Polyamidoamine dendrimer and dextran conjugates: preparation, characterization, and in vitro and in vivo evaluation

2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Prabhat Shrivastava ◽  
Royana Singh ◽  
Sushant Shrivastava

AbstractAmide and ester conjugates of aceclofenac with polyamidoamine (PAMAM-G0) dendrimer zero generation and dextran (40 kDa) polymeric carrier, respectively, are presented. The prepared conjugates were characterized by UV, TLC, HPLC, IR, and 1H NMR spectroscopy. The average degrees of substitution of amide and ester conjugates were determined and found to be (12.5 ± 0.24) % and (7.5 ± 0.25) %, respectively. The in vitro hydrolysis studies showed that dextran ester conjugate hydrolyzed faster in a phosphate buffer solution of pH 9.0 as compared to PAMAM dendrimer G0 amide conjugate, and followed the first order kinetics. No amount of the drug was regenerated at pH 1.2 in simulated gastric fluid. The dextran conjugate showed short half-life as compared to the PAMAM dendrimer conjugate. Anti-inflammatory and analgesic activities of the dendrimer conjugate were found to be similar to those of the standard drug. Results of chronic ulceroginic activity showed deep ulceration and high ulcer index for aceclofenac, whereas lower ulcer index was found for the PAMAM dendrimer and dextran (40 kDa) conjugates. Experimental data suggest that PAMAM dendrimer and dextran (40 kDa) can be used as carriers for the sustained delivery of aceclofenac along with a remarkable reduction in gastrointestinal toxicity.

2011 ◽  
Vol 8 (4) ◽  
pp. 1209-1223 ◽  
Author(s):  
Raghavendra S. Navath ◽  
Anupa R. Menjoge ◽  
Hui Dai ◽  
Roberto Romero ◽  
Sujatha Kannan ◽  
...  

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1624
Author(s):  
Lili Qin ◽  
Xinyu Zhao ◽  
Yiwei He ◽  
Hongqiang Wang ◽  
Hanjing Wei ◽  
...  

Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.


2013 ◽  
Vol 63 (4) ◽  
pp. 545-551 ◽  
Author(s):  
Wei Li ◽  
Cai-Hong Shi ◽  
Yi-Ling Sheng ◽  
Ping Cui ◽  
Yu-Qing Zhao ◽  
...  

Abstract The aim of this study was to investigate the in vitro and in vivo performance of salbutamol sulfate press-coated tablets for delayed release. The in vitro release behavior of press-coated tablets with the outer layer of PEG 6000/ Eudragit S100 blends (2:1) in pH 1.2 (0.1 mol L-1 HCl) and then pH 6.8 buffer solution was examined. Morphological change of the press-coated tablet during in vitro release was recorded with a digital camera. Release of salbutamol sulfate from press-coated tablets was less than 5 % before 3 h and was completed after 8 h in pH 6.8 phosphate buffer solution. In vivo gamma scintigraphy study carried out on healthy men indicated that the designed system released the drug in lower parts of the GI tract after a lag time of 5 hours. The results showed the capability of the system of achieving delayed release of the drug in both in vitro and in vivo gamma scintigraphy studies.


2018 ◽  
Vol 11 (4) ◽  
pp. 2043-2050
Author(s):  
G. Nagarajaperumal ◽  
V.E. Idachristi ◽  
M. Karpakavalli ◽  
S. Mohan

Diabetes mellitus (DM) is most significant health problem in various developed and developing countries due to alteration of various clinical and pathological factors. Current work was intended for examine in vitro and in vivo anti diabetic competence of Cassia Auriculata flowers and its phytochemical analysis. The inhibitory effects on carbohydrate digestive enzyme α- amylase interaction with various extracts of Cassia Auriculata were contrast with acarbose. Hypoglycemic activity was executed with standard as a glibenclamide. Study indicated ethanolic extract showed higher action on α- amylase inhibition with assessment of IC50 value; 43.6%. Based on the above results of in vitro studies were used to selected ethanolic extract of Cassia Auriculata flower used for further study. Results of animal studies indicated that the ethanolic extract of C. Auriculata has shown dose dependent action (200 mg/ kg (1.20±0.91↓) and 400 mg / kg (4 ± 0.01↓) when compared to control and standard drug treated groups. Our study confirmed to ethanolic extract work through the α- amylase inhibition mechanism. Our view bioactive constituents confirm anti diabetic capacity and afford methodical source for validation of Cassia Auriculata flowers in ayurvedic formulations on diminution of DM prevalence.


Author(s):  
Dhadde Gurunath S ◽  
◽  
Mali Hanmant S ◽  
Sapate Rohit B ◽  
Vakhariya Rohan R ◽  
...  

In current study of natural antiparasiticin-vitroanthelmintic activity of methanolic extracts of Tylophoraindica leaves against Haemonchus contortusconducted. This study was conducted by preparing the plant extract in methanol by using maceration process. This methanolic extract of Tylophoraindica exhibited greater anthelminthic activity, thismethanolic extract resulted 100% mortality after 6 hours exposure at 50 mg/ml of concentration, the 90% of mortality shows after 6 hours exposure at the concentration of 25 mg/ml and 80% of mortality shows after exposure 6 hours at 12.5 mg/ml concentration. In the presence of albendazole (used as a reference standard drug)100 percent of worm mortality observed within 4 hours. After Post-exposureworm mortality was not found in phosphate buffer solution. Leading to the nature of phytoconstituents such as alkaloids, tannins and flavonoids etc., the extract shows greater worm mortality operation.


1998 ◽  
Vol 4 (S2) ◽  
pp. 1108-1109
Author(s):  
C.E. Gagna ◽  
J.H. Chen ◽  
H.R. Kuo ◽  
W.C. Lambert

The purpose of this scientific investigation was to determine the presence and specific cellular localization of left-handed Z-RNA, within germinative zone (GZ) epithelium of the lens (Fig. 1), using anti-Z-RNA IgG polyclonal antibodies. Right-handed B-DNA has the ability to adopt the Z-DNA conformation in vitro (Sinden, 1994). Right-handed A-RNA can be transformed into Z-RNA under specific conditions (Hall et al., 1984), and Z-RNA has been identified in cultured cells (Zarling et al., 1990). Strong evidence supports the idea of Z-DNA in vivo (Sinden, 1994). Removal of proteins by fixatives can induce supercoiling which stabilizes Z-DNA (Sinden, 1994).Anti-Z-RNA antibodies were produced in rabbits immunized with injections of Z-RNA: brominated-poly[ribosomal(G-C)]. For light microscopy, immunohistochemical studies (ABC method), normal dog lens tissues (1 yr old) were fixed in Carnoy's, embedded in paraffin and sectioned 2 μm thick. For electron microscopy (immunogold staining), pieces of epithelium from the GZ of normal dog lens (1 yr old) were fixed with 5% glutaraldehyde in 0.05 M phosphate buffer solution, pH 7.3.


2015 ◽  
Vol 104 (11) ◽  
pp. 3814-3823 ◽  
Author(s):  
Burçin Yavuz ◽  
Sibel Bozdagğ Pehlivan ◽  
İmran Vural ◽  
Nurşen Ünlü

Polymers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1074 ◽  
Author(s):  
Yun Zhao ◽  
Hui Liang ◽  
Shiqiang Zhang ◽  
Shengwei Qu ◽  
Yue Jiang ◽  
...  

Biodegradable devices for medical applications should be with an appropriate degradation rate for satisfying the various requirements of bone healing. In this study, composite materials of polylactic acid (PLA)/stearic acid-modified magnesium oxide (MgO) with a 1 wt% were prepared through blending extrusion, and the effects of the MgO shapes on the composites’ properties in in vitro and in vivo degradation were investigated. The results showed that the long-term degradation behaviors of the composite samples depended significantly on the filler shape. The degradation of the composites is accelerated by the increase in the water uptake rate of the PLA matrix and the composite containing the MgO nanoparticles was influenced more severely by the enhanced hydrophilicity. Furthermore, the pH value of the phosphate buffer solution (PBS) was obviously regulated by the dissolution of MgO through the neutralization of the acidic product of the PLA degradation. In addition, the improvement of the in vivo degrading process of the composite illustrated that the PLA/MgO materials can effectively regulate the degradation of the PLA matrix as well as raise its bioactivity, indicating the composites for utilization as a biomedical material matching the different requirements for bone-related repair.


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