Sustained-release hydroxycamptothecin polybutylcyanoacrylate nanoparticles as a liver targeting drug delivery system.
Sustained release hydroxycamptothecin polybutylcyanoacrylate nanoparticles (HCPT-PBCA-NP) associated with polybutylpyrolidone (PVP) for liver targeting were prepared by the adsorption-entrapping method. The morphology, sizes, drug loading efficiencies, release characteristics in vitro, distribution and pharmacokinetic parameters in vivo of the HCPT-PBCA-NP associated with PVP were studied. The median diameter of the particles was 81 nm and the drug loading was 1.2%. The release characteristics in vitro were in accordance with the Higuchi equation: Q = 0.0615 + 0.0940 mean square root t. 64.5% of the HCPT were concentrated in the liver at 15 min after i.v. administration of HCPT-PBCA-NP associated with PVP. The plasma drug concentration-time curve of the HCPT in rabbits was fitted to a two-compartment open model. The Vc, T 1/2 and CL were 3.5L; 147h; 0.18L x h(-1), respectively. The method of preparation presented in this paper seems to bean alternative for the preparation of PBCA-NP of poorly soluble drugs both in water and in lipid.
Sun
Xun
X
West China School of Pharmacy, Sichuan University, Chengdu, PR China.
Wu
Fang
F
Lu
Wei
W
Zhang
Zhi-Rong
ZR
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003102:Colloids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005612:Freeze Drying; D007275:Injections, Intravenous; D008099:Liver / Q000378:metabolism*; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D011134:Polysaccharides / Q000737:chemistry*; D011817:Rabbits; D012996:Solutions; D013816:Thermodynamics; D014018:Tissue Distribution
D000972:Antineoplastic Agents, Phytogenic; D003102:Colloids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011134:Polysaccharides; D012996:Solutions; C493955:mannoglucan