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. 2021 Feb 17;6(8):5560-5568.
doi: 10.1021/acsomega.0c05963. eCollection 2021 Mar 2.

Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study

Joby Jacob  1 , Nimisha Pulikkal Sukumaran  1 , Shintu Jude  1
Affiliations

Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study

Joby Jacob et al. ACS Omega. .

Abstract

l-ascorbic acid (AA) or vitamin C is a crucial nutrient needed for optimal health. However, being unable to be synthesized by the body, it is thus necessary to be included in health care products. Moreover, AA is one of the antioxidants that occur naturally, which is used in pharmaceutical and food products as an antioxidant additive. However, AA is vulnerable to environmental settings and undergoes oxidative degradation to dehydroascorbic acid and further to inactive products. Therefore, new research strategies and approaches are required to augment its stability. The objective of this study is to develop and characterize a fiber-reinforced-phospholipid (FRP) matrix-based vehicle, Zeal-AA, for the delivery of AA and optimize the oral bioavailability of the obtained AA powder using an efficacy study by open-label, randomized, single-dose, two-treatment, two-sequence, two-period, two-way crossover. The structural and surface morphologies were analyzed by Fourier transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy, and differential scanning calorimetry studies. Encapsulation efficiency, mean particle size, size distribution, ζ-potential measurements, and ADMET profiling revealed the potential delivery system for AA. AUC0-t was found to be 55.23 (mg/dL) for Zeal-AA, whereas it was 9.38 (mg/dL) for AA, and C max was found to be 6.69 (mg/dL) for Zeal-AA, whereas it was 1.23 (mg/dL) for AA, with a fold difference of bioavailability in terms of AUC found to be 5.9 fold. The results show that a single oral dose of Zeal-AA is capable of rising the AA levels in the body relative to the control up to 24 h.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Scanning electron microscopy photographs of AA (A) and Zeal-AA (B); transmission electron microscopy of Zeal-AA (C).
Figure 2
Figure 2
ζ-potential of AA (a) and Zeal-AA (b).
Figure 3
Figure 3
Size distribution curve of Zeal-AA.
Figure 4
Figure 4
FTIR chromatograms of phospholipid (a), TNF (b), AA (c), and Zeal-AA (d).
Figure 5
Figure 5
DSC chromatograms of AA (a) and Zeal-AA (b).
Figure 6
Figure 6
Mean plasma concentrations (mg/dL) of AA (control) compared with Zeal-AA. All of the values stated are mean ± SD.
Scheme 1
Scheme 1. Schematic Representation of the Preparation of Zeal-AA
See this image and copyright information in PMC

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