Polyelectrolyte stabilized multilayered liposomes for oral delivery of paclitaxel

Jain, Sanyog; Kumar, Dinesh; Swarnakar, Nitin K.; Thanki, Kaushik

doi:10.1016/j.biomaterials.2012.05.026

Cited by 173 publications

(140 citation statements)

References 36 publications

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“…[22][23][24][25][26][27][28] Furthermore, the liposomes can improve the oral bioavailability of drugs poorly absorbed through the gastrointestinal tract and alter the in vivo distribution of the drugs encapsulated into liposomes, to increase the therapeutic index. 22,[29][30][31][32] Currently, liposomes have been considered one of the most promising drug delivery carriers. Several preparation technologies for liposome development have been studied in recent years, including the film hydration method, ethanol injection method, and high-pressure homogenization.…”

Section: Discussionmentioning

confidence: 99%

“…[22][23][24][25][26][27][28] Thus, a number of studies showed the liposome carrier could improve the oral bioavailability of poorly bioavailable drugs and change the in vivo distribution of entrapped drugs. [29][30][31][32] For example, Wang et al developed long-circulating nanoliposomes of quercetin, prepared by the emulsified evaporation-low temperature solidification method, using glyceryl behenate and Tween ® 80 as carriers. The researchers showed that the oral absorption of the longcirculating quercetin liposomes in the liposomal formulation, in mice, was better than that of quercetin suspension.…”

Section: Introductionmentioning

confidence: 99%

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Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween ® 80, Phospholipon ® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of −20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1−Q)) =0.609 lnt −1.230 ( r =0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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“…There are cellular models such as HT29-MTX, 20 HT29-FU, 21 HT29-GlucH, 22 and co-cultures Caco-2/ HT29-MTX, 23 Caco-2/HT29-H, 24 Caco-2/HT29-M6. 25 Various protocols have been developed to evaluate interactions between particles and mucus; for example, multiple particle tracking, 12 modified microfiltration device, 14 mucoadhesion assay, 15 in vivo experimentation 26 with radioactivity studies 27 or pharmacokinetic studies, 28 binding properties, 29 side-byside system, 30 side-on-3-compartment, 31 19 and cell association. 37 Some techniques are inconvenient to use, such as the complicated equipment used for multiple particle tracking, a fluorophore such as FRAP, or radioactive materials.…”

Section: Groo Et Almentioning

confidence: 99%

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Groo¹,

Saulnier²,

Gimel³

et al. 2013

IJN

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The bioavailability of paclitaxel (Ptx) has previously been improved via its encapsulation in lipid nanocapsules (LNCs). In this work, the interactions between LNCs and intestinal mucus are studied because they are viewed as an important barrier to successful oral delivery. The rheological properties of different batches of pig intestinal mucus were studied under different conditions (the effect of hydration and the presence of LNCs). Fluorescence resonance energy transfer (FRET) was used to study the stability of LNCs in mucus at 37°C for at least 3 hours. Diffusion through 223, 446, and 893 μm mucus layers of 8.4, 16.8, and 42 μg/mL Ptx formulated as Taxol® (Bristol-Myers Squibb, Rueil-Malmaison, France) or encapsulated in LNCs (Ptx-LNCs) were investigated. The effect of the size of the LNCs on their diffusion was also investigated (range, 25–110 nm in diameter). Mucus behaves as a non-Newtonian gel with rheofluidifying properties and a flow threshold. The viscous (G″) and elastic (G′) moduli and flow threshold of the two mucus batches varied with water content, but G′ remained below G″. LNCs had no effect on mucus viscosity and flow threshold. The FRET efficiency remained at 78% after 3 hours. Because the destruction of the LNCs would lead to a FRET efficiency below 25%, these results suggest only a slight modification of LNCs after their contact with mucus. The diffusion of Taxol® and Ptx-LNCs in mucus decreases if the mucus layer is thicker. Interestingly, the apparent permeability across mucus is higher for Ptx-LNCs than for Taxol® for drug concentrations of 16.8 and 42 μg/mL Ptx ( P <0.05). The diffusion of Ptx-LNCs through mucus is not size-dependent. This study shows that LNCs are stable in mucus, do not change mucus rheological properties, and improve Ptx diffusion at low concentrations, thus making these systems good candidates for Ptx oral delivery. The study of the physicochemical interaction between the LNC surface and its diffusion in mucus is now envisioned.

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“…At first, it was considered to result from the too low water-solubility of these drugs. But many reports show that paclitaxel and calcein could be released into water medium (Veltkamp et al, 2007;Chen et al, 2009;Jain et al, 2012). Then, the main obstruction should come from the gel shell and/or the hydrophobic interaction between the hydrophobic drug and carrier, which increases with the increase of drug hydrophobicity.…”

Section: Drug Release From the Corementioning

confidence: 99%

Synthesis of mesoporous silica-gel core-shell structural microparticles and their multiple drug delivery

Zhi

et al. 2013

Drug Delivery

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(2015) Synthesis of mesoporous silica-gel core-shell structural microparticles and their multiple drug delivery, Drug Delivery, 22:1, 69-78, DOI: 10.3109/10717544.2013 Context: Release of two drugs safely and independently should be necessary in medical or reaction engineering fields to overcome many complex problems such as multi-drug resistance in treatment of disease. Objectives: Core-shell structural microparticles that can load/release two drugs simultaneously are designed and prepared. Materials: The microparticles are composed of mesoporous silica core and hyaluronate (HA)/poly (N-isopropylacrylamide) hybrid gel shell. Methods: The synthesis processes are monitored by powder x-ray diffraction and Fourier transform infrared spectroscopy. The properties of microparticles are characterized by nuclear magnetic resonance, dynamic light scattering and transmission electron microscope methods. Two kinds of drugs are loaded into the mesoporous-core and gel-shell, respectively, and then released under various conditions. Results: The microparticles show uniform spherical shapes with core-shell structures. When temperature is higher than the lower critical solution temperature, the microparticles shrink abruptly and assemble. The drug release rates have been found to depend on the concentration of the microparticle suspensions and pH of the release medium. Discussion: The swellability of the microparticles are controlled by the HA size and gel crosslink density; and the main effect factors on drug releasing behavior are the drug properties and drug diffusion ability. Conclusion:The experimental results confirmed different drugs could be safely loaded into the core-shell structural microparticles and released independently, which might be potential carriers for drugs or catalysts. These microparticles would be expected to make sense for applying in medical or reaction engineering fields. KeywordsCore-shell structure, hybrid gel, mesoporous silica, multiple drug release, temperature sensitive History

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Polyelectrolyte stabilized multilayered liposomes for oral delivery of paclitaxel

Cited by 173 publications

References 36 publications

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Synthesis of mesoporous silica-gel core-shell structural microparticles and their multiple drug delivery

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