Fully synthetic macromolecular prodrug chemotherapeutics with EGFR targeting and controlled camptothecin release kinetics

2018 ◽  
Vol 9 (42) ◽  
pp. 5224-5233 ◽  
Author(s):  
Hanna Freeman ◽  
Selvi Srinivasan ◽  
Debobrato Das ◽  
Patrick S. Stayton ◽  
Anthony J. Convertine
Keyword(s):  
Release Kinetics ◽  
Macromolecular Prodrug

The development of fully polymerizable, peptide-targeted, camptothecin polymeric prodrugs are reported.

ROLE OF ADDED PHOSPHOGYPSUM AND HUMIC ACIDS IN THE KINETIC RELEASE OF SALT FROM SALT AFFECTED SOIL (SALINE – SODIC)

2020 ◽  
pp. 15-27
Keyword(s):  
Electrical Conductivity ◽  
Humic Acids ◽  
Release Rate ◽  
Release Kinetics ◽  
Sodium Adsorption Ratio ◽  
Salt Affected Soil ◽  
Two Factors ◽  
Dissolved Ions ◽  
Kinetic Release

In order to study the effect of phosphogypsum and humic acids in the kinetic release of salt from salt-affected soil, a laboratory experiment was conducted in which columns made from solid polyethylene were 60.0 cm high and 7.1 cm in diameter. The columns were filled with soil so that the depth of the soil was 30 cm inside the column, the experiment included two factors, the first factor was phosphogypsum and was added at levels 0, 5, 10 and 15 tons ha-1 and the second-factor humic acids were added at levels 0, 50, 100 and 150 kg ha-1 by mixing them with the first 5 cm of column soil and one repeater per treatment. The continuous leaching method was used by using an electrolytic well water 2.72 dS m-1. Collect the leachate daily and continue the leaching process until the arrival of the electrical conductivity of the filtration of leaching up to 3-5 dS m-1. The electrical conductivity and the concentration of positive dissolved ions (Ca, Mg, Na) were estimated in leachate and the sodium adsorption ratio (SAR) was calculated. The results showed that the best equation for describing release kinetics of the salts and sodium adsorption ratio in soil over time is the diffusion equation. Increasing the level of addition of phosphogypsum and humic acids increased the constant release velocity (K) of salts and the sodium adsorption ratio. The interaction between phosphogypsum and humic acids was also affected by the constant release velocity of salts and the sodium adsorption ratio. The constant release velocity (K) of the salts and the sodium adsorption ratio at any level of addition of phosphogypsum increased with the addition of humic acids. The highest salts release rate was 216.57 in PG3HA3, while the lowest rate was 149.48 in PG0HA0. The highest release rate of sodium adsorption ratio was 206.09 in PG3HA3, while the lowest rate was 117.23 in PG0HA0.

Evaluation of release kinetics and mitogenic capacity of collagen barrier membranes supplemented with the secretome of activated platelets

2016 ◽  
Author(s):  
Eva-Maria Mozgan ◽  
Michael Edelmayer ◽  
Klara Janjić ◽  
Manuela Pensch ◽  
Michael Fischer ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Barrier Membranes ◽  
Activated Platelets

Gastroretentive System of Fluvastatin Sodium by Using Natural Mucilage and Synthetic Polymer

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Umamaheswara G. ◽  
Anudeep D.
Keyword(s):  
Half Life ◽  
Release Kinetics ◽  
Kinetic Studies ◽  
Diffusion Path ◽  
Synthetic Polymer ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Drug Content ◽  
Biological Half Life

Fluvastatin sodium is a novel compound used as cholesterol lowering agent which acts through the inhibition of 3- hydroxyl-3- methyl glutaryl- coenzyme A (HMG-Co A) reductase. It has short biological half life (1-3h) in humans required a dosing frequency of 20 to 40mg twice a day. Due to its short variable biological half life it has been developed to a sustained gastroretentive system with a natural and synthetic polymer and to study how far the natural mucilage improves the sustained activity. Floating tablets were prepared by direct compression method using in combination of natural mucilage and synthetic polymer. Prior to the preparation of tablets the physical mixtures were subjected to FT IR studies and pre compression parameters. After preparation of tablets they were subjected to various tests like swollen index, drug content, In vitro dissolution and release kinetics with pcp disso software etc. The tablets prepared by direct compression shown good in thickness, hardness and uniformity in drug content, the prepared tablets floated more than 12h except FS1 and FS2 shows 9 and 11h. Swollen index studies shows with increase in concentration of polymer the swelling increases the diffusion path length by which the drug molecule may have to travel and cause lag time. In vitro results shows that on increasing the amount of hibiscus polymer the sustain activity is increased because of its integrity and forms a thick swollen mass and reduces the erosion property of the HypromelloseK100M, kinetic studies shows that FS 1, FS2, FS3 followed the Korsmeyer peppas model and the rest FS 4, FS 5, FS6 follows the zero order respectively. Based on n value indicating that the drug release followed super case II transport mechanism due to the erosion of the polymer.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

A 3D-printed Microfluidic System for Automated and Near Real-time Quantitation of Biofilm-induced indole

2019 ◽  
Author(s):  
Giraso Kabandana ◽  
Curtis G. Jones ◽  
Sahra Khan Sharifi ◽  
Chengpeng Chen
Keyword(s):  
Real Time ◽  
Release Kinetics ◽  
Microfluidic System ◽  
3D Printed

We developed a novel microfluidic system that enables automated and near real-time quantitation of indole release kinetics from biofilms.

Analysis of K+ release kinetics of biomass ash with different pH

2014 ◽  
Vol 22 (2) ◽  
pp. 171-176
Author(s):  
Kan WANG ◽  
Zifang WANG ◽  
Ming GAO ◽  
Yaohua HUANG ◽  
Xiaofei HAN ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Biomass Ash ◽  
Kinetics Of ◽  
K Release

Optimization Study to Develop Once-a-day Controlled Release Formulation of Metoclopramide with Predictable Design Space

1970 ◽  
Vol 1 (1) ◽  
pp. 71-76
Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Design Space ◽  
Release Kinetics ◽  
Release Profile ◽  
Release Formulation ◽  
Linear Effect ◽  
Controlled Release Formulation ◽  
The Difference ◽  
Face Centered

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile

Phosphorus Release Kinetics in Biofilm Reactors

1992 ◽  
Vol 26 (3-4) ◽  
pp. 567-576 ◽  
Author(s):  
F. A. Ruiz-Treviño ◽  
S. González-Martínez ◽  
C. Doria-Serrano ◽  
M. Hernández-Esparza
Keyword(s):  
Phosphorus Removal ◽  
Release Kinetics ◽  
Phosphorus Release ◽  
Organic Substrate ◽  
Biofilm Reactor ◽  
Substrate Uptake ◽  
Biofilm Reactors ◽  
Initial Substrate ◽  
Linear Behaviour ◽  
Substrate Concentrations

This paper presents the kinetic analysis, using Generalized Power-Law equations to describe the results of an experimental investigation conducted on a batch submerged biofilm reactor for phosphorus removal under an anaerobic/aerobic cycle. The observed rates and amounts of phosphorus release and organic substrate uptake in the anaerobic phase leads to a kinetic model in which these two variables are dependent on each other with a non-linear behaviour and reach equilibrium values in both cases, at different times and are function of rate constants ratio. The model has a good fit with experimental data except for C uptake at anaerobic contact times longer than four hours, where other kinetics are implied. Kinetic parameters were obtained with different initial substrate concentrations, anaerobic contact cycles, and type of substrates.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

Utilizing ICG Spectroscopical Properties for Real-Time Nanoparticle Release Quantification In vitro and In vivo in Imaging Setups

2020 ◽  
Vol 26 (31) ◽  
pp. 3828-3833 ◽  
Author(s):  
Tuula Peñate-Medina ◽  
Eike Kraas ◽  
Kunliang Luo ◽  
Jana Humbert ◽  
Hanwen Zhu ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Pure Water ◽  
Squamous Carcinoma ◽  
Peak Shift ◽  
Intensity Increase ◽  
Nude Mouse Model ◽  
Absorption And Emission ◽  
Squamous Carcinoma Cells

Background: Nanoparticle imaging and tracking the release of the loaded material from the nanoparticle system have attracted significant attention in recent years. If the release of the loaded molecules could be monitored reliably in vivo, it would speed up the development of drug delivery systems remarkably. Methods: Here, we test a system that uses indocyanine green (ICG) as a fluorescent agent for studying release kinetics in vitro and in vivo from the lipid iron nanoparticle delivery system. The ICG spectral properties like its concentration dependence, sensitivity and the fluctuation of the absorption and emission wavelengths can be utilized for gathering information about the change of the ICG surrounding. Results: We have found that the absorption, fluorescence, and photoacoustic spectra of ICG in lipid iron nanoparticles differ from the spectra of ICG in pure water and plasma. We followed the ICG containing liposomal nanoparticle uptake into squamous carcinoma cells (SCC) by fluorescence microscopy and the in vivo uptake into SCC tumors in an orthotopic xenograft nude mouse model under a surgical microscope. Conclusion: Absorption and emission properties of ICG in the different solvent environment, like in plasma and human serum albumin, differ from those in aqueous solution. Photoacoustic spectral imaging confirmed a peak shift towards longer wavelengths and an intensity increase of ICG when bound to the lipids. The SCC cells showed that the ICG containing liposomes bind to the cell surface but are not internalized in the SCC-9 cells after 60 minutes of incubation. We also showed here that ICG containing liposomal nanoparticles can be traced under a surgical camera in vivo in orthotopic SCC xenografts in mice.

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