Formulation, characterization and permeability study of nano particles of lipo-endomorphin-1 for oral delivery.

Eskandari, Sharareh, Varamini, Pegah and Toth, Istvan (2013) Formulation, characterization and permeability study of nano particles of lipo-endomorphin-1 for oral delivery.. Journal of Liposome Research, 23 4: 311-317. doi:10.3109/08982104.2013.805339

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Author Eskandari, Sharareh
Varamini, Pegah
Toth, Istvan
Title Formulation, characterization and permeability study of nano particles of lipo-endomorphin-1 for oral delivery.
Journal name Journal of Liposome Research   Check publisher's open access policy
ISSN 0898-2104
1532-2394
Publication date 2013-12
Year available 2013
Sub-type Article (original research)
DOI 10.3109/08982104.2013.805339
Volume 23
Issue 4
Start page 311
End page 317
Total pages 7
Place of publication New York, NY, United States
Publisher Informa Healthcare
Collection year 2014
Language eng
Formatted abstract
Three different formulations of a lipid-modified endomorphin-1 peptide (C10LAA-Endo-1) were prepared, characterized, and evaluated for their permeability through Caco-2 cell membranes. Solid lipid nanoparticles (SLN), enteric coated (EC), and the EC-SLN of C10LAA-Endo-1 is a modified structure of endomorphin-1 for oral delivery. Physico–chemical characterization of the formulations showed that among all formulations, EC-[C10LAA-Endo-1] had the lowest particle size and the highest EE% and absolute zeta potential. Release of drug from SLN, EC-SLN and EC-[C10LAA-Endo-1] in acid media was 14.30 (±2.7)%, 3.0 (±1.0)% and 10.2 (±3.0)%, respectively. Release data in buffer media (pH = 7.4) showed that enteric coated formulations released C10LAA-Endo-1 more slowly than uncoated formulations. It was also demonstrated that direct coating of C10LAA-Endo-1 with Eudragit® S100 significantly enhanced the permeability of the compound through Caco-2 cell membranes with a 39-fold higher Papp compared to C10LAA-Endo-1. These findings indicated that EC-C10LAA-Endo-1 is a promising candidate to promote the oral delivery of the previously modified endomorphin-1 peptide analogue and is worthy of future animal investigations.
Keyword Endomorphin-1
Eudragit S100
Lipoamino acid
Oral delivery
Peptide delivery
Solid lipid nanoparticle
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Posted online on: 12 August 2013.

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2014 Collection
School of Chemistry and Molecular Biosciences
 
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Created: Mon, 02 Sep 2013, 14:06:58 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences