BACKGROUND Glucagon-like peptide-1(GLP1)is an endogenous peptide that regulates blood glucose level.But its susceptibility to rapid metabolic degradation limits its therapeutic use.AIM To prepare GLP1-encapsulated nan...BACKGROUND Glucagon-like peptide-1(GLP1)is an endogenous peptide that regulates blood glucose level.But its susceptibility to rapid metabolic degradation limits its therapeutic use.AIM To prepare GLP1-encapsulated nanosize particle with controlled release property to improve the systemic half-life of GLP1.METHODS GLP1 nanoparticles were prepared by complexation of GLP1 with carbonate apatite nanoparticles(CA NPs).The physicochemical properties of the CA NPs,the effects of GLP1-loaded CA NPs on cell viability,and the systemic bioavailability of GLP1 after CA NPs administration were determined.RESULTS The GLP1-loaded CA NPs was within 200 nm in size and stable in fetal bovine serum.The formulation did not affect the viability of human cell lines suggesting that the accumulation of CA NPs in target tissues is safe.In Sprague Dawley rats,the plasma GLP1 Levels as measured from the GLP1-loaded CA NPs-treated rats,were significantly higher than that of the control rats and free GLP1-treated rats at 1 h post-treatment(P<0.05),and the level remained higher than the other two groups for at least 4 h.CONCLUSION The GLP1-loaded CA NPs improved the plasma half-life of GLP1.The systemic bioavailability of GLP1 is longer than other GLP1 nanoparticles reported to date.展开更多
基金Supported by an FRGS grant from the Ministry of Education,Malaysia,No.FRGS/2/2014/SG05/MUSM/03/1.
文摘BACKGROUND Glucagon-like peptide-1(GLP1)is an endogenous peptide that regulates blood glucose level.But its susceptibility to rapid metabolic degradation limits its therapeutic use.AIM To prepare GLP1-encapsulated nanosize particle with controlled release property to improve the systemic half-life of GLP1.METHODS GLP1 nanoparticles were prepared by complexation of GLP1 with carbonate apatite nanoparticles(CA NPs).The physicochemical properties of the CA NPs,the effects of GLP1-loaded CA NPs on cell viability,and the systemic bioavailability of GLP1 after CA NPs administration were determined.RESULTS The GLP1-loaded CA NPs was within 200 nm in size and stable in fetal bovine serum.The formulation did not affect the viability of human cell lines suggesting that the accumulation of CA NPs in target tissues is safe.In Sprague Dawley rats,the plasma GLP1 Levels as measured from the GLP1-loaded CA NPs-treated rats,were significantly higher than that of the control rats and free GLP1-treated rats at 1 h post-treatment(P<0.05),and the level remained higher than the other two groups for at least 4 h.CONCLUSION The GLP1-loaded CA NPs improved the plasma half-life of GLP1.The systemic bioavailability of GLP1 is longer than other GLP1 nanoparticles reported to date.
