scholarly journals Characterization and biodistribution of trans resveratrol-PEG-folic acid-gold nanoparticle conjugates

2022 ◽  
Vol 20 (2) ◽  
pp. 223-230
Author(s):  
Azhoma Gumala ◽  
Sutriyo ◽  
Fadlina Chany Saputri

Purpose: To evaluate the characteristics and biodistribution of trans resveratrol-PEG-folic acid-gold nanoparticle conjugates (rsv-PEG-FA-AuNP). Methods: Gold nanoparticles were produced by citric reduction followed by conjugation of PEG-folic acid and resveratrol. Characterization of rsv-PEG-FA-AuNP conjugates including their particle size, zeta potential, and by Fourier transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM) was carried out. Biodistribution study of rsv-PEG-FA-AuNP was carried out using female Sprague Dawley rats. Biodistribution data were obtained from high performance liquid chromatography (HPLC) analysis. Results: The mean particle size and zeta potential of rsv-PEG-FA-AuNP were 249.03 ± 10.31 and - 36.33 ± 3.12 mV, respectively. TEM images showed rsv-PEG-FA-AuNP conjugates formed spherical shape. Rsv-PEG-FA-AuNP conjugates found in plasma, kidney (1.90 ± 0.20 μg/g), spleen (2.65 ± 1.18 μg/g), liver (1.74 ± 0.03 μg/g), and lung (1.82 ± 0.12 μg/g), after 90 minutes intravenous administration (i.v.) in female Sprague Dawley rats. No free resveratrol was found in plasma, kidney, or spleen after i.v administration in female dawdle Sprague Dawley rats. Conclusion: Resveratrol-PEG-FA-AuNP conjugates appear to be a potential chemotherapy delivery system for active targeting purposes because of its longer systemic circulation and its accumulation in the kidney.

Amino Acids ◽  
2021 ◽  
Author(s):  
Tomohisa Yoshimura ◽  
Yuki Inokuchi ◽  
Chikako Mutou ◽  
Takanobu Sakurai ◽  
Tohru Nagahama ◽  
...  

AbstractTaurine, a sulfur-containing amino acid, occurs at high concentrations in the skin, and plays a role in maintaining the homeostasis of the skin. We investigated the effects of aging on the content and localization of taurine in the skin of mice and rats. Taurine was extracted from the skin samples of hairless mice and Sprague Dawley rats, and the taurine content of the skin was determined by high-performance liquid chromatography (HPLC). The results of the investigation revealed that the taurine content in both the dermis and epidermis of hairless mice declined significantly with age. Similar age-related decline in the skin taurine content was also observed in rats. In contrast, the taurine content in the sole remained unchanged with age. An immunohistochemical analysis also revealed a decreased skin taurine content in aged animals compared with younger animals, although no significant differences in the localization of taurine were observed between the two age groups. Supplementation of the drinking water of aged mice with 3% (w/v) taurine for 4 weeks increased the taurine content of the epidermis, but not the dermis. The present study showed for the first time that the taurine content of the skin decreased with age in mice and rats, which may be related to the impairment of the skin homeostasis observed with aging. The decreased taurine content of the epidermis in aged animals was able to be rescued by taurine supplementation.


2009 ◽  
Vol 29 (2) ◽  
pp. 93-101 ◽  
Author(s):  
Amal A El-Bakary ◽  
Sahar A El-Dakrory ◽  
Sohayla M Attalla ◽  
Nawal A Hasanein ◽  
Hala A Malek

Methanol poisoning is a hazardous intoxication characterized by visual impairment and formic acidemia. The therapy for methanol poisoning is alcohol dehydrogenase (ADH) inhibitors to prevent formate accumulation. Ranitidine has been considered to be an inhibitor of both gastric alcohol and hepatic aldehyde dehydrogenase enzymes. This study aimed at testing ranitidine as an antidote for methanol acute toxicity and comparing it with ethanol and 4-methyl pyrazole (4-MP). This study was conducted on 48 Sprague-Dawley rats, divided into 6 groups, with 8 rats in each group (one negative control group [C1], two positive control groups [C2, C3] and three test groups [1, 2 and 3]). C2, C3 and all test groups were exposed to nitrous oxide by inhalation, then, C3 group was given methanol (3 g/kg orally). The three test groups 1, 2 and 3 were given ethanol (0.5 g/kg orally), 4-MP (15 mg/kg intraperitoneally) and ranitidine (30 mg/kg intraperitoneally), respectively, 4 hours after giving methanol. Rats were sacrificed and heparinized, cardiac blood samples were collected for blood pH and bicarbonate. Non-heparinized blood samples were collected for formate levels by high performance liquid chromatography. Eye balls were enucleated for histological examination of the retina. Ranitidine corrected metabolic acidosis (p = .025), decreased formate levels (p = .014) and improved the histological findings in the retina induced by acute methanol toxicity.


1995 ◽  
Vol 268 (6) ◽  
pp. E1065-E1069 ◽  
Author(s):  
M. Yamashita ◽  
D. N. Darlington ◽  
E. J. Weeks ◽  
R. O. Jones ◽  
D. S. Gann

Large hemorrhage leads to hypercoagulability, a phenomenon that has never been well explained. Because an elevation of plasminogen activator inhibitor (PAI)-1 increases procoagulant activity, we have determined whether plasma PAI activity and tissue PAI-1 mRNA are elevated after hemorrhage. Sprague-Dawley rats were bled (20 or 15 ml/kg) 4 days after cannulation. Plasma PAI activity was determined by the capacity of plasma to inhibit tissue-type plasminogen activator activity. Changes of PAI-1 mRNA in various tissues were detected by high-performance liquid chromatography after reverse transcription and polymerase chain reaction. Hemorrhage (20 ml/kg) significantly elevated plasma PAI activity at 0.5, 1, 2, 4, 6, and 8 h after hemorrhage and PAI-1 mRNA in liver at 1, 2, 4, and 6 h after hemorrhage. The PAI-1 message was also significantly elevated in lung, heart, and kidney at 4 h after hemorrhage. The increases of PAI-1 mRNA after 20 ml/kg hemorrhage were significantly greater than those after 15 ml/kg hemorrhage. These findings indicate that large hemorrhage can induce the increases in PAI activity and PAI-1 message and suggest that induction of PAI-1 may be involved in the thrombogenic responses observed after large hemorrhage.


2021 ◽  
Vol 17 ◽  
Author(s):  
Xingxing Zhuang ◽  
Li Zhou ◽  
Renhua Miao ◽  
Shoudong Ni ◽  
Meng Li

Introduction:: Asari Radix et Rhizoma (ARR) and dried ginger (Zingiber officinalis) (DG) are often used together in drug preparations in traditional Chinese medicine (TCM) to treat respiratory diseases including cold, bronchitis and pneumonia. Previous studies suggested that ARR and/or DG may influence the pharmacokinetics of other herbal components. In the current study, we examined pharmacokinetic interactions between ARR and DG in rats after oral administration. Methods:: We developed a method based on ultra-high-performance liquid chromatography-tandem mass spectrometry to simultaneously measure serum concentrations of two active components each in ARR (L-asarinin and sesamin) and DG (6-gingerol and 6-shogaol). Adult Sprague-Dawley rats were starved overnight, then given ARR extract, DO extract, or a co-decoction of ARR and DG by gastric gavage (6 g raw material per kg body weight; n = 6 per group). Blood samples were collected prior to drug administration and at the following times (h) afterward: 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12.0 and 24.0. Pharmacokinetic parameters were compared using Student’s t test for independent samples. Results:: A simple, rapid, sensitive analytical method has been developed to detect four bioactive components simultaneously in the ARR-DG herbal pair. Pharmacokinetic parameters including Cmax, Tmax, T1/2 and AUC(0~t) were calculated using the non-compartmental model with the DAS 2.0 pharmacokinetic software. For L-asarinin, Tmax was 2.00 ± 0.00 h in ARR animals and 1.67±0.26 h in ARR-DG animals (P<0.05), T1/2 was 8.58 ± 1.75 h in ARR and 11.93 ± 2.13 h in ARR-DG (P<0.05). For 6-gingerol, Cmax was 350.48 ± 23.85 ng/mL in DG animals and 300.21 ± 20.02 ng/mL in ARR-DG (P<0.01), Tmax was 2.83 ± 0.41 h in DG and 2.17 ± 0.41 h in ARR-DG (P<0.05) and AUC(0~t) was 1.93 ± 0.15 mg/mL•h in ARR and 1.70 ± 0.15 mg/mL•h in ARR-DG (P<0.05). For 6-shogaol, Cmax was 390.28 ± 26.02 ng/mL in DG animals and 455.63 ± 31.01 ng/mL in ARR-DG (P<0.01), Tmax was 2.93 ± 0.10 h in DG and 1.92 ± 0.10 h in ARR-DG (P<0.01), T1/2 was 3.74 ± 0.29 h in DG and 3.28 ± 0.22 h in ARR-DG (P<0.01), and AUC(0~t) was 2.15 ± 0.18 mg/mL•h in DG and 2.73 ± 0.15 mg/mL•h in ARR-DG (P<0.01). Conclusions:: Pharmacokinetic interations between ARR and DG decrease Tmax, increase T1/2 but do not affect overall bioavailability of L-asarinin in ARR. The interactions in ARR-DG decrease Cmax and Tmax but increase T1/2 and AUC(0~t) of 6-gingerol in DG. The interactions increase Cmax and AUC(0~t) but decrease Tmax and T1/2 of 6- shogaol in DG. Interactions in ARR-DG do not affect the pharmacokinetics of sesamin.


Author(s):  
RADITYA ISWANDANA ◽  
RICHA NURSELVIANA ◽  
SUTRIYO SUTRIYO

Objective: Gold nanoparticles (AuNPs) are highly useful for drug delivery, but their application is limited by their stability as they readily aggregate.This issue can be prevented by adding a stabilizing agent such as resveratrol (RSV), which is a polyphenol derived from plants, that is used to preventcancer. Therefore, we propose a novel method to prepare stable RSV-conjugated nanoparticles modified with polyethylene glycol (RSV-AuNP-PEG).Methods: In the first step, the Turkevich method was used to synthesize the AuNPs. Then, PEG was added as stabilizer agent and conjugated with RSV.The synthesized conjugates were characterized using ultraviolet-visible spectrophotometry, Fourier transform infrared spectroscopy, particle sizeanalysis, and high-performance liquid chromatography.Results: The obtained RSV-AuNP-PEG had a particle size of 83.93 nm with a polydispersity index (PDI) of 0.562 and formed a translucent purple-redfluid in solution. The zeta potential was −22.9 mV, and the highest entrapment efficiency was 75.86±0.66%. For comparison, the RSV-AuNP solutionwas purple and turbid, the particle size was 51.97 nm with a PDI of 0.694, and the zeta potential was −24.6 mV. The stability test results showed thatthe storage stability of RSV-AuNP-PEG was better than that of AuNP-RSV. Further, the RSV-AuNP-PEG was shown to be most stable in 2% bovine serumalbumin (BSA) while the AuNP-RSV was most stable in 2% BSA in phosphate-buffered saline pH 7.4.Conclusion: These results show that modification of RSV-conjugated AuNPs with PEG effectively prevents their aggregation in storage, but only incertain mediums.


2014 ◽  
Vol 30 (1) ◽  
pp. 55-63 ◽  
Author(s):  
Cheol Hong Lim ◽  
Jeong-Hee Han ◽  
Hae-Won Cho ◽  
Mingu Kang

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 328 ◽  
Author(s):  
Zhuang Ding ◽  
Lili Wang ◽  
Yangyang Xing ◽  
Yanna Zhao ◽  
Zhengping Wang ◽  
...  

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Amir Reza Sadrolhosseini ◽  
A. S. M. Noor ◽  
Nastaran Faraji ◽  
Alireza Kharazmi ◽  
Mohd. Adzir Mahdi

Gold nanoparticles were prepared in graphene oxide using laser ablation technique. The ablation times were varied from 10 to 40 minutes, and the particle size was decreased from 16.55 nm to 5.18 nm in spherical shape. The nanoparticles were capped with carboxyl and the hydroxyl groups were obtained from Fourier transform infrared spectroscopy. Furthermore, the UV-visible peak shifted with decreasing of nanoparticles size, appearing from 528 nm to 510 nm. The Z-scan technique was used to measure the nonlinear refractive indices of graphene oxide with different concentrations and a gold nanoparticle graphene oxide nanocomposite. Consequently, the optical nonlinear refractive indices of graphene oxide and gold nanoparticle graphene oxide nanocomposite were shifted from1.63×10-9 cm2/W to4.1×10-9 cm2/W and from1.85×10-9 cm2/W to5.8×10-9 cm2/W, respectively.


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