scholarly journals Protection Effect of Self-Nanoemulsifying Drug Delivery System (SNEDDS) Piroxicam as Ulcerogenic Agent towards Malondialdehid Level and Protein Expression of Caspase-3, COX-1, COX-2 at Rat Gastric

2020 ◽  
pp. 273-283
Author(s):  
Iis Wahyuningsih ◽  
Kurnia Ambarwati ◽  
Erninda Ayu Hapsari ◽  
Afifah Fauziyyah ◽  
Azis Ikhsanudin ◽  
...  

The aim of this study was to determine the protection effect of SNEDDS piroxicam ulcerogenic agent against malondialdehyde (MDA) level and protein expression of caspase-3, COX-1, COX-2. The research was conducted using the test animals as much as 30 male white Sprague dawley (SD) rats aged 1-2 months with a weight of 100-200 grams divided into 5 groups. Treatment was given for 28 days orally. On the 29th day blood samples were also taken for the determination of MDA (Malondialdehid) levels by Thiobarbituric Acid Reactive Substance (TBARs) method using a visible spectrophotometer. Rats were sacrificed, then gastric organs were taken for immunohistochemical testing of caspase-3 and COX-1 expression, COX-2. The statistical analysis showed that the piroxicam SNEDDS group and the piroxicam suspension group decreased expression of the caspase-3 protein, increased COX-1 expression, decreased COX-2 and significantly decreased MDA levels. The piroxicam-containing SNEDDS (Self-Nanoemulsifying Drug Delivery System) form has protection against ulcogenic piroxicam.


2019 ◽  
Vol 12 (1) ◽  
Author(s):  
Ehsan Ahmadpour ◽  
Zahra Godrati-Azar ◽  
Adel Spotin ◽  
Roghayeh Norouzi ◽  
Hamed Hamishehkar ◽  
...  

Abstract Background The larval stage of the tapeworm Echinococcus granulosus is the causative agent of hydatid disease in humans. This zoonotic parasitic infection remains a major health problem in certain areas of the world where is still endemic. In view of the ineffectiveness of some drug treatments, the surgical removal of cysts remains the preferred treatment option together with the administration of albendazole and mebendazole. However, severe side effects of these drugs have been reported which demands developing new scolicidal agents that confer suitable efficacy and fewer side effects during surgery. Methods To that purpose, in the present work we assessed the effectiveness of ivermectin (IVM), a macrocyclic lactone endectocide that has shown to be an effective nematocidal drug against other important parasitic infections. To overcome the limitations observed in some drug formulations and resistance, we used nano lipid carriers (NLCs) as a targeted and sustained drug delivery system for IVM. We evaluated the in vitro cestocidal and apoptotic effects of NLCs-loaded IVM versus IVM by quantifying the expression of caspase-3 mRNA. Results We found that after 60 and 120 min of administration, 800 μg/ml and 400 μg/ml NLCs-loaded IVM induced 100% mortality, respectively. On the other hand, the 800 μg/ml of IVM induced 100% mortality rate 150 min after administration. Additionally, we found that NLCs-loaded IVM induced higher mRNA caspase-3 expression suggesting a more potent apoptotic effect on the parasite. Conclusions These data suggest that NLCs-loaded IVM may be a promising alternative to current treatments although in vivo studies are needed.



Blood ◽  
2015 ◽  
Vol 126 (23) ◽  
pp. 5558-5558 ◽  
Author(s):  
Wen Bao ◽  
Ran Liu ◽  
Baoan Chen ◽  
Fei Wang ◽  
Haijun Zhang ◽  
...  

Abstract Chemotherapy offers a systemic cancer treatment; however, it is limited in clinical administration due to its serious side effects. In cancer medicine, the use of nanoparticles (NPs) drug delivery system (DDS) can sustainedly release anticancer drug at the specific site and reduce the incidence of toxicity in normal tissues. In the present study, we aimed to evaluate the benefit of a novel chemotherapeutic DDS and its underlying mechanisms. Daunorubicin (DNR) was loaded into poly (lactic-co-glycolic acid) (PLGA)-poly-L-lysine (PLL)-polyethylene glycol (PEG)-transferrin (Tf) NPs to construct DNR-PLGA-PLL-PEG-Tf-NPs (DNR-loaded NPs) as a DDS. After incubating with PLGA-PLL-PEG-Tf-NPs, DNR, and DNR-loaded NPs, the leukemia K562 cells were collected and the intracellular concentration of DNR was detected by flow cytometry, respectively. Furthermore, the effect of drugs on the growth of tumors in K562 xenografts was observed and the relevant toxicity of therapeutic drugs on organs was investigated in vivo. Meanwhile, cell apoptosis in the excised xenografts was measured by transferase-mediated dUTP nick-end labeling assay, and the expression of apoptosis-related proteins, including Bcl-2, Bax, Caspase-9, Caspase-3, and cleaved-PARP, was determined by Western blotting analysis. Results showed that DNR-loaded NPs increased intracellular concentration of DNR in K562 cells in vitro and induced a remarkable improvement in anticancer activity in the xenografts in vivo. The expression of Bcl-2 protein was downregulated and that of Bax, Caspase-9, Caspase-3, and cleaved-PARP proteins were obviously upregulated in the DNR-loaded NPs group than that in other ones. Interestingly, pathological assessment showed no apparent damage to the main organs. In summary, the results obtained from this study showed that the novel NPs DDS could improve the efficacy of DNR in the treatment of leukemia and induce apoptosis via intrinsic pathway. Thus, it can be inferred that the new drug delivery may be a useful clinical tool. Disclosures No relevant conflicts of interest to declare.



Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
AR Bilia ◽  
G Capecchi ◽  
MC Salvatici ◽  
B Isacchi ◽  
MC Bergonzi


2017 ◽  
Author(s):  
A Uzunovic ◽  
S Pilipovic ◽  
A Sapcanin ◽  
Z Ademovic




2019 ◽  
Vol 43 (2) ◽  
pp. 101-116
Author(s):  
NABANITA MUKHERJEE ◽  
◽  
RITA LALA ◽  
INDRAJIT MUKHERJEE ◽  
◽  
...  


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