Self-assembled "nanocubicle" as a carrier for peroral insulin delivery.
OBJECTIVE
A patient with (insulin-dependent) diabetes mellitus receives at least one subcutaneous insulin injection a day to maintain low serum glucose concentrations. Since patients' compliance with such dosage regimens is too low, the development of an oral formula is clearly attractive. We present the development of a liquid formula that can be easily dispersed in water to produce particles named "nanocubicles" which efficiently encapsulate insulin.


METHODS
Fasted streptozotocin-induced diabetic rats were administered orally with particles encapsulating insulin, and particles without insulin or soluble insulin in water. Groups of rats were also injected soluble insulin in PBS for control. Blood glucose concentration and insulin concentration were measured 1, 2, 3, 4 and 6 h after the administration of the insulin formulas.


RESULTS
In vitro experiments show that the particles can be taken up by the Caco-2 cells at a high ratio. The serum glucose concentration was controlled for more than 6 h after oral insulin administration but returned to the basal concentration in 3 h when 1 IU/kg of insulin was injected intravenously.


CONCLUSIONS
Our biocompatible and stable oral insulin formulation is easy to prepare and produces reproducible hypoglycaemic effects, therefore we anticipate clinical acceptance and utilization of this form of insulin therapy.
Chung
H
H
Biomedical Research Center, Korea Institute of Science and Technology, Seoul, Korea.
Kim
J
J
Um
J Y
JY
Kwon
I C
IC
Jeong
S Y
SY
D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D003922:Diabetes Mellitus, Type 1 / Q000188:drug therapy*; D004337:Drug Carriers; D006801:Humans; D007279:Injections, Subcutaneous; D007328:Insulin / Q000008:administration & dosage* / Q000097:blood / Q000627:therapeutic use; D010349:Patient Compliance; D051381:Rats
D001786:Blood Glucose; D004337:Drug Carriers; D007328:Insulin