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The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-11-11 , DOI: 10.2147/ijn.s261932 Morteza Yaghoobian 1 , Azadeh Haeri 1 , Noushin Bolourchian 1 , Soraya Shahhosseni 2 , Simin Dadashzadeh 1, 3
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-11-11 , DOI: 10.2147/ijn.s261932 Morteza Yaghoobian 1 , Azadeh Haeri 1 , Noushin Bolourchian 1 , Soraya Shahhosseni 2 , Simin Dadashzadeh 1, 3
Affiliation
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.
中文翻译：
Niosomes 的表面活性剂成分和表面电荷对瑞格列奈作为 BCS II 模型药物的口服吸收的影响
背景： Niosomes 是由非离子表面活性剂自组装形成的双层囊泡，作为潜在的口服给药系统受到越来越多的关注，但尚未系统研究 niosomal 制剂参数对其口服能力的影响。本研究的目的是研究表面活性剂组成和 niosomes 的表面电荷对提高瑞格列奈 (REG) 作为 BCS II 模型药物的口服生物利用度的影响。
方法：制备了来自 HLB 范围为 4-28 的各种非离子表面活性剂（Tweens、Spans、Brijs、Myrj、泊洛沙姆 188、TPGS 和 Labrasol）的 Niosomes（13 种配方），并对其负载效率、流体动力学直径、zeta 电位、药物进行了表征发布配置文件和稳定性。在大鼠（8 个体内组）中研究了所选制剂的口服药代动力学。
结果：结果表明，表面活性剂的类型显着影响纳米体的体外和体内电位。C最大值选择的 niosomes 以及药物混悬剂（作为对照）给药后 REG 和 AUC 值的顺序为 Tween 80> TPGS> Myrj 52> Brij 35> Span 60≈Suspension。将硬脂胺作为正电荷诱导剂添加到基于 Tween 80 的 niosomes 中，导致药物吸收的额外增加，AUC 和 C max的值分别比药物悬浮液高 3.8 倍和 4.7 倍。
结论：基于阳离子 Tween 80 的 niosomes 可能代表了开发 BCS II 药物口服递送系统的有前景的平台。
更新日期：2020-11-12
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.
中文翻译：
Niosomes 的表面活性剂成分和表面电荷对瑞格列奈作为 BCS II 模型药物的口服吸收的影响
背景： Niosomes 是由非离子表面活性剂自组装形成的双层囊泡，作为潜在的口服给药系统受到越来越多的关注，但尚未系统研究 niosomal 制剂参数对其口服能力的影响。本研究的目的是研究表面活性剂组成和 niosomes 的表面电荷对提高瑞格列奈 (REG) 作为 BCS II 模型药物的口服生物利用度的影响。
方法：制备了来自 HLB 范围为 4-28 的各种非离子表面活性剂（Tweens、Spans、Brijs、Myrj、泊洛沙姆 188、TPGS 和 Labrasol）的 Niosomes（13 种配方），并对其负载效率、流体动力学直径、zeta 电位、药物进行了表征发布配置文件和稳定性。在大鼠（8 个体内组）中研究了所选制剂的口服药代动力学。
结果：结果表明，表面活性剂的类型显着影响纳米体的体外和体内电位。C最大值选择的 niosomes 以及药物混悬剂（作为对照）给药后 REG 和 AUC 值的顺序为 Tween 80> TPGS> Myrj 52> Brij 35> Span 60≈Suspension。将硬脂胺作为正电荷诱导剂添加到基于 Tween 80 的 niosomes 中，导致药物吸收的额外增加，AUC 和 C max的值分别比药物悬浮液高 3.8 倍和 4.7 倍。
结论：基于阳离子 Tween 80 的 niosomes 可能代表了开发 BCS II 药物口服递送系统的有前景的平台。
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