Dendrimers are a potential drug carrier. Because modification with polyethylene glycol (PEG) is known to improve the blood retention, PEGylated dendrimers have been studied as a useful drug carrier. In this study, three types of PEGylated L-lysine-bearing polyamidoamine dendrimers (PEG2k-Lys-PAMAM (G4), PEG5k-Lys-PAMAM (G4), PEG2k-Lys-PAMAM (G5)) were synthesized, which are composed of a dendrimer of different generations (generations 4 and 5) and PEG chains with different molecular weights (2k and 5k). An acetylated L-lysine-bearing dendrimer was also synthesized as a non-PEGylated dendrimer. Bifunctional diethylenetriaminepentaacetic acid (pSCN-benzyl-DTPA) was bound to the epsilon -amino group of lysine in a dendrimer, to be labeled with radioactive indium-111. These PEGylayed dendrimers showed longer blood retention and lower accumulation in other normal organs such as the kidneys than the non-PEGylated dendrimer. The PEGylated dendrimers with the higher generation and the longer PEG led the greater blood retention.
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http://dx.doi.org/10.1016/j.ijpharm.2009.09.015 | DOI Listing |
Mol Pharm
January 2025
School of Pharmacy and Technology Management, SVKM's Narsee Monjee Institute of Management Studies (NMIMS), Deemed to be University, Shirpur, Dhule, Maharashtra 425405, India.
Cancer has emerged as a global health crisis, claiming millions of lives annually. Dendrimers and dendronized nanoparticles, a novel class of nanoscale molecules with highly branched three-dimensional macromolecular structures, have gained significant attention in cancer treatment and diagnosis due to their unique properties. These dendritic macromolecules offer a precisely controlled branching architecture, enabling functionalization with specific targeting molecules to enhance the selective delivery of therapeutic agents to tumor cells while minimizing systemic toxicity.
View Article and Find Full Text PDFSci Rep
November 2024
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.
J Inorg Biochem
January 2025
University of Alcalá, Department of Organic and Inorganic Chemistry, and Research Institute in Chemistry "Andrés M. Del Río" (IQAR), Madrid, Spain; Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Madrid, Spain; Ramón y Cajal Health Research Institute (IRYCIS), IRYCIS, Madrid 28034, Spain. Electronic address:
A synthetic procedure was designed for the preparation and characterization of Ag and Ru complexes containing NHC ligands functionalized with PEG fragments. Stability studies were conducted to gain insight of the species in water and other solvents like DMSO, or with reagents like imidazole as representative group for histidine amino acid. The presence of Cl atoms instead of H in the 4,5 positions of the N-heterocyclic carbene afforded higher water stability.
View Article and Find Full Text PDFJ Control Release
November 2024
Department of Pharmaceutical Nanotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Leicester School of Pharmacy, De Montfort University, Leicester, United Kingdom. Electronic address:
Nanoparticles fabricated to deliver anticancer drugs are usually designed to present optimized tumor penetration and cell internalization. However, there are some barriers and difficulties with most current technologies. Herein, size and charge switchable polyamidoamine (PAMAM) megamers (SChPMs) were prepared for the delivery of doxorubicin (DOX).
View Article and Find Full Text PDFMalar J
August 2024
Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, MO, USA.
Background: Plasmodium falciparum, the malaria-causing parasite, is a leading cause of infection-induced deaths worldwide. The preferred treatment approach is artemisinin-based combination therapy, which couples fast-acting artemisinin derivatives with longer-acting drugs, such as lumefantrine, mefloquine, and amodiaquine. However, the urgency for new treatments has risen due to the parasite's growing resistance to existing therapies.
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