PCL-b-PEO micelles as a delivery vehicle for FK506: assessment of a functional recovery of crushed peripheral nerve.
The aim of this work was to test in vivo a new block copolymer-based delivery system containing lipophilic drug FK506, known as Tacrolimus. Tacrolimus is currently used in clinics as an immunosupressant agent, and more recently it has been shown that it can exert neurotrophic effects. We prepared, characterized, and assessed polycaprolactone-b-polyethylenoxyde (PCL-b-PEO) micelles containing FK506 in vitro and in vivo. By using well-established animal model of peripheral nerve injury (crushed sciatic nerve), we show that the rate of functional recovery of injured nerve is significantly enhanced in rats treated with micellar FK506. These findings support the notion that PCL-b-PEO is a suitable polymer material for FK506 and suggest its wider applicability as a delivery vehicle for other biologically active, poorly soluble therapeutic agents.
Allen
C
C
Department of Chemistry, McGill University, Montreal, Canada.
Eisenberg
A
A
Mrsic
J
J
Maysinger
D
D
D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D008823:Micelles; D009409:Nerve Crush; D011091:Polyesters / Q000008:administration & dosage / Q000493:pharmacokinetics*; D020959:Polyethylene / Q000008:administration & dosage / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012584:Sciatic Nerve / Q000293:injuries / Q000378:metabolism*; D016559:Tacrolimus / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D007166:Immunosuppressive Agents; D008823:Micelles; D011091:Polyesters; C016240:polycaprolactone; D020959:Polyethylene; D016559:Tacrolimus