Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN®) versus drug nanocrystals

Müller, Rainer H.; Runge, Stephan; Ravelli, V.; Mehnert, W.; Thünemann, Andreas F.; Souto, Eliana B.

doi:10.1016/j.ijpharm.2006.02.045

Cited by 288 publications

(127 citation statements)

References 24 publications

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“…Pharmaceutical applications for solid lipid particles include oral, parenteral, and topical drug delivery. 7,[10][11][12][13][14][15][16][17][18] Advantages include improved bioavailability, controlled release, and stabilization. Limitations include drug loading capacity and reports of drug expulsion during storage.…”

Section: Introductionmentioning

confidence: 99%

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Holser

2011

Lipid�Insights

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Encapsulation of structurally sensitive compounds within a solid lipid matrix provides a barrier to prooxidant compounds and effectively limits the extent of oxidative degradation. This offers a simple approach to preserve the bioactivity of labile structures. The technology was developed for cosmetic and pharmaceutical products but may be applied to additives used in food and feed formulations. The encapsulation of docosahexaenoic acid (DHA) and α-linolenic acid (ALA) was examined as model compounds of current interest in functional foods and feeds. Solid lipid particles were prepared from triglycerides containing saturated and unsaturated fatty acids and evaluated by differential scanning calorimetry. The thermal characteristics of the lipids used to form the particle were related to molecular structure and could be adjusted by selection of the appropriate component fatty acids. Encapsulation by solid lipid particles provides a method to inhibit oxidation and improve shelf life of products formulated with DHA and ALA.

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Section: Introductionmentioning

confidence: 99%

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Holser

2011

Lipid�Insights

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“…Solid lipid nanoparticles (SLNs) have recently been under consideration for drug delivery because they offer the possibility of modulating drug release and provide both stability and compatibility while avoiding the shortcomings of liposomes, including undesired stability problems and the potential toxicity of the materials such as polymeric nanoparticles (Saupe & Rades, 2006;Vaghasiya et al, 2013). Sufficient data implicated that the bioavailability of some poorly hydrophilic and lipophilic drugs, such as retinoic acid, cyclosporine (Müller et al, 2006) and vinpocetine (Luo et al, 2006) can be improved when encapsulated in SLNs.…”

Section: Introductionmentioning

confidence: 99%

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

Tang

et al. 2014

Drug Delivery

132

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Purpose: The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin. Methods: The formulation was optimized by Plackett-Burman screening design and Box-Behnken experiment design. Then physiochemical properties, entrapment efficiency and in vitro release of Cur-SLNs were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin. Results: The optimized formulations showed an average size of 135.3 ± 1.5 nm with a zeta potential value of À24.7 ± 2.1 mV and 91.09% ± 1.23% drug entrapment efficiency, meanwhile displayed a sustained release profile. In vivo pharmacokinetic study showed AUC 0!t for Cur-SLNs was 12.27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942.53%. Meanwhile, T max and t 1/2 of curcumin for Cur-SLNs were both delayed comparing to the suspensions (p50.01). The in situ intestinal absorption study revealed that the effective permeability (P eff ) value of curcumin for SLNs was significantly improved (p50.01) comparing to curcumin solution. Conclusion: Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively. KeywordsCurcumin, in situ intestinal absorption, oral bioavailability, P-glycoprotein, solid lipid nanoparticles History

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“…To date, lipid nanosystems (LN) seem to be a promising strategy to overcome the limitations associated with certain drug characteristics including low solubility, poor permeability, instability in the gastrointestinal medium, Pglycoprotein efflux and presystemic drug metabolism [2]. Scientific efforts have therefore been employed to design novel delivery systems based on LN for CyA oral administration leading to better alternatives to those currently available on the market, which will be capable of enhancing its oral bioavailability and thus its efficacy [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Ultra high performance liquid chromatography–tandem mass spectrometry method for cyclosporine a quantification in biological samples and lipid nanosystems

Guada

Imbuluzqueta

Mendoza

et al. 2013

Journal of Chromatography B

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Cyclosporine A (CyA) is an immunosuppressant cyclic undecapeptide used for the prevention of organ transplant rejection and in the treatment of several autoimmune disorders. An ultra high performance liquid chromatography-tandem mass spectrometry method (UHPLC-MS/MS) to quantify CyA in lipid nanosystems and mouse biological matrices (whole blood, kidneys, lungs, spleen, liver, heart, brain, stomach and intestine) was developed and fully validated.Chromatographic separation was performed on an Acquity UPLC ® BEH C18 column with a gradient elution consisting of methanol and 2 mM ammonium acetate aqueous solution containing 0.1% formic acid at a flow rate of 0.6 mL/min. Amiodarone was used as internal standard (IS). Retention times of IS and CyA were 0.69 min and 1.09 min, respectively. Mass spectrometer operated in electrospray ionization positive mode (ESI+) and multiple reaction monitoring (MRM) transitions were detected, m/z 1220.69→1203.7 for CyA and m/z 646→58 for IS. The extraction method from biological samples consisted of a simple protein precipitation with 10% trichloroacetic acid aqueous solution and acetonitrile and 5 µL of supernatant were directly injected into the UHPLC-MS/MS system. Linearity was observed between 0.001 µg/mL-2.5 µg/mL (r ≥ 0.99) in all matrices. The precision expressed in coefficient of variation (CV) was below 11.44% and accuracy in bias ranged from −12.78% to 7.99% including methanol and biological matrices. Recovery in all cases was above 70.54% and some matrix effect was observed. CyA was found to be stable in post-extraction whole blood and liver homogenate samples exposed for 6 h at room temperature and 72 h at 4 o C. The present method was successfully applied for quality control of lipid nanocarriers as well as in vivo studies in BALB/c mice.

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Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN®) versus drug nanocrystals

Cited by 288 publications

References 24 publications

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

Ultra high performance liquid chromatography–tandem mass spectrometry method for cyclosporine a quantification in biological samples and lipid nanosystems

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