Chelates are used in cancer as cytotoxic agent, as radioactive agent in imaging studies and in radioimmunotherapy.Various chelates based on ruthenium, copper, zinc, organocobalt, gold, platinum, palladium, cobalt, nickel and iron are reported as cytotoxic agent. Monoclonal antibodies labeled with radioactive metals such as yttrium-90, indium-111 and iodine-131 are used in radioimmunotherapy. This review is an attempt to compile the use of chelates as cytotoxic drugs and in radioimmunotherapy.
The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 32 full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t50%) and 70% (t70%) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t50% and t70% indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.
The present study was designed to evaluate the cardioprotective potential of aqueous flower extract of Bombax ceiba L., Malvaceae (BC), on the basis of biochemical and histopathological parameters in Adriamycin (Adr) induced myocardial infarction in rats and to compare with vitamin E, a known cardioprotective antioxidant. Male Wister rats were used as in vivo model for the study. BC was administered orally to Wister rats at different doses (150 mg/kg, 300 mg/kg and 450 mg/kg, b.w.) for six days/week for four weeks. Thereafter, all the groups except saline were administered Adr (20 mg/kg, i.p.). There was a significant decrease in myocardial superoxide dismutase, catalase and reduced glutathione in animals treated with Adr. Concurrently marked increase in extent of lipid peroxidation was reported. Co-treatment of BC/vitamin E and Adr resulted in an increase in the cardiac antioxidant enzymes and reduction in lipid peroxidation as compared to Adr-treated animals. Adr showed significant decrease (p<0.001) in the level of cardiac marker enzymes [Lactate dehydrogenase (LDH) and Serum glutamic oxaloacetic transaminase (SGOT)] in heart homogenate with corresponding increase in their level in serum. In BC/vitamin E treated groups significant increase (p<0.001) of LDH in heart homogenate and decrease of SGOT and LDH in serum were observed. Microscopic studies in Adr-treated animals revealed mitochondrial swelling, leukocyte infiltration, lipid inclusions and myofibrillar loss whereas the pre-treatment with BC/vitamin E led to a lesser degree of Adr-induced histological alterations. These findings suggest that aqueous flower extract of BC has protective effect against Adr-induced cardiotoxicity and may have potential as a cardioprotective agent.
The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.
The objective of this study was the selection of the most influential variable for the preparation of gastroretentive mucoadhesive nanoparticles of acyclovir. Nanoparticles were prepared by one-step desolvation method; effect of formulation and processing variables on various response variables were studied by a Taguchi standard orthogonal array L8 design. Independent variables studied were the amount of gelatin, amount of glutaraldehyde, amount of Pluronic F-68, acetone addition rate, pH, stirring time, and stirring speed. The dependent variables studied were the particle size, polydispersity index, amount of drug released in 6 h, time required to release 60% of drug, entrapment efficiency, loading efficiency, and mucoadhesiveness. The size of all nanoparticulate formulations prepared as per the experimental design (Taguchi screening design) varied between 165 and 1610 nm, PDI between 0.360 and 1.00, bioadhesiveness between 3.959 and 11.02 g, cumulative percent drug release in 24 h between 40.74 and 72.48, entrapment efficiency between 15.70 and 83.12, and loading efficiency between 39.72 and 80.49. Pareto ranking analyses showed that the two most important factors affecting the selected responses were amount of gelatin and amount of Pluronic F-68 (P<0.05).
The aim of our study was to improve the bioavailability of acyclovir (ACV) by delivery of mucoadhesive nanoparticles (NPs) and controlled delivery of drug at its absorption window. Central composite design was used by which the effects of independent variables (gelatin and Pluronic F-68) on various responses such as particle size, polydispersity index, entrapment efficiency, loading efficiency, drug release and mucoadhesive strength were studied. The optimised formulation was evaluated for morphology, stability, pharmacokinetic and gastrointestinal tracking. The optimised NPs were found to be nearly spherical. Changes in characteristics of NPs were not significant after six months of accelerated stability studies. In vivo mucoadhesion study showed significant retention of mucoadhesive NPs in upper gastro-intestinal tract for more than 12 h. Pharmacokinetic study in rats revealed that mucoadhesive NPs could maintain relatively steady plasma concentration of ACV for more than 10 h. The AUC0-∞ and mean residence time of optimised formulation (7527.9 ng h/mL and 12.09 h) were significantly high than tablet dispersion (3841.13 ng h/mL and 7.97 h).
Azetidin-2-one fused 2-chloro-3-formyl quinolines derivatives, 3-chloro-4-(2-chloro-8/7/6-methoxyquinolin-3-yl)-1-(2,4-dinitro/4-nitro phenylamino)azetidin-2-one,3-chloro-4-(2-chloro-8/7/6-chloroquinolin-3-yl)-1-(2,4-dinitro/4-nitro phenylamino)azetidin-2-one, 3-chloro-4-(2-chloro-8/7/6-methylquinolin-3-yl)-1-(2,4-dinitro/4-nitrophenylamino) azetidin-2-one were synthesized by four steps, respectively from N-arylacetamides, 2-chloro-3-formyl quinolines, 2,4-dinitro/4-nitro phenyl hydrazine reflux with chloroacetyl chloride and triethyl amine. However yields of quinolines having electron donating groups in all cases. The structures of the synthesized compounds have been established on the basis of physical and spectral data. The antibacterial and antifungal activity of these compounds was tested by filter paper disc method against Staphylococcus aureus (MTCC96), Escherichia coli (MTCC722) and Candida albicans (MTCC183). The results showed that azetidin-2-one fused 2-chloro-3-formyl quinolines derivatives are better in inhibiting the growth of both types of organisms. Compounds AZT b2, AZT b3 to AZT g2, AZT g3 were found to be more potent compared to standard drug.
Background The present study was designed to investigate the therapeutic effects against oxidative stress and alleviative effects of Peganum harmala seeds (PH) in rats with Complete Freund’s Adjuvant (CFA) induced arthritis. Methods The extract was evaluated for its phytoconstituents, antiarthritic and antioxidant properties. The action of chloroform (PHC) and ethanolic (PHE) extracts of PH was evaluated in adult Lewis rats (150-200 g).with CFA induced arthritis. Arthritic rats received PH extracts 100 mg/kg orally for 28 consecutive days (Prophylactic treatment) and from 14th day of CFA injection (Therapeutic treatment). Results PHE significantly suppressed the arthritis severity in rats than PHC in 28 days. All complications shown significant reduction (p< 0.05) in arthritic rats including paw volume (63.09%), body weight loss, decreased locomotor activity, erythrocyte sedimentation rate and synovial/hepatic tissues lipid peroxidation and increase in cellular antioxidants superoxide dismutase (U/mg) activities and hemoglobin counts. The results showed the presence of alkaloids and flavonoids in PHE. Histology and radiographic analysis of arthritic ankle joints indicated abnormal changes. Marked reduction in inflammation and arthritic changes were observed after treatment with PHE. Conclusion Therefore, the investigation suggests that PHE at 100 mg/kg will be useful in the management of rheumatoid arthritis complications which may possibly be due to boosting the intracellular antioxidant defense.
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