• Journal of Pharmaceutical Investigation
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• 제39권1호
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• pp.13-18
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• 2009

Docetaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated docetaxel in the propyleneglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 10 mg/mL docetaxel, 10% (w/v) oil blend, 4% (w/v) PG, 3% (w/v) Solutol HS 15 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at $40^{\cird}C$, and the docetaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around $10{\mu}m$ for at least 3 months. The formulated emulsion is a promising carrier for docetaxel and other lipophilic drugs.

• Korean Chemical Engineering Research
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• 제54권2호
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• pp.200-205
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• 2016

본 연구에서는 최근 많은 분야에서 응용되고 있는 형광물질인 양자점을 생명고분자인 키토산과 반응시켜 얻은 나노입자와 금속성 골드 나노입자, 그리고 실버 나노입자로 외부를 코팅하여 나노약물 전달체를 얻을 수 있었다. 키토산은 생체고분자로써 무독성이며 인체적합성 고분자이다. 양자점은 2~10 nm의 크기를 가지는 반도체성 나노입자이다. 양자점은 생명분자나 생명단백질의 비슷한 크기를 갖으며, 그 크기에 따라 알맞은 가시광선 영역의 빛을 발산할 수 있도록 조절 가능하므로, 세포 바이오 마킹, 약물전달체 등에 효과적으로 쓰일 수 있다. 따라서 키토산 나노입자 말단의 아민기와 양자점의 카르복실기가 아미드결합을 형성하여 반응하게 조절하였다. 양자점의 독성을 완화시키기 위해 코팅재료로 사용된 금속성 나노입자 중 골드나노입자는 약 5~10 nm의 크기를 가지고 있고, 인체에 무해하고 음전하를 띄어서 양전하를 띈 고분자와 쉽게 복합체를 형성할 수 있는 장점이 있다. 향균성으로 잘 알려진 실버나노입자는 약 5 nm의 크기를 가지고 있고, 은 나노입자로 코팅을 하면 미생물 감염을 미리 방지 할 수 있는 장점을 가지고 있다. 본 연구에서 만들어진 QDs-키토산-골드 & QDs-키토산-실버 나노쉘의 입자크기는 약 100 nm의 크기를 갖었으며, 목적하는 바 형광특성을 잘 보여주고 있었다. 이러한 입자들은 정전기적 상호작용에 의하여 각각 골드나노입자와 실버나노입자로 코팅되어 나노 약물전달체로 완성할 수 있었다.

• Advances in nano research
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• 제13권1호
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• pp.87-96
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• 2022

Drug self-delivery systems can easily realize combination drug therapy and avoid carrier-induced toxicity and immunogenicity because they do not need non-therapeutic carrier materials. So, designing appropriate drug self-delivery systems for specific diseases can settle most of the problems existing in traditional drug delivery systems. Retinal pigment epithelium is very important for the homeostasis of retina. However, it is vulnerable to oxidative damage and difficult to repair. Worse still, the antioxidants can hardly reach the retina by non-invasive administration routes due to the ocular barriers. Herein, the targeted group (folic acid) and antioxidant (melatonin) have been grafted on the surface of ZnO quantum dots to fabricate a new kind of drug self-delivery systems as a protectant via eyedrops. In this study, the negative nanoparticles with size ranging in 4~6 nm were successfully synthesized. They could easily and precisely deliver drugs to retinal pigment epithelium via eyedrops. And they realized acid degradation to controlled release of melatonin and zinc in retinal pigment epithelium cells. Consequently, the structure of retinal pigment epithelium cells were stabilized according to the expression of ZO-1 and β-catenin. Moreover, the antioxidant capacity of retinal pigment epithelium were enhanced both in health mice and photic injury mice. Therefore, such new drug self-delivery systems have great potential both in prevention and treatment of oxidative damage induced retinal diseases.

• 한국식품위생안전성학회지
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• 제23권4호
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• pp.291-296
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• 2008

현재 미국 및 유럽에서 공정시험법 중 하나로 인정되고 있는 표면시험법을 사용하여 유기물과 함께 또는 유기물 없이 세균만 건조된 식품접촉 표면에서의 살균소독제 유효성에 대한 정보를 제공하고자 식품접촉표면으로 사용되는 스테인리스, 폴리프로필렌 및 실리콘에 Escherochia coli ATCC 10536 또는 Staphylococcus aureus ATCC 6538을 접종하고 살균소독제로서 염화벤잘코늄, 차아염소산나트륨 또는 에탄올을 $20^{\circ}C$에서 5분간 처리하였다. 그 결과, 각 표면의 종류는 살균소독제의 유효성에 큰 영향을 미치지 않았으며, 200 ppm 농도의 염화벤잘코늄 및 차아염소산나트륨은 유기물질이 존재할 경우 생균수를 $4\;cfu\;\log_{10}$/carrier 이상 감소시키지 못하였으나, 40% 에탄올은 생균수를 $4\;cfu\;\log_{10}$/carrier 이상 감소시키는 것으로 나타났다.

• Journal of Pharmaceutical Investigation
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• 제6권3호
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• pp.58-69
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• 1976

It is well established that dissolution is freruently the rate limiting step in the gastrointestinal absorpton of a drug from a solid dosage from. The relationship between the dissolution rate and absorption is particularly distinct when considering drugs of low solubility. Consequently, numerous attempts have been made to modify the dissolution characteristics of poorly water soluble drugs. Since dissolution rate is directly proportional to surface area, one may increase the rate by decreasing the particle size of the drug. Levy has considered a number of methods by which a drug may be presented to the GI fludids in finely divided from. The direct method is the utilization of microcrystalline or micronized particles. A second method involves the administration of solutions from which, upon dilution with gastric fluids, the dissolved drug will precipitate in the form of very fine particles. A more unique way of obtaining microcrystalline dispersions of a drug has been ercently suggested by Sekiguchi et al. They have first proposed the formation of a eutectic mixture of a poorly water soruble drug with a physiologically inert, easily soluble carrier. When such systems are exposed to water or GI fluids, the soluble carrier will dissolve rapidly and the finely dispersed drug particles will then be released. It has been suggested by Shefter and Higuchi that the formation of crystalline solvate could be a powerful tool in affecting rapid disslution of highly insoluble substances. Goldberg et al. have noted that the formation of solid solution could reduce the particle size to a minimum and increase the dissolution rate as well as the solubility of the durgs. It has also been shown that the rates of solution of drugs were appreciably increased by coprectipitating the drug with soluble polymers. The increase was found to be sensitive to the method of preparation, the molecular weight of polymer and the particular ratio of drugs to polymer. Although several investigations have demontrated that the solubility and/or dissolution rates of drugs can be increased in this manner, little information is available in the literature related to the in vivo absorption pattern of drugs orally administered as PVP coprecipitates. Recently, however, it was demonstrated that both the rate and extent of absorption of the insoluble drug could be markedly enhanced when orally administered to rats in the form of a coprecipitate with PVP. The purpose of the present investigation was to ascertain the general appility of soluble polymer coprectation technique as a method for enhancing the in vitro dissolution rate of hydrophobic indomethacin. To accomplish this aim, the dissolution characteristics of pure indomethacin, indomethcin-polymer physical mixtures and indomethacin-polymer coprecipitates were quantitatively studied by comparing their relative dissolution rates. The solubility and dissolution behavior of these systems were also examined.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2005년도 생물공학의 동향(XVII)
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• pp.711-712
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• 2005

• Archives of Pharmacal Research
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• 제12권2호
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• 폴리머
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• 제35권2호
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• pp.119-123
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• 2011

본 연구에서는 항암제 전달체로 응용하기 위하여 천연고분자인 히알루론산(hyaluronic acid, HA)에 소수 성기 도입을 위하여 담즙산(bile acid) 중 하나인 디옥시콜산(deoxycholic acid)(DA)을 개질하여 양친성 공중합체를 제조하였고, 이를 항암제 전달체로 응용하고자 하였다. 디옥시콜산이 결합된 히알루론산(HADA)의 물리화학적 특성은 $^1H$ NMR, FTIR, spectrophotometer와 TEM을 이용하여 측정하였다. 디옥시콜산이 결합된 히알루론산에 항암제(파클리탁셀)를 투석방법을 통하여 봉입시켰고, in vitro에서 KB 세포에 대한 항암활성을 확인하였다. 제조된 디옥시콜산이 결합된 히알루론산이 항암제 전달체로서의 응용 가능성을 제시하였다.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.301-302
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• 2003

With the aim of obtaining the early bone regeneration efficacy, poly (L-lactide) particulates were developed as a long-term drug carrier system.Biodegradable microparticulates have been used extensively as drug delivery devices. However, problems like poor encapsulation efficiencies of the drugs and complicated fabrication process are still remained to be solved. (omitted)

• 공업화학
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• 제29권2호
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• pp.147-154
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• 2018

현재 항암제의 낮은 치료 효율과 부작용을 해결하기 위해 고분자 기반의 약물전달체의 연구가 활발하게 진행되고 있다. 기존의 고분자기반의 약물 전달체는 우수한 결과를 보이는 등 상당한 진전이 있었음에도 불구하고, 대부분 혈중에서 안정성이 감소하여 표적 부위에 도달하기 전에 약물이 방출될 뿐만 아니라 오랜 시간 동안에 약물을 방출함으로써 부작용 및 낮은 치료 효율을 초래한다는 문제점을 가지고 있다. 본 총론에서는 이러한 비효율적인 약물 방출의 문제점을 개선하기 위한 방법으로 독성이 없고 생체 적합한 천연 고분자 키토산에 자극 응답성 물질을 도입하여 혈중에서 안정성을 높이고 표적 부위에서 약물을 과다 방출하여 치료 효율을 극대화할 수 있는 방법을 제시하고자 한다.