1.Construction of biotin-modified polymeric micelles for pancreatic cancer targeted photodynamic therapy.
Chunyue DENG ; Yingying LONG ; Sha LIU ; Zhangbao CHEN ; Chong LI
Acta Pharmaceutica Sinica 2015;50(8):1038-44
In this study, we explored the feasibility of biotin-mediated modified polymeric micelles for pancreatic cancer targeted photodynamic therapy. Poly (ethylene glycol)-distearoyl phosphatidyl ethanolamine (mPEG2000-DSPE) served as the drug-loaded material, biotin-poly(ethylene glycol)-distearoyl phosphatidyl ethanolamine (Biotin-PEG3400-DSPE) as the functional material and the polymeric micelles were prepared by a thin-film hydration method. The targeting capability of micelles was investigated by cell uptake assay in vitro and fluorescence imaging in vivo and the amounts of Biotin-PEG-DSPE were optimized accordingly. Hypocrellin B (HB), a novel photosensitizer was then encapsulated in biotinylated polymeric micelles and the anti-tumor efficacy was evaluated systemically in vitro and in vivo. The results showed that micelles with 5 mol % Biotin-PEG-DSPE demonstrated the best targeting capability than those with 20 mol % or 0.5 mol % of corresponding materials. This formulation has a small particle size [mean diameter of (36.74 ± 2.16) nm] with a homogeneous distribution and high encapsulation efficiency (80.06 ± 0.19) %. The following pharmacodynamics assays showed that the biotinylated micelles significantly enhanced the cytotoxicity of HB against tumor cells in vitro and inhibited tumor growth in vivo, suggesting a promising potential of this formulation for treatment of pancreatic cancer, especially those poorly permeable, or insensitive to radiotherapy and chemotherapy.
2.Long-circulating liposomal daptomycin enhances protection against systemic methicillin-resistant Staphylococcus aureus infection with improved therapeutic potential.
Xingliang HUANG ; Jin WU ; Tingting SU ; Yanhong LI ; Zhangbao CHEN ; Chong LI
Acta Pharmaceutica Sinica 2014;49(5):701-10
In the face of escalating problems with pathogen control, the development of proper formulations of existing antibiotics is as important as the development of novel antibiotics. Daptomycin is a lipopeptide antibiotic with potent activity against Gram-positive bacteria. Currently, only injectable solution of daptomycin has been approved for clinical use. In the present study, the formulation of PEGylated liposomal daptomycin (PLD) was prepared and optimized, and its efficacy against methicillin-resistant Staphylococcus aureus (MRSA252) strains was investigated. The obtained PLD had a mean vesicle diameter of (111.5 +/- 15.4) nm and a mean percent drug loading of (5.81 +/- 0.19) % with high storage stability. Potent activity of PLD against MRSA was demonstrated in vitro with a more sustained effect than that of conventional liposomal daptomycin and daptomycin solution. In addition, intravenous administration of a single dose (equal to human use) of PLD significantly increased the survival of mice in a MRSA252 systemic infection model compared with other formulations. Drug distribution in the lung was significantly enhanced following administration of PLD, and no measurable tissue lesions or pathological changes were detected during PLD treatment. Taken together, PEGylated liposomes loaded with daptomycin may represent a promising approach to reduce MRSA252 infections, especially those involving bloodstream dissemination, such as hematogenous pulmonary infection.
3.Silica-coated ethosome as a novel oral delivery system for enhanced oral bioavailability of curcumin.
Chong LI ; Li DENG ; Yan ZHANG ; Tingting SU ; Yin JIANG ; Zhangbao CHEN
Acta Pharmaceutica Sinica 2012;47(11):1541-7
The aim of this study is to investigate the feasibility of silica-coated ethosome as a novel oral delivery system for the poorly water-soluble curcumin (as a model drug). The silica-coated ethosomes loading curcumin (CU-SE) were prepared by alcohol injection method with homogenization, followed by the precipitation of silica by sol-gel process. The physical and chemical features of CU-SEs, and curcumin release were determined in vitro. The pharmacodynamics and bioavailability measurements were sequentially performed. The mean diameter of CU-SE was (478.5 +/- 80.3) nm and the polydispersity index was 0.285 +/- 0.042, while the mean value of apparent drug entrapment efficiency was 80.77%. In vitro assays demonstrated that CU-SEs were significantly stable with improved release properties when compared with curcumin-loaded ethosomes (CU-ETs) without silica-coatings. The bioavailability of CU-SEs and CU-ETs was 11.86- and 5.25-fold higher, respectively, than that of curcumin suspensions (CU-SUs) in in vivo assays. The silica coatings significantly promoted the stability of ethosomes and CU-SEs exhibited 2.26-fold increase in bioavailablity relative to CU-ETs, indicating that the silica-coated ethosomes might be a potential approach for oral delivery of poorly water-soluble drugs especially the active ingredients of traditional Chinese medicine with improved bioavailability.
4.Effect of Quality Control Circle on the Reasonable Ratio of Emergency Orthopedics Prescriptions
Xi CHENG ; Lei XI ; Ziming QIAN ; Tong YIN ; Yongwu CHEN ; Chenxia DU ; Hechun JIANG ; Zhangbao WU ; Tianlu SHI
China Pharmacist 2016;19(5):949-951
Objective:To study the effect of quality control circle(QCC)on the reasonable ratio of clinical prescriptions. Methods:The dispensed prescriptions in orthopedic emergency department were reviewed in our hospital,and the reasons of unreasonable prescriptions were analyzed. According to the QCC technique,the activities were implemented,the standardized work process was made out and the results were studied. Results:After the six-month QCC activities,the unreasonable ratio of emergency orthopedics prescriptions was reduced from 70% to 21% ,and the target yield rate was 140% and the improvement rate was 70% . Conclusion:The QCC has obvious effect on the improvement of reasonable ratio of emergency orthopedics prescriptions.