high surface protein ratio could be a good candidate for the sustained delivery of BST.

• Journal of Pharmaceutical Investigation
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• 제40권3호
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• pp.167-173
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• 2010

Repeated oral administration of hydrochlorothiazide, a loop diuretic, due to transient high blood levels, may cause adverse effects such as gastric disturbance, nausea, high blood sugar, and hyper lipidemia. Transdermal administration could avoid some of these systemic side effects and gastric disorders. We have developed a matrix using ethylene-vinyl acetate (EVA), a heat-processible and flexible material, for transdermal delivery of hydrochlorothiazide. Drug solubility was highest at 40% PEG-400 volume fraction. Drug release increased as concentration increased with a linear relationship between the release rate and the square root of loading dose. Increasing temperature increased drug release from the EVA matrix. The activation energy, measured from the slope of log P versus 1000/T, was 11.9 kcal/mol for a 2.5% loading dose from EVA matrix. Diethyl phthalate had the highest plasticizing effects on the release of hydrochlorothiazide. To increase the skin permeation of hydrochlorothiazide from the EVA matrix, enhancers such as the saturated fatty acids, the unsaturated fatty acids, and the non-ionic surfactants were added to the EVA matrix, and skin permeation was evaluated using a modified Keshary-Chien diffusion cell fitted with intact excised rat skin. Polyoxyethylene 23-lauryl ether showed the highest enhancing effects. In conclusion, transdermal delivery of hydrochlorothiazide could be improved from an EVA matrix containing plasticizer and permeation enhancer.

• Journal of Pharmaceutical Investigation
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• 제36권3호
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• pp.175-184
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• 2006

Poly(D,L-lacic acid)(PLA) microshperes containing loazepam were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of lorazepam to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like lorazepam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of lorazepam for long-acting injectable delivery system in vitro, which would aid in Predicting in vivo release Profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

• Journal of Pharmaceutical Investigation
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• 제35권1호
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• pp.33-38
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• 2005

Recently increasing attention has been focused on solid lipid nanoparticles (SLN) as a parenteral drug carrier due to its numerous advantages that can come from both polymeric particle and fat emulsions, together with the possibility of controlled release and increasing drug stability. Lipophilic drugs such as paclitaxel, cyclosporin A, and all-trans retinoic acid have been successfully entrapped in SLN but the incorporation of hydrophilic drugs in SLN is very limited because of their very low affinity to the lipid. Therefore, as a new approach to improve the loading of hydrophilic drugs, a w/o/w emulsion technique has been developed. The primary objective of the current study was to improve the loading efficiency of a model hydrophilic drug, glycine (Log P = -3.44) into SLN. The proposed preparation process is as follows: A heated aqueous phase consisting of 0.1 ml of glycine solution in water (100 mg/ml), and poloxamer 188 (5 mg) were then added to a molten oil phase containing precirol (100 mg) and lecithin (5 mg). This mixture was dispersed by sonicator, leading to a w/o emulsion. A double emulsion (w/o/w) was formed after the addition of 2% poloxamer solution to the above dispersed system. After cooling the double emulsion, solid lipid nanosuspensions were successfully formed. The lipid nanoparticles had the mean particle size of 441.25 nm, and the average zeta potential of -20.98 mV. The drug loading efficiency was measured to be 8.54% and the drug loading amount was measured to be 0.92%. The w/o/w emulsion method showed an increased loading efficiency compared to conventional o/w emulsion method.

• Advances in materials Research
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• 제9권2호
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• pp.109-114
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• 2020

The purpose of this study was to observe the trend of compounds release from acrylic resin oral prosthesis when used for drug delivery as well as a restoration. In this study, 10 specimens of heat-cured polymethylmethacrylate material were prepared and loaded with methylene blue biological stain. The specimens were then submerged in vials with 5 ml distilled water for 24 hours. The extraction procedure continued for 4 days, each day the specimens were immersed in another 5 ml distilled water vial. All extracted solutions were analyzed by visible light spectroscopy for absorbance comparison. The statistical results showed that the absorbance values were significantly different in the first day of extraction than the following days. However, there was no statistical difference among the 2^nd, 3^rd and 4^th days of extraction. Biological stain loading to acrylic resin at the mixing stage, and then after extraction in distilled water, showed a burst release during the first day followed by a constant release during the following few days.

• 공업화학
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• 제7권4호
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• pp.735-742
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• 1996

장시간에 걸쳐 약물의 흡수가 일어날 수 있는 고분자 matrix을 개발하고자, 글리세린과 증류수를 혼합 교반 시킨 후, 분자량이 서로 다른 세 종류의 dextran을 각각 첨가하여 용해시켰다. 이 용액에 silver sulfadiazine을 분산시켜 matrix를 제조하였다. 이렇게 제조된 고분자 matrix로부터 약물 방출 양상을 규명하기 위해 인산염 완충용액 중에서 약물의 함유량 변화, dextran의 분자량 변화 및 글리세린의 농도 변화에 영향을 미치는 인자들에 관하여 연구 검토한 바 다음과 같은 결론을 얻었다. 고분자 matrix내의 silver sulfadiazine의 함유량이 증가할수록 약물 방출 지속 시간은 11.2일, 14.0일 및 15.8일로 지연되었다. Dextran의 분자량 변화에 대해서는 약 14.0일로 거의 같은 약물 방출 pattern을 보임으로써 겉보기 방출속도상수 (K)값과의 관계와 일치하는 결과를 얻었다. 그러나 글리세린의 함유량이 증가함에 따라 약물 방출 지속 시간은 각각 18.0일, 17.0일, 14.0일, 13.0일 및 10.0일로 감소하였다.

• Journal of Pharmaceutical Investigation
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• 제40권1호
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• pp.33-38
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• 2010

Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. $Crovol^{(R)}$ PK40 and $Crovol^{(R)}$ A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% $Crovol^{(R)}$ A40 as permeation enhancer, in $80\;{\mu}m$ thick Duro-$Tak^{(R)}$ 87-9301 matrix.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2003년도 생물공학의 동향(XII)
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• pp.739-742
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• 2003

생분해성인 Curdlan을 이용하여 pH 의존성 약물 전달계 개발을 위한 실험을 수행한 결과, pH 1,4에서 약물 방출 보다 pH 7.4에서 약물 방출이 10배 이상 증가하였다. 이러한 결과로 curdlan acetate microsphere는 pH 의존성 약물 전달계로 유용하다고 판단된다.

• Journal of Pharmaceutical Investigation
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• 제39권6호
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• pp.437-443
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• 2009

To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.

• Bulletin of the Korean Chemical Society
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• 제28권3호
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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.