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. 2020 Nov 11:15:8767-8781.
doi: 10.2147/IJN.S261932. eCollection 2020.

The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug

Morteza Yaghoobian  1 , Azadeh Haeri  1 , Noushin Bolourchian  1 , Soraya Shahhosseni  2 , Simin Dadashzadeh  1   3
Affiliations

The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug

Morteza Yaghoobian et al. Int J Nanomedicine. .

Abstract

Background: Niosomes, bilayer vesicles formed by the self-assembly of nonionic surfactants, are receiving increasing attention as potential oral drug delivery systems but the impact of niosomal formulation parameters on their oral capability has not been studied systematically. The aim of this study was to investigate the impact of surfactant composition and surface charge of niosomes in enhancing oral bioavailability of repaglinide (REG) as a BCS II model drug.

Methods: Niosomes (13 formulations) from various nonionic surfactants having HLB in the range of 4-28 (Tweens, Spans, Brijs, Myrj, poloxamer 188, TPGS and Labrasol) were prepared and characterized concerning their loading efficiency, hydrodynamic diameter, zeta potential, drug release profile, and stability. The oral pharmacokinetics of the selected formulations were studied in rats (8 in vivo groups).

Results: The results revealed that type of surfactant markedly affected the in vitro and in vivo potentials of niosomes. The Cmax and AUC values of REG after administration of the selected niosomes as well as the drug suspension (as control) were in the order of Tween 80> TPGS> Myrj 52> Brij 35> Span 60≈Suspension. Adding stearyl amine as a positive charge-inducing agent to the Tween 80-based niosomes, resulted in an additional increase in drug absorption and values of AUC and Cmax were 3.8- and 4.7-fold higher than the drug suspension, respectively.

Conclusion: Cationic Tween 80-based niosomes may represent a promising platform to develop oral delivery systems for BCS II drugs.

Keywords: BCS II; HLB; niosome; oral bioavailability; repaglinide; surface charge; surfactant type.

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Conflict of interest statement

The authors report no conflicts of interest.

Figures

Figure 1
Figure 1
In vitro release profiles of REG from the various formulations in SGF (A and B), SIF (C and D) and B-SIF (E and F) at 37°C. Data represent mean ± SD (n=3).
Figure 2
Figure 2
Hydrodynamic diameter (A), PDI (B) and ZP (C) of the selected niosomes immediately after preparation and after incubation in SGF (2 hours) and B-SIF (10 hours) at 37°C.
Figure 3
Figure 3
The mean plasma concentration of REG after a single oral dose (1 mg/kg) of drug suspension and the selected niosomal formulations to rats (n=6, mean ± SD).
Figure 4
Figure 4
Morphology of the optimal REG-loaded niosomes (T80-STA) by AFM observation.
Figure 5
Figure 5
In vitro release profiles of REG from the T80-STA formulation in SGF (A), SIF (B) and B-SIF (C) at 37°C. Data represent mean ± SD (n=3).
Figure 6
Figure 6
The mean plasma concentration of REG after a single oral dose of T80-STA and T80-STA empty niosomes with suspension of REG compared to suspension of REG after oral administration in rats (n=6, mean ± SD).
Figure 7
Figure 7
Cell viability of Caco-2 after 3 hours incubation with T80 and T80-STA niosomes (mean ± SD, n = 3).
Figure 8
Figure 8
Histological sections of small intestinal segments from Wistar rats after oral administration of (A) Control and (B) T80-STA formulation.
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