Enhanced intestinal absorption and bioavailability of raloxifene hydrochloride via lyophilized solid lipid nanoparticles

Burra, Madhu; Jukanti, Raju; Janga, Karthik Yadav; Sunkavalli, Sharath; Velpula, Ashok; Ampati, Srinivas; Jayaveera, K. N.

doi:10.1016/j.apt.2012.09.002

Cited by 60 publications

(19 citation statements)

References 32 publications

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“…It is noteworthy that free SLN and PBS elicited similar levels of parasitemia (Supporting Information: Figure S2). Therefore, the use of SLNs as a drug delivery system increased the oral bioavailability of the target drug, as previously described [59], [60], [61], [62], [63]. H 2 bdtc loading into SLNs overcame the problems inherent to the poor water solubility of the compound and may be could make it more accessible to the parasite (however, detailed pharmacokinetic data will be presented in a separate forthcoming paper).…”

Section: Discussionmentioning

confidence: 91%

In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles

et al. 2014

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The parasite Trypanosoma cruzi causes Chagas disease, which remains a serious public health concern and continues to victimize thousands of people, primarily in the poorest regions of Latin America. In the search for new therapeutic drugs against T. cruzi, here we have evaluated both the in vitro and the in vivo activity of 5-hydroxy-3-methyl-5-phenyl-pyrazoline-1-(S-benzyl dithiocarbazate) (H2bdtc) as a free compound or encapsulated into solid lipid nanoparticles (SLN); we compared the results with those achieved by using the currently employed drug, benznidazole. H2bdtc encapsulated into solid lipid nanoparticles (a) effectively reduced parasitemia in mice at concentrations 100 times lower than that normally employed for benznidazole (clinically applied at a concentration of 400 µmol kg−1 day−1); (b) diminished inflammation and lesions of the liver and heart; and (c) resulted in 100% survival of mice infected with T. cruzi. Therefore, H2bdtc is a potent trypanocidal agent.

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Section: Discussionmentioning

confidence: 91%

In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles

et al. 2014

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“…The drug loading capacity of SLNs mainly depends on the solubility behavior of the drug in the lipid melt during and after formulation of the SLNs (26). So, in order to obtain sufficient drug loading and stable incorporation of breviscapine into the SLN lipid matrix, lipid solubility test for breviscapine in various lipids was performed by evaluating the DSC thermograms of breviscapine/lipid solid dispersions.…”

Section: Results and Discussion Preparation And Physicochemical Charmentioning

confidence: 99%

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

et al. 2014

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Abstract. Breviscapine is used in the treatment of ischemic cerebrovascular diseases, but it has a low bioavailability in the brain due to its poor physicochemical properties and the activity of P-glycoprotein efflux pumps located at the blood-brain barrier. In the present study, breviscapine-loaded solid lipid nanoparticles (SLN) coated with polyethylene glycol (PEG) derivatives were formulated and evaluated for their ability to enhance brain bioavailability. The SLNs were either coated with polyethylene glycol (40) (PEG-40) stearate alone (Bre-GBSLN-PS) or a mixture of PEG-40 stearate and 1,2-distearoyl-snglycero-3-phosphoethanolamine-N-PEG2000 (DSPE-PEG 2000 ) (Bre-GBSLN-PS-DSPE) and were characterized both in vitro and in vivo. The mean particle size, polydispersity index, and entrapment efficiency for Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE were 21.60±0.10 and 22.60±0.70 nm, 0.27±0.01 and 0.26 ±0.04, and 46.89±0.73% and 47.62±1.86%, respectively. The brain pharmacokinetic parameters revealed that the brain bioavailability of breviscapine from the Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE was significantly enhanced (p<0.01) with the area under concentration-time curve (AUC) of 1.59±0.39 and 1.42±0.58 μg h/mL of breviscapine, respectively, in comparison to 0.11±0.02 μg h/mL from the commercial breviscapine injection. The ratios of the brain AUC for scutellarin in comparison with the plasma scutellarin AUC for commercial breviscapine injection, Bre-GBSLN-PS, and Bre-GBSLN-PS-DSPE were 0.66%, 2.82%, and 4.51%, respectively. These results showed that though both SLN formulations increased brain uptake of breviscapine, Bre-GBSLN-PS-DSPE which was coated with a binary combination of PEG-40 stearate and DSPE-PEG 2000 had a better brain bioavailability than Bre-GBSLN-PS. Thus, the coating of SLNs with the appropriate PEG derivative combination could improve brain bioavailability of breviscapine and can be a promising tool for brain drug delivery.

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“…Several cosmetic products based on SLNs are already marketed. Secondly, providing an advantage over liposomes or polymeric nanoparticles, preparation methods feasible at industrial scale are available, and these methods avoid the use of organic solvents [20][21][22] . Furthermore, in vitro tolerability of SLNs appears to be much higher than that of polymeric nanoparticles.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and in Vivo Antitumor Efficacy of Berberine-solid Lipid Nanoparticles Against H22 Tumor

Meng¹,

Wang²,

Wang³

2016

Proceedings of the 2016 6th International Conference on Applied Science, Engineering and Technology

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Hepatocarcinoma, a malignant cancer, threaten human life badly. It is a current issue to seek the effective natural remedy from plant to treat cancer due to the resistance of the advanced hepatocarcinoma to chemotherapy. Berberine (Ber), an isoquinoline derivative alkaloid, has a wide range of pharmacological properties and is considered to have anti-hepatocarcinoma effects. However its low oral bioavailability restricts its wide application. In this report, Ber loaded solid lipid nanoparticles (Ber-SLN) was prepared by hot melting and then high pressure homogenization technique. Both in vitro and in vivo anti-hepatocarcinoma effects of Ber-SLN relative to efficacy of bulk Ber were evaluated. The particle size and zeta potential of Ber-SLN were 154.2 ± 0.8 nm and −18.63±0.99mV, respectively. MTT assay showed that Ber-SLN effectively inhibited the proliferation of H22 cells, and the corresponding IC 50 values were 11.6 µg/ml (18.3 µg/ml of bulk Ber). In vivo studies also showed higher antitumor efficacy, and inhibition rates was 65.1% (41.4 % of bulk Ber) at 100mg/kg intragastric administration in H22 solid tumor bearing mice. These results suggest that the delivery of Ber-SLN is a promising approach for treating tumors.

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Enhanced intestinal absorption and bioavailability of raloxifene hydrochloride via lyophilized solid lipid nanoparticles

Cited by 60 publications

References 32 publications

In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles

In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

In Vitro and in Vivo Antitumor Efficacy of Berberine-solid Lipid Nanoparticles Against H22 Tumor

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