Preparation, Pharmacokinetics and Body Distribution of Silymarin-Loaded Solid Lipid Nanoparticles After Oral Administration

He, Jun; Hou, Shaoping; Lu, Wenyue; Zhu, Lin; Jiao, Feng

doi:10.1166/jbn.2007.024

Cited by 49 publications

(22 citation statements)

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“…Besides liposomes, solid lipid nanoparticles (SLN) can also be used to delay an active ingredient's release, as demonstrated for Silymarin (mixture of flavonolignans extracted from blessed milk thistle (Silybum marianum) consisting of silibinin A and B, isosibilinin A and B, silicristin, silidianin) in vitro as well as in vivo in a mouse model (32), and melatonin, which was administered orally to 7 volunteers in a release-delaying formulation of soy phosphatidylcholine (77), resulting in increased elimination half-life period and AUC.…”

Section: Retarded Release Of Active Substancesmentioning

confidence: 99%

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Kromp²,

et al. 2010

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Phospholipids become increasingly important as formulation excipients and as active ingredients per se. The present article summarizes particular features of commonly used phospholipids and their application spectrum within oral drug formulation and elucidates current strategies to improve bioavailability and disposition of orally administered drugs. Advantages of phospholipids formulations not only comprise enhanced bioavailability of drugs with low aqueous solubility or low membrane penetration potential, but also improvement or alteration of uptake and release of drugs, protection of sensitive active agents from degradation in the gastrointestinal tract, reduction of gastrointestinal side effects of non-steroidal anti-inflammatory drugs and even masking of bitter taste of orally applied drugs. Technological strategies to achieve these effects are highly diverse and offer various possibilities of liquid, semi-liquid and solid lipid-based formulations for drug delivery optimization.

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Section: Retarded Release Of Active Substancesmentioning

confidence: 99%

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Kromp²,

et al. 2010

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“…Compared to other formulations, IN-SLNs demonstrated higher transcorneal permeability, which may be ascribed to endocytosis or transcytosis uptake mechanisms [44, 45]. The in vitro transcorneal permeability of IN from the NLC formulations was comparatively lower than that of the SLNs, probably because of higher entrapment in the oily phase and thus lower partitioning into the membrane.…”

Section: Discussionmentioning

confidence: 99%

Topical ophthalmic lipid nanoparticle formulations (SLN, NLC) of indomethacin for delivery to the posterior segment ocular tissues

Balguri

Adelli

Majumdar

2016

European Journal of Pharmaceutics and Biopharmaceutics

153

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Purpose The objective of the present study was to formulate indomethacin (IN)-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) and to investigate their potential use in topical ocular delivery. Methods IN SLNs (0.1% w/v) and NLCs (0.8% w/v) were prepared, characterized and evaluated. Their in vitro release and flux profiles across the cornea and sclera-choroid-RPE (trans-SCR) tissues and in vivo ocular tissue distribution were assessed. Furthermore, chitosan chloride (CS) (mol. wt. < 200 kDa), a cationic and water-soluble penetration enhancer, was used to modify the surface of the SLNs, and its effect was investigated through in vitro transmembrane penetration and in vivo distribution tissue studies. Results For the IN-SLNs, IN-CS-SLNs and IN-NLCs, the particle size was 226 ± 5, 265 ± 8, and 227 ± 11 nm, respectively; the zeta potential was −22 ± 0.8, 27 ± 1.2, and −12.2 ± 2.3 mV, respectively; the polydispersity index (PDI) was 0.17, 0.30, and 0.23, respectively; and the entrapment efficiency (EE) was 81 ± 0.9, 91.5 ± 3.2 and 99.8 ± 0.2%, respectively. The surface modification of the SLNs with CS increased the ocular penetration of IN. The NLCs maintained significantly higher IN concentrations in all ocular tissues tested compared to the other formulations evaluated in vivo. Conclusion The results suggest that lipid-based particulate systems can serve as viable vehicles for ocular delivery. The NLC formulations demonstrated increased drug loading capability, entrapment and delivery to anterior and posterior segment ocular tissues.

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“…When the nanoparticles with a diameter of 50-100 nm enter the circulatory system, they are not released into the systemic circulation directly. Instead, they are absorbed by the RES, leading to greatest drug accumulation in the liver and thus achieving the targeting effect (He et al, 2007;Lu et al, 2008;Hu et al, 2013).…”

Section: Biodistribution Studiesmentioning

confidence: 99%

Formulation, characterization, and in vitro/vivo studies of aclacinomycin A-loaded solid lipid nanoparticles

Jia

Wang

et al. 2014

Drug Delivery

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Objective: The aim of this study was to prepare aclacinomycin A (ACM)-loaded solid lipid nanoparticles (SLNs) and to evaluate their in vitro and in vivo characteristics. Methods: SLNs were prepared using an emulsion evaporation-solidification method, and characterized in accordance with the morphological examination, particle size distribution, entrapment efficiency, drug-loading, and in vitro release. Pharmacokinetic and biodistribution studies were employed to evaluate the in vivo of SLNs. Results: The SLNs were spherical in shape, uniform in size, and appropriate for administration via intravenous injection. The drug content, encapsulation efficiency, and drug loading of prepared SLNs were 96.4% ± 4.6%, 86.7% ± 2.3%, and 4.8% ± 0.7% (n ¼ 3), respectively, and the mean diameter was 68.2 ± 5.6 nm from three batches. The SLNs were produced with stable physical properties and demonstrated significantly sustained release. The pharmacokinetic behavior of ACM was greatly improved by lyophilized injection of SLN with sustained drug release and high bioavailability. In addition, the results obtained from tissue distribution showed that ACM-SLNs were hepatic targeting in vivo.Conclusions: The present work demonstrated the feasibility of liver-targeted delivery of ACM utilizing SLNs.

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Preparation, Pharmacokinetics and Body Distribution of Silymarin-Loaded Solid Lipid Nanoparticles After Oral Administration

Cited by 49 publications

References 0 publications

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Topical ophthalmic lipid nanoparticle formulations (SLN, NLC) of indomethacin for delivery to the posterior segment ocular tissues

Formulation, characterization, and in vitro/vivo studies of aclacinomycin A-loaded solid lipid nanoparticles

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