Enhanced oral paclitaxel bioavailability after administration of paclitaxel-loaded nanosponges.
The aim of this study was to evaluate the pharmacokinetics of paclitaxel-loaded nanosponges (PLN) in rats. The study also evaluates the intrinsic effect of the dosage form on the improvement of paclitaxel oral bioavailability. Paclitaxel-loaded nanosponges were prepared and characterized in terms of size distribution, drug solubilization, and the kinetics of paclitaxel sedimentation. Taxol((R)) and paclitaxel-loaded nanosponges were administered orally to rats. The plasma concentration of paclitaxel was determined using liquid chromatography. The average size of PLN was 350 +/- 25 nm. The drug payload of paclitaxel was 500 +/- 0.27 mg/g of lyophilized powder. The encapsulation efficiency was 99.1 +/- 1.0%, and 1.7 +/- 0.2% of paclitaxel was crystallized after 48 h. The relative oral bioavailability of paclitaxel-loaded nanosponges was 256. After oral administration of paclitaxel-loaded PLN, the area under the plasma concentration time curve was significantly increased ( approximately 3-fold) in comparison to the control group (p < 0.05). The results indicated that PLN provided a promising new formulation to enhance the oral bioavailability of paclitaxel while avoiding the use of cremophore El: Ethanol in Taxol((R)).
Torne
Satyen J
SJ
Pharmaceutical Sciences and Technology, University Institute of Chemical Technology, Mumbai, 400019 India.
Ansari
Khalid A
KA
Vavia
Pradeep R
PR
Trotta
Francesco
F
Cavalli
Roberta
R
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D003460:Crystallization; D004337:Drug Carriers / Q000493:pharmacokinetics*; D004339:Drug Compounding; D006207:Half-Life; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D008657:Metabolic Clearance Rate; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000097:blood / Q000493:pharmacokinetics*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D011108:Polymers; D047392:beta-Cyclodextrins; D017239:Paclitaxel