Hydroxyapatite reinforced inorganic-organic hybrid nanocomposite as high-performance adsorbents for bilirubin removal in vitro and in pig models

Abstract. We have partially purified a tumour factor capable of stimulating both bone resorption in vitro and cAMP accumulation in osteoblastic ROS 17/2 cells from three human tumours associated with humoral hypercalcaemia of malignancy. Purification of tumour factor by sequential acid urea extraction, gel filtration and cation-exchange chromatography, reverse-phase high performance liquid chromatography followed by analytical isoelectric focussing provided a basic protein (pI > 9.3) with a molecular weight of approximately 13 000 as a major component of the final preparation which retained both the two bioactivities. Bone resorbing activity and cAMP-increasing activity in purified factor correlated with each other. cAMP-increasing activity of the factor was heat- and acid-stable, but sensitive to alkaline ambient pH. Treatment with trypsin destroyed cAMP-increasing activity of the factor. Synthetic parathyroid hormone (PTH) antagonist, human PTH-(3– 34) completely inhibited the cAMP-increasing activity of the factor. The results suggest that this protein factor, having its effects on both osteoclastic and osteoblastic functions, may be involved in development of enhanced bone resorption in some patients with humoral hypercalcaemia of malignancy.

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Simultaneous determination of eight derivatives of propranolol in cornea perfusate in vitro by high performance liquid chromatography

Chinese Journal of Chromatography ◽

10.3724/sp.j.1123.2012.06039 ◽

2013 ◽

Vol 30 (11) ◽

pp. 1183-1187

Author(s):

Haitao WU ◽

Chuanbing CHEN ◽

Ningsheng WANG ◽

Suiqing MI ◽

Nanying LIAO

Keyword(s):

High Performance Liquid Chromatography ◽

Liquid Chromatography ◽

Simultaneous Determination ◽

High Performance ◽

Derivatives Of

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Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2013.6.2.8 ◽

2013 ◽

Vol 6 (2) ◽

pp. 2058-2063

Author(s):

G D Chandrethiya ◽

P K Shelat ◽

M N Zaveri

Keyword(s):

Drug Delivery ◽

Targeted Delivery ◽

High Performance ◽

Entrapment Efficiency ◽

Stability Study ◽

Spherical Particles ◽

Precipitation Method ◽

Antitumoral Activity ◽

Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin. Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized. Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation. Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay. The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.

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Effect of carbon source on Phenobarbital metabolism by Rhizopus stolonifer

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.2.17 ◽

2010 ◽

Vol 3 (2) ◽

pp. 1022-1027

Author(s):

Kavitha K ◽

Asha S ◽

Hima Bindu T.V.L ◽

Vidyavathi M

Keyword(s):

Carbon Source ◽

High Performance ◽

Carbon Sources ◽

In Vitro Models ◽

Rhizopus Stolonifer ◽

Safety And Efficacy ◽

Alternative Systems ◽

Toxicological Studies ◽

Microbial Model

The safety and efficacy of a drug is based on its metabolism or metabolite formed. The metabolism of drugs can be studied by different in vitro models, among which microbial model became popular. In the present study, eight microbes were screened for their ability to metabolize phenobarbital in a manner comparable to humans with a model to develop alternative systems to study human drug metabolism. Among the different microbes screened, a filamentous fungi Rhizopus stolonifer metabolized phenobarbital to its metabolite which is used for further pharmacological and toxicological studies. The transformation of phenobarbital was identified by high- performance liquid chromatography (HPLC). Interestingly, Rhizopus stolonifer sample showed an extra metabolite peak at 3.11min. compared to its controls. The influence of different carbon sources in media used for growth of fungus, on metabolite production was studied, to find its effect in production of metabolite as the carbon source may influence the growth of the cell.

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Phytochemical, Analytical and Medicinal Studies of Holoptelea integrifolia Roxb. Planch - A Review

Current Traditional Medicine ◽

10.2174/2215083805666190521103308 ◽

2019 ◽

Vol 5 (4) ◽

pp. 270-277 ◽

Cited By ~ 2

Author(s):

Vijay Kumar ◽

Simranjeet Singh ◽

Ragini Bhadouria ◽

Ravindra Singh ◽

Om Prakash

Keyword(s):

Liquid Chromatography ◽

Thin Layer ◽

Thin Layer Chromatography ◽

High Performance ◽

Biologically Active ◽

Toxicological Studies ◽

Wide Range ◽

Layer Chromatography

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.

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Polymer/Iron-Based Layered Double Hydroxides as Multifunctional Wound Dressings

Pharmaceutics ◽

10.3390/pharmaceutics12111130 ◽

2020 ◽

Vol 12 (11) ◽

pp. 1130

Author(s):

Mariana Pires Figueiredo ◽

Ana Borrego-Sánchez ◽

Fátima García-Villén ◽

Dalila Miele ◽

Silvia Rossi ◽

...

Keyword(s):

Drug Release ◽

High Performance ◽

Mechanical Performance ◽

Release Kinetics ◽

Wound Dressings ◽

In Vitro Drug Release ◽

Improved Performance ◽

Double Hydroxide ◽

Double Hydroxides

This work presents the development of multifunctional therapeutic membranes based on a high-performance block copolymer scaffold formed by polyether (PE) and polyamide (PA) units (known as PEBA) and layered double hydroxide (LDH) biomaterials, with the aim to study their uses as wound dressings. Two LDH layer compositions were employed containing Mg2+ or Zn2+, Fe3+ and Al3+ cations, intercalated with chloride anions, abbreviated as Mg-Cl or Zn-Cl, or intercalated with naproxenate (NAP) anions, abbreviated as Mg-NAP or Zn-NAP. Membranes were structurally and physically characterized, and the in vitro drug release kinetics and cytotoxicity assessed. PEBA-loading NaNAP salt particles were also prepared for comparison. Intercalated NAP anions improved LDH–polymer interaction, resulting in membranes with greater mechanical performance compared to the polymer only or to the membranes containing the Cl-LDHs. Drug release (in saline solution) was sustained for at least 8 h for all samples and release kinetics could be modulated: a slower, an intermediate and a faster NAP release were observed from membranes containing Zn-NAP, NaNAP and Mg-NAP particles, respectively. In general, cell viability was higher in the presence of Mg-LDH and the membranes presented improved performance in comparison with the powdered samples. PEBA containing Mg-NAP sample stood out among all membranes in all the evaluated aspects, thus being considered a great candidate for application as multifunctional therapeutic dressings.

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Native Chilean Berries Preservation and In Vitro Studies of a Polyphenol Highly Antioxidant Extract from Maqui as a Potential Agent against Inflammatory Diseases

Antioxidants ◽

10.3390/antiox10060843 ◽

2021 ◽

Vol 10 (6) ◽

pp. 843

Author(s):

Tamara Ortiz ◽

Federico Argüelles-Arias ◽

Belén Begines ◽

Josefa-María García-Montes ◽

Alejandra Pereira ◽

...

Keyword(s):

High Performance ◽

Large Scale ◽

Inflammatory Diseases ◽

In Vitro Studies ◽

Aminosalicylic Acid ◽

Colon Cells ◽

Antioxidant Power ◽

Maqui Berry ◽

Physiological Benefits

The best conservation method for native Chilean berries has been investigated in combination with an implemented large-scale extract of maqui berry, rich in total polyphenols and anthocyanin to be tested in intestinal epithelial and immune cells. The methanolic extract was obtained from lyophilized and analyzed maqui berries using Folin–Ciocalteu to quantify the total polyphenol content, as well as 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), and oxygen radical absorbance capacity (ORAC) to measure the antioxidant capacity. Determination of maqui’s anthocyanins profile was performed by ultra-high-performance liquid chromatography (UHPLC-MS/MS). Viability, cytotoxicity, and percent oxidation in epithelial colon cells (HT-29) and macrophages cells (RAW 264.7) were evaluated. In conclusion, preservation studies confirmed that the maqui properties and composition in fresh or frozen conditions are preserved and a more efficient and convenient extraction methodology was achieved. In vitro studies of epithelial cells have shown that this extract has a powerful antioxidant strength exhibiting a dose-dependent behavior. When lipopolysaccharide (LPS)-macrophages were activated, noncytotoxic effects were observed, and a relationship between oxidative stress and inflammation response was demonstrated. The maqui extract along with 5-aminosalicylic acid (5-ASA) have a synergistic effect. All of the compiled data pointed out to the use of this extract as a potential nutraceutical agent with physiological benefits for the treatment of inflammatory bowel disease (IBD).

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Olive Fruit and Leaf Wastes as Bioactive Ingredients for Cosmetics—A Preliminary Study

Antioxidants ◽

10.3390/antiox10020245 ◽

2021 ◽

Vol 10 (2) ◽

pp. 245

Author(s):

María de la Luz Cádiz-Gurrea ◽

Diana Pinto ◽

Cristina Delerue-Matos ◽

Francisca Rodrigues

Keyword(s):

Olive Oil ◽

High Performance ◽

Value Added ◽

Bioactive Compound ◽

In Vitro Assays ◽

Oil Consumption ◽

Cosmetic Ingredients ◽

Bioactive Ingredients ◽

Olive Industry

Olea europaea cultivar, native in the Mediterranean basin, has expanded worldwide, mainly due to the olive oil industry. This expansion is attributed to the benefits of olive oil consumption, since this product is rich in nutritional and bioactive compounds. However, the olive industry generates high amounts of wastes, which could be related to polluting effects on soil and water. To minimize the environmental impact, different strategies of revalorization have been proposed. In this sense, the aim of this work was to develop high cosmetic value added oleuropein-enriched extracts (O20 and O30), a bioactive compound from olive byproducts, performing a comprehensive characterization using high performance liquid chromatography coupled to mass spectrometry and evaluate their bioactivity by in vitro assays. A total of 49 compounds were detected, with oleuropein and its derivatives widely found in O30 extract, whereas iridoids were mainly detected in O20 extract. Moreover, 10 compounds were detected for the first time in olive leaves. Both extracts demonstrated strong antioxidant and antiradical activities, although O30 showed higher values. In addition, radical oxygen and nitrogen species scavenging and enzyme inhibition values were higher in O30, with the exception of HOCl and hyaluronidase inhibition assays. Regarding cell viability, olive byproduct extracts did not lead to a decrease in keratinocytes viability until 100 µg/mL. All data reported by the present study reflect the potential of industrial byproducts as cosmetic ingredients.

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Heparin-mediated antibiotic delivery from an electrochemically-aligned collagen sheet

Bio-Medical Materials and Engineering ◽

10.3233/bme-201133 ◽

2021 ◽

pp. 1-12

Author(s):

Olivia T. Cheng ◽

Andrew P. Stein ◽

Eric Babajanian ◽

Kathryn R. Hoppe ◽

Shawn Li ◽

...

Keyword(s):

High Performance ◽

Inhibitory Concentration ◽

Medical Implants ◽

Implantable Medical Devices ◽

Antibiotic Solution ◽

Inhibition Zones ◽

Antibiotic Release ◽

Local Antibiotic ◽

Antibiotic Delivery

BACKGROUND: Implantable medical devices and hardware are prolific in medicine, but hardware associated infections remain a major issue. OBJECTIVE: To develop and evaluate a novel, biologic antimicrobial coating for medical implants. METHODS: Electrochemically compacted collagen sheets with and without crosslinked heparin were synthesized per protocol developed by our group. Sheets were incubated in antibiotic solution (gentamicin or moxifloxacin) overnight, and in vitro activity was assessed with five-day diffusion assays against Pseudomonas aeruginosa. Antibiotic release overtime from gentamicin infused sheets was determined using in vitro elution and high performance liquid chromatography (HPLC). RESULTS: Collagen-heparin-antibiotic sheets demonstrated larger growth inhibition zones against P. aeruginosa compared to collagen-antibiotic alone sheets. This activity persisted for five days and was not impacted by rinsing sheets prior to evaluation. Rinsed collagen-antibiotic sheets did not show any inhibition zones. Elution of gentamicin from collagen-heparin-gentamicin sheets was slow and remained above the minimal inhibitory concentration for gentamicin sensitive organisms for 29 days. Conversely, collagen-gentamicin sheets eluted their antibiotic payload within 24 hours. Overall, heparin associated sheets demonstrated larger inhibition zones against P. aeruginosa and prolonged elution profile via HPLC. CONCLUSION: We developed a novel, local antibiotic delivery system that could be used to coat medical implants/hardware in the future and reduce post-operative infections.

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A novel PET tracer 18F-deoxy-thiamine: synthesis, metabolic kinetics, and evaluation on cerebral thiamine metabolism status

EJNMMI Research ◽

10.1186/s13550-020-00710-5 ◽

2020 ◽

Vol 10 (1) ◽

Author(s):

Changpeng Wang ◽

Siwei Zhang ◽

Yuefei Zou ◽

Hongzhao Ma ◽

Donglang Jiang ◽

...

Keyword(s):

High Performance ◽

Specific Activity ◽

High Accumulation ◽

Metabolic Kinetics ◽

Thiamine Metabolism ◽

Pet Tracer ◽

The Status ◽

The Brain

Abstract Background Some neuropsychological diseases are associated with abnormal thiamine metabolism, including Korsakoff–Wernicke syndrome and Alzheimer’s disease. However, in vivo detection of the status of brain thiamine metabolism is still unavailable and needs to be developed. Methods A novel PET tracer of 18F-deoxy-thiamine was synthesized using an automated module via a two-step route. The main quality control parameters, such as specific activity and radiochemical purity, were evaluated by high-performance liquid chromatography (HPLC). Radiochemical concentration was determined by radioactivity calibrator. Metabolic kinetics and the level of 18F-deoxy-thiamine in brains of mice and marmosets were studied by micro-positron emission tomography/computed tomography (PET/CT). In vivo stability, renal excretion rate, and biodistribution of 18F-deoxy-thiamine in the mice were assayed using HPLC and γ-counter, respectively. Also, the correlation between the retention of cerebral 18F-deoxy-thiamine in 60 min after injection as represented by the area under the curve (AUC) and blood thiamine levels was investigated. Results The 18F-deoxy-thiamine was stable both in vitro and in vivo. The uptake and clearance of 18F-deoxy-thiamine were quick in the mice. It reached the max standard uptake value (SUVmax) of 4.61 ± 0.53 in the liver within 1 min, 18.67 ± 7.04 in the kidney within half a minute. The SUV dropped to 0.72 ± 0.05 and 0.77 ± 0.35 after 60 min of injection in the liver and kidney, respectively. After injection, kidney, liver, and pancreas exhibited high accumulation level of 18F-deoxy-thiamine, while brain, muscle, fat, and gonad showed low accumulation concentration, consistent with previous reports on thiamine distribution in mice. Within 90 min after injection, the level of 18F-deoxy-thiamine in the brain of C57BL/6 mice with thiamine deficiency (TD) was 1.9 times higher than that in control mice, and was 3.1 times higher in ICR mice with TD than that in control mice. The AUC of the tracer in the brain of marmosets within 60 min was 29.33 ± 5.15 and negatively correlated with blood thiamine diphosphate levels (r = − 0.985, p = 0.015). Conclusion The 18F-deoxy-thiamine meets the requirements for ideal PET tracer for in vivo detecting the status of cerebral thiamine metabolism.

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