Vesicles from Pluronic/poly(lactic acid) block copolymers as new carriers for oral insulin delivery.
The morphologies of poly(lactic acid)-b-Pluronic-b-poly(lactic acid) (PLA-F127-PLA) aggregates in aqueous solutions were reported previously to be vesicular nano-particles by our group. In the present study, we seek to investigate the feasibility of using PLA-F127-PLA vesicles as oral delivery carrier for insulin. Both in vitro and in vivo release behavior of insulin loaded in PLA-F127-PLA vesicles were studied. A biphasic release behavior was observed for the in vitro release of insulin from PLAF127-29 vesicles. More importantly, it was found in the diabetic mice tests that the blood glucose concentration of oral insulin-loaded PLAF127-29 vesicles decreased from 18.5 to 5.3 mmol/L within 4.5 h and the minimum blood glucose concentration (about 4.5 mmol/L) was achieved after about 5 h. Furthermore, the blood glucose concentration was maintained at this level for at least an additional 18.5 h. These results proved that PLA-F127-PLA vesicles could be promising polymeric carriers for oral insulin delivery application due to their prolonged hypoglycemic effect.
Xiong
Xiang Yuan
XY
School of Life Science, Jiangxi Science & Technology Normal University, Nanchang, China. xyxiong@gmail.com <xyxiong@gmail.com>
Li
Yu Ping
YP
Li
Zi Ling
ZL
Zhou
Chun Li
CL
Tam
Kam Chiu
KC
Liu
Zhi Yong
ZY
Xie
Guo Xiu
GX
D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D004337:Drug Carriers; D004339:Drug Compounding; D005240:Feasibility Studies; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007700:Kinetics; D008297:Male; D051379:Mice; D053758:Nanoparticles; D011060:Poloxalene / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry*; D012995:Solubility
D001786:Blood Glucose; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D011091:Polyesters; C430808:poly(lactide-pluronic)copolymer; D011060:Poloxalene