Methocel-Lipid Hybrid Nanocarrier for Efficient Oral Insulin Delivery

Even with the use of double-emulsion technique for preparation, the hydrophobic nature of solid lipid nanoparticles (SLNs) limits their encapsulation efficiency (EE%) for peptides such as insulin. In this study, we hypothesize that inclusion of Methocel into SLN to form Methocel-lipid hybrid nanocar...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2016-05, Vol.105 (5), p.1733-1740
Main Authors: Boushra, Mariam, Tous, Sozan, Fetih, Gihan, Xue, Hui-Yi, Tran, Ngoc T., Wong, Ho Lun
Format: Article
Language:English
Subjects:
Administration, Oral
Caco-2 Cells
Cell Survival - drug effects
Cell Survival - physiology
Dose-Response Relationship, Drug
Drug Carriers - administration & dosage
Drug Carriers - metabolism
Drug Delivery Systems - methods
encapsulation
Humans
Insulin - administration & dosage
Insulin - metabolism
Lipids
Methylcellulose - administration & dosage
Methylcellulose - metabolism
Nanoparticles - administration & dosage
Nanoparticles - metabolism
nanotechnology
oral drug delivery
peptides
stability
toxicity
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Summary:Even with the use of double-emulsion technique for preparation, the hydrophobic nature of solid lipid nanoparticles (SLNs) limits their encapsulation efficiency (EE%) for peptides such as insulin. In this study, we hypothesize that inclusion of Methocel into SLN to form Methocel-lipid hybrid nanocarriers (MLNs) will significantly enhance insulin EE% without compromising the various characteristics of SLN favorable for oral drug delivery. Our data show that incorporation of 2% wt/wt of Methocel A15C had doubled insulin EE% (around 40%) versus conventional SLN prepared using standard double emulsion technique. MLN significantly protected the entrapped insulin against chymotrypsin degradation at gastrointestinal pH. Using intestinal epithelial cells Caco2 as a model, it was shown that MLN could be extensively taken up by Caco2 cells while demonstrating low cytotoxicity. The results indicate that MLN have preserved the key advantages of SLN (biocompatibility, low cytotoxicity, good drug protection, and good interaction with cells) while overcoming their key limitation for efficient peptide entrapment. Based on this, MLN may serve as a promising nanocarrier for oral delivery of peptides.
ISSN:0022-3549
1520-6017
DOI:10.1016/j.xphs.2016.02.018