Lecithin-Based Novel Cationic Nanocarriers (Leciplex) II: Improving Therapeutic Efficacy of Quercetin on Oral Administration

2011 ◽  
Vol 8 (3) ◽  
pp. 716-726 ◽  
Author(s):  
Abhijit A. Date ◽  
Mangal S. Nagarsenker ◽  
Shilpa Patere ◽  
Vivek Dhawan ◽  
R. P. Gude ◽  
...  
2015 ◽  
Vol 50 (3) ◽  
pp. 123-126
Author(s):  
Tomokazu Takano ◽  
Yoshitsugu Mizuno ◽  
Yutaka Fukuda ◽  
Tomomasa Matsuyama ◽  
Takamits Sakai ◽  
...  

2021 ◽  
Author(s):  
Amirhosein Kefayat ◽  
Maryam Hosseini ◽  
Fatemeh Ghahremani ◽  
mohammad rafienia

Abstract Background: Mebendazole (MBZ) is a well-known anti-parasite drug with significant anti-cancer properties. However, MBZ exhibits low solubility, limited absorption efficacy, extensive first-pass effect, and low bioavailability. Therefore, multiple oral administration of high dose MBZ is required daily for achieving the therapeutic serum level which can cause severe side effects and patients’ non-compliance. Method: In the present study, MBZ-loaded/folic acid-targeted chitosan nanoparticles (CS-FA-MBZ) were synthesized, characterized, and used to form cylindrical subcutaneous implants for 4T1 triple-negative breast tumor (TNBC) treatment in BALB/c mice. The therapeutic efficacy of the CS-FA-MBZ implants was investigated after subcutaneous implantation in comparison with Control (no-treatment), MBZ (40 mg/kg, oral administration, twice a week for 2 weeks), and CS-FA implants, according to 4T1 tumors’ growth progression, metastasis, and tumor-bearing mice survival time. Also, their biocompatibility was evaluated by blood biochemical analyzes and histopathological investigation of vital organs. Results: The CS-FA-MBZ implants were completely degraded 15 days after implantation and caused about 73.3%, 46.5%, 37.3% decrease in the mean tumors’ volume in comparison with the Control (1050.5±120.7 mm3), MBZ (561.7±70.3 mm3), and CS-FA (658.3±88.1 mm3) groups, respectively. Average liver metastatic colonies’ number per microscope field at the CS-FA-MBZ (8.6±1.9) group was significantly (P<0.05) lower than the Control (24.5±4.1), MBZ (14.1±2.5), and CS-FA (15.7±3.1) groups. In addition, the CS-FA-MBZ treated mice exhibited about 51%, 24%, and 17% more survival time (days) after the cancer cells injection in comparison with the Control, MBZ, and CS-FA groups, respectively. Moreover, the CS-FA-MBZ implants were completely biocompatible based on histopathology and blood biochemical analyzes. Conclusion: Taking together, CS-FA-MBZ implants were completely biodegradable and biocompatible with high therapeutic efficacy in a murine TNBC model.


Author(s):  
V.V. Petrov ◽  
M.S. Matsinovich ◽  
A.A. Belko ◽  
A.A. Matsinovich ◽  
E.V. Romanova

Determination was carried out of indicators of acute toxicity and therapeutic efficacy of a veterinary drug “Gamitrovet”, containing gamithromycin as AAS, for respiratory diseases in calves, lambs and piglets. Indicators of acute toxicity were defined, and LD50 for a veterinary drug “Gamitrovet” was calculated, which after a single subcutaneous injection to white laboratory mice made 3757.5 mg / kg, and after a single oral administration to white laboratory mice made 04376.25 mg / kg. A veterinary drug “Gamitrovet” is an effective means in treatment of cattle, pigs and sheep with respiratory diseases, and allows achieving therapeutic efficacy in the range of 90 – 100%.


2021 ◽  
Vol 9 (1) ◽  
pp. 43-57
Author(s):  
E. V. Mazukina ◽  
E. V. Shekunova ◽  
V. M. Kosman ◽  
I. N. Urakova ◽  
I. G. Kotelnikova ◽  
...  

Chondroitin sulfate is used for osteoarthritis combination therapy. It should be taken into account that the structure and properties of polysaccharides included in chondroitin sulfate, as well as the raw materials used for its production, have a significant effect on its absorption, bioavailability, and, as a consequence, on the safety and efficacy of orally administered products.The aim of the study was to assess toxic properties, local irritant effect, immunotoxicity, basic pharmacokinetic parameters, and therapeutic efficacy of the new Chondroitin sulfate product (produced by Federal State Unitary Enterprise “Moscow Endocrine Plant”, Russia) as compared to Structum (produced by “Pierre Fabre Medicament Production”, France).Materials and methods: White Giant rabbits were used in the experiments. Toxicity, immunotoxicity and local irritation effects of the products were assessed following daily oral administration at the dose of 168 mg/kg (about 6 Maximum Recommended Therapeutic Doses) to male and female rabbits for 28 days. The follow-up period was 14 days. The pharmacokinetic study included blood sampling on days 1‒2 of the experiment, complete blood count and blood chemistry tests were performed on days 28 and 43. After killing the animals, pathomorphological and histological examinations were performed on their organs and tissues. Therapeutic efficacy was studied in an osteoarthritis model made by cruciate ligament transaction in rabbits. The animals received therapy at doses of 16.8 mg/kg, 33.6 mg/kg, and 67.2 mg/kg for 56 days starting from day 8 after the pathology induction.Results: the medicines had no toxic, local irritant, or immunotoxic effect. The NOAEL was established at 168 mg/kg. The study demonstrated the comparability of the pharmacokinetic profiles of the studied products following single oral administration. The maximum concentration of the active ingredient (Cmax = 79 ± 6 μg/mL—Chondroitin sulfate; Cmax = 71 ± 4 μg/mL— Structum) in blood plasma was observed within 3–4 hours after administration. A decrease in the severity of cartilage structural damage was observed for the doses of 33.6 mg/kg and 67.2 mg/kg. The results of quantitative determination of sulfated glycosaminoglicans in the proteoglycans of the cartilage articular surface in the animals with osteoarthritis demonstrated an increase in the level of sulfated glycosaminoglicans in the groups treated with the maximum doses of the studied products, as compared to the other groups.Conclusions: the obtained data confirm that the test product has a favourable safety profile, and therapeutic (chondroprotective) effect. All the tested properties of Chondroitin sulfate were comparable to those of Structum.


2019 ◽  
Vol 2019 (7) ◽  
pp. 25-32
Author(s):  
Владимир Оробец ◽  
Vladimir Orobec ◽  
Ольга Севостьянова ◽  
Ol'ga Sevost'yanova ◽  
Игорь Заиченко ◽  
...  

The effectiveness of the anthelmintic drug «Prazitel® Specialis suspension» for dogs and cats over 6 years of age in puppies and kittens with intestinal worm infection was studied. Suspension Prazitel® Specialis refers to low-hazard substances (hazard class IV according to GOST 12.1.007-76), contains a unique active substance R-praziquantel in combination with pyrantel pamoat and silybin. Efficiency of «Prazitel® Specialis suspension» for dogs weighing up to 5 kg after double oral administration to puppies at a dose of 1.0 ml/kg BW, which corresponds to a dose of R-praziquantel 1.5 mg/kg, pyrantel pamoate 15.0 mg/kg and silybin 1.7 mg/kg for toxocariasis, hookworm infection, dipylidiosis, teniosis and mixed invasion was 100 %. The effectiveness of «Prazitel® Special suspension» for dogs weighing from 5 to 25 kg after double oral administration to puppies at a dose of 1.0 ml/5,0 kg BW, which corresponds to a dose of R-praziquantel 1.5 mg/kg, pyrantel pamoate 20.0 mg/kg and silybin 1.7 mg/kg for toxocariasis, hookworm infection, dipylidiosis, teniosis and mixed invasion was 100 %. Anthelmintic drug «Prazitel® Specialis suspension» for cats after double oral administration to kittens at a dose of 1.0 ml/kg BW, which corresponds to a dose of R-praziquantel 1.5 mg/kg, pyrantel pamoate 15.0 mg/kg and silybin 1.7 mg/kg provides complete exemption animals from helminths with toxocariasis, hookworm infection, dipylidiosis, teniosis and mixed invasion. Thus, the high therapeutic effectiveness of the anthelmintic drug «Prazitel® Specialis suspension» for dogs and cats in puppies and kittens with intestinal worm infection has been experimentally confirmed.


Cancer ◽  
2004 ◽  
Vol 100 (4) ◽  
pp. 869-877 ◽  
Author(s):  
Hiroshi Kobayashi ◽  
Tatsuo Yagyu ◽  
Kiyokazu Inagaki ◽  
Toshiharu Kondo ◽  
Mika Suzuki ◽  
...  

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