The Therapeutic Potential of Anti-HER2 2Rs15d Nanobody Labeled with 225Ac – an In Vitro and In Vivo Evaluation

2019 ◽  
Vol 50 (4) ◽  
pp. S73-S74 ◽  
Author(s):  
Marek Pruszynski ◽  
Matthias D’huyvetter ◽  
Magdalena Rodak ◽  
Yana Dekempeneer ◽  
Edyta Cedrowska ◽  
...  
Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 333 ◽  
Author(s):  
Zhou ◽  
Ichikawa ◽  
Ikeuchi-Takahashi ◽  
Hattori ◽  
Onishi

A novel anionic nanogel system was prepared using succinylated glycol chitosan-succinyl prednisolone conjugate (S-GCh-SP). The nanogel, named NG(S), was evaluated in vitro and in vivo. S-GCh-SP formed a nanogel via the aggregation of hydrophobic prednisolone (PD) moieties and the introduced succinyl groups contributed to the negative surface charge of the nanogel. The resultant NG(S) had a PD content of 13.7% (w/w), was ca. 400 nm in size and had a -potential of −28 mV. NG(S) released PD very slowly at gastric pH and faster but gradually at small intestinal pH. Although NG(S) was easily taken up by the macrophage-like cell line Raw 264.7, it did not decrease cell viability, suggesting that the toxicity of the nanogel was very low. The in vivo evaluation was performed using rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis. NG(S) and PD alone were not very effective at 5 mg PD eq./kg. However, NG(S) at 10 mg PD eq./kg markedly suppressed colonic damage, whereas PD alone did not. Furthermore, thymus atrophy was less with NG(S) than with PD alone. These results demonstrated that NG(S) is very safe, promotes drug effectiveness and has low toxicity. NG(S) has potential as a drug delivery system for the treatment of ulcerative colitis.


2019 ◽  
Vol 50 (1) ◽  
pp. S7
Author(s):  
Marek Pruszynski ◽  
Matthias D’huyvetter ◽  
Magdalena Rodak ◽  
Yana Dekempeneer ◽  
Edyta Cedrowska ◽  
...  

2021 ◽  
Vol 16 (12) ◽  
pp. 18-23
Author(s):  
Shweta Dhanda ◽  
Praveen Kumar ◽  
Manjusha Choudhary ◽  
Suman Dhanda

Probiotics are live microbes which positively influence the health when consumed in adequate amount. Lactic acid bacteria (LAB) are commonly used probiotics and are generally found in yogurt and fermented foods. They provide barrier for pathogens by secreting peptides and other metabolites. Pediococcus acidilactici NCDC 252 is a LAB of dairy origin with probiotic attributes. NCDC 252 was studied for in vitro anti-inflammatory, antioxidant and antihyperglycemic activities. Anti-inflammatory activity was studied by human red blood cell (HRBC) membrane stabilization method, protein (albumin) denaturation inhibitory activity and heat induced haemolysis. Antioxidant activity was evaluated by α, α-diphenyl-β- picrylhydrazyl (DPPH) radical and hydrogen peroxide (H2O2) scavenging assays. Alpha amylase inhibition assay was performed to examine antihyperglycemic effect. NCDC 252 exhibited potent anti-inflammatory but moderate antioxidant and antihyperglycemic activities as compared to control. NCDC 252 exhibited 65%, 70% and 49% membrane stabilization, protein denaturation and heat induced activity respectively. Scavenging effect was 45 % and 60% in H2O2 and DPPH assays respectively. Alpha amylase inhibition was 48 %. These results suggest therapeutic potential of NCDC 252 and open new avenues to treat disorders related to free radical generation such as inflammation and diabetes mellitus after in vivo evaluation of NCDC 252 to confirm its efficacy in animals.


2021 ◽  
Vol 9 (2) ◽  
pp. 212
Author(s):  
Tatsuma Kishimoto ◽  
Waka Ishida ◽  
Tadahiro Nasukawa ◽  
Takako Ujihara ◽  
Isana Nakajima ◽  
...  

Post-operative endophthalmitis caused by Enterococcus spp. progresses rapidly and often results in substantial and irreversible vision loss. Therefore, novel alternative treatments that are effective against enterococcal endophthalmitis are required. Bacteriophage therapy has the potential to be an optional therapy for infectious diseases. Therefore, we investigated the therapeutic potential of three newly isolated enterococcal phages, phiEF7H, phiEF14H1, and phiEF19G, in E. faecalis-induced endophthalmitis. These phages could lyse the broad-range E. faecalis, including strains derived from endophthalmitis and vancomycin-resistant E. faecalis in vitro, as determined by the streak test. Morphological and genomic analyses revealed that these phages were classified into the Herelleviridae genus Kochikohdavirus. The whole genomes of these phages contained 143,399, 143,280, and 143,400 bp, respectively. Endophthalmitis was induced in mice by injection of three strains of E. faecalis derived from post-operative endophthalmitis or vancomycin-resistant strains into the vitreous body. The number of viable bacteria and infiltration of neutrophils in the eye were both decreased by intravitreous injection of phiEF7H, phiEF14H1, and phiEF19G 6 h after injection of all E. faecalis strains. Thus, these results suggest that these newly isolated phages may serve as promising candidates for phage therapy against endophthalmitis.


Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
J Bauer ◽  
F Dehm ◽  
A Koeberle ◽  
F Pollastro ◽  
G Appendino ◽  
...  

Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.


Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.


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