Affiliation:
1. Faculty of Pharmacy, Cyprus International University, Nicosia 99258 Cyprus
2. Department of Pharmaceutical Sciences,
Faculty of Pharmacy, Isra University, Queen Alya Airport Street, Amman 11622 Jordan
3. Department of Pharmaceutical
Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid 22110 Jordan
4. Department of Pharmacology, Faculty of Medicine, Jordan University of Science and Technology, Irbid 22110 Jordan
Abstract
Aim:
In this study, four fluorescein hydrophobic ionic complexes were formed with the
cationic polymers Eudragit RS, Eudragit RL, Eudragit E, and polyethyleneimine (PEI) to provide
fluorescein sustained release, sustained cellular uptake, and stability.
Methods:
Complexes were loaded in a self-emulsifying drug delivery system (SEDDS) composed
of 40% Tween 80, 20% Kolliphor EL, 15% 2-n-Octyl-1-dodecanol, and 25% dipropylene glycol.
SEDDS were investigated regarding their size, polydispersity index (PDI), zeta potential, and cytotoxicity.
Fluorescein release from SEDDS was performed in phosphate buffer (pH 6.8 and pH 8),
and the released fluorescein was evaluated for cellular uptake. Moreover, fluorescein from all of
the SEDDS pre-concentrates was released at different time points to check its long-term stability
over six months.
Results:
The average fluorescein load in SEDDS was 0.045%. SEDDS showed an average droplet
size of 24.9 ± 1.6 nm with PDI ≤ 0.3. SEDDS complexes diluted 1:100 increased the zeta potential
from -7.3 mV to +3.7 mV and provided > 85% cell viability. A 92.27 ± 3.18% fluorescein exhibited
a few seconds of immediate release when used as control or PEI complex in SEDDS. On the
contrary, Eudragit-fluorescein complexes in SEDDS showed sustained release of 87.01 ± 5.22%
fluorescein in ≤ 70 min with 22.19 ± 14.56% and 59.27 ± 16.57% released at 10 min in pH 6.8 and
pH 8 release media, respectively. Comparatively, the medium at pH 6.8 maintained a significantly
improved sustained fluorescein release (p ≤ 0.001). Furthermore, Eudragit RS/RL compared to
Eudragit E, significantly exhibited a slower fluorescein release rate from SEDDS (p ≤ 0.01). The
cellular uptake of the released fluorescein was 72.4 ± 8.2% for all SEDDS complexes after 3 h.
Eudragit complexes compared to PEI complex in SEDDS significantly showed m ore sustained
fluorescein cellular uptake at 1 h and 2 h (p ≤ 0.001). However, SEDDS complexes showed the
longest fluorescein stability with PEI after six months, whereas fluorescein stability for SEDDS
containing fluorescein as Eudragit complex and control showed 39.1% and 82.5% fluorescence
decrease, respectively, after three months.
Conclusion:
In the developed SEDDS, the presence of hydrophobic ionic complexes can significantly
promote longer stability and sustained cellular uptake of fluorescein while releasing in a
sustained manner.
Publisher
Bentham Science Publishers Ltd.
Subject
Biomedical Engineering,Pharmaceutical Science
Cited by
1 articles.
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