Improved oral bioavailability of breviscapine via a Pluronic P85-modified liposomal delivery system.
OBJECTIVE
Breviscapine, a hydrophobic drug used for treating cardiovascular disease, was encapsulated in liposomes to improve its pharmaceutical characteristics. This study describes a novel liposome composition approach to specifically inhibit the P-glycoprotein efflux system.


METHODS
Breviscapine-loaded Pluronic P85-coated liposomes were prepared by the thin film hydration technique. The particle size, zeta potential and encapsulation efficiency of the formulations were characterized. In-vitro drug release and permeability of Caco-2 cells were investigated. In-vitro characteristics and pharmacokinetics of the liposomes were evaluated in rat studies.


RESULTS
The Pluronic P85-modified liposomes dispersed individually and had an approximate diameter of 118.8 ± 4.9 nm and a zeta potential of -35.4 ± 1.5 mV. Encapsulation efficiency was more than 90%. The use of the P85-coated liposomes resulted in significantly (P<0.05) increased absorption of breviscapine in Caco-2 cells and in 5.6-fold enhancement in its oral bioavailability in rats.


CONCLUSIONS
The P85-modified liposomes for the oral delivery of breviscapine were prepared using l-α-phosphatidylcholine (soy-hydrogenated) and cholesterol with a narrow size distribution. This method seems to effectively enhance the bioavailability of breviscapine in rats.
Hospital of Traditional Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Lianyungang, China.
Yue
Y
Zhou
Qing
Q
Ning
Dan-Ni
DN
Yu
Wei-Guang
WG
Li
Jin
J
Deng
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells; D002214:Capsules; D002317:Cardiovascular Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D002784:Cholesterol; D016503:Drug Delivery Systems; D005419:Flavonoids / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007408:Intestinal Absorption; D008081:Liposomes; D008297:Male; D010316:Particle Size; D010539:Permeability; D010713:Phosphatidylcholines; D011060:Poloxalene; D020442:Poloxamer; D017207:Rats, Sprague-Dawley
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002214:Capsules; D002317:Cardiovascular Agents; D005419:Flavonoids; D008081:Liposomes; D010713:Phosphatidylcholines; C422648:pluronic block copolymer p85; D020442:Poloxamer; C061097:breviscapine; D011060:Poloxalene; D002784:Cholesterol
Pluronic P85; breviscapine; liposome; oral bioavailability