,Kzuki Tguchi,Keishi Ymski, Min Skurgi,Shun’ichi Kurod,Mski Otgiri,

aFaculty of Pharmaceutical Sciences,Sojo University,Kumamoto 860-0082,Japan

bDepartment of Nanoscience,Sojo University,Kumamoto 860-0082,Japan

cThe Institute of Scientifc and Industrial Research,Osaka University,Osaka 567-0047,Japan dGraduate School of Bioagricultural Sciences,Nagoya University,Nagoya 464-8601,Japan

Effect of PEGylation on the physicochemical and pharmacokinetic characteristics of bovine serum albumin-encapsulated liposome

Yuko Okamotoa,Kazuaki Taguchia,Keishi Yamasakia, Mina Sakuragib,Shun’ichi Kurodac,d,Masaki Otagiria,*

aFaculty of Pharmaceutical Sciences,Sojo University,Kumamoto 860-0082,Japan

bDepartment of Nanoscience,Sojo University,Kumamoto 860-0082,Japan

cThe Institute of Scientifc and Industrial Research,Osaka University,Osaka 567-0047,JapandGraduate School of Bioagricultural Sciences,Nagoya University,Nagoya 464-8601,Japan

A R T I C L E I N F O

Article history:

Available online 25 November 2015

Liposome

PEGylation

Bovine serum albumin

There is now little doubt that PEGylation is useful and is in widespreadusebecauseitprovidesaprolongedhalf-life,ahigher stabilityandalowerimmunogenicity[1].However,itisofconcern that PEGylation may affect the physicochemical and pharmacokineticcharacteristicsofprotein-encapsulatedliposome.Thus, we prepared the bovine serum albumin(BSA)-encapsulated liposome(BSA-liposome)withorwithoutPEGandthencompared their physicochemical and pharmacokinetic characteristics (Fig.1).BSA-liposomes were prepared by the thin-flm hydration method.The particle diameter was regulated using the extrusion method.The lipid bilayer was a mixture of egg phosphatidylcholine(PC)and cholesterol at a molar ratio of 2/1,or egg PC,cholesterol and DSPE-PEG2000 at a molar ratio of 12/6/1.

The aggregation of encapsulated BSA was examined by SDS–PAGE.In addition,pharmacokinetic characteristics of non-PEGylated and PEGylated BSA-liposome were examined by using IVIS.As a result,mean diameter and zeta potential were not different between non-PEGylated and PEGylated BSA-liposome. However,loading effciency was slightly reduced from 89%to 70%by the presence of PEG.In addition,encapsulated BSA in both non-PEGylated and PEGylated BSA-liposome existed in the monomer(no aggregation).Furthermore,PEGylation prolonged the blood retention to evade accumulation in the liver. In conclusion,PEGylation had little infuence on the physicochemical characteristics of BSA-liposome but might enhance the retention in the circulation.

Fig.1–Schematic representation of BSA-liposome.

R E F E R E N C E

[1]He X,Li L,Su H,et al.Poly(ethylene glycol)-block-poly(εcaprolactone)-and phospholipid-based stealth nanoparticles with enhanced therapeutic effcacy on murine breast cancer by improved intracellular drug delivery.Int J Nanomedicine 2015;10:1791–1804.

*E-mail address:otagirim@ph.sojo-u.ac.jp.

Peer review under responsibility of Shenyang Pharmaceutical University.

http://dx.doi.org/10.1016/j.ajps.2015.11.101

1818-0876/?2016 Production and hosting by Elsevier B.V.on behalf of Shenyang Pharmaceutical University.This is an open access article under the CC BY-NC-ND license(http://creativecommons.org/licenses/by-nc-nd/4.0/).