• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.426.1-426.1
• /
• 2002

In this study. we modified the cationic liposomes by polyethylene glycol (PEG)-grafted or PEG-added methods. The PEG-grafted transfection complexes were prepared by adding the plasmid DNA to the PEG-grafted cationic liposomes, composed of PEG and cationic lipids. PEG-added transfection complexes were prepared by adding the PEG to the mixture of cationic lipids and plasmid DNA. The particle sizes of PEG-modified transfection complexes did not change during storage compared to conventional transfection complexes. (omitted)

• Journal of Pharmaceutical Investigation
• /
• 제26권4호
• /
• pp.291-297
• /
• 1996

Liposomes of $pSV-{\beta}-Galactosidase$ vector plasmid DNA with various lipid composition were prepared by the thin-film method. Size distribution, shape and the efficiency of plasmid DNA encapsulation were investigated. Effect of sonication time on the plasmid DNA entrapment in liposomes and stability at $4^{\circ}C$ were also examined. Sizes of neutral liposomes were about 100-200 nm and above $1\;{mu}m$, and those of cationic liposomes were about 400-600 nm and above $1\;{mu}m$. Shapes of liposomes entrapped plasmid DNA were spherical. Proper sonication time for better entrapment was below 15 minutes and stability at $4^{\circ}C$ was decreased rapidly after 1 day. Plasmid DNA entrapments of complex liposomes of various lipids were higher than those of liposomes made from one sort of lipid. Plasmid DNA entrapments of cationic liposomes were higher than those of neutral liposomes.

• 대한화학회지
• /
• 제52권1호
• /
• pp.57-65
• /
• 2008

나노 또는 마이크로 크기를 가지는 구형의 약물 전달체이다. 그러나 일반적인 리포솜은 혈류 순환시 혈장 단백질과의 흡착이 일어나 안정성이 떨어지고, 세망내피계의 대식세포에 의해 옵소닌작용이 일어나 혈중에서 쉽게 소실되는 단점이 있다. 이에 본 연구에서는 모델단백질로 소혈청 알부민(BSA)을 사용하였고, BSA의 등전점보다 높은 pH를 나타내는 수용액에 용해하여 BSA가 음이온성을 갖도록 제조하였으며 이를 양이온성 리포솜 표면에 정전기적 인력에 의해 결합시켰다. 그리고 리포솜 표면에 코팅된 알부민을 60oC 이상의 온도에서 변성시켜 알부민이 코팅된 리포솜을 제조하였다. 대조 리포솜과 양이온성 리포솜의 입자크기는 104±1nm를 나타내었고, 변성된 알부민이 결합된 리포솜은 109±1nm의 입자크기를 나타내었다. 모델약물로서는 독소루비신(doxorubicin, DOX)을 사용하였고, 이온구배에 의한 리모트 로딩 방법을 사용하여 리포솜 내부에 DOX를 봉입시켰다. 혈장 내에서 리포솜의 안정성을 평가한 결과, 알부민이 결합된 리포솜은 입자크기의 변화가 관찰되지 않았고, 대조 리포솜과 양이온 리포솜에 비해 단백질 흡착이 억제되어 변성된 알부민으로 코팅된 리포솜은 혈류 내에서 장기 순환이 가능한 약물전달체로서 유용할 것이라 사료된다.

• 대한의생명과학회지
• /
• 제10권3호
• /
• pp.187-194
• /
• 2004

A short peptide corresponding to the nuclear localization signal (NLS) of human immunodeficiency virus (HIV)-l Tat protein, Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg, was employed to improve the efficiency of cellular uptake of nucleic acids. The peptide was first mixed with a reporter plasmid and then with cationic liposomes to form a tripartite complex of DNA/peptide/liposomes (DPL). Transfection efficiency of the DPL complex was compared with that of the conventional DNA/liposomes (DL) complex. When the DPL complex was formed with various cationic liposomes, DOTAP/DOPE (DP) liposome exhibited superior transfection efficiency to other liposomes tested in vitro. With the inclusion of the peptide, the DPL complex showed much enhanced transfection in various cancer cell lines. Particularly, transfection of the DPL complex in serum increased cellular uptake of a transgene up to 2 fold when compared with that in a serum free condition. Further, when the DPL complex was infused through the ureteric route of a rat, transfection efficiency was shown to be better in reporter gene expression than that obtained with the DL complex. This study shows that the DPL complex that is easy to formulate can be employed for much enhanced cellular uptake of a trans gene.

• Journal of Pharmaceutical Investigation
• /
• 제40권3호
• /
• pp.187-192
• /
• 2010

We aimed to evaluate the effect of temperature, pH, and light conditions on the stability of porcine placental extract (PPE)-loaded liposomes with different surface charges. The size distribution profiles and in vitro release patterns were investigated by dynamic light scattering method and spectrophotometry. The stability of PPE-loaded liposomes was affected by the surface charges of the liposomes. As compared to neutral and anionic liposomes, cationic liposome formulations showed significantly lower physical stability. At the test storage conditions of different temperatures and pHs, the mean sizes of cationic PPE-loaded liposomes substantially increased. In contrast, neutral and anionic liposomes did not reveal significant changes in mean sizes upon various storage conditions. The neutral and anionic liposomes showed no significant differences in the release profiles of PPE after storage at various temperatures and pHs. Our results indicate that anionic and neutral liposome compositions might be more suitable for the formulations of PPE providing the higher stability.

• 한국응용과학기술학회지
• /
• 제33권3호
• /
• pp.428-434
• /
• 2016

본 연구에서는 알킬체인의 길이가 서로 다른 benzyltrialkylammonium chloride계 화합물을 합성하여 리포좀 제조에 응용하였다. 제조된 리포좀의 평균 입도분포, 제타전위, 방출거동 및 항균성을 조사하였으며, 사슬 길이에 따른 특성을 비교하였다. 리포좀의 평균 입도는 120~140 nm의 크기분포를 가졌으며 소수성 사슬의 길이가 증가할수록 큰 입자크기를 가졌다. 리포좀 용액의 제타전위는 양이온성 계면활성제인 benzyltrialkylammonium chloride를 첨가함에 따라 +80~90 mV의 값을 가지며 향상된 분산 안정성을 보였다. 방출거동에서는 사슬 길이에 따라 방출 속도를 조절할 수 있었으며 긴 사슬의 계면활성제를 첨가한 리포좀은 증가된 서방형 방출특성을 보였다. 또한, 리포좀의 포집효율은 25.9~27.5% 이었다.

• Journal of Microbiology and Biotechnology
• /
• 제20권4호
• /
• pp.821-827
• /
• 2010

Gene delivery that provides targeted delivery of therapeutic genes to the cells of a lesion enhances therapeutic efficacy and reduces toxic side effects. This process is especially important in cancer therapy when it is advantageous to avoid unwanted damage to healthy normal cells. Incorporating cancer-specific ligands that recognize receptors overexpressed on cancer cells can increase selective binding and uptake and, as a result, increase targeted transgene expression. In this study, we investigated whether a peptide capable of homing to hepatocellular carcinoma (HCC) could facilitate targeted gene delivery by cationic liposomes. This homing peptide (HBP) exhibited selective binding to a human hepatocarcinoma cell line, HepG2, at a concentration ranging from 5 to 5,000 nM. When conjugated to a cationic liposome, HBP substantially increased cellular internalization of plasmid DNA to increase the transgene expression in HepG2 cells. In addition, there was no significant enhancement in gene transfer detected for other human cell lines tested, including THLE-3, AD293, and MCF-7 cells. Therefore, we demonstrate that HBP provides targeted gene delivery to HCC by cationic liposomes.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.427.1-427.1
• /
• 2002

To improve stability and transfection efficiency, a novel combination of cationic emulsion and galactosylated chitosan was developed for targeted gene delivery. Six formulations of cationic liposome and our novel emulsion were prepared for comparison of stability and transfection efficiency. Cationic liposomes composed of 3［N-(N.N dimethylaminoethylene) carbamoyl］ cholesterol (DC-Chol) and dioleyl phophatidyl ethanolamine (DOPE) were prepared by extrusion method and cationic emulsions composed of DC-Chol. DOPE. castor oil, and Tween 80 were prepared by sonication method. (omitted)

• Biomolecules & Therapeutics
• /
• 제19권2호
• /
• pp.231-236
• /
• 2011

The aim of this study was to investigate the effect of charge carrier lipid on the skin penetration, retention, and hair growth of topically applied finasteride-containing liposomes. Finasteride-containing liposomes were prepared by traditional thin film hydration method using Phospholipon$^{(R)}$ 85 G and cholesterol with or without charge carrier lipid (1,2 dimyristoyl-sn-glycero-3-phosphate or 1,2-dioleoyl-trimethylammonium-propane for anionic and cationic charge, respectively). Freshly prepared finasteride-containing liposome suspension was applied on the hairless mouse skin, and skin penetration and retention were measured using Keshary-Chien diffusion cell. Non-liposomal formulation (ethanol 10% solution containing 0.5 mg/ml of FNS) was also used as a control. The amount of finasteride in the diffusion cell and mouse skin was measured by HPLC. The hair growth was evaluated using depilated male C57BL/6N mice. Mean particle size of all finasteride-containing liposomes was less than a micron, and polydispersity index revealed size homogeneity. Skin penetration and retention studies showed that significantly less amount of finasteride was penetrated when applied as anionic liposome while more amount of the drug was retained. Specifically, in liposome prepared with 10% anionic charge carrier lipid, penetration was 12.99 ${\mu}g/cm^2$ while retention was 79.23 ${\mu}g/cm^2$ after 24 h of application. In hair growth study, finasteride-containing anionic liposomes showed moderate efficacy, but the efficacy was not found when applied as cationic liposomes. In conclusion, topical application of finasteride using anionic liposome formulation appears to be useful option for the treatment of androgenetic alopecia to avoid systemic side effects of the drug.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.300.2-300.2
• /
• 2003

Unlike cationic liposome/DNA complexes, neutralliposomes containing plasmid DNA are stable in blood and does not selectively entrapped in the lung. The objective of this study was to construct neutral liposomes containing plasmid DNA with optimal encapsulation efficiency. Plasmid DNA (pGL2 clone 753,-6 kb) was encapsulated by the freeze/thawing method into liposomes composed of 1-palmitoyl-2-oleyl-sn-glycerol-3-phosphocholine(POPC), didodecyldimethylammonium bromide(DDAB), distaroylphosphatidyl-ethanolamine polyethylene glycol 2000(DSPE-PEG 2000) and DSPE-PEG 2000-maleimide. (omitted)