Enhanced oral absorption of insulin-loaded liposomes containing bile salts: A mechanistic study

Niu, Mengmeng; Tan, Yanan; Guan, Peipei; Hovgaard, Lars; Lü, Yi; Qi, Jianping; Lian, Ruyue; Li, Xiaoyang; Wu, Wei

doi:10.1016/j.ijpharm.2013.11.028

Cited by 151 publications

(101 citation statements)

References 41 publications

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“…Recently, BS-liposomes have been investigated as stable carriers for delivering sensitive therapeutic agents and proteins by replacing a fraction of the CH in the lipid bilayers with bile salts (Guan et al, 2011;Niu et al, 2011Niu et al, , 2012Niu et al, , 2014. Schematic illustrations of different types of liposomes comprising bile salts in comparison to conventional liposome are presented in Figure 3.…”

Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

“…Several studies have demonstrated the superiority of BS-liposomes to conventional liposomes in improving the oral absorption of different therapeutic agents and proteins (Chen et al, 2009;Niu et al, 2011). Although the exact underlying mechanisms of oral absorption enhancement of drugs or proteins loaded in BS-liposomes have not been comprehensively elucidated, several authors acknowledged the capability of intact BSliposomes to permeate across the unstirred water layer followed by uptake of the vesicles by membranous epithelial cells (M-cells) in the Payer's patch (Aramaki et al, 1993) and transcellular through enterocytes (Niu et al, 2014) in addition to the facilitated transport through the paracellular pathway (Chen et al, 2009;Niu et al, 2012). Furthermore, it is expected that upon contact with the intestinal epithelial, the included bile salts may increase the membrane fluidity followed by membrane-destabilizing effect, which facilitate internalization of the vesicles (Chen et al, 2009).…”

Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

“…Furthermore, BS-liposomes can freely convert into mixed micelles in the GI environment and hence enhance transmembrane drug absorption (Chen et al, 2009). Using imaging method, Niu et al (2014) demonstrated that the in vivo residence time of oral administrated BSliposomes in the GIT was longer than its conventional counterpart. The transenterocytic internalization of BS-liposomes in Caco-2 cells was confirmed using fluorescence imaging (Niu et al, 2014).…”

Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

“…Nevertheless, the efficacy of conventional vesicles has been compromised by their instability in the GIT, which necessitated modification in their bilayers constructs to improve their in vivo resistance (Andrieux et al, 2009). Different research efforts conducted over the past decade has demonstrated the effectiveness of including bile salts into vesicular systems bilayers in improving their in vivo resistance and performance after oral administration (Chen et al, 2009;Niu et al, 2014). However, these attempts have not gained considerable attention in relation to their demonstrated positive outcomes.…”

Section: Introductionmentioning

confidence: 99%

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Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

103

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Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment exemplified by low pH, presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by inclusion of bile salts into lipid bilayers constructs. The effectiveness of orally administrated BS-vesicles in improving the performance of vesicles has been demonstrated in researches. Yet, these attempts did not gain considerable attention. This is the first review that provides a comprehensive overview of utilizing BS-vesicles as a promising pharmaceutical carrier with a special focus on their successful applications in oral delivery of therapeutic macromolecules and vaccines. Insights on the possible mechanisms by which BSvesicles improve the oral bioavailability of the encapsulated drug or immunological response of entrapped vaccine are explained. In addition, methods adopted to prepare and characterize BSvesicles are described. Finally, the gap in the scientific researches tackling BS-vesicles that needs to be addressed is highlighted.

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Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

Section: Bile Salts-containing Liposomes (Bs-liposomes)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

103

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“…Immunocytochemical studies suggest that the major route for absorption of free insulin is by the transcellular route through the enterocytes [41] in which macromolecules are taken up at the luminal membrane by phagocytosis or pinocytosis followed by exocytosis at the basolateral membrane and absorption into the mesenteric circulation [42]. This route of absorption is facilitated by co-infusion of insulin with cell-penetrating peptides [23, 43,44] and bile salt liposomes [45]. In addition, there may be uptake through pores in the mucosa which form transiently as a consequence of the shedding of the enterocytes at the tips of the villi [46].…”

Section: Promotion Of Absorption Of Natural Insulinmentioning

confidence: 99%

Investigations into the absorption of insulin and insulin derivatives from the small intestine of the anaesthetised rat

McGinn¹,

Morrison

2016

Journal of Controlled Release

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Investigations into the absorption of insulin and insulin derivatives from the small intestine of the anaesthetised rat. Journal of Controlled Release, 232, pp. 120-130. (doi:10.1016Release, 232, pp. 120-130. (doi:10. /j.jconrel.2016 This is the author's final accepted version.There may be differences between this version and the published version. You are advised to consult the publisher's version if you wish to cite from it.http://eprints.gla.ac.uk/120651/ ABSTRACTExperiments have been undertaken to determine the extent to which cholic acid conjugates of insulin were absorbed from the small intestine of anaesthetised rats by means of the bile salt transporters of the ileum. The measure used to assess the absorption of the cholyl-insulins was the amount of hypoglycaemia following infusion into the small intestine. Control experiments involving infusion of natural insulin into the ileum showed either nil absorption or absorption of a small amount of insulin as indicated by transient dip in the blood glucose concentration. However, when insulin was co-infused with the bile salt taurocholate, this was followed by a marked hypoglycaemic response which was specific to the ileum and did not occur on infusion into the jejunum. When the two cholyl conjugates of insulin were tested viz. B 29 -Lys-cholyl-insulin and B 1 -Phe-cholyl-insulin, both were biologically active as indicated by hypoglycaemic responses on systemic injection, though their potency was about 40% of that of natural insulin. While there was no evidence for the absorption of B 29 -Lys-cholyl-insulin when infused into the ileum, B 1 -Phe-cholyl-insulin did cause a long lasting hypoglycaemic response, indicating that absorption had occurred. Since the hypoglycaemic response was blocked on co-infusion with taurocholate and was absent for infusion of the conjugate into the jejunum, these results were taken as evidence that B 1 -Phe-cholyl-insulin had been taken up by the ileal bile salt transporters. This would indicate that B 1 -Phe-cholyl-insulin is worthy of further investigation for use in an oral insulin formulation.

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Engineering Nano‐ and Microparticles as Oral Delivery Vehicles to Promote Intestinal Lymphatic Drug Transport

et al. 2021

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Enhanced oral absorption of insulin-loaded liposomes containing bile salts: A mechanistic study

Cited by 151 publications

References 41 publications

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Investigations into the absorption of insulin and insulin derivatives from the small intestine of the anaesthetised rat

Engineering Nano‐ and Microparticles as Oral Delivery Vehicles to Promote Intestinal Lymphatic Drug Transport

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