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. 2017 Nov 20:8:844.
doi: 10.3389/fphar.2017.00844. eCollection 2017.

Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

Md K Anwer  1 , Ramadan Al-Shdefat  2 , Essam Ezzeldin  3   4 , Saad M Alshahrani  1 , Abdullah S Alshetaili  1 , Muzaffar Iqbal  3   4
Affiliations

Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

Md K Anwer et al. Front Pharmacol. .

Abstract

Eluxadoline is a newly approved orally administered drug used for the treatment of Irritable Bowel Syndrome with Diarrhea. It is reported as a poorly water-soluble drug due to which its dissolution rate and oral bioavailability are very poor. In this work, various plain PLGA nanoparticles (NPs) (F1-F4) were prepared and optimized based on particle size, PDI, zeta potential and percent drug entrapment efficiency (EE). The developed plain NPs (F1-F4) showed average particle size ranging from 260.19 to 279.76 nm with smooth surface and EE of 17.83-56.29%. The optimized plain NPs (F3) had particle size of 273.76 ± 7.25 nm with a low PDI value 0.327, zeta potential - 30.63 ± 2.47 mV and % EE of 56.29 ± 2.56%. The optimized F3 NPs was further submitted for enteric coating using Eudragit S100 polymer and evaluated in terms of particles characterization, in vitro release and pharmacokinetic studies in rats. The bioavailability of plain and coated nanaoparticles were enhanced by 6.8- and 18.5-fold, respectively, compared to normal suspension. These results revealed that the developed coated NPs could be used for its oral delivery for an effective treatment of Irritable Bowel Syndrome with Diarrhea.

Keywords: PLGA; eluxadoline; enteric coating; nanoparticles; pharmacokinetics.

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Figures

FIGURE 1
FIGURE 1
Zeta potential of plain PLGA NPs.
FIGURE 2
FIGURE 2
Zeta potential of Eudragit coate PLGA NPs.
FIGURE 3
FIGURE 3
Comparative in vitro release profile.
FIGURE 4
FIGURE 4
FTIR spectra of Eluxadoline (ELUX), plain and coated PLGA NPs.
FIGURE 5
FIGURE 5
XRF spectra of ELUX, plain and coated PLGA NPs.
FIGURE 6
FIGURE 6
Scanning electron microscopic (SEM) images of (A) plain and (B) coated PLGA NPs.
FIGURE 7
FIGURE 7
Multiple reaction monitoring (MRM) chromatogram of ELUX and IS in plasma samples after administration of ELUX normal suspension.
FIGURE 8
FIGURE 8
Mean ± SD plasma concentration vs. time profiles of ELUX.
See this image and copyright information in PMC

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