Liraglutide-loaded multivesicular liposome as a sustained-delivery reduces blood glucose in SD rats with diabetes.
Subcutaneous liraglutide-loaded multivesicular liposomes (Lrg-MVLs) were developed as a sustained drug-delivery system for treating diabetes and their properties were characterized. The Lrg-MVLs prepared using a two-step water-in-oil-in-water double emulsification process had a spherical appearance with a mean diameter of 6.69 μm and an encapsulation efficiency of 82.23 ± 4.78% without any initial burst release. Their pharmacodynamics (PD) and pharmacokinetics (PK) were also studied after a single subcutaneous administration to Sprague-Dawley (SD) rats with diabetes. The PD results demonstrated that Lrg-MVLs presented sustained glucose-lowering effects for nearly a week, while the pharmacokinetic parameters showed that the plasma liraglutide concentration of the designed preparation produced Cmaxof 81.979 ± 12.140 pg/ml and an MRT0-tof 88.224 ± 3.893 h. Furthermore, retention of Lrg-MVLs at the injection site was studied semiquantitatively by an in vivo imaging system, which can be used to evaluate the drug release from MVLs in vivo. In conclusion, MVLs are a promising carrier for liraglutide and Lrg-MVLs deserve further study for the treatment of diabetes.
a Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.
Lixue
L
Zhang
a Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.
Lei
L
Ding
a Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.
Chengcheng
C
Tang
a Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.
Yang
Y
Li
a Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.
Li
L
Yang
D000279:Administration, Cutaneous; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects*; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D000069450:Liraglutide / Q000008:administration & dosage* / Q000737:chemistry*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
D001786:Blood Glucose; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008081:Liposomes; D000069450:Liraglutide
Liraglutide; multivesicular liposome; pharmacodynamics; pharmacokinetics; sustained-delivery