Folate-targeted drug-delivery systems prepared by nano-comminution.
BACKGROUND
The size reduction ability of conventional wet comminution has been improved by proper polymeric stabilizer systems, and the resulting nano-comminution methods have led to the commercialization of many poorly water-soluble drugs after improving their bioavailability. During nano-comminution, polymer steric stabilizers physically adsorb onto the surface of drug particles.


METHODS
In this study, the cross-linking and subsequent functionalization methods of the physically adsorbed polymers were used to widen the applicability of the nano-comminution. Chitosan was used as a steric stabilizer for two hydrophobic drugs, naproxen and paclitaxel.


RESULTS
Chitosan was successfully cross-linked (immobilized) by tripolyphosphate. The cross-linked stable polymer layer on drug nanoparticles was conjugated with folic acid, a model targeting moiety. The chemical reactions were performed without destroying the stabilities of drug nanosuspensions. The cross-linking and conjugation reactions significantly modified the release profiles of drug nanoparticles.


CONCLUSIONS
This simple preparation method can be utilized to prepare novel drug encapsulations and folate-targeted delivery systems.
Kim
Sujung
S
Department of Chemical Engineering and Materials Science, Chung-Ang University, Seoul, South Korea.
Lee
Jonghwi
J
D048271:Chitosan / Q000737:chemistry*; D003432:Cross-Linking Reagents / Q000737:chemistry; D016503:Drug Delivery Systems; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D005492:Folic Acid / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D053758:Nanoparticles; D009288:Naproxen / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry
D003432:Cross-Linking Reagents; D005079:Excipients; D011122:Polyphosphates; D009288:Naproxen; D048271:Chitosan; D005492:Folic Acid; C005692:triphosphoric acid; D017239:Paclitaxel