The perfluorocarbon (PFC) nanoparticle is a sort of new drug carrier in recent years, and it has lots of unique properties such as chemical stability, favourable biocompatibility, high aerobic capacity, targeting action to tissues or cells and so on. In this paper, we summarize the physico-chemical properties of the PFC nanoparticles. We also show the research progress of the PFC nanoparticles as a kind of drug carrier for targeted therapy of cardiovascular system, nervous system diseases and tumor. Further more, its characteristics of being selectively in target cells, tissues, and rapid release of drugs are expounded. PFC nanoparticles, as drug carriers for targeted diagnosis and treatment, have good prospect and clinical application value.
Animals ; Biocompatible Materials ; pharmacology ; Chemical Phenomena ; Drug Carriers ; pharmacology ; Drug Delivery Systems ; Fluorocarbons ; pharmacology ; Humans ; Nanoparticles

This study aimed to prepare andrographolide (AP)-loaded glycyrrhizic acid (GA) micelles (AP-GA)-PMs to enhance the solubility and anti-tumor effect of andrographolide. Firstly, andrographolide (AP) was used as the model drug and glycyrrhizic acid (GA) as carriers to prepare (AP-GA)-PMs. Then the preparation methods and the ratios of drug and carrier were screened and optimized based on particle size, encapsulation efficiency (EE) and loading capacity of micelles. Finally, the pharmaceutical characters and the inhibition rate on HepG2 cells were evaluated on the (AP-GA)-PMs prepared by optimal process. The results showed that the prepared micelles under the optimal process had a nanosize of (127.11±1.38) nm, zeta potential of (-24.01±0.55) mV, the entrapment efficiency rate of (92.01±4.02)% , the drug loading rate of (51.44±1.24)% and high storage stability at 4 °C in 30 d, with slow but highly stable release. Moreover, (AP-GA)-PMs with the IC₅₀ value of 19.25 mg·L⁻¹ had a more synergistic and better anti-tumor effect in comparison with AP (IC₅₀=122.40 mg·L⁻¹) on HepG2 cells (P<0.01). In conclusion, the (AP-GA)-PMs prepared with glycyrrhizic acid as a carrier had a small particle size, large drug loading capacity, and high stability, and could significantly improve the anti-tumor effects of AP.
Antineoplastic Agents ; pharmacology ; Diterpenes ; pharmacology ; Drug Carriers ; chemistry ; Glycyrrhizic Acid ; chemistry ; Micelles ; Particle Size ; Polymers

Dendrimers are highly branched macromolecules that have attractive nano-sized architectures. It seems that they can enter various cells easily because of their unique nanostructures and chemical properties, which make them to be one of important candidates of non-virus carriers for drug delivery or gene therapy. However, the understanding of cytotoxicity and related mechanisms of dendrimers are still limited. In recent years there has been rapid increases of researches regarding the biological effects of dendrimers, including the interactions of dendrimers to cells, transport mechanisms, intracellular distribution and biodistribution in vivo, as well as improvement of biocompatibility of dendrimers by surface engineering. In this paper, recent advances in the investigations of biological effect and surface modification for the dendrimers as drug or gene delivery systems were reviewed.
Animals ; Dendrimers ; chemistry ; pharmacology ; Drug Carriers ; chemistry ; Drug Delivery Systems ; methods ; Humans ; Macromolecular Substances ; chemistry ; Nanostructures

L_9(3~4) orthogonal experiment design was used to optimize the preparation of the patches,and investigate its affecting factors and skin irritation. Eugenol was taken as the index component to study the release behavior in vitro and percutaneous penetration of Cangai oil transfersomes patches by HPLC.The results showed that the optimal prescription for preparing Cangai oil transfersomes patches were Eudragit E100 0.6 g, succinic acid 0.08 g,triethyl citrate 0.25 g,glycerol 0.2 g.Patches prepared by the preferred preparation had a flat appearance without obvious bubbles.The initial adhesion was 18.33±2.52, the stickiness was(30.01±2.45) min,and the peel strength was(5.62±0.95) kN·m~(-1).The results of affecting factors experiment showed the order of factors affecting its adhesion was humidity>temperature>lighting,and the skin irritation test results showed no significant skin irritation after 24 h of single administration. The results of drug release behavior in vitro showed that the release and the percutaneous penetration of both Cangai oil patches and Cangai oil transfersomes patches conformed to the Higuchi equation.The release amount of eugenol were 80.66% and 82.25% at 72 h, with no significant difference. The cumulative permeation area of eugenol per unit area reached(0.195 6±0.065 9),(0.131 0±0.045 5) mg·cm~(-2) at 72 h, with significant differences(P<0.05).The experiment results proved that the preparation process of Cangai oil transfersomes patches was stable,and the prepared patches had a good adhesion. At the same time,the preparation of transfersomes patches could alleviate and control the release of the drug to a certain extent, and provide a certain experimental basis for clinical pediatric drug safety.
Administration, Cutaneous ; Drug Carriers ; Drug Liberation ; Humans ; Plant Oils/pharmacology* ; Polymethacrylic Acids ; Skin/drug effects* ; Skin Absorption ; Transdermal Patch

1,3,5-Trimethylbenzene (1,3,5-TMB) was used as the pore-enlarging modifier to expand the pore size of MCM-41 (mobil company of matter) mesoporous silica nanoparticles. The solvent impregnation method was adopted to assemble non-water-soluble β-carotene into the pore channel of MCM-41. The MCM-41 and drug assemblies were characterized by TEM, FT-IR, elemental analysis and N2 adsorption-desorption. The results showed that MCM-41 has good sphericity and regular pore structure. The research also investigated the optimal loading time, the drug loading and the vitro stability of the β-carotene. As a drug carrier, the modified MCM-41 showing a shorter drug loading time, the drug loading as high as 85.58% and the stability of β-carotene in drug assemblies has improved. The study of this new formulation provides a new way for β-carotene application.
Drug Carriers ; chemistry ; Drug Delivery Systems ; Drug Stability ; Nanoparticles ; chemistry ; Silicon Dioxide ; chemistry ; beta Carotene ; chemistry ; pharmacology

To prepare Fe(3)O(4)-magnetic nanoparticles loaded with adriamycin and investigate the reversal role of drug-loaded nanoparticles in K562 and resistant cell line K562/A02, the drug-loaded nanoparticles were prepared by using mechanical absorption polymerization at different conditions of 4 degrees C or 37 degrees C for 24 or 48 hours. The survival of cells cultured with drug-loaded nanoparticles for 48 hours was detected by MTT assay, then the growth inhibition efficacy of cells was calculated. The results showed that the growth inhibition efficacy of both two cell lines was enhanced with increasing concentration of Fe(3)O(4)-magnetic nanoparticles. The inhibitory ratio of two cell lines obtained at 4 degrees C and for 48 hours was significantly better than that at 37 degrees C and 24 hours. In conclusion, Fe(3)O(4)-magnetic nanoparticles can load adriamycin by using mechanical absorption polymerization, but depended on proper temperature and time. Furthermore, drug-loaded nanoparticles showed an ability reversing multidrug resistance.
Doxorubicin ; chemistry ; pharmacology ; Drug Carriers ; chemistry ; Drug Resistance, Multiple ; drug effects ; Drug Resistance, Neoplasm ; drug effects ; Ferric Compounds ; pharmacology ; Humans ; K562 Cells ; Magnetics ; Nanoparticles ; chemistry ; Particle Size

Hyaluronan (HA), a natural glycoaminoglycan featuring an extracellular matrix, has been suggested as an effective biocompatible material. In this study, the effectiveness of HA microparticles as a carrier system for antibiotics was evaluated, and their physicochemical characteristics were determined. Microparticles were fabricated by the gelation of sulfadiazine (SD) loaded HA solution with calcium chloride through either a granulation (GR-microparticles) or encapsulation (EN-microparticles) process, and atelocollagen was incorporated into the microparticles as an additive in order to improve their physical properties. The characteristics of the microparticles were examined by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and swelling test. In vitro release experiments were performed for 7 days and the released amount of SD was determined using high-performance liquid chromatography (HPLC). Microscopic observations revealed that the collagen incorporated HA particles had a more compact surface than the HA particles. DSC analysis determined a loss of SD crystallinity in the particles. Calcium chloride retarded the swelling of particles, whereas the loaded drug contents did not affect this property. Both GR-and EN-microparticles sustained SD release with initial bursting effect. SD release from EN-microparticles was faster than from GR- microparticles. In addition, the release rate was dependent on the SD content in the microparticles. These results suggest that collagen modified HA microparticles have a potential as a release rate controlling material for crystalline drugs such as SD.
Antibiotics/*administration & dosage ; Calcium Chloride/pharmacology ; Collagen/*pharmacology ; *Drug Carriers ; Hyaluronic Acid/*administration & dosage ; Sulfadiazine/administration & dosage

OBJECTIVE: To construct a polylactic acid-glycolic acid-polyethylene glycol (PLGA-PEG) nanocarrier (N-Pac-CD133) coupled with a CD133 nucleic acid aptamer carrying paclitaxel for eliminating lung cancer stem cells (CSCs). METHODS: Paclitaxel-loaded N-Pac-CD133 was prepared using the emulsion/solvent evaporation method and characterized. CD133⁺ lung CSCs were separated by magnetic bead separation and identified for their biological behaviors and gene expression profile. The efficiency of paclitaxel-loaded N-Pac-CD133 for targeted killing of lung cancer cells was assessed in vitro. SCID mice were inoculated with A549 cells and received injections of normal saline, empty nanocarrier linked with CD133 aptamer (N-CD133), paclitaxel, paclitaxel-loaded nanocarrier (N-Pac) or paclitaxel-loaded N-Pac-CD133 (n=8, 5 mg/kg paclitaxel) on days 10, 15 and 20, and the tumor weight and body weight of the mice were measured on day 40. RESULTS: Paclitaxel-loaded N-Pac-CD133 showed a particle size of about 100 nm with a high encapsulation efficiency (>80%) and drug loading rate (>8%), and was capable of sustained drug release within 48 h. The CD133⁺ cell population in lung cancer cells showed the characteristic features of lung CSCs, including faster growth rate (30 days, P=0.001) and high expressions of tumor stem cell markers OV6(P < 0.001), CD133 (P=0.001), OCT3/4 (P=0.002), EpCAM (P=0.04), NANOG (P=0.005) and CD44 (P=0.02). Compared with N-Pac and free paclitaxel, paclitaxel-loaded N-Pac-CD133 showed significantly enhanced targeting ability and cytotoxicity against lung CSCs in vitro (P < 0.001) and significantly reduced the formation of tumor spheres (P < 0.001). In the tumor-bearing mice, paclitaxel-loaded N-Pac-CD133 showed the strongest effects in reducing the tumor mass among all the treatments (P < 0.001). CONCLUSION CD133 aptamer can promote targeted delivery of paclitaxel to allow targeted killing of CD133⁺ lung CSCs. N-Pac-CD133 loaded with paclitaxel may provide an effective treatment for lung cancer by targeting the lung cancer stem cells.
Animals ; Cell Line, Tumor ; Drug Carriers ; Lung ; Mice ; Mice, SCID ; Nanoparticles ; Neoplasms ; Neoplastic Stem Cells ; Paclitaxel/pharmacology* ; Polyethylene Glycols/pharmacology*

OBJECTIVETo compare the differences in antitumor activity between cisplatin (CDDP)-loaded liposomes and nanoparticles in vitro.

METHODSCDDP-gelatin nanoparticles (GPs-Pt) and CDDP-liposomes with similar size, zeta potential, drug loading efficiency and in vitro release property were prepared. The uptake in A549 cells and elimination kinetics were evaluated and antitumor activity was determined by MTT test. The internalization pathways of nanocarriers were studied with inhibitors.

RESULTSInternalization of two nanocarriers was clathrin and actin dependent. Pt accumulation delivered by GPs-Pt was significantly higher than that of liposomes. However, the results of kinetic analysis showed that liposomes had longer cellular retention, and the MRT and AUC were 3 times and twice of GPs-Pt, respectively. The IC(50) of liposomes was significantly lower than GPs-Pt. The values were 2.94±0.21 and 20.70±1.05 μg/ml, respectively.

CONCLUSIONNanocarriers with similar pharmaceutical parameters can induce differences in cellular internalization and elimination, which influence the antitumor activity eventually. Compared with gelatin nanoparticle, liposome is preferable for cisplatin delivery.

Adenocarcinoma ; pathology ; Antineoplastic Agents ; pharmacology ; Cell Line, Tumor ; Cisplatin ; pharmacokinetics ; pharmacology ; Drug Carriers ; Humans ; Liposomes ; Lung Neoplasms ; pathology ; Nanoparticles

Dendrimers are new macromolecules synthesized in recent years, which are of great interests in many fields where they have potential important applications because of their hyperbranched, well defined and monodisperse structures. In this paper, the unique structures, general synthesis routes and basic physical and chemical properties of dendrimers are introduced in brief, and the progress in the research of dendrimers in drug (gene) delivery, contrast agents, cancer therapy were reviewed, as well as the perspective in research and applications.
Contrast Media ; chemistry ; Dendrimers ; chemistry ; pharmacology ; Drug Carriers ; chemistry ; Drug Delivery Systems ; Gene Transfer Techniques ; Humans ; Polyamines