ABSTRACT
Tripterygium glycosides liposome(TPGL) were prepared by thin film-dispersion method, which were optimized accor-ding to their morphological structures, average particle size and encapsulation rate. The measured particle size was(137.39±2.28) nm, and the encapsulation rate was 88.33%±1.82%. The mouse model of central nervous system inflammation was established by stereotaxic injection of lipopolysaccharide(LPS). TPGL and tripterygium glycosides(TPG) were administered intranasally for 21 days. The effects of intranasal administration of TPG and TPGL on behavioral cognitive impairment of mice due to LPS-induced central ner-vous system inflammation were estimated by animal behavioral tests, hematoxylin-eosin(HE) staining of hippocampus, real-time quantitative polymerase chain reaction(RT-qPCR) and immunofluorescence. Compared with TPG, TPGL caused less damage to the nasal mucosa, olfactory bulb, liver and kidney of mice administered intranasally. The behavioral performance of treated mice was significantly improved in water maze, Y maze and nesting experiment. Neuronal cell damage was reduced, and the expression levels of inflammation and apoptosis related genes [tumor necrosis factor-α(TNF-α), interleukin-1β(IL-1β), BCL2-associated X(Bax), etc.] and glial activation markers [ionized calcium binding adaptor molecule 1(IBA1) and glial fibrillary acidic protein(GFAP)] were decreased. These results indicated that liposome technique combined with nasal delivery alleviated the toxic side effects of TPG, and also significantly ameliorated the cognitive impairment of mice induced by central nervous system inflammation.
Subject(s)
Mice , Animals , Tripterygium , Liposomes , Glycosides/therapeutic use , Administration, Intranasal , Lipopolysaccharides , Central Nervous System , Cognitive Dysfunction/drug therapy , Inflammation/metabolism , Tumor Necrosis Factor-alpha/metabolism , Cardiac GlycosidesABSTRACT
AIM: The DNA plasmid lipidosome (LP) vaccine based VEGFR2 extracellular region (exVEGFR2) was prepared in order to provide a new approach for cancer active immunotherapy. METHODS: High fidelity PCR was used to amplify the target sequence of exVEGFR2 with two restriction site of Kpn and Xba. The plasmid of pCMV/exVEGFR2 was constructed by connected exVEGFR2 with pCMV empty plasmid. The activity of immune activation was detected by ELISA. CTLs mediated cytotoxic activity was analyzed by
ABSTRACT
Small interfering RNA (siRNA) has been used to treat various skin diseases. However, siRNA is limited in application due to its electronegativity, strong polarity, easy degradation by nuclease and difficulty in breaking through the skin barrier. Therefore, safe and efficient siRNA delivery vector is the premise of effective treatment of skin diseases by siRNA. In recent years, with the deepening of research on siRNA, great progress has been made in the development of delivery systems based on lipids, polymers, peptides and nanoparticles, some new transdermal delivery vectors of siRNA have emerged, such as liposomes, dendrimers, cell penetrating peptides, and spherical nucleic acid nanoparticles. This review will focus on the recent advance in siRNA transdermal delivery vectors.
Subject(s)
Humans , Administration, Cutaneous , Genetic Vectors , RNA, Small Interfering , Skin Diseases , TherapeuticsABSTRACT
Triptolide had broad-spectrum and high-efficient anti-cancer activity, however, its clinical application was limited by the poor water solubility, in vivo rapid elimination, and strong toxicities and side effects. New drug delivery system was the ideal vehicle for targeted delivery of triptolide, which can effectively deliver triptolide to the cancer tissue, and increase the efficiency of tumor therapy. New drug delivery system had great application prospect in improving solubility of triptolide, reducing side effect, and increasing bioavailability. This article reviewed the research progress of new drug delivery system of triptolide based on liposome, polymer micelle and nanoparticle in the past decade, providing some references for the development and application of new drug delivery system of triptolide.
ABSTRACT
Baicalin is a kind of flavonoids derived from Scutellaria baicalensis with obvious pharmacological activities. Studies have shown that baicalin can be used in the treatment of pneumonia, tumor and hepatitis and other diseases. However, the poor water solubility and liposolubility of baicalin lead to the low bioavailability of it, which limits the clinical efficacy of baicalin. Therefore, in recent years, new dosage forms of baicalin have been prepared by new technology to improve its physical properties. Based on this, this paper reviews the research progress of pharmacological action and new dosage forms of baicalin based on the relevant literatures at home and abroad, in order to provide reference for the application and research of baicalin.
ABSTRACT
Objective To constract and evaluate the cationic anticancer peptide Temporin-1CEa liposomes and evaluate anti-breast cancer activity in vitro.Methods The polyethylene glycol (PEG)-modified liposomes containing Temporin-1CEa, one recently discovered cationic anticancer peptide ( CAP) , were constructed by using reverse-phase evaporation method.The encapsulation efficiency, particle size and Zeta potential of the Temporin-1CEa-containing liposomes (Temporin-1CEa-LIP) were characterized.In addition, that had the furhter evaluated of the stability and specific toxicity against human breast cancer MCF-7 cells in vitro.Results The data suggested that the PEG-modified liposomes served a promising drug delivery system for CAPs, those indicated by the encapsulation efficiency was (55.57 ±1.56)%, the particle size was (105.3 ±1.37) nm and the Zeta potential was ( -16.17 ±0.964) mV.Moreover, the in vitro test also indicated that Temporin-1CEa-LIP exerted good stability in serum, and it could be efficiently uptaken by MCF-7 cells.Most importantly, after 24h exposure, Temporin-1CEa-LIP showed toxicity against MCF-7 cells, as potent as Temporin-1CEa. Conclusion The results demonstrates that the PEG-modified liposome is a good drug-delivery system and Temporin-1CEa-LIP could serve as potential anti-tumor candidate for cancer therapy.
ABSTRACT
Objective: To prepare the nepeta oil-oxymatrine (OMT) lipidosome pro vagina thermosensitive gel, and to investigate its in vitro drug release behavior. Methods: P-407 and P-188 were used as gel matrix to prepare the gel, and gelatinization temperature was applied as a target to optimize the prescription. The OMT lipidosome was prepared based on the multiple emulsion method, and the nepeta oil-OMT lipidosome pro vagina thermosensitive gel was obtained by cold-dissolving method. The content of OMT was determined by HPLC, and in vitro release properties of nepeta oil-OMT lipidosome thermosensitive in situ gel was investigated by dialysis method. Results: After optimization, the gel prescription was finally confirmed as 18% P-407, 5% P-188, and 0.2% hydroxy-propyl methyl cellulose (HPMC). The gelatination temperature for nepeta oil-OMT lipidosome thermosensitive gel was (36.8 ± 0.2)°C, and the in vitro accumulating release ratio of sinomenine in the nepeta oil-OMT lipidosome gel system was (58.89 ± 0.34)% and (66.38 ± 0.12)% after 48 h. Conclusion: The prepared nepeta oil-OMT lipidosome thermosensitive gel has the temperature sensitivity and sustained release effect, can effectively delay the release of the drug in vagina and improve the residence time in the vagina.