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Objective To investigate whether poly arginine as the carrier can carry foreign proteins to penetrate the cell membrane and even penetrate the eyeball barrier.Methods Poly-Args (R9) was used as a CPP in this study.R9-green fluorescent protein (GFP) and GFP were constructed.In vitro,human lens epithelial cells were treated with these two proteins.Then,MTT assay were used to detect whether the protein could affect the proliferation of the cells.Flow cytometry and laser confocal microscopy were used to detect the penetrability of CPPs on the cells.In vivo,eyes of mice were treated with protein in eye drops way for 7 days.Then total protein were extracted,ELISA were used to detect the penetrability of CPPs.Results The results of MTT,flow cytometry and laser confocal microscopy showed that CPPs could carry protein into cells in a dose dependent manner without affecting cell proliferation.In vivo,slit lamp showed that the mice eyeballs had no any abnormal after treated by GFP,R9-GFP,and ELISA results also showed that R9 could effectively get foreign protein into the eyeball.Conelusion R9 can carry foreign protein into the cell membrane and eyeball barrier.This study provides the basis for the eye medication and dosing mode improvement.
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Objective To investigate the therapeutic effect of ciprofloxacin (Cipro) conjugated with 11 poly-arginine peptide (R11) on rabbit model with bacterial cystitis (BC). Methods 50 New Zealand rabbits of 4-month old were chosen to establish the models and evenly divided into 5 groups randomly : Group A: normal control; Group B: intravesical instillation (II) of R11; Group C: II of Cipro; Group D: II of R11-Cipro; Group E: intravenous injection of Cipro. Several parameters were observed which included: urinary frequency, positive rate of urine culture, histopathological analysis of cystitis stained with hematoxylin and eosin. Results Severe inflammatory responses and massive infiltration of inflammatory cells were observed after the models were established. R11-Cipro group was better than intravenous injection of Cipro group in treating cystitis (P < 0.05). R11-Cipro group was better than the other four groups in urinary frequency and urine culture. Conclusions Intravesical instillation of R11-Cipro demonstrated significant therapeutic effect on bacterial cystitis. R11 , as an efficient vector, could deliver specific antibiotics to bladder mucosa precisely and function well locally.
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Objective:To study the effect of molecular weight and degree of substitution (DS) of chitosan-poly-arginine (CS-R9) on transdermal penetration enhancement in vitro. Methods:Low molecular CS, medium molecular CS or high molecular CS was respectively used to synthesize CS-R9 with different molecular weight (LCS-R9-1, MCS-R9 and HCS-R9). Low molecular CS was used to synthesize CS-R9 with various degree of substitution by changing the mole ratio between R9 and CS (LCS-R9-1, LCS-R9-2 and LCS-R9-3). The in vitro transdermal penetration enhancement of the different CS-R9 on tinidazole ( TNZ) was studied using Franz diffusion cells. Results:According to the results of FTIR and 1 H-NMR, a series of target CS-R9 were synthesized including LCS-R9-1 with the DS of 2. 30, MCS-R9 with the DS of 2. 17, HCS-R9 with the DS of 2. 20, LCS-R9-2 with the DS of 8. 05 and LCS-R9-3 with the DS of 15. 87. Compared with the blank control group, Azone group, LCS group, R9 group and LCS+R9 group, LCS-R9-1 could enhance the in vitro transdermal penetration of TNZ significantly (P0. 05). When the molecular weight of CS was unchanged, the effect was increased with the rise of DS in the first 21h, however, after that, the effect was decreased with the rise of DS. Conclusion:Molecular weight and DS both have significant effect on the in vitro transdermal penetration enhancement of CS-R9, and it is valuable to further study the in vivo transdermal penetration enhancement of CS-R9 and underlying mechanisms.