Hepatoprotective and Antioxidant Effects of Saponarin, Isolated From Gypsophila Trichotoma Wend. on Paracetamol-Induced Liver Damage in Rats.

Hepatoprotective and Antioxidant Effects of Saponarin, Isolated from Gypsophila trichotoma Wend. on Paracetamol-Induced Liver Damage in Rats.

Biomed Res Int. 2013; 2013: 757126
Simeonova R, Vitcheva V, Kondeva-Burdina M, Krasteva I, Manov V, Mitcheva M

The hepatoprotective potential of saponarin, isolated from Gypsophila trichotoma, was evaluated in vitro/in vivo using a hepatotoxicity model of paracetamol-induced liver injury. In freshly isolated rat hepatocytes, paracetamol (100? ? mol) led to a significant decrease in cell viability, increased LDH leakage, decreased levels of cellular GSH, and elevated MDA quantity. Saponarin (60-0.006? ? g/mL) preincubation, however, significantly ameliorated paracetamol-induced hepatotoxicity in a concentration-dependent manner. The beneficial effect of saponarin was also observed in vivo. Rats were challenged with paracetamol alone (600?mg/kg, i.p.) and after 7-day pretreatment with saponarin (80?mg/kg, oral gavage). Paracetamol toxicity was evidenced by increase in MDA quantity and decrease in cell GSH levels and antioxidant defence system. No changes in phase I enzyme activities of AH and EMND and cytochrome P 450 quantity were detected. Saponarin pretreatment resulted in significant increase in cell antioxidant defence system and GSH levels and decrease in lipid peroxidation. The biochemical changes are in good correlation with the histopathological data. Protective activity of saponarin was similar to the activity of positive control silymarin. On the basis of these results, it can be concluded that saponarin exerts antioxidant and hepatoprotective activity against paracetamol liver injury in vitro/in vivo. HubMed – drug

Assessment of palmitoyl and sulphate conjugated glycol chitosan for development of polymeric micelles.

Bioimpacts. 2013; 3(2): 97-100
Ullah Khan I, Ayub G, Ranjha NM

Introduction: Amphiphilic copolymers are capable of forming core shell-like structures at the critical micellar concentration (CMC); hence, they can serve as drug carriers. Thus, in the present work, polymeric micelles based on novel chitosan derivative were synthesized. Methods: Block copolymer of palmitoyl glycol chitosan sulfate (PGCS) was prepared by grafting palmitoyl and sulfate groups serving as hydrophobic and hydrophilic fractions, respectively. Then, fourier transform infrared spectra (FTIR) and spectral changes in iodine/iodide mixture were carried out. Results: FTIR studies confirmed the formation of palmitoyl glycol chitosan sulfate (PGCS) and spectral changes in iodine/iodide mixture indicated CMC which lies in the range of 0.003-0.2 mg/ml. Conclusion: Therefore, our study indicated that polymeric micelles based on palmitoyl glycol chitosan sulphate could be used as a prospective carrier for water insoluble drugs. HubMed – drug

Application of response surface methodology in development of sirolimus liposomes prepared by thin film hydration technique.

Bioimpacts. 2013; 3(2): 75-81
Ghanbarzadeh S, Valizadeh H, Zakeri-Milani P

Introduction : The present investigation was aimed to optimize the formulating process of sirolimus liposomes by thin film hydration method. Methods : In this study, a 3(2) factorial design method was used to investigate the influence of two independent variables in the preparation of sirolimus liposomes. The dipalmitoylphosphatidylcholine (DPPC) /Cholesterol (Chol) and dioleoyl phosphoethanolamine(DOPE) /DPPC molar ratios were selected as the independent variables. Particle size (PS) and Encapsulation Efficiency (EE %) were selected as the dependent variables. To separate the un-encapsulated drug, dialysis method was used. Drug analysis was performed with a validated RP-HPLC method. Results : Using response surface methodology and based on the coefficient values obtained for independent variables in the regression equations, it was clear that the DPPC/Chol molar ratio was the major contributing variable in particle size and EE %. The use of a statistical approach allowed us to see individual and/or interaction effects of influencing parameters in order to obtain liposomes with desired properties and to determine the optimum experimental conditions that lead to the enhancement of characteristics. In the prediction of PS and EE % values, the average percent errors are found to be as 3.59 and 4.09%. This value is sufficiently low to confirm the high predictive power of model. Conclusion : Experimental results show that the observed responses were in close agreement with the predicted values and this demonstrates the reliability of the optimization procedure in prediction of PS and EE % in sirolimus liposomes preparation. HubMed – drug

Inhibition of hTERT Gene Expression by Silibinin-Loaded PLGA-PEG-Fe3O4 in T47D Breast Cancer Cell Line.

Bioimpacts. 2013; 3(2): 67-74
Ebrahimnezhad Z, Zarghami N, Keyhani M, Amirsaadat S, Akbarzadeh A, Rahmati M, Mohammad Taheri Z, Nejati-Koshki K

Introduction : Nowadays, using drug delivery is an essential method to improve cancer therapy through decreasing drug toxicity and increasing efficiency of treatment. Silibinin (C25H22O10), a polyphenolic flavonoid which is isolated from the milk thistle plant, has various applications in cancer therapy but it has hydrophobic structure with low water solubility and bioavailability. To increase the effect of silibinin, silibinin-loaded PLGA-PEG-Fe3O4 was prepared to determine the inhibitory effect of this nanodrug on Telomerase gene expression. Methods : The rate of silibinin loaded into PLGA-PEG-Fe3O4 was measured. Then, the cytotoxic effect of silibinin-loaded PLGA-PEG-Fe3O4 was determined by Methyl Thiazol Tetrazolium (MTT) assay. After that, inhibition of Telomerase gene expression was indicated through Real-time PCR. Results : Data analysis from MTT assay showed that silibinin-loaded PLGA-PEG-Fe3O4 had dose dependent cytotoxic effect on T47D cell line. MTT assay showed no cytotoxic effect of free PLGA-PEG-Fe3O4 on T47D breast cancer cell line. Real Time PCR analysis showed that the level of telomerase gene expression more efficiently decreased with silibinin-loaded PLGA-PEG-Fe3O4 than with free silibinin alone. Conclusion : The present study indicates that this nanodrug causes down-regulation of Telomerase gene expression in cancer cells. Therefore, PLGA-PEG-Fe3O4 could be an appropriate carrier for hydrophobic agents such as silibinin to improve their action in cancer therapy. HubMed – drug

Complications due to the use of BMP/INFUSE in spine surgery: The evidence continues to mount.

Surg Neurol Int. 2013; 4(Suppl 5): S343-52
Epstein NE

Increasingly, adverse events (AE) attributed to utilizing BMP/INFUSE (Bone Morphogenetic Protein, Medtronic, Memphis, TN, USA) “off-label” in spine surgery are being reported. In 2008, the Food and Drug Administration (FDA) issued a warning that in anterior cervical spine surgery, the “off-label” use of BMP/INFUSE contributed to marked dysphagia, hematoma, seroma, swelling, and/or the need for intubation/tracheostomy. Subsequent studies have cited the following AE; heterotopic ossification (HO), osteolysis, infection, arachnoiditis, increased neurological deficits, retrograde ejaculation, and cancer. Furthermore, in 2011, Carragee et al. noted that 13 of the original industry-sponsored BMP/INFUSE spinal surgery studies failed to acknowledge multiple AE. Additionally, in 2012, Comer et al. observed that the frequency of retrograde ejaculation reported for BMP/INFUSE used “on-label” to perform Anterior Lumbar Interbody Fusion/Lumbar Tapered Fusion-Cage Device (ALIF/LT-Cage) was also largely “under-reported.” To summarize, there is mounting evidence in the spinal literature that utilizing BMP/INFUSE in spinal fusions contributes to major perioperative and postoperative morbidity. HubMed – drug