• Journal of Pharmaceutical Investigation
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• 제26권2호
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• pp.125-135
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• 1996

Solid lipid nanoparticles(SLN) are particulate systems for parenteral drug administration and suitable for controlled release. SLN were prepared by homogenization process. Dispersion at increased temperature (molten lipid) was performed to yield SLN loaded with lipophilic drugs. Tetracaine base, lidocaine base, prednisolone, methyltestosterone and ethinylestradiol were used as model drugs to access the loading capacity and to study the release behavior. To investigate production parameters(lipids, surfactant concentration, homogenizing rpm) in the formation of SLN, particle size was performed by laser diffraction analysis. The mean particle size of SLN with stearic acid or trilaurin was below 1 micron. By decreasing the particle size and increasing the surfactant concentration, the release rate was increased especially in the case of highly lipophilic drug loaded SLN. Methyltestosterone or ethinylestradiol loaded SLN showed a distinctly prolonged release over a few days.

• 대한화장품학회지
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• 제33권4호
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• pp.219-225
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• 2007

비스에칠헥실옥시페놀메톡시페닐트리아진(Bis-ethylhexyloxyphenolmeth oxyphenyltrizine; BEMT)은 식품의약품안전청 고시 기능성 원료로 자외선 차단 제품에 널리 사용되는 UVA와 UVB의 화학적 자외선 흡수제이다. 그러나 BEMT는 실제 적용에 있어 여러 가지 결점이 있어 사용이 제한되고 있다. 본 연구의 목적은 BEMT가 적용된 고형지질나노입자(BEMT- SLN)의 자외선차단제품 응용에 있다. 제조된 고형지질나노입자의 입도는 약 330 nm, 봉입율은 93.3 %, 결정화지표는 4.3 %였다. In vitro 방출 및 투과 실험 결과에서, BEMT는 SLN보다 O/W 에멀젼이 대체로 높았다. In vivo 실험에서 SLN의 BEMT 방출비는 80 % 감소하였다. 또한 in vitro UV 방어 효과 실험에서 SLN이 적용된 처방의 자외선방어지수(SPF) 값은 약 2.5배 증가하였다. 결국 SLN은 BEMT를 효과적으로 봉입하고 있었으며, 자외선 차단 상승 효과를 나타낸다.

• KSBB Journal
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• 제19권3호
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• pp.178-186
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• 2004

복합한방 재료인 옥용산에 대해 UV 흡수능, tyrosinase 저해활성 그리고 free radical 소거활성을 측정함으로서 미백활성을 검정하고 비교 시험군으로서 비타민C와 함께 Eudragit 이 코팅된 coconut oil을 이용한 SLN을 제조할 수 있었다. 실험 결과, 옥용산은 UV 영역에서 흡수능을 가지며 tyrosinase 저해 활성과 free radical 소거활성을 가진 것으로 확인되었다. 제조된 E-SLN을 TEM을 이용하여 관찰한 결과 크기 50∼300 nm인 구형의 양호한 입자를 형성하고 있음을 확인하였다. 또한 그 크기분포와 캡슐화 효율 분석을 통해 EUD의 농도가 2.0% (w/v), w/o 비율은 1 ： 9, emulsion과 pour solution의 비율은 1 : 10, 그리고 실온에서 제조한 E-SLN의 캡슐화 효율이 가장 높고 크기의 분포가 가장 양호한 것을 알 수 있었다. E-SLN을 이용하여 in vitro 방출시험을 실시한 결과 E-SLN은 pH와 온도 의존적으로 약물을 방출하는 경향을 나타냈다. 결과적으로 제조된 E-SLN은 pH와 온도 의존적으로 약물을 전달할 필요가 있는 계에 대한 약물전달 시스템으로 적합할 것으로 보인다. 폐쇄 첩포시험과 자외선 조사에 의한 인공색소침착과 시료도포에 의한 미백효능 판정에 의한 임상시험 결과 옥용산과 비타민C, 그리고 이를 포함하는 E-SLN은 대조군의 경우와 비교하여 미백효과를 가지는 것으로 확인되었으며 이는 기능성화장품에의 응용 가능성을 높여주었다.

• Asian Pacific Journal of Cancer Prevention
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• 제15권3호
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• pp.1481-1488
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• 2014

Background: To avoid performing axillary lymph node dissection (ALND) for non-sentinel lymph node (SLN)-negative patients with-SLN positive axilla, nomograms for predicting the status have been developed in many centers. We created a new nomogram predicting non-SLN metastasis in SLN-positive patients with invasive breast cancer and evaluated 14 existing breast cancer models in our patient group. Materials and Methods: Two hundred and thirty seven invasive breast cancer patients with SLN metastases who underwent ALND were included in the study. Based on independent predictive factors for non-SLN metastasis identified by logistic regression analysis, we developed a new nomogram. Receiver operating characteristics (ROC) curves for the models were created and the areas under the curves (AUC) were computed. Results: In a multivariate analysis, tumor size, presence of lymphovascular invasion, extranodal extension of SLN, large size of metastatic SLN, the number of negative SLNs, and multifocality were found to be independent predictive factors for non-SLN metastasis. The AUC was found to be 0.87, and calibration was good for the present Ondokuz Mayis nomogram. Among the 14 validated models, the MSKCC, Stanford, Turkish, MD Anderson, MOU (Masaryk), Ljubljana, and DEU models yielded excellent AUC values of > 0.80. Conclusions: We present a new model to predict the likelihood of non-SLN metastasis. Each clinic should determine and use the most suitable nomogram or should create their own nomograms for the prediction of non- SLN metastasis.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2003년도 생물공학의 동향(XIII)
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• pp.655-659
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• 2003

수용성 약물의 캡슐화 효율을 높이기 위하여 eudragit이 코팅된 SLN을 제조하였고 TEM을 이용하여 그 형태가 양호하게 형성된 것을 확인하였다. DLS를 이용하여 형성된 입자의 분포와 크기를 확인하였으며 옥용산을 포함하는 E-SLN은 ${\pm}180$ nm, ascorbic acid는 ${\pm}150$ nm의 크기를 가지는 것으로 확인되었다. 캡슐화 효율은 옥용산을 경우 41%, ascorbic acid는 33%로 나타났으며, 이는 E-SLN이 수용성 약물을 캡슐화하는 데 유용함을 보여준다.

• Journal of Dairy Science and Biotechnology
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• 제25권2호
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• pp.5-10
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• 2007

Ultrasonication was employed to prepare solid lipid nanoparticles (SLN) for smart probiotic nanoparticles as a nanofood. The model probiotic material, lactocin from Lactobacillus plantarum (CBT-LP2), was incorporated into SLN. The CBT-LP2 loaded SLN (CBT-LP2-SLN) were spherical in the photograph of scanning electron microscope (SEM). The particle size measured by laser diffraction (LD) was found to be $97.3{\pm}8.2nm$. Zeta potential analyzer suggested the zeta potential of LP-SLN was $-29.36{\pm}3.68$ mV in distilled water. The entrapment efficiency (EE%) was determined with the sephadex gel chromatogram and high-performance liquid chromatogram (HPLC), and up to 90.59% of nanofood was incorporated. Stability evaluation showed relatively long-term stability with only slight particle growth (P>0.05) after storage at room temperature for 4 weeks. Therefore, ultrasonication is demonstrated to be a simple, available and effective method to prepare high quality SLN loaded probiotic material.

• Archives of Pharmacal Research
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• 제26권12호
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• pp.1096-1101
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• 2003

To enhance the liver targeting and reduce the side effects of 5-fluorouracil (5-Fu), it was acylated by stearyl chloride to obtain .$\b{N}_{\b{1}}$stearyl-5-Fu (5-FuS). The chemical structure of the prodrug was confirmed by Nuclear Magnetic Resonance and Infrared Spectrometry. 5-FuS was incorporated into solid lipid nanoparticles (SLN), which were prepared by the physical agglomeration method. The mean diameter of 5-FuS-SLN was 240.19 nm and the drug loading was 20.53%. The release characteristics in vitro of 5-FuS-SLN were fitted to the first-order pharmacokinetic model. Compared with 5-Fu injection, a study on the distribution of 5-FuS-SLN in mice showed that 5-FuS-SLN could double 5-Fu concentration in mice livers. The main pharmacokinetic parameters of 5-FuS-SLN in rabbits is shown as follows: $V_d$=0.04336L/kg, $T_{1/2} \beta$=1.2834h, CL=0.1632 L/h. In conclusion, 5-FuS-SLN has significant liver targeting properties. The employment of a prodrug to enhance drug liposoluble properties and the preparation method presented in this paper, seem to be an alternative strategy to the traditional colloidal delivery system.

• Macromolecular Research
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• 제16권8호
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• pp.682-685
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• 2008

The aim of this work was to develop and evaluate solid lipid nanoparticles (SLN) containing all-trans-retinoic acid (ATRA) for topical delivery. SLN composed of coconut oil and curdlan improved the suspension instability of ATRA in aqueous solution. The photodegradation of ATRA by light was reduced by incorporation in SLN. The loading efficiency of ATRA in SLN was higher than 95% (w/w). The amounts of ATRA released from SLN at $4^{\circ}C$ and at $37^{\circ}C$ were less than 15% and more than 60% (w/w) for 96 h, respectively. The ATRA-loaded SLN can be used as a potential carrier for topical delivery.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.248.1-248.1
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• 2003

Keloids are characterized by abnormal proliferation of fibroblasts and overproduction of collagen. Recently, it is reported that transforming growth factor beta (TGFb) and its signaling molecule, SMAD3 are related to the mitogenic effect of fibroblasts and a stimulatory factor for collagen synthesis. Cationic SLN was developed to improve the complex formation of DNA/SLN and enhance the uptake efficiency to cells. SLN was formulated by DC-Chol, DOPE, trimyristin as a solid core and other surfactant. The physical properties of the SLN and the ATS-SLN complex were characterized. (omitted)

• Journal of Pharmaceutical Investigation
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• 제26권4호
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• pp.245-256
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• 1996

Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.