Enhancement of oral bioavailability of the poorly water-soluble drug silybin by sodium cholate/phospholipid-mixed micelles

Yu, Jiangnan; Zhu, Yuan; Wang, Li; Peng, Min; Tong, Shanshan; Cao, Xia; Qiu, Hui; Xu, Ximing

doi:10.1038/aps.2010.55

Cited by 112 publications

(64 citation statements)

References 20 publications

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“…The equilibrium solubility of silybin in water is approximately 51.06 μg/mL at 37 °C. Therefore, some preparations have been made in recent years to improve the solubility and bioavailability of silybin, including phospholipid complexes [28] , sodium cholate/phospholipid complexes and povidone-sodium cholate-phospholipid mixed micelles [29,30] . Recently, 2,3-dehydrosilybin, an oxidized form of silybin, has been reported to exhibit a significantly greater antioxidant and anticancer activity in comparison with silybin [22] .…”

Section: Discussionmentioning

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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Section: Discussionmentioning

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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“…Taking advantage of the aforementioned property, various mixed micelles systems based on bile acids and salts were successfully employed for improving the solubility of extremely lipophilic drugs. Mixed micelles composed of sodium cholate with PL, linoleic acid and lecithin were found to improve the solubility and intestinal absorption of silybin (Yu et al, 2010), clofazimine (O'Reilly et al, 1994) and Cyclosporine A (Guo et al, 2005), respectively. Furthermore, the applicability of bile salts in the preparation of nanoparticulate systems was demonstrated in different researches.…”

Section: Bile Salts In Drug Delivery Systemsmentioning

confidence: 99%

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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“…Pharmacokinetic parameters of the drug, namely, peak plasma concentration (C max ), time to C max (T max ), mean residence time (MRT) and area under the concentration-time curve (AUC t ) were calculated using the BAPP 2.3 pharmacokinetic software (purchased from the Center of Drug Metabolism of China Pharmaceutical University, China) [20] . All parameter values are reported as the mean value±standard deviation unless otherwise noted.…”

Section: Analysis Of Pharmacokinetic Parametersmentioning

confidence: 99%

Oral delivery of capsaicin using MPEG-PCL nanoparticles

et al. 2014

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Aim: To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality. Methods: CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining. Results: CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation. Conclusion: CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.

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Enhancement of oral bioavailability of the poorly water-soluble drug silybin by sodium cholate/phospholipid-mixed micelles

Cited by 112 publications

References 20 publications

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

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

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

Oral delivery of capsaicin using MPEG-PCL nanoparticles

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