• Journal of Pharmaceutical Investigation
• /
• 제38권3호
• /
• pp.163-169
• /
• 2008

Liposomes are spherical vesicles composed of lipid bilayer membranes. However, the conventional liposomes have been found to be plagued by rapid opsonization and taken up by the reticuloendothelial system (RES), resulting in shortened circulation time and limited intracellular uptake to target cell. In this study, polyethyleneglycol-cationic liposomes (PCL) containing cationic lipid and DSPE-mPEG were prepared by thin film cast-hydration method. The PEG liposomes had approximately $97.0{\pm}1.3\;nm$ of mean particle diameter and $-21.7{\pm}1.2\;mV$ of zeta potential value. PCL had $96.4{\pm}1.8\;nm$ of mean particle diameter and $-8.7{\pm}1.1\;mV$ of zeta potential value with a decrease of about 10 mV compared to the PEG liposomes. Loading of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX in liposomes was about $95.0{\pm}1.9%$. Intracellular uptake and cytotoxicity of PCL were higher than that of PEG liposomes to murine B16F10 melanoma cells. In addition, anti-tumor activity of PCL was similar to that of PEG liposomes on growth of A549 human lung carcinoma in BALB/c mice. Consequently, PCL modified with cationic lipid may be applicable as anticancer drug carriers that can increase intracellular uptake and therapeutic efficacy.

• Journal of Pharmaceutical Investigation
• /
• 제41권2호
• /
• pp.95-102
• /
• 2011

An amphiphilic cationic branched methoxy poly (ethylene glycol)-branched polyethylenimine - poly(L-phenylalanine) (mPEG-bPEI-pPhe) block copolymer was successfully synthesized by ring-opening polymerization (ROP) of N-carboxyanhydride of L-phenylalanine (Phe-NCA) with mPEG-bPEI for the preparation of more stable polyelectrolyte complex (PEC) included a hydrophobic interaction. mPEG-bPEI was firstly prepared by the coupling of mPEG and bPEI using hexamethylene diisocyanate (HMDI). The structural properties of mPEG-bPEI-pPhe copolymers were confirmed by $^1H$ NMR. The copolymers exhibited a self-assemble behavior in water above critical aggregate concentration (CAC) in the range of 0.01-0.14 g/L. The CAC of copolymers obviously depended on the hydrophobic block content in the copolymers (the value decreased with the increase of the pPhe block content). The cationic copolymers have the ability to form multi-interaction complex (MIC) with bovine serum albumin (BSA) and plasmid DNA through multi-interaction (electrostatic and hydrophobic interaction). The physicochemical characterization of the complex was carried out by the measurement of zeta potential and particle size. Their zeta-potentials were positive (approximately +10 mV) and their sizes decreased with increasing pPhe contents in the copolymers (PPF/BSA wt% ratio = 2). The complex showed good stability at high ionic strength. Therefore, mPEG-bPEI-pPhe block copolymer was considered as a potential material to enhance the stability of complex including biotherapuetic drugs.

• 한국응용과학기술학회지
• /
• 제30권4호
• /
• pp.779-789
• /
• 2013

This study aimed to investigate the emulsifying properties of bovine lactoferrin in food emulsion system. First, lactoferrin solution was prepared to study its surface activities, such as surface adsorption characteristics and ${\zeta}$-potential. Second, some physicochemical properties of lactoferrin emulsion which resulted from variations of environmental conditions (i.e., pH or NaCl addition) were determined. As for surface adsorption characteristics evaluated by surface tension, it was decreased with increasing lactoferrin concentration in solution ($1{\times}10^{-5}{\rightarrow}0.2wt%$) and showed a plateau (${\fallingdotseq}44$mN/m) above 0.01 wt%. It was also changed with pH and the minimum value of 53.8 mM/m was observed at pI of lactoferrin. This was related to changes in ${\zeta}$-potential of the lactoferrin solution with respect to pH. Fat globule size of lactoferrin emulsion was decreased with increasing lactoferrin concentration and a stable emulsion was formed above 0.5 wt% lactoferrin in emulsion with fat globule size $d_{32}$ of ca. 0.33 ${\mu}m$ as confirmed by creaming stability experiment (i.e., Turbiscan). As with surface tension, fat globule size of lactoferrin emulsion also changed with pH and showed a maximum value at pI. As evaluated by Turbiscan, in the presence of NaCl, the lactoferrin emulsion showed instability in particular above 10 mM.

• Archives of Pharmacal Research
• /
• 제28권6호
• /
• pp.722-729
• /
• 2005

With the aim to improve the specificity and to reduce the cytotoxicity of polyethylenimine (PEI), we have synthesized the conjugates of the branched PEI (25 kDa) with transferrin. The trans-ferrin-PEI (TP) conjugates with five compositions were synthesized using periodate oxidation method and confirmed by FT-IR spectroscopy and gel permeation chromatography. The free amine contents of TP conjugates, which were able to condense and deliver DNA, increased as the amount of PEI increased. TP/DNA polyplexes were characterized by measuring gel elec-trophoresis, ethidium bromide fluorescence quenching, particle size and zeta potential of complexes. Complete complexation of the polyplexes was observed above the N/P ratio of 5 in TP/DNA, and above 3 in PEI/DNA, respectively. The zeta potential of the complexes decreased as the amount of transferrin in TP conjugates increased. Transfection efficiency of TP conjugates was evaluated in HeLa cell and Jurkat cell systems. Among the five compositions of TP conjugates, TP-2 system mediated a higher $\beta$-galactosidase gene expression than PEI system in Jurkat cell which was known to express elevated numbers of transferrin receptors. From the results of the cell viability based on MTT assay, TP conjugates showed lower cytotoxicity com-pared with the PEI system. We expect that the TP conjugate can be used efficiently as a non-viral gene delivery vector.

• Asian Pacific Journal of Cancer Prevention
• /
• 제17권8호
• /
• pp.3835-3838
• /
• 2016

Background: Breast cancer is one of the most frequent cancer types within female populations. Silibinin is a chemotherapeutic agent ative against cancer. Niosomes are biodegradable, biocompatible, safe and effective carriers for drug delivery. Objective:To prepare nanoniosomal silibinin and evaluate its cytotoxicity inthe T-47D breast cancer cell line. Materials and Methods: Niosomes were prepared by reverse phase evaporation of a mixture of span 20, silibinin, PEG-2000 and cholesterol in chloroform and methanol solvent (1:2 v/v). The solvent phase was evaporated using a rotary evaporator and the remaining gel phase was hydrated in phosphate buffer saline. Mean size, size distribution and zeta potential of niosomes were measured with a Zetasizer instrument and then nanoparticles underwent scanning electron microscopy. The drug releasing pattern was evaluated by dialysis and the cytotoxicity of nanoniosomes in T-47D cells was assessed by MTT assay. Results: Particle size, size variation and zeta potential of the niosomal nanoparticles were measured as $178.4{\pm}5.4nm$, $0.38{\pm}0.09$ and $-15.3{\pm}1.3mV$, respectively. The amount of encapsulated drug and the level of drug loading were determined $98.6{\pm}2.7%$ and $22.3{\pm}1.8%$, respectively; released drug was estimated about $18.6{\pm}2.5%$ after 37 hours. The cytotoxic effects of nanoniosome were significantly increased when compared with the free drug. Conclusions: This study finding suggests that silibinin nanoniosomes could serve as a new drug formulation for breast cancer therapy.

• 한국세라믹학회지
• /
• 제54권1호
• /
• pp.49-54
• /
• 2017

In this study, based on hydrolysis and condensation via $St{\ddot{o}}ber$ process of sol-gel method, synthesis of mono-dispersed silica nanoparticles was carried out with hydrophilic solvent. This operation was expected to be a more simplified process than that with organic solvent. Based on the sol-gel method, which involves simply controlling the particle size, the particle size of the synthesized silica specimens were ranged from 30 to 300 nm by controlling the composition of tetraethylorthosilicate (TEOS), DI water and ammonia solution, and by varying the stirring speeds while maintaining a fixed amount of ethanol. Increasing the content of DI water and decreasing the content of ammonia caused the particle size to decrease, while controlling the stirring speed at a high level of RPMs enabled a decrease of the particle size. X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) were utilized to investigate the success factors for synthesizing process; Field emission scanning electron microscopy (FE-SEM) was used to study the effects of the size and morphology of the synthesized particles. To analyze the dispersion properties, zeta potential and particle size distribution (PSD) analyses were utilized.

• Bulletin of the Korean Chemical Society
• /
• 제35권8호
• /
• pp.2290-2294
• /
• 2014

For the present study, rhEGF was encapsulated into solid lipid nanoparticles (SLNs). The SLNs were prepared by the $W_1/O/W_2$ double emulsification method combined with the high pressure homogenization method and the physical properties such as particle size, zeta-potential and encapsulation efficiency were measured. The overall particle morphology of SLNs was investigated using a transmission electron microscopy (TEM). The percutaneous skin permeation and accumulation property of rhEGF was evaluated using Franz diffusion cell system along with confocal laser scanning microscopy (CLSM). The mean particle size of rhEGF-loaded SLNs was $104.00{\pm}3.99nm$ and the zeta-potential value was in the range of -$36.99{\pm}0.54mV$, providing a good colloidal stability. The TEM image revealed a spherical shape of SLNs about 100 nm and the encapsulation efficiency was $18.47{\pm}0.22%$. The skin accumulation of rhEGF was enhanced by SLNs. CLSM image analysis provided that the rhEGF rat skin accumulation is facilitated by an entry of SLNs through the pores of skin.

• Asian-Australasian Journal of Animal Sciences
• /
• 제26권6호
• /
• pp.896-904
• /
• 2013

Cattle breeds have a striking effect on milk, including milk composition and technological characteristics. This study aims to compare milk composition, acidification activity, viscosity, milk dispersion system stability and casein molecular weight among three buffalo breeds in China. The technological characteristics of milk produced by three cattle breeds of river buffalo (Murrah), crossbreed 1st generation ($F_1$), crossbreed multiple generation ($F_H$, $H{\geq}3$) buffaloes were investigated. Cattle breeds showed evident effect on milk protein, fat and total solids content, but little effect on most of buffalo casein molecular weight. Milk fat, protein content and the viscosity of buffalo milk from river buffalo were lower than those of $F_1$ and $F_H$, so was the buffer capacity. The viscosity was negatively correlated to temperature and concentration. Results of stability coefficient showed that milk dispersion system had the best dynamic stability characteristics under pH 6.6 and 6 times dilution, while zeta potential of Murrah milk was slightly higher than that of hybrid offspring ($F_1$, $F_H$). SDS-PAGE results showed that buffalo ${\alpha}_s$-casein had a slightly faster mobility than standard ${\alpha}_s$-casein; while buffalo ${\beta}$-casein showed a slightly slower mobility than standard ${\beta}$-casein. There is no clear differences in molecular weight of ${\alpha}_s$-, ${\beta}$-, and ${\kappa}$-casein among Murrah, $F_1$ and $F_H$.

• Asian Pacific Journal of Cancer Prevention
• /
• 제17권4호
• /
• pp.2277-2284
• /
• 2016

Ribosome-inactivating protein (RIP) from Mirabilis jalapa L. leaves has cytotoxic effects on breast cancer cell lines but is less toxic towards normal cells. However, it can easily be degraded after administration so it needs to be formulated into nanoparticles to increase its resistance to enzymatic degradation. The objectives of this study were to develop a protein extract of M. jalapa L. leaves (RIP-MJ) incorporated into nanoparticles conjugated with Anti-EpCAM antibodies, and to determine its cytotoxicity and selectivity in the T47D breast cancer cell line. RIP-MJ was extracted from red-flowered M. jalapa L. leaves. Nanoparticles were formulated based on polyelectrolyte complexation using low viscosity chitosan and alginate, then chemically conjugated with anti-EpCAM antibody using EDAC based on carbodiimide reaction. RIP-MJ nanoparticles were characterised for the particle size, polydispersity index, zeta potential, particle morphology, and entrapment efficiency. The cytotoxicity of RIP-MJ nanoparticles against T47D and Vero cells was then determined with MTT assay. The optimal formula of RIP-MJ nanoparticles was obtained at the concentration of RIP-MJ, low viscosity chitosan and alginate respectively 0.05%, 1%, and 0.4% (m/v). RIP-MJ nanoparticles are hexagonal with high entrapment efficiency of 98.6%, average size of 130.7 nm, polydispersity index of 0.380 and zeta potential +26.33 mV. The $IC_{50}$ values of both anti-EpCAM-conjugated and non-conjugated RIP-MJ nanoparticles for T47D cells (13.3 and $14.9{\mu}g/mL$) were lower than for Vero cells (27.8 and $33.6{\mu}g/mL$). The $IC_{50}$ values of conjugated and non-conjugated RIP-MJ for both cells were much lower than $IC_{50}$ values of non-formulated RIP-MJ (>$500{\mu}g/mL$).

• Journal of Pharmaceutical Investigation
• /
• 제39권5호
• /
• pp.339-343
• /
• 2009

Recently, co-delivery of drug and gene has been attempted for higher therapeutic effects of anticancer agents. In this study, cationic liposomes were prepared using 1,2-dioleoyl-3-trimethylammoniopropane (DOTAP) as a cationic lipid to investigate the effect of drug loading on the physicochemical characteristics of cationic liposomes/DNA complexes. The complex formation between cationic liposomes and negatively charged plasmid DNA was confirmed and the protection from DNase was observed. Particle size of complexes was reduced not by drug loading, but by the increased ratio of cationic lipid to plasmid DNA. Meanwhile, zeta potential of complex was increased by the addition of cationic liposomes to complexes and the effect of drug loading on the zeta potential was not much higher than on particle size. Gel retardation of complexes was indicated when the complexation weight ratios of cationic lipid to plasmid DNA were higher than 24:1 for drug free complexes and 20:1 for drug loaded ones, respectively. Agarose gel retardation showed the similar complexation between plasmid DNA and drug free liposomes or drug loaded liposomes. Both complexes protected plasmid DNA from DNase independent of complexation temperature. From the results, drug loading may affect not the complex formation of cationic liposomes and plasmid DNA, but the particle size of complex.