On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency In Vivo

2021 ◽  
Author(s):  
Zhou Zhou ◽  
Shun Feng ◽  
Jujun Zhou ◽  
Xingyue Ji ◽  
Ya-Qiu Long
Keyword(s):  
Reaction Kinetics ◽  
Fast Reaction ◽  
On Demand

scholarly journals Development, Characterization and In Vivo Pharmacokinetic Assessment of Rectal Suppositories Containing Combination Antiretroviral Drugs for HIV Prevention

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1110
Author(s):  
Kunal Jhunjhunwala ◽  
Charles W. Dobard ◽  
Sunita Sharma ◽  
Natalia Makarova ◽  
Angela Holder ◽  
...  
Keyword(s):  
Hiv Prevention ◽  
Antiretroviral Drugs ◽  
Water Soluble ◽  
Fixed Dose ◽  
Receptive Anal Intercourse ◽  
On Demand ◽  
Dose Combination ◽  
Rectal Suppositories

Receptive anal intercourse (RAI) contributes significantly to HIV acquisition underscoring the need to develop HIV prevention options for populations engaging in RAI practices. We explored the feasibility of formulating rectal suppositories with potent antiviral drugs for on-demand use. A fixed-dose combination of tenofovir (TFV) and elvitegravir (EVG) (40 mg each) was co-formulated in six different suppository bases (three fat- and three water-soluble). Fat-soluble witepsol H15 and water-soluble polyethylene glycol (PEG) based suppositories demonstrated favorable in vitro release and were advanced to assess in vivo pharmacokinetics following rectal administration in macaques. In vivo drug release profiles were similar for both suppository bases. Median concentrations of TFV and EVG detected in rectal fluids at 2 h were 1- and 2-logs higher than the in vitro IC50, respectively; TFV-diphosphate levels in rectal tissues met or exceeded those associated with high efficacy against rectal simian HIV (SHIV) exposure in macaques. Leveraging on these findings, a PEG-based suppository with a lower dose combination of tenofovir alafenamide (TAF) and EVG (8 mg each) was developed and found to achieve similar rectal drug exposures in macaques. This study establishes the utility of rectal suppositories as a promising on-demand strategy for HIV PrEP and supports their clinical development.

scholarly journals Ultra-small Fe3O4 nanodots encapsulated in layered carbon nanosheets with fast kinetics for lithium/potassium-ion battery anodes

RSC Advances ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 1261-1270
Author(s):  
Qianqian Peng ◽  
Chuan Guo ◽  
Shuo Qi ◽  
Weiwei Sun ◽  
Li-Ping Lv ◽  
...  
Keyword(s):  
Reaction Kinetics ◽  
Robust Stability ◽  
Potassium Ion ◽  
High Conductivity ◽  
Fast Reaction ◽  
Fast Kinetics ◽  
Carbon Nanosheets

Ultra-small Fe3O4 nanodots encapsulated in layered carbon nanosheet nanocomposites were synthesized, showing fast reaction kinetics, high conductivity, and robust stability.

PET-RAFT single unit monomer insertion of β-methylstyrene derivatives: RAFT degradation and reaction selectivity

2021 ◽  
Author(s):  
Lei Zhang ◽  
Ruizhe Liu ◽  
Shiyang Lin ◽  
Jiangtao Xu
Keyword(s):  
Reaction Kinetics ◽  
Single Unit ◽  
Chain Transfer ◽  
Fast Reaction ◽  
Reaction Selectivity ◽  
Reversible Addition

Reversible addition-fragmentation chain transfer (RAFT) single unit monomer insertion (SUMI) of β-Methylstyrene derivatives into diverse RAFT agents presented fast reaction kinetics, but a significant degradation of the SUMI products occurred...

Understanding Microdroplet Formations for Biomedical Applications

2008 ◽  
Author(s):  
Salil Desai ◽  
Anthony Moore ◽  
Benjamin Harrison ◽  
Jagannathan Sankar
Keyword(s):  
Drug Delivery ◽  
Sodium Chloride ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Biomedical Applications ◽  
Tissue Scaffolds ◽  
Ambient Conditions ◽  
On Demand ◽  
Drop On Demand

This paper focuses on understanding microdroplet formation of sodium alginate biopolymer at various concentrations utilizing drop-on-demand inkjet technology. We investigate the effect of sodium chloride on the rheology of sodium alginate and derive a correlation between the size of the droplet versus the size of the microcapsules formed. Varying sizes of microcapsules are formed based on different concentrations of calcium chloride solvent. This understanding will give insight for fabricating drug delivery capsules and tissue scaffolds that are subject to extreme ambient conditions when interfaced with in-vivo environments.

Fast reaction kinetics of porphyrin dimerization in aqueous solution

1970 ◽  
Vol 92 (11) ◽  
pp. 3312-3316 ◽  
Author(s):  
Radha R. Das ◽  
Robert F. Pasternack ◽  
Robert A. Plane
Keyword(s):  
Aqueous Solution ◽  
Reaction Kinetics ◽  
Fast Reaction ◽  
Kinetics Of

scholarly journals Development and long-term evaluation of a new 68Ge/68Ga generator based on nano-SnO2 for PET imaging

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Eduardo Romero ◽  
Alfonso Martínez ◽  
Marta Oteo ◽  
Marta Ibañez ◽  
Mirentxu Santos ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Mouse Model ◽  
Pet Imaging ◽  
Research Reactor ◽  
On Demand ◽  
Term Evaluation ◽  
Investigation Period ◽  
Direct Use

AbstractRadionuclide generator systems can routinely provide radionuclides on demand such as 68Ga produced by a 68Ge/68Ga generator without the availability of an on-site accelerator or a research reactor. Thus, in this work nano-SnO2 was used to develop a new 68Ge/68Ga generator which was evaluated over a period of 17 months and 305 elution cycles. The elution yield was 91.1 ± 1.8% in the first 7 mL (1 M HCl as eluent) when the generator was new and then it decreased with time and use to 73.8 ± 1.9%. Around 80% of the elutable 68Ga activity was obtained in 1 mL and the 68Ge content in the eluate did not exceed 1 × 10–4% over the investigation period when it was eluted regularly. The described generator provided adequate results for radiolabelling of DOTA-TOC with direct use of eluate. In addition, [68Ga]Ga-DOTA-TOC was tested satisfactorily for in vivo tumor detection by microPET/CT imaging in a lung cancer mouse model.

scholarly journals Interdisciplinary Tasks in the Cyclotron Production of Radiometals for Medical Applications. The Case of 47Sc as Example

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 444 ◽  
Author(s):  
Alessandra Boschi ◽  
Petra Martini ◽  
Valentina Costa ◽  
Antonella Pagnoni ◽  
Licia Uccelli
Keyword(s):  
Target Material ◽  
Current Status ◽  
Production Cycle ◽  
Medical Applications ◽  
Chemical Processing ◽  
Cyclotron Production ◽  
On Demand ◽  
Radiochemical Yields ◽  
The Ideal

The growing number of cyclotrons of different sizes installed in the territory has given a strong impulse to the production of conventional and emerging radionuclides for medical applications. In particular, the great advantage of using medical cyclotrons is the possibility to produce on-site, when needed (on-demand), with medical radionuclides of interest encouraging the personalized medicine approach. Radiometals satisfy the ideal characteristics that radionuclides should have for routine employment in nuclear medicine, especially since they have a robust chemistry suitable to synthetize stable in vivo radiopharmaceuticals with high radiochemical yields. In this letter several interdisciplinary aspects involved in the radiometals cyclotron production cycle are summarized focusing the attention on cyclotron production facilities, target material, and chemical processing available for medical applications. As an example, the current status and recent development in the production of the theranostic radionuclide scandium-47 have been reported.

A photo-triggerable aptamer nanoswitch for spatiotemporal controllable siRNA delivery

Nanoscale ◽  
2020 ◽  
Vol 12 (20) ◽  
pp. 10939-10943 ◽  
Author(s):  
Deyao Zhao ◽  
Ge Yang ◽  
Qing Liu ◽  
Wenjing Liu ◽  
Yuhua Weng ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Sirna Delivery ◽  
Gene Modulation ◽  
On Demand

Spatiotemporal controllable siRNA delivery and gene modulation by light-triggerable aptamer nanoswitcher was reported in this study, which achieved on-demand siRNA internalization by cancer cells at desired site and time in vitro and in vivo.

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