• Journal of Pharmaceutical Investigation
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• 제38권1호
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• pp.39-43
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• 2008

Cyclosporin A (CyA), a potent immunosuppressive drug used in allogeneic transplants and autoimmune disease, is a typical water-insoluble drug. Recently, nanoparticle carriers were investigated to improve the intestinal absorption of drugs. In this study, CyA-loaded nanostructured lipid carriers (NLCs) were prepared from a hot o/w emulsion using the high pressure homogenization method. The NLCs were consisted of cationic lipids, solid lipids, liquid lipids (oils), surfactant and stabilizer. Encapsulation efficiency of CyA in NLCs was approximately 71%. The average particle size and zeta potential of NLCs were below 250 nm and above +40 mV, respectively. The morphology of NLCs was confirmed by transmission electron microscopy (TEM) analysis. Compared to the CyA powder, higher in vitro release of CyA from NLCs was observed after burst release within 30 min. Thus, CyA-loaded NLCs could be applied not only for parenteral route but also for gastrointestinal administration, which needs further investigation.

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.956-960
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• 2011

The objective of this investigation was to develop nanostructured lipid carriers (NLCs) of tacrolimus by the hot homogenization technique by sonication. NLCs are commonly prepared by emulsification and lyophilization. The feasibility of fabricating tacrolimus-loaded NLCs was successfully demonstrated in this study. The developed NLCs were characterized in terms of their particle size, zeta potential, entrapment efficiency (EE) of tacrolimus, and morphology. Studies were conducted to evaluate the effectiveness of the NLCs in improving the penetration rate through hairless mouse skin. Tacrolimus-loaded NLCs were found to have an average size of $123.4{\pm}0.3\;nm$, a zeta potential of $-24.3{\pm}6.2\;mV$, and an EE of 50%. In vitro penetration tests revealed that the tacrolimus-loaded NLCs have a penetration rate that is 1.64 times that of the commercial tacrolimus ointment, Protopic$^{(R)}$.

• Asian Pacific Journal of Cancer Prevention
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• 제17권12호
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• pp.5185-5188
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• 2016

Objective: Targeted-drug-delivery based lipid nanoparticles has emerged as a new and effective approach in cancer chemotherapy. Here, we investigated the ability of folate-modified nanostructured lipid carriers (NLCs) to enhance letrozol (LTZ) efficacy in MCF-7 breast cancer cells. Methods: New formulations were evaluated regarding to particle size and scanning electron microscope (SEM) features. Anti-proliferative effects of LTZ loaded nanoparticles were examined by MTT assay. To understand molecular mechanisms of apoptosis and cell cycle progression, flow cytometric assays were applied. Results: Optimum size of nanoparticles was obtained in mean average of $98{\pm}7nm$ with a poly dispersity index (PDI) of 0.165. The IC50 value was achieved for LTZ was $2.2{\pm}0.2{\mu}M$. Folate-NLC-LTZ increased the percentage of apoptotic cells from 24.6% to 42.2% compared LTZ alone (p<0.05). Furthermore, LTZ loaded folate targeted NLCs caused marked accumulation of cells in the subG1 phase. Conclusion: Taken together, our results concluded that folate targeted LTZ can be considered as potential delivery system which may overcome limitations of clinical application of LTZ and improve drug efficacy in tumor tissue.

• 공업화학
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• 제26권6호
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• pp.659-665
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• 2015

지용성 토코페롤(${\alpha}$-tocopherol)의 산화 안정성을 높이기 위하여 nanostructured lipid carrier (NLC)에 봉입을 시도하였다. 먼저 구성 성분과 혼합 비율을 달리한 여러 NLC를 만들고 각각의 특성을 살펴보았다. 고체 지질로 세틸 팔미테이트 또는 글리세릴 모노스테아레이트를 사용했을 때는 안정한 상태의 NLC 입자가 만들어지지만 스테아린 산으로 만든 NLC에서는 상분리가 일어났다. NLC 입자는 수백 나노미터 크기로 만들어지는데 지질대비 용매의 비율이 높을수록 입자크기가 작게 나타났다. 고급 지방알콜인 옥틸도데칸올을 고체 지질에 첨가하면 결정화도가 감소하면서 지질 매트릭스의 배열규칙성 이 약해짐을 DSC (Differential Scanning Calorimetry) 열차트와 anisotropy 측정을 통해서 확인하였다. 고온($45^{\circ}C$) 또는 UV 빛이 조사되는 조건에서 토코페롤이 NLC에 봉입되어 있으면 용액이나 에멀젼 상태로 있는 것에 비해 산화 안정성이 크게 향상됨을 DPPH 테스트와 과산화물가 측정으로 확인하였다.