Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt

Chen, Yaping; Lü, Yi; Chen, Jianming; Lai, Jie; Sun, Jing; Hu, Fuqiang; Wu, Wei

doi:10.1016/j.ijpharm.2009.04.022

Cited by 229 publications

(177 citation statements)

References 37 publications

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“…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, 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). Chen et al (2009) related the ultra-deformability of liposomes due to the inclusion of bile salts to the enhanced carrier-mediated transmembrane absorption. Furthermore, BS-liposomes can freely convert into mixed micelles in the GI environment and hence enhance transmembrane drug absorption (Chen et al, 2009).…”

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: 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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“…Recently, great interest has been shown in the use of liposomes for improving oral absorption and bioavailability of hydrophobic drugs [6] . Liposomes are enclosed vesicles composed of phosphatidylcholine and cholesterol lipid bilayers, which have been extensively studied as drug carriers [7,8] .…”

Section: Introductionmentioning

confidence: 99%

Proliposomes for oral delivery of dehydrosilymarin: preparation and evaluation in vitro and in vivo

Chu

Tong

et al. 2011

Acta Pharmacol Sin

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Aim: To formulate proliposomes with a polyphase dispersed system composed of soybean phospholipids, cholesterol, isopropyl myristate and sodium cholate to improve the oral bioavailability of dehydrosilymarin, an oxidized form of herbal drug silymarin. Methods: Dehydrosilymarin was synthesized from air oxidation of silymarin in the presence of pyridine, and proliposomes were prepared by a film dispersion-freeze drying method. Morphological characterization of proliposomes was observed using a transmission electron microscope. Particle size and encapsulation efficiency of proliposomes were measured. The in vitro release of dehydrosilymarin from suspension and proliposomes was evaluated. The oral bioavailability of dehydrosilymarin suspension and proliposomes was investigated in rabbits. Results: The proliposomes prepared under the optimum conditions were spherical and smooth with a mean particle size in the range of 7 to 50 nm. Encapsulation efficiency was 81.59%±0.24%. The in vitro accumulative release percent of dehydrosilymarinloaded proliposomes was stable, which was slow in pH 1.2, and increased continuously in pH 6.8, and finally reached 86.41% at 12 h. After oral administration in rabbits, the relative bioavailability of proliposomes versus suspension in rabbits was 228.85%. Conclusion: Proliposomes may be a useful vehicle for oral delivery of dehydrosilymarin, a drug poorly soluble in water.

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“…A major reason for the increased stability might be due to structural changes in the vesicles. As seen in literature, the incorporation of BS made the lipid membrane more deformable (49)(50) which might alter the ion permeation. Changing the membrane viscosity might also change the interaction and uptake of physiological BS.…”

Section: Discussionmentioning

confidence: 77%

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

et al. 2017

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-PURPOSE: Liposomes have been studied as a colloidal carrier in drug delivery systems, especially for oral administration. However, their low structural integrity in the gut is still a major shortcoming. Membrane disruptive effects of physiological bile salts in the small intestine result in premature drug release prior to intestinal absorption. Thus, we analyzed the stabilizing effect of sodium deoxycholate when incorporated into nano-sized liposomes. METHOD: Cefotaxime-loaded liposomes were prepared with different sodium deoxycholate concentrations (3.75-30 mM) by rotary film evaporation followed by nanosize reduction. The physical integrity of liposomes was evaluated by monitoring cefotaxime leakage, particle sizes in different simulated physiological media. The oral bioavailability and pharmacokinetics of cefotaxime was assessed in rats (n = 6 per group) after single dose of drug-encapsulated in liposomes containing bile salt, drug in conventional liposomes, and cefotaxime solution (oral and intravenous). RESULTS: Simulated gastric fluid with low pH showed less effect on the stability of liposomes in comparison to media containing physiological bile salts. Liposomes containing 15 mM sodium deoxycholate were most stable in size and retained the majority of encapsulated cefotaxime even in fed state of simulated intestinal fluid being the most destructive media. Pharmacokinetics data showed an increase in Cmax and AUC0-inf in the following order: cefotaxime solution < conventional liposomes < liposomes made with bile salts. The total oral bioavailability of cefotaxime in liposomes containing bile salt was found to be 5-times higher compared to cefotaxime solution and twice as much as in conventional liposomes. CONCLUSION: Incorporation of bile salts, initially used as membrane permeation enhancer, also acted as a stabilizer against physiological bile salts. The nanosized liposomes containing sodium deoxycholate were able to reduce the leakage of encapsulated cefotaxime in the gut due to the improved vesicle stability and to enhance the oral bioavailability of acid-labile drugs up to 5-fold.

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Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt

Cited by 229 publications

References 37 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

Proliposomes for oral delivery of dehydrosilymarin: preparation and evaluation in vitro and in vivo

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

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