Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.3.1.21 (
CPT
)
4,580
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
We report here a unique method of formulating camptothecin-polylactide (CPT-PLA) conjugate nanoparticles, termed nanoconjugates (NCs), through
CPT
/(BDI)ZnN(
TMS
)(2) [(BDI) = 2-((2,6-diisopropylphenyl)amido)-4-((2,6-bisalkyl)-imino)-2-pentene] mediated polymerization of lactide (LA) followed by nanoprecipitation. When
CPT
was used as the initiator to polymerize LA in the presence of (BDI)ZnN(
TMS
)(2), the polymerization was completed within hours with nearly 100%
CPT
loading efficiency and 100% LA conversion.
CPT
loading as high as 19.5% can be achieved for the
CPT
-polylactide (CPT-PLA) conjugate prepared at a LA/
CPT
ratio of 10. The steric bulk of the chelating ligands and the type of metals used had a dramatic effect on the initiation of the LA polymerization and the tendency of the ring-opening of the
CPT
lactone. The
CPT
/(BDI)ZnN(
TMS
)(2)-mediated LA polymerization yielded
CPT
-PLA conjugates with well-controlled molecular weights and narrow molecular weight distributions (1.02-1.18). The nanoprecipitation of
CPT
-PLA led to the formation of NCs around 100 nm in size with narrow particle size distributions. Sustained release of
CPT
from
CPT
-PLA NCs was achieved without burst release.
CPT
-PLA NCs were toxic to PC-3 cells with tunable IC(50) possible by adjusting the drug loading of the
CPT
-PLA NCs.
...
PMID:Controlled synthesis of camptothecin-polylactide conjugates and nanoconjugates. 2000 Apr 58
