Pharmacokinetics study of arteether loaded solid lipid nanoparticles: An improved oral bioavailability in rats

“…Improved bioavailability, safety, and protection against degradation of the drug payload in the stomach are some of the desirable attributes associated with oral delivery of SLNs. Furthermore, it is possible to tailor formulations to ensure controlled release of the payload from the SLNs (6)(7)(8)(9)(10). Uptake of intact SLNs via the lymphatic route into blood has been reported in some studies after oral and duodenal administrations of SLNs to rats.…”

Section: Introductionmentioning

confidence: 99%

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

et al. 2015

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Abstract. Amphotericin B (AmB) is poorly absorbed from the gastrointestinal tract. Recent studies have suggested enhanced drug absorption from solid lipid nanoparticles (SLN). Little is known of the fate of AmB absorption within the gastrointestinal tract, and no gastrointestinal transit study has yet been performed on AmB-containing nano-formulations. We aimed to investigate the effect of food on the gastrointestinal transit properties of an AmB-containing SLN in rats. Three SLNs containing AmB, paracetamol, or sulfasalazine were formulated using cocoa butter and beeswax as lipid matrices and simultaneously administered orally to Sprague-Dawley rats. Paracetamol and sulfapyridine were used as marker drugs for estimating gastric emptying and cecal arrival, respectively. The pharmacokinetic data generated for paracetamol and sulfapyridine were used in estimating the absorption of the AmB SLNs in the small and large intestines, respectively. A delayed rate of AmB absorption was observed in the fed state; however, the extent of absorption was not affected by food. Specifically, the percentages of AmB absorption during the fasted state in the stomach, small intestine, and colon were not significantly different from absorption within the respective regions in the fed state. In both states, however, absorption was highest in the colon and appeared to be a combination of absorption from the small intestine plus absorption proper within the colon. The study suggests that AmB SLN, irrespective of food status, is slowly but predominantly taken up by the lymph, making the small intestine the most favorable site for the delivery of the AmB SLNs.

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“…In addition, drug was shielded by a lipid layer in order to protect it from harsh gastric conditions and to overcome the first-pass by lymphatic uptake (Bhandari & Kaur, 2013). On the other hand, the surfactants might contribute to enhanced permeability of the drug through the intestinal membrane (Dwivedi et al, 2014). Increasing adhesion into intestinal membrane of the colloidal system and higher solubility facilitated faster and more continuous saturated drug concentration between the intestinal membrane and blood vessel, resulting in enhanced absorption (Yuan et al, 2013).…”

Section: Pharmacokinetics Studiesmentioning

confidence: 99%

Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

et al. 2014

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Background: Vorinostat (VRS), a histone deacetylases inhibitor, has significant cytotoxic potential in a large number of human cancer cell lines. Objective: To clarify its promising anticancer potential and to improve its drawback related to physical properties and in vivo performance of VRS. Methods: VRS was successfully incorporated into nanostructured lipid carriers (NLCs) by the hot microemulsion method using sonication following a homogenization technique. Results: After the optimization process, VRS-loaded NLCs (VRS-NLCs) were obtained as ideal quality nanoparticles with a spherical shape, small size ($150 nm), negative charge ($À22 mV), and narrow size distribution. In addition, the high entrapment efficiency ($99%) and sustained drug release profile were recorded. Cytotoxicity study in three different cell lines (A549, MCF-7, and SCC-7) demonstrated higher cytotoxicity of VRS-NLCs than free drug. Finally, the AUC of VRS (118.16 ± 17.35 mgh/mL) was enhanced $4.4 times compared with that of free drug (27.03 ± 3.25 mgh/mL). Conclusion: These results suggest the potential of NLCs as an oral delivery system for enhancement of cellular uptake, in vitro cytotoxicity in cancer cell lines and the oral bioavailability of VRS.

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Pharmacokinetics study of arteether loaded solid lipid nanoparticles: An improved oral bioavailability in rats

Cited by 84 publications

References 30 publications

In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells

In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

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