Subscribe: pubmed: "Journal of controll...
Added By: Feedage Forager Feedage Grade B rated
Language: English
amphiphilic star  controlled release  cpt  drugs  hydrophobic  journal controlled  peg cpt  peg  pubmed  release  star peg  star  water 
Rate this Feed
Rate this feedRate this feedRate this feedRate this feedRate this feed
Rate this feed 1 starRate this feed 2 starRate this feed 3 starRate this feed 4 starRate this feed 5 star

Comments (0)

Feed Details and Statistics Feed Statistics
Preview: pubmed: "Journal of controll...

pubmed: "Journal of controll...

NCBI: db=pubmed; Term=("Journal of controlled release : official journal of the Controlled Release Society"[Jour])


Amphiphilic star PEG-Camptothecin conjugates for intracellular targeting.

Amphiphilic star PEG-Camptothecin conjugates for intracellular targeting.

J Control Release. 2016 Sep 24;

Authors: Omar R, Slakman EC, Leichtmann-Bardoogo Y, Mizrahi B

Camptothecin (CPT) is a naturally occurring cytotoxic alkaloid having a broad spectrum of antitumor activity. Unfortunately, it has low bioavailability and encapsulation efficiency, limiting its clinical use. We report on our efforts to develop a novel drug delivery prototype composed of a short, star hydrophilic polyethylene glycol (PEG) backbone and hydrophobic CPT (PEG4-CPT). The amphiphilic bio-conjugate self-assembles in water into stable spherical nano-particles with a mean diameter of 200nm and CPT substitution percentage of 27%w/w. CPT is released in a sustained release profile without burst effect. In addition, PEG4-CPT nano-particles are able to load a co-drug, water soluble or non-water soluble doxorubicin and release them simultaneously with the free CPT. The biological evaluation of PEG4-CPT against HeLa cells showed improved cellular uptake and enhanced cytotoxicity compared to free CPT. Thus, in this approach CPT acts in two ways: As the hydrophobic segment that enables self-assembly in water and as a potent anticancer agent. This concept of combining hydrophobic drugs and short star polymers shows great potential for efficient delivery of hydrophobic chemotrophic drugs as well as for drugs with inherent stability and pharmacokinetic barriers.

PMID: 27677603 [PubMed - as supplied by publisher]