Novel mucosal insulin delivery systems based on fusogenic liposomes.

Abstract:

PURPOSE:Fusogenic liposomes (FLs) are unique delivery vehicles capable of introducing their contents directly into the cytoplasm with the aid of envelope glycoproteins of Sendai virus (SeV). The objective of this study was to evaluate the potential of FL to improve the mucosal absorption of insulin from rat intestinal membranes. METHOD:The FLs containing insulin were prepared by fusing insulin-loaded liposomes with inactivated SeV particles and were administered directly into the ileal, the colonic, and the rectal loops (10 IU/kg). RESULTS:The FL successfully enhanced the insulin absorption and induced a significant hypoglycemic effect following the colonic and the rectal administration without detectable mucosal damage. This enhancing effect of insulin absorption was further improved by increasing the amount of insulin loaded in the FL and by coencapsulating insulin-degrading enzyme inhibitor. In contrast, the insulin absorption was not increased by the ileal administration of FL because the mucous/glycocalyx layers overlaid on the ileal epithelium impede the fusion of FL to the intestinal mucosa. CONCLUSION:Our results indicated that FL is a useful carrier for improving the absorption of poorly absorbable drugs, such as insulin, via the intestinal tract.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Goto T,Morishita M,Nishimura K,Nakanishi M,Kato A,Ehara J,Takayama K

doi

10.1007/s11095-005-9175-7

subject

Has Abstract

pub_date

2006-02-01 00:00:00

pages

384-91

issue

2

eissn

0724-8741

issn

1573-904X

journal_volume

23

pub_type

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