Enhanced hypoglycemic effect of biotin-modified liposomes loading insulin: effect of formulation variables, intracellular trafficking, and cytotoxicity
Open accessAbstract
Peroral protein/peptide delivery has been one of the most challenging, but encouraging topics in pharmaceutics. This article was intended to explore the potential of biotin-modified liposomes (BLPs) as oral insulin delivery carriers. By incorporating biotin-DSPE into the lipid bilayer, we prepared BLPs using reverse evaporation/sonication method. We investigated hypoglycemic effects in normal rats after oral administration of BLPs, and the possible absorption mechanism by a series of in vitro tests. The relative pharmacological bioavailability of BLPs was up to 11.04% that was as much as 5.28 folds of conventional liposomes (CLPs). The results showed that the enhanced oral absorption of insulin mainly attributed to biotin ligand-mediated endocytosis. The results provided proof of BLPs as effective carriers for oral insulin delivery.
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Liposome with lipid:cholesterol ratio 3:1 shows maximum insulin trapping efficiency along with good membrane fluidity and minimum insulin leakage.
“The liposome with a lipid:cholesterol ratio of 3:1 shows maximum insulin trapping efficiency along with good membrane fluidity and minimum insulin leakage from internal aqueous components.79”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [79]
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Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles
Singh, A. P., Biswas, A., Shukla, A., & Maiti, P. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0068-3 · Cited by 645 · see citing works
- Authors
- Zhang, X., Qi, J., Lu, Y., Hu, X., He, W., & Wu, W.
- Affiliations
- Jinan University (CN)
- Fudan University (CN)
- Corresponding author
- Qi, Jianping
- Venue
- Nanoscale Research Letters
- Published
- 2014-04-16
- Volume
- 9
- Issue
- 1
- Pages
- 185-185
- ISSN
- 1556-276X (ISSN-L)
- PMC
- PMC3996857
- OpenAlex
- W2162943325
- Cited by
- 54
- References
- 37
- Citations by year
- 2026: 3 · 2025: 5 · 2024: 8 · 2023: 5 · 2022: 8 · 2021: 3 · 2020: 7 · 2019: 5 · 2018: 3 · 2017: 3 · 2016: 3 · 2014: 1
- FWCI
- 1.32
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- cc-by
- Locations
- Nanoscale Research Letters (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- Program for New Century Excellent Talents in University (NCET-11-)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- oral insulin delivery, hypoglycemic effect, oral absorption, intracellular trafficking, cytotoxicity
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