Insulin Sublingual Film Former

Insulin was chosen as a model drug for the study of enhancing effect of various absorption enhancers and their combinations NAC as a mucolytic agent on sublingual delivery.Sublingual patch was prepared using bioadhensive polymers and evaluated in vitro and in vivo.Enhancing effect of transmucosal absorption enhancers was studied.In vitro and in situ methods were conducted to compare the effect of various transsublingul absorption enhancers and their combinations.In the in vitro transport study,no insulin was found in the receptor cell.In the in situ study,5%sodium taurodeoxycholate(TDC),5% polyxyethylene-9-lauryl ether(BL-9),5%tartaric acid(TA),5%sodium caprate(C10), 5%nonylphenoxy polyoxyethylene-10(NP-10),5%N-acetylcysteine(NAC), 5%sodium dodecyl sulfate(SDC),5%p-t-octyl phenol polyoxyethylene-9.5(TX-100) showed no significant enhancing effect.While their combinational absorption enhancer 5%NAC+5%TX-100 enhanced the transublingual absorption of insulin significantly.Insulin sublingual patch was prepared and the in vivo study was conducted. Different patches were fabricated using several mucoadhesive and film-forming polymers.These patches were evaluated in terms of appearence,mucoadhesive time, dissolution time and mucoadhesion.The best patch was loaded with insulin and absorption enhancers.In vitro evaluation was performed.Optimized formulation turned out to be:Alginate sodium 0.75 g,CMC-Na 0.375 g,PVA 0.75 g,glycerol 0.8 g,NAC 1 g,TX-100g,insulin 40 mg.Statistical investigation of in vitro release revealed that Higuchi's model provided the best fit.In vivo study of insulin sublingual patch was conducted.The hypoglycemic response and AAC were examined after sublingual delivery of insulin patch to both normal and diabetec rabbits.The results showed that the glucose level of normal and diabetic rabbits were both significantly decreased versus blank patch control.The AAC of the normal rabbits were(2140±834.3)%·min and the diabetic rabbits were (3487.8±136.2)%·min.Insulin sublingual patch is a good hypoglycemic.Oral sublingual delivery system is hopeful to be a insulin to non-parental dosage.