Formulation, characterization and permeability study of nano particles of lipo-endomorphin-1 for oral delivery.
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 P(app) 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.
School of Chemistry and Molecular Biosciences (SCMB), University of Queensland , St Lucia, Brisbane, QLD 4072 , Australia.
Sharareh
S
Eskandari
Pegah
P
Varamini
Istvan
I
Toth
D000284:Administration, Oral; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D006863:Hydrogen-Ion Concentration; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D010539:Permeability
D009842:Oligopeptides; C105293:endomorphin 1