[The enhancing effect of tomato lectin modified liposomes of insulin on oral absorption in mice].
OBJECTIVE
To investigate the enhancing effect on insulin absorption through GI tract in mice by using tomato lectin (TL) modified liposomes as the carrier.


METHODS
TL-phosphatidylethanolamine (PE) conjugate (TL-PE) was synthesized by using carbodiimide cross-linking method, then the compound was incorporated into the conventional liposomes of insulin. The agglutination test was performed to examine TL biological activities after synthesis and incorporation. When TL modified liposomes were administrated orally to the normal mice or diabetic mice at insulin dose of 350 u x kg(-1), the hypoglycemic effect was determinated according to the blood glucose level.


RESULTS
The blood glucose levels of the normal mice were reduced by modified liposomes. The glucose levels were (85 +/- 5)% at 4 h, (54 +/- 11)% at 8 h, (57 +/- 6)% at 12 h postdose compared with the glucose levels prior to oral administration respectively. However, the conventional liposomes and saline have no hypoglycemic effect. The blood glucose levels of the diabetic mice were obviously reduced by TL modified liposomes, the glucose levels were (38 +/- 13)% at 4 h, (50 +/- 15)% at 8 h, (50 +/- 16)% at 12 h respectively.


CONCLUSIONS
TL modified liposomes promote the oral absorption of insulin due to the specific-site combination on GI cell membrane.
Zhang
Na
N
China Pharmaceutical University, Nanjing 210009, China.
Ping
Qi-neng
QN
Xu
Wen-fang
WF
D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D003692:Delayed-Action Preparations; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000378:metabolism*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D007328:Insulin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D007408:Intestinal Absorption / Q000187:drug effects*; D007421:Intestine, Small / Q000378:metabolism; D008081:Liposomes; D051379:Mice; D010714:Phosphatidylethanolamines / Q000737:chemistry; D037121:Plant Lectins / Q000737:chemistry* / Q000494:pharmacology; D013678:Technology, Pharmaceutical / Q000379:methods
D001786:Blood Glucose; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D008081:Liposomes; D010714:Phosphatidylethanolamines; D037121:Plant Lectins; C034981:tomato lectin; C483858:phosphatidylethanolamine