Antilung cancer effect of ergosterol and cisplatin-loaded liposomes modified with cyclic arginine-glycine-aspartic acid and octa-arginine peptides.

BACKGROUND: Lung cancer is one of the most important diseases threatening human health, and targeted therapy has become the main research direction. This work, therefore, aimed to develop cyclic arginine-glycine-aspartic (RGD) and octa-arginine (R8) peptide-modified ergosterol (ERG)-combined cisplatin (diamminedichloridoplatinum(II) [DDP]) liposomes (LIP) as a drug delivery system. METHODS: Soybean phospholipids (SPC) and cholesterol (Chol) were selected to prepare different LIPs: ERG-loaded LIP (ERG-LIP), DDP and ERG-LIP (DDP/ERG-LIP), R8 peptide-modified DDP and ERG-LIP (R8-DDP/ERG-LIP), and cyclic RGD and R8-DDP/ERG-LIP (RGD/R8-DDP/ERG-LIP). The quality, tumor sphere penetrating ability, in vitro cellular uptake, mechanism of cellular uptake, and in vitro cytotoxicity of RGD/R8-DDP/ERG-LIP were evaluated. RESULTS: The LIP quality evaluation revealed that RGD/R8-DDP/ERG-LIP is round with a double-layer structure. The average particle size, dispersion coefficient of the polydispersity index (PDI), and zeta potential of RGD/R8-DDP/ERG-LIP were 155.2 ±â€Š8.7 nm, 0.102, and 4.74 ±â€Š0.7 mV, respectively. Furthermore, the LIPs were stable in the serum, and obviously inhibited the growth of A549 lung cancer cells with RGD/R8-DDP/ERG-LIP exhibiting the strongest inhibitory effect. The highest cellular uptake rate, which was at 4 hours, was exhibited by RGD/R8-DDP/ERG-LIP in a concentration-dependent manner. CONCLUSION: The results showed that LIP uptake by A549 cells was mainly by the clathrin-mediated endocytosis pathway (chlorpromazine). The results also suggest that RGD/R8-DDP/ERG-LIP might be a promising drug delivery system to improve antilung cancer drug effect and tumor-targeting in vitro.

Magnetic nanoparticles in cancer diagnosis, drug delivery and treatment.

In recent years, magnetic nanoparticles (MNPs) have demonstrated marked progress in the field of oncology. General nanoparticles are widely used in tumor targeting, and the intrinsic magnetic property of MNPs makes them the most promising nanomaterial to be used as contrast agents for magnetic resonance imaging (MRI) and induced magnetic hyperthermia. The properties of MNPs are fully exploited when they are used as drug delivery agents, wherein drugs may be targeted to the desired specific location in vivo by application of an external magnetic field. Early diagnosis of cancer may be achieved by MRI, therefore, individualized treatment may be combined with MRI, so as to achieve the precise definition and appropriate treatment. In the present review, research on MNPs in cancer diagnosis, drug delivery and treatment has been summarized. Furthermore, the future perspectives and challenges of MNPs in the field of oncology are also discussed.

[Study on determination method for components in monocrotalinum liposomes and their entrapment efficiency].

To establish an HPLC method for determining components in monocrotalinum liposomes. The results showed a good linear relationship in monocrotalinum liposomes within the concentration range between 1.6-102.4 mg x L(-1) (r = 0.999 8), with RSDs of intra-day precision, inter-day precision, stability and reproducibility of 0.61%, 0.92%, 1.7%, 1.6%, respectively. The recovery rate of monocrotaline was (99.96 +/- 0.50)%. These data indicated that the HPLC method could accurately determine components in monocrotalinum liposomes. Meanwhile, the microcolumn centrifugation method was established to determine the entrapment efficiency of components in monocrotalinum liposomes. As a result, the recovery rate and the blank liposome recovery of free components were (94.44 +/- 0.77)%, (95.86 +/- 0.68 )%, respectively. According to the parallel determination of the entrapment efficiency of three monocrotaline liposomes, their RSD was 4.0%. The data indicated that the microcolumn centrifugation method was an accurate and feasible method for determining the entrapment efficiency of monocrotaline liposomes.