Abstract
Purpose: To potentially enhance the bioavailability and extend the bioactivity effectiveness of Isoleucine-Proline-Proline (IPP, an antihypertensive bioactive peptide of dairy origin), a novel Lyotropic Liquid Crystalline Pharmacosomal Nanoparticle (LLCPNP) was synthesized, and its physicochemical and technological characteristics were studied.Methods: LLCPNPs precursors were developed using IPP and soy phosphatidylcholine via complex formation. Polarized light microscopy, small angle X-ray scattering, differential scanning calorimetry, dynamic light scattering and Fourier transform infrared spectroscopy were employed to characterize the physicochemical properties of the nanoparticles. The in-vitro release and its related mechanisms were also studied.Results: Fourier transform infrared spectroscopy confirmed the complexation between the components of LLCPNPs. Phase behavior evaluation by polarized light microscope showed the characteristic birefringent texture. These findings along with those of small angle X-ray scattering and differential scanning calorimetry proved the formation of lamellar LLCPNPs. These particles represented nanometric size (<100 nm), high incorporation efficiency (93.72%) and proper physicochemical stability during long-term storage. In-vitro studies demonstrated a sustained release behavior fitted to non-Fickian diffusion and Higuchi kinetic models.Conclusion: The present study results emphasized that LLCPNPs could be proposed as an unrivaled carrier to promote the bioavailability, stability and shelf-life of nutraceutical and biopharmaceutical formulations containing bioactive peptides.
Highlights
In recent decades, application of the Lyotropic Liquid Crystals (LLCs) in the field of drug delivery has gained considerable attraction from many scientists and research communities.[1,2,3,4,5,6] The unique and peculiar physicochemical and structural characteristics of LLCs, similarity to the bio-systems and providing superior advantages than traditional delivery systems are the causes of this scientific interest
The present study aims to investigate the physicochemical characteristics of Lyotropic Liquid Crystalline Pharmacosomal Nanoparticle (LLCPNP), for potential application in oral delivery formulations containing bioactive peptides with extended antihypertensive therapeutic effects
Fourier Transform Infrared (FTIR) spectroscopy To substantiate the complex formation in LLCPNPs precursor, its infrared spectrum and the spectra of its components were evaluated, which showed the significant changes in the former compared to the latters (Figure 2)
Summary
Application of the Lyotropic Liquid Crystals (LLCs) in the field of drug delivery has gained considerable attraction from many scientists and research communities.[1,2,3,4,5,6] The unique and peculiar physicochemical and structural characteristics of LLCs, similarity to the bio-systems and providing superior advantages than traditional delivery systems are the causes of this scientific interest These structures are considered as an intermediate state of matter between a crystalline solid (consisting the long-range positional and orientational order in three dimensions) and an isotropic liquid (with no long-range order), which need a solvent to be formed. The utilization of these bioactive peptides reduces the cost of hypertension treatment and adverse side effects.[15,16,17,18] In this regard, the function of IPP has been prominent, but its undesirable pharmacokinetics, including low bioavailability, short half-life, rapid clearance from the body and probable interaction with the other components in oral delivery
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