Objective: To prepare a valuable nanodevice targeting for hepatic parenchymal cells to improve the effects of drugs for treatment of hepatitis B and liver cancer.
Methods: Generation 3.5 dendrimer (G3.5 PAMAM) was conjugated with fluoresceine isothiocyanate (FITC) to obtain G3.5 PAMAM-FITC, which was then conjugated with 2-aminoethyl ß-D-galactopyranoside (Dgal) in different molar ratios (1:5, 1:10, 1:15, 1:20) to obtain Dgal(n)-PAMAM-FITC. Flow cytometry was applied to examine which of the molar ratios was the best.
Results: Through active ester method, we got conjugates in different molar ratios of G3.5 PAMAM-FITC to Dgal (1:5, 1:10, 1:15, 1:20). Cellular entry of FITC-labeled PAMAM conjugated with different numbers of Dgal was evaluated in vitro by using rat hepatocytes with flow cytometry, and it was found that one molecule of PAMAM conjugated with 20 molecules of Dgal was the best ratio.
Conclusion: Dgal(20)-G3.5 PAMAM-FITC can be used for liver-targeting drug delivery system.
Download full-text PDF |
Source |
---|
Bioconjug Chem
December 2024
Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Kasetsart University, Bangkok 10900, Thailand.
Int J Nanomedicine
November 2024
Key Laboratory for Regenerative Medicine of Ministry of Education, Institute of Hematology, School of Medicine, Jinan University, Guangzhou, 510632, People's Republic of China.
Introduction: T-cell acute lymphoblastic leukemia (T-ALL) is a malignant hematological disease with limited targeted therapy options. Overexpression of B-cell lymphoma/leukemia 11B is frequently observed in T-ALL and contributes to leukemogenesis. Knockdown of BCL11B inhibits T-ALL cell proliferation and induces apoptosis, making it a potential therapeutic target.
View Article and Find Full Text PDFBioconjug Chem
November 2024
Department of Chemistry, Materials and Chemical Engineering "Giulio Natta", Politecnico di Milano, via Mancinelli 7, 20131 Milan, Italy.
This study presents the synthesis, characterization, and application of multifunctional PAMAM G2 and G4 dendrimers decorated with a linear fluorinated guanidino linker designed to improve gene delivery efficiency while minimizing cytotoxicity. For the first time, we were able to fine-tune the degree of grafting (DG) during the functionalization process through efficient "click" Michael addition, achieving the synthesis of a collection of six PAMAM conjugates that showed a significant enhancement in transfection efficiency (TE), surpassing the performance of traditional nonviral vectors. The incorporation of fluorinated moieties not only facilitated better deoxyribonucleic acid (DNA) condensation and TE but also introduced potential applications in F magnetic resonance imaging thanks to the sharp and intense fluorine nuclear magnetic resonance signals and favorable relaxation parameters.
View Article and Find Full Text PDFJ Drug Target
November 2024
PGTD Chemistry, RTM Nagpur University, Nagpur, India.
3-D multi-faceted, nano-globular PAMAM dendritic skeleton is a highly significant polymer that offers applications in biomedical, industrial, environmental and agricultural fields. This is mainly due to its enhanced properties, including adjustable surface functionalities, biocompatibility, non-toxicity, high uniformity and reduced cytotoxicity, as well as its numerous internal cavities. This trait inspires further exploration and advancements in tailoring approaches.
View Article and Find Full Text PDFToxicol Rep
December 2024
Laser Research Centre, Faculty of Health Science, University of Johannesburg, Doornfontein 2028, South Africa.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!