scholarly journals Successful Dendrimer and Liposome-Based Strategies to Solubilize an Antiproliferative Pyrazole Otherwise Not Clinically Applicable

Nanomaterials ◽  
2022 ◽  
Vol 12 (2) ◽  
pp. 233
Author(s):  
Silvana Alfei ◽  
Andrea Spallarossa ◽  
Matteo Lusardi ◽  
Guendalina Zuccari
Keyword(s):  
Release Profile ◽  
Water Soluble ◽  
Attenuated Total Reflectance ◽  
Prolonged Release ◽  
Antiproliferative Effects ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Fifth Generation ◽  
Zero Order Kinetics

Water-soluble formulations of the pyrazole derivative 3-(4-chlorophenyl)-5-(4-nitrophenylamino)-1H-pyrazole-4-carbonitrile (CR232), which were proven to have in vitro antiproliferative effects on different cancer cell lines, were prepared by two diverse nanotechnological approaches. Importantly, without using harmful organic solvents or additives potentially toxic to humans, CR232 was firstly entrapped in a biodegradable fifth-generation dendrimer containing lysine (G5K). CR232-G5K nanoparticles (CR232-G5K NPs) were obtained with high loading (DL%) and encapsulation efficiency (EE%), which showed a complex but quantitative release profile governed by Weibull kinetics. Secondly, starting from hydrogenated soy phosphatidylcholine and cholesterol, we prepared biocompatible CR232-loaded liposomes (CR232-SUVs), which displayed DL% and EE% values increasing with the increase in the lipids/CR232 ratio initially adopted and showed a constant prolonged release profile ruled by zero-order kinetics. When relevant, attenuated total reflectance Fourier transformed infrared spectroscopy (ATR-FTIR) and nuclear magnetic resonance (NMR) spectroscopy, scanning electron microscopy (SEM) and dynamic light scattering (DLS) experiments, as well as potentiometric titrations completed the characterization of the prepared NPs. CR232-G5K NPs were 2311-fold more water-soluble than the pristine CR232, and the CR232-SUVs with the highest DL% were 1764-fold more soluble than the untreated CR232, thus establishing the success of both our strategies.

Synthesis and Characterization of Polyesters Containing 5-Fluorouracil in the Main Chain

2012 ◽  
Vol 499 ◽  
pp. 99-103
Author(s):  
Jun Chang ◽  
Cheng Wu Li ◽  
Gang Li
Keyword(s):  
Main Chain ◽  
Slow Release ◽  
Uv Spectroscopy ◽  
Release Profile ◽  
Drug Release Profile ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antitumor

A series of polyesters containing 5-fluorouracil in the main chain were prepared by reacting potassium salt of 5-fluorouracil with different molecular weight ω-chloroalkyl chloroacetyl esters.The copolymers were characterized by FT-IR, 1H-NMR, VPO and UV spectroscopy. The drug release profile in vitro of the copolymers were studied, the results showed prodrug could slow release 5-FU or 5-FU units in different solution, they may be likely to become potential antitumor prodrug.

Fabrication and characterization of ferritin–chitosan–lutein shell–core nanocomposites and lutein stability and release evaluation in vitro

RSC Advances ◽  
2016 ◽  
Vol 6 (42) ◽  
pp. 35267-35279 ◽  
Author(s):  
Rui Yang ◽  
Yunjing Gao ◽  
Zhongkai Zhou ◽  
Padraig Strappe ◽  
Chris Blanchard
Keyword(s):  
Gastrointestinal Tract ◽  
Prolonged Release ◽  
Core System ◽  
Improved Stability ◽  
Fabrication And Characterization

The nano-sized ferritin and chitosan provide a platform for fabricating shell–core system to encapsulate lutein, exhibiting improved stability and prolonged release of lutein in simulated gastrointestinal tract digestion.

scholarly journals In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation

2021 ◽  
Vol 5 (Supplement_2) ◽  
pp. 1328-1328
Author(s):  
Mastaneh Sharafi ◽  
Tyler White ◽  
Kelli Fowler ◽  
Kevin Ewell ◽  
Noe Galvan ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Los Angeles ◽  
Vitamin C ◽  
Phosphatidyl Choline ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Prolonged Release ◽  
Lauryl Sulfate

Abstract Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).

scholarly journals EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY

2021 ◽  
pp. 114-121
Author(s):  
S. DUBEY ◽  
S. P. VYAS
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Particle Diameter ◽  
Release Profile ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and characterize paclitaxel (Ptx) loaded sterically stabilized emulsomes to provide non-toxic and biocompatible carriers with high Ptx loading efficiency. Methods: Plain (P-Es) and sterically stabilized emulsomes (SS-Es) were prepared by a modified solvent evaporation method using tristearin as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/ tristearin ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein. Results: The emulsomes so formed were uniform in size with a mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulations showed pH dependent drug release with a slow and sustained release profile. Slower drug release was observed from sterically stabilized emulsomes than the plain emulsomes. The drug release profile followed the Higuchi model with the Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption. Conclusion: The sterically stabilized emulsome can serve as a novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water-soluble drugs as well.

scholarly journals Fabrication and Characterization of Electrospun Nanofibers for the Modified Release of the Chronobiotic Hormone Melatonin

2018 ◽  
Vol 16 (1) ◽  
pp. 79-85 ◽  
Author(s):  
Marilena Vlachou ◽  
Stefanos Kikionis ◽  
Angeliki Siamidi ◽  
Konstantina Tragou ◽  
Stefania Kapoti ◽  
...  
Keyword(s):  
Cellulose Acetate ◽  
Electrospun Nanofibers ◽  
Release Profile ◽  
Modified Release ◽  
Gelatin Capsules ◽  
Fiber Matrices ◽  
Fabrication And Characterization ◽  
Hard Gelatin Capsules

Objective: Aiming at the modified release of melatonin (MLT), electrospun-MLT loaded nanofibers, filled into hard gelatin and DRcapsTM capsules, were used as formulants. Methods: Cellulose acetate, polyvinylpyrrolidinone and hydroxypropylmethylcellusose (HPMC 2910) were used for the preparation of the fiber matrices through electrospinning. The in vitro modified release profile of MLT from the fabricated matrices in gastrointestinal-like fluids was studied. At pH 1.2, the formulations CA1, CA2, PV1, HP1, HP2 and the composite formulations CAPV1-CAPV5 in hard gelatin capsules exhibited fast MLT release. Results: In general, the same trend was observed at pH 6.8, with the exception of CAPV1 and CAPV2. These two composite formulations delivered 52.08% and 75.25% MLT, respectively at a slower pace (6 h) when encapsulated in DRcapsTM capsules. In all other cases, the release of MLT from DRcapsTM capsules filled with the MLT-loaded nanofibers reached 100% at 6h. Conclusion: These findings suggest that the MLT-loaded nanofibrous mats developed in this study exhibit a promising profile for treating sleep dysfunctions.

Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

2015 ◽  
Vol 8 (2) ◽  
pp. 2851-2857
Author(s):  
Kiran Kumar Vangara ◽  
Kishore K. Konda ◽  
Shiva K. Ravula ◽  
Pradeep K Vuppala ◽  
Vijay K. Sripuram ◽  
...  
Keyword(s):  
Weight Gain ◽  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Film Coating ◽  
Release Profile ◽  
Water Soluble ◽  
Metoprolol Succinate ◽  
Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.  

Characterization of triticale silage inoculated with homolactic bacteria and exposed to aerobic stress during storage

1969 ◽  
Vol 100 (2) ◽  
pp. 155-170
Author(s):  
Luis C. Solórzano ◽  
Luis L. Solórzano ◽  
Abner Rodríguez-Carías
Keyword(s):  
Water Soluble ◽  
Neutral Detergent Fiber ◽  
Soluble Carbohydrates ◽  
Inorganic Matter ◽  
Whole Plant ◽  
Spring Triticale ◽  
Fermentation Pattern ◽  
The One

Fresh whole plant spring triticale (x Triticosecale spp.) was field wilted and chopped prior to either being sprayed or not with a homolactic bacterial inoculant (HBI). Wilted triticale was ensiled for 120 d at 20 to 23 °C using 16 PVC mini-silos of 3 L capacity fitted with two-way mechanics to vent gas (which imposed aerobic stress (ASTS) when it remained open), and filled with about 2 kg of the crop containing 35% dry matter (DM) and 5.2% water soluble carbohydrates (WSC) in the DM. Four treatments of a 2x2 factorial were: 1) No HBI/vent closed; 2) HBI/ vent closed; 3) No HBI/vent open; 4) HBI/vent open. Upon opening the mini-silos, chemical composition, fermentation characteristics and in vitro 30 h neutral detergent fiber (NDF) digestibility of the silages were determined. Relative to pre-ensiled forage, either sprayed or not with HBI, ensiling increased (P<0.05) contents of moisture, inorganic matter, fibrous fractions (acid detergent fiber (ADF) and lignin), and ether extract (EE), while decreasing contents of WSC and non-fibrous carbohydrates (NFC). However, treatment had no consistent effect on content of silage nutrients. Of the two non-inoculated silages, the one subjected to ASTS was more than 20 percentage points lower (66 vs. 88 %) in DM recovery (DMR), whereas the HBI silage subjected to ASTS was protected from DM losses. Ensiling and ASTS during the 120 d fermentation decreased NDF digestibility, whereas inoculated non-ASTS silage was nearly as digestible (57.5) as the pre-ensiled forages (58.2 and 60.7%, without and with HBI). Inoculation tended to steer fermentation in a homolactic direction. On balance, HBI is recommended because of the benefits in the fermentation pattern, fiber digestibility and DMR, especially in the presence of ASTS.

scholarly journals Studies on gastric mucoproteins. The isolation and characterization of the mucoprotein of the water-soluble mucus from pig cardiac gastric mucosa

1971 ◽  
Vol 123 (5) ◽  
pp. 845-853 ◽  
Author(s):  
D. Snary ◽  
A. Allen
Keyword(s):  
Sialic Acid ◽  
Gastric Mucosa ◽  
Gel Filtration ◽  
Water Soluble ◽  
Group Activities ◽  
Isolation And Characterization ◽  
Two Peaks ◽  
Sepharose 4B

1. Gel filtration of the water-soluble radioactive mucus produced three radioactive fractions, fraction A excluded on Sepharose 4B, fraction B included on Sepharose 4B but excluded on Sephadex G-200, and fraction C included on Sephadex G-200. 2. The specific radioactivities of fractions A and B were the same, with fraction C a little lower, whether the material was labelled with 14C-labelled carbohydrate or with 3H-labelled protein prepared by incubation of mucosal scrapings in vitro with [U-14C]glucose or [G-3H]threonine respectively. 3. Fractions A and B had an analysis of protein 22%, hexose 28%, hexosamine 28%, fucose 10% and sialic acid 1%; fraction C had an analysis closely similar to this, except that it contained about 10% of a protein contaminant. 4. All three fractions had closely similar A and H blood-group activities. 5. Ultracentrifuge studies showed fractions A, B and C were polydisperse with s025,w values of 18.7S, 4.9S and 3.9S respectively. 6. The unfractionated water-soluble mucus contained only two peaks, fraction A 18.7S and a peak of 4.4S, which was a combination of fractions B and C. 7. The radioactive mucoprotein accounted for 85% by weight of the soluble mucus and the results show that it consisted of two distinct fractions A and B–C, which were chemically, biosynthetically and immunologically very similar.

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