• Asian Pacific Journal of Cancer Prevention
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• 제15권5호
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• pp.2335-2340
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• 2014

Paclitaxel is hydrophobic in nature and is recognized as a highly toxic anticancer drug, showing adverse effects in normal body sites. In this study, we developed a polymeric nano drug carrier for safe delivery of the paclitaxel to the cancer that releases the drug in a sustained manner and reduces side effects. N-isopropylacrylamide/vinyl pyrrolidone (NIPAAm/VP) nanoparticles were synthesized by radical polymerization. Physicochemical characterization of the polymeric nanoparticles was conducted using dynamic light scattering, transmission electron microscopy, scanning electron microscopy and nuclear magnetic resonance, which confirmedpolymerization of formulated nanoparticles. Drug release was assessed using a spectrophotometer and cell viability assays were carried out on the MCF-7 breast cancer and B16F0 skin cancer cell lines. NIPAAm/VP nanoparticles demonstrated a size distribution in the 65-108 nm range and surface charge measured -15.4 mV. SEM showed the nanoparticles to be spherical in shape with a slow drug release of ~70% in PBS at $38^{\circ}C$ over 96 h. Drug loaded nanoparticles were associated with increased viability of MCF-7 and B16F0 cells in comparison to free paclitaxel. Nano loaded paclitaxel shows high therapeutic efficiency by sustained release action for the longer period of time, i increasing its efficacy and biocompatibility for human cancer therapy. Therefore, paclitaxel loaded (NIPAAm/VP) nanoparticles may provide opportunities to expand delivery of the drug for clinical selection.

• 폴리머
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• 제33권3호
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• pp.219-223
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• 2009

전기방사 공정을 이용하여 제조된 나노파이버는 나노 소자, 필터, 방호닦, 항균성 드레싱 및 약물전달 등 다양한 분야에서 이용되고 있다. 약물전달시스템(drug delivery system, DDS)은 기존 의약품의 부작용을 최소화하며 그 효능 및 효과를 극대화할 수 있어야 하고 필요한 양의 약물을 원하는 환부에 효율적으로 전달할 수 있어야 한다. 본 연구에서는 전기유체역학공정의 하나인 전기방사공정을 이용하여, poly($\varepsilon$-carprolactone)(PCL) poly(ethylene oxide(PEO)를 나노파이버 매트로 만들었으며, 고분자와 동시 방사된 Rhodamine B의 방출량을 측정하였다. PCL/Rhodamine B/PEO/PCL 나노파이버 매트는 전기방사 시간을 통한 두께 조절을 통하여 약물전달 거동이 조절될 수 있음을 확인하였으며, 실제 Peptide를 PEO와 동시 전기방사시켜 얻어진 나노파이버 peptide가 방출되는 거동을 확인하였다. PCL/Peptide/PEO/PCL시스템에서 방출된 peptide는 약물방출 시험 후에도 약물로서의 활성도를 잃지 않았으며, 이러한 나노파이버를 이용한 Peptide 방출메커니즘은 새로운 약물전달시스템으로 적용 및 응용될 수 있을 것으로 예상된다.

• 한국음향학회지
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• 제41권5호
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• pp.564-569
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• 2022

인체의 다른 장기들과 달리, 뇌는 혈뇌장벽(Blood-Brain Barrier, BBB)라는 보호 장치가 존재하여 뇌혈관내 물질들이 뇌조직으로 투과되는 것을 제한하는 역할을 한다. 이러한 BBB는 알츠하이머, 뇌종양 등 다양한 뇌질환에 직접적으로 전달이 필요한 약물의 투과까지 제한하기 때문에 치료 효능 검증 및 임상 적용이 어려운 것으로 보고되고 있다. 이러한 문제를 극복하기 위해 비침습적 특성의 집속 초음파(Focused Ultrasound, FUS)를 뇌의 국소 부위에 조사할 경우 마이크로버블의 음향공동화 현상으로 인해 BBB가 일시적으로 개방될 수 있는 기술이 개발되었으며, 해당 기술을 안전성 및 유효성 검증, 약물 전달 효율을 증대시킬 수 있는 다양한 연구가 전 세계적으로 수행되고 있다. 따라서, 본 논문에서는 알츠하이머, 뇌종양 등 뇌질환 치료를 위해 활발히 연구가 진행중인 집속초음파 기반 BBB 개방 기술에 대한 연구 동향을 분석하였다.

• 공업화학
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• 제34권2호
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• pp.121-125
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• 2023

카세인(casein)은 포유류의 우유에서 발견되는 단백질로 우유에서는 80% 이상 함유되어 있다. 사람의 모유에는 약 20~45%가 포함되어 있으며 생체 적합성이 높아 의료 및 산업 소재로 사용되고 있다. 카세인은 양친매성 구조로 내부는 소수성이기 때문에 수용액에서 마이셀로 자가 조립이 가능하여 난용성 약물을 봉입할 수 있다. 또한, 단백질 고분자 소재로 생분해성을 갖고 있어 약물의 전달체로서 적합한 특징을 가진다. 본 연구에서는 칼슘 이온 외에 마그네슘, 아연, 철 등 생체 내 존재하는 다양한 금속 이온들을 사용하여 각각 효과적인 카세인 나노입자 형성 조건을 규명하였다. 동적 광산란 측정기와 제타 전위 측정을 통해 150 nm 이하의 균일한 사이즈를 유지하고 음전하를 띠는 나노입자가 형성됨을 확인하였다. 또한, 각각의 카세인 나노입자가 HeLa 세포주에서 80% 이상의 생존율을 나타내 낮은 세포 독성을 확인하였고, 카세인 나노입자 내부에 시험 약물로서 나일 레드를 봉입하여 세포 내부로 효과적으로 유입됨을 공초점 현미경으로 입증하였다. 본 실험들을 통해 제조된 카세인 나노입자의 약물 전달체로서의 가능성을 확인하였다.

• Journal of Ginseng Research
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• 제44권2호
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• pp.222-228
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• 2020

Background: 20(S)-ginsenoside-Rg3 (C₄₂H₇₂O₁₃), a natural triterpenoid saponin, is extracted from red ginseng. The increasing use of 20(S)-ginsenoside Rg3 has raised product safety concerns. Methods: In acute toxicity, 20(S)-ginsenoside Rg3 was singly and orally administrated to Kunming mice and Sprague-Dawley (SD) rats at the maximum doses of 1600 mg/kg and 800 mg/kg, respectively. In the 26-week toxicity study, we used repeated oral administration of 20(S)-ginsenoside Rg3 in SD rats over 26 weeks at doses of 0, 20, 60, or 180 mg/kg. Moreover, a 4-week recovery period was scheduled to observe the persistence, delayed occurrence, and reversibility of toxic effects. Results: The result of acute toxicity shows that oral administration of 20(S)-ginsenoside Rg3 to mice and rats did not induce mortality or toxicity up to 1600 and 800 mg/kg, respectively. During a 26-week administration period and a 4-week withdrawal period (recovery period), there were no significant differences in clinical signs, body weight, food consumption, urinalysis parameters, biochemical and hematological values, or histopathological findings. Conclusion: The mean oral lethal dose (LD₅₀) of 20(S)-ginsenoside Rg3, in acute toxicity, is above 1600 mg/kg and 800 mg/kg in mice and rats, respectively. In a repeated-dose 26-week oral toxicity study, the no-observed-adverse-effect level for female and male SD rats was 180 mg/kg.

• 대한의생명과학회지
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• 제30권2호
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• pp.37-48
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• 2024

Liposomes are one of the most actively studied and promising drug delivery systems for the treatment of various diseases. In this study, an aptamer-conjugated liposome called "aptamosome" was used, in which an anti-PD-L1 aptamer targeting cancer cells was conjugated to the liposome. These aptamosomes showed remarkable cellular uptake and efficient delivery to Lewis lung carcinoma 2 (LL/2) cancer cells. In addition, suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor (HDACi), was delivered through this aptamer to induce a strong anticancer immunotherapeutic effect. The results of this study showed that when LL/2 cells were treated with SAHA-entrapped aptamosome [SAHA] and liposome [SAHA] and free SAHA, aptamosome [SAHA] improved cell death compared with that of liposomes [SAHA] or free SAHA, and it has demonstrated anticancer efficacy. Moreover, aptamosome [SAHA] induce the secretion of chemokines that promote the migration of activated T cells into tumor tissues. Finally, in vivo experiments showed that aptamosome [SAHA] significantly inhibited the growth rate of LL/2 tumors. Therefore, liposomes combined with an anti-PD-L1 aptamer for efficient SAHA delivery are suggested as an excellent model for drug delivery systems suitable for targeting cancer cells.

• 한국환경보건학회지
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• 제23권4호
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• pp.50-56
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• 1997

Applied for Drug Delivery System, polymer drug was prepared with chitosan and phthalylsulfathiazole. In spite of various application of chitin derivatives, commercial use of chitin has been limited due to highly resistance to chemicals and the absense of proper solvents. In this study, Chitosan were prepared from chitin which were deacetylated under various condition. The synthetic procedures of polymer drug were performed by acid chloride methods. The antibiotic activities of polymer drug exhibited growth-inhibitory activity against Staphylococcus aureus, Staphylococcus epidermidis, E. coli, Salmonella typhimurium, Klebsiella pneumoniae at the concentration of 471-514 $\mu$g/ml in general. Comparatively, Polymer drug exhibited broad antibacterial activity on MICs 897-1280 $\mu$g/ml against Gram-positive and Gram-negative bacteria including Staphylococcus aureus, Staphylococcus epidermidis and E. coli.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.87-92
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• 1999

Drug delivery to the brain may be achieved by producing chimeric peptide, attaching the drug to protein 'vectors' which are transported into the brain from the blood by a receptor-mediated transcytosis through the blood-brain barrier (BBB). Since the BBB expresses high concentrations of transferrin receptor, and it was reported that anti-transferrin receptor mouse monoclonal antibody (OX26) undergoes transcytosis through the BBB, it is logical to assume that a drug delivery system via transferrin receptor-mediated transcytosis is a promising strategy. In the present study, therefore, we tested feasibility of several OX26 based vectors for the brain delivery of a model drug. Avidin-based delivery vectors such as OX26-streptavidin (OX26-SA), OX26-neutralite avidin (OX26-NLA) were chemically synthesized vectors and OX26 immunoglobulin G 3 type $C_{H}3$ fusion avidin $(OX26\;IgG3C_H3-AV)$ was genetically engineered. To improve the efficiency of producing chimeric peptide, we used avidin-biotin technology. Pharmacokinetics of $[^3H]biotin$ bound to OX26-SA, OX26-NLA and $OX26\;IgG3C_H3-AV$ was determined by intravenous injection technique, and their stabilities in plasma were analyzed using HPLC. The brain delivery of $[^3H]biotin$ bound to OX26-SA, OX26-NLA and OX26\;$IgG3C_{H}3-AV$ (expressed as %ID/g brain) was $0.22{\pm}0.01$, $0.18{\pm}0.01$ and $0.25{\pm}0.09$, respectively. The areas under the plasma concentration versus time curve (AUC) for OX26-SA, OX26-NLA, $OX26\;IgG3C_H3-AV$ from time zero to 60 min were $209{\pm}10$, $195{\pm}9$, $134{\pm}29\;%ID\;min/ml$ respectively and their total clearances $(CL_{tot})$ were $1.00{\pm}0.09$, $1.08{\pm}0.07$ and $1.54{\pm}0.29\;ml/min/kg$, espectively. These results showed that these vectors possess preferable pharmaceutical (e.g., resonable stability) and pharmacokinetics (e.g., significant brain uptake and enhanced AUC) for brain delivery. Therefore, these vectors may be broadly useful in the brain delivery of drugs that are not transported into the brain to a significant extent.

• Bulletin of the Korean Chemical Society
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• 제33권10호
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• pp.3208-3212
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• 2012

Controlled drug delivery systems employing microparticles offer lots of advantages over conventional drug dosage formulations. Microencapsulation technique have been conducted with biodegradable polymers such as poly(lactic-co-glycolic acid) (PLGA) and poly(lactic acid) (PLA) for its adjustable biodegradability and biocompatibility. In this study, we evaluated two techniques, oil-in-water (o/w) emulsion solvent evaporation and spray drying, for preparation of polymeric microparticles encapsulating a newly synthesized drug, SS-AG20, for the long-term drug delivery of this low-molecular-weight drug with a very short half-life. Drug-loaded microparticles prepared by the solvent evaporation method showed a smoother morphology; however, relatively poor encapsulation efficiency and drastic initial burst were discovered as drawbacks. Spray-dried drug-loaded microparticles had an imperfect surface with pores and distorted portions so that its initial burst was critical (70.05-87.16%) when the preparation was carried out with a 5% polymeric solution. By increasing the concentration of the polymer, the morphology was refined and undesirable initial burst was circumvented (burst was reduced to 35.93-74.85%) while retaining high encapsulation efficiency. Moreover, by encapsulating the drug with various biodegradable polymers using the spray drying method, gradual and sustained drug release, for up to 2 weeks, was achieved.

• 한국진공학회:학술대회논문집
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• 한국진공학회 2016년도 제50회 동계 정기학술대회 초록집
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• pp.360.1-360.1
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• 2016

Hydroxyapatite (Ca10(PO4)6(OH)2, HAP) particles have attracted a great deal of attention in biomedical fields due to their good biocompatibility, bioactivity and fairly broad applications as drug delivery, dental implant, bone cement, and etc. Thus, many researchers have made an effort to add new functionalities such as luminescence, drug delivery, and bone regeneration properties up to HAP powders by controlling their nanostructure as well as composition. In this research, the mesoporous strontium substituted HAP (Sr-HAP) microspheres were synthesized using a hydrothermal method. In this synthesis, aspartic acid monomers were utilized to form microsphere by controlling surface energy of HAP particles and Sr ions were substituted into Ca ion sites, which induced luminescence property in HAP powders. Moreover, the change in the amount of Sr substitution was found to influence the particle size, morphology, and concurrently surface area, which led to changing drug loading as well as drug release property. The amount of Sr influences the morphology, luminescent properties, particle size, surface area cell viability and drug loading property, which are investigated by SEM, TEM, XRD, FTIR, BET, XPS and in vitro test such as MTT assay and drug release test. In particular, the multifunctional Sr-HAP with molar ratios of 0.25 (Sr/(Ca+Sr)) possessed the strongest luminescent property as well as the superior drug loading and sustained release properties that were correspondent with large surface area and pore size. Our study indicates that the fabricated multifunctional Sr-HAP microspheres are quite useful for bone regeneration and drug delivery.