Sylysia 350/Eudragit S100 solid nanomatrix as a promising system for oral delivery of cyclosporine A

Dai, Wenbing; Guo, Yinglu; Zhang, Hua; Wang, Xueqing; Zhang, Qiang

doi:10.1016/j.ijpharm.2014.11.030

Cited by 20 publications

(6 citation statements)

References 19 publications

(4 reference statements)

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“…Researchers have spent major efforts on developing alternatives, such as self-nano-emulsifying drug delivery systems, 6 lipidbased nanoparticles, 11,12 polymeric-based nanoparticles, 13 micelles, 14,15 liposomes, 16,17 pH sensitive nanoparticles, 7 etc. These novel design CsA carriers offer several advantages compared to the formulations commercialized previously.…”

Section: Results and Discussion Ln Preparation And Characterizationmentioning

confidence: 99%

“…High concentrations of emulsifying agents and organic solvents lead to incompatibility with the shells of soft gelatin capsules as well as precipitation of components when stored at certain temperatures. 6,7 During the last decade, lipid nanoparticles (LN), which consist of a solid lipid matrix stabilized by surfactants, have gained considerable interest as suitable oral delivery systems for drugs that exhibit poor and variable gastrointestinal absorption, not only because of their adequate in vivo performance but also as a result of their versatility in manufacturing processes. Their numerous advantages combine those presented by oil-based formulations and polymeric colloidal carriers.…”

Section: Introductionmentioning

confidence: 99%

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Lipid nanoparticles for cyclosporine A administration: development, characterization, and in vitro evaluation of their immunosuppression activity

Guada¹,

Sebastián²,

Irusta³

et al. 2015

IJN

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Cyclosporine A (CsA) is an immunosuppressant commonly used in transplantation for prevention of organ rejection as well as in the treatment of several autoimmune disorders. Although commercial formulations are available, they have some stability, bioavailability, and toxicity related problems. Some of these issues are associated with the drug or excipients and others with the dosage forms. With the aim of overcoming these drawbacks, lipid nanoparticles (LN) have been proposed as an alternative, since excipients are biocompatible and also a large amount of surfactants and organic solvents can be avoided. CsA was successfully incorporated into LN using the method of hot homogenization followed by ultrasonication. Three different formulations were optimized for CsA oral administration, using different surfactants: Tween ® 80, phosphatidylcholine, taurocholate and Pluronic ® F127 (either alone or mixtures). Freshly prepared Precirol nanoparticles showed mean sizes with a narrow size distribution ranging from 121 to 202 nm, and after freeze-drying were between 163 and 270 nm, depending on the stabilizer used. Surface charge was negative in all LN developed. High CsA entrapment efficiency of approximately 100% was achieved. Transmission electron microscopy was used to study the morphology of the optimized LN. Also, the crystallinity of the nanoparticles was studied by X-ray powder diffraction and differential scanning calorimetry. The presence of the drug in LN surfaces was confirmed by X-ray photoelectron spectroscopy. The CsA LN developed preserved their physicochemical properties for 3 months when stored at 4°C. Moreover, when the stabilizer system was composed of two surfactants, the LN formulations were also stable at room temperature. Finally, the new CsA formulations showed in vitro dose-dependent immuno-suppressive effects caused by the inhibition of IL-2 levels secreted from stimulated Jurkat cells. The findings obtained in this paper suggest that new lipid nanosystems are a good alternative to produce physicochemically stable CsA formulations for oral administration.

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Section: Results and Discussion Ln Preparation And Characterizationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Lipid nanoparticles for cyclosporine A administration: development, characterization, and in vitro evaluation of their immunosuppression activity

Guada¹,

Sebastián²,

Irusta³

et al. 2015

IJN

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“…SFN is slightly absorbed in the GI due to its poor solubility in water. It has been reported that mesoporous materials, such as, mesoporous silica or mesoporous carbon, could be used as poorly water-soluble drug carriers (Jia et al, 2011 ; Minagawa et al, 2012 ; Dai et al, 2015 ; Zhang et al, 2015 ). Usually, nanomatrix were prepared by absorbed the poorly water-soluble drug on the surface or in the nano-structure of the mesoporous material and then coated with suitable excipients.…”

Section: Discussionmentioning

confidence: 99%

“…The contribution for enhancing the solubility and dissolution rate of the poorly water-soluble drugs is since the small nanopores of mesoporous silica can convert a crystalline drug to an amorphous form (Ukmar et al, 2011 ; Wani et al, 2012 ). Sylysia 350 (Sylysia) is a desired mesoporous silica material with a particle size of 3.9 μm and a large number of internal pores about 21 nm which could be used as carrier material to improve the solubility of poorly water-soluble drugs (Jia et al, 2011 ; Wang et al, 2011 ; Dai et al, 2015 ).…”

Section: Introductionmentioning

confidence: 99%

Improving anti-tumor activity of sorafenib tosylate by lipid- and polymer-coated nanomatrix

et al. 2017

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In the present study, we select the Sylysia 350 (Sylysia) as mesoporous material, distearoylphosphatidylethanolamine-poly(ethylene glycol) 2000 (DSPE-PEG) as absorption enhancer and hydroxy propyl methyl cellulose (HPMC) as crystallization inhibitor to prepare sorafenib tosylate (SFN) nanomitrix (MSNM@SFN) for improving the anti-tumor activity of SFN. The MSNM@SFN was prepared by solvent evaporation method. The solubility, dissolution, and bioavailability of SFN in MSNM@SFN were also investigated. The anti-tumor activity of MSNM@SFN was evaluated in vitro and in vivo. Our results indicated that the solubility and dissolution of SFN in MSNM@SFN were significantly increased. The oral bioavailability of SFN in MSNM@SFN was greatly improved 7.7-fold compared with that in SFN suspension. The enhanced anti-tumor activity of MSNM@SFN was confirmed in vitro and in vivo experiments. This nanomatrix developed in this study could be a promising drug delivery platform for improving the therapeutic efficacy of poorly water-soluble drugs.

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“…The CyA was highly dispersed in the nanomatrix in an amorphous or molecular state and partly filled into the nanopores of Sylysia 350. The relative bioavailability of optimized nanomatrix was 90.8% compared with Neoral® (Dai et al, 2015 ). Drugs with poor solubility, such as sorafenib (Wang et al, 2011 ) and fenofibrate (Jia et al, 2011 ) were also incorporated into the system.…”

Section: Formulation Approaches For Ph-responsive Oral Delivery Systemsmentioning

confidence: 99%

pH-Responsive carriers for oral drug delivery: challenges and opportunities of current platforms

et al. 2017

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PR China AbstractOral administration is a desirable alternative of parenteral administration due to the convenience and increased compliance to patients, especially for chronic diseases that require frequent administration. The oral drug delivery is a dynamic research field despite the numerous challenges limiting their effective delivery, such as enzyme degradation, hydrolysis and low permeability of intestinal epithelium in the gastrointestinal (GI) tract. pH-Responsive carriers offer excellent potential as oral therapeutic systems due to enhancing the stability of drug delivery in stomach and achieving controlled release in intestines. This review provides a wide perspective on current status of pH-responsive oral drug delivery systems prepared mainly with organic polymers or inorganic materials, including the strategies used to overcome GI barriers, the challenges in their development and future prospects, with focus on technology trends to improve the bioavailability of orally delivered drugs, the mechanisms of drug release from pH-responsive oral formulations, and their application for drug delivery, such as protein and peptide therapeutics, vaccination, inflammatory bowel disease (IBD) and bacterial infections.

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Sylysia 350/Eudragit S100 solid nanomatrix as a promising system for oral delivery of cyclosporine A

Cited by 20 publications

References 19 publications

Lipid nanoparticles for cyclosporine A administration: development, characterization, and in vitro evaluation of their immunosuppression activity

Lipid nanoparticles for cyclosporine A administration: development, characterization, and in vitro evaluation of their immunosuppression activity

Improving anti-tumor activity of sorafenib tosylate by lipid- and polymer-coated nanomatrix

pH-Responsive carriers for oral drug delivery: challenges and opportunities of current platforms

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