Niosomes with sorbitan monoester as a carrier for vaginal delivery of insulin: studies in rats.
To prepare and investigate the potential of the niosomes vaginal delivery system for systemic treatment of insulin is the goal of this study. Two kinds of vesicles with Span 40 and Span 60 were prepared by lipid phase evaporation methods with sonication. The niosomal entrapment efficiency was determined by column chromatography. The particle size and morphology of the vesicles also were evaluated. The results showed optimized niosomes prepared in this study had niosomal entrapment efficiency 26.68 +/- 1.41% for Span 40 and 28.82 +/- 1.35% for Span 60, respectively. The particle sizes of Span 40 niosomes and Span 60 niosomes were 242.5 +/- 20.5 nm and 259.7 +/- 33.8 nm, respectively. There were no significant differences in appearance between the two types of vesicles. The hypoglycemic effects, and insulin concentrations after vaginal administration of insulin vesicles to rats were investigated. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability of vaginal administration of insulin vesicles were determined. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability of insulin-Span 60 vesicles group were 8.43% and 9.61%, and insulin-Span 40 niosomes were 9.11% and 10.03% (p > 0.05). Span 60 and Span 40 niosomes were both higher than blank Span 40, Span 60 vesicles, and free insulin physical mixture groups (p < 0.05). The results indicates insulin-Span 60, Span 40 niosomes had an enhancing effect on vaginal delivery of insulin. Although the factors controlling the process for penetration of a portion of vaginally administrated niosomes into bloodstream from vaginal tract is still not fully understood, our results demonstrated that after encapsulation in niosomes of definite type, insulin became an active and efficiently therapeutic agent when administrated vaginally and might be a good carrier for vaginal delivery of protein drugs.
Ning
Meiying
M
Beijing Union Medical University, Beijing, PR China. mayning999@yahoo.com.cn
Guo
Yingzhi
Y
Pan
Huaizhong
H
Yu
Heming
H
Gu
Zhongwei
Z
D000282:Administration, Intravaginal; D000496:Alloxan; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D001786:Blood Glucose; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004355:Drug Stability; D005260:Female; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007279:Injections, Subcutaneous; D007328:Insulin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D010052:Ovariectomy; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
D001786:Blood Glucose; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D011136:Polysorbates; D000496:Alloxan