Lipid nanoparticles for oral delivery of raloxifene: Optimization, stability, in vivo evaluation and uptake mechanism

Ravi, Punna Rao; Aditya, N.P.; Kathuria, Himanshu; Malekar, Srinivas; Vats, Rahul

doi:10.1016/j.ejpb.2013.12.015

Cited by 116 publications

(56 citation statements)

References 34 publications

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“…The clear difference between T max values of TQ-loaded NLCs and TQ suspension confirmed that the rates of absorption of two systems were different. Faster absorption of F9 and F12 was because incorporation of TQ into lipid-based nanoparticles helped in avoiding passing extensive gut wall metabolism due to intimate association of drug with lipid and absorption through oral lymphatic region (26). As the pharmacological effects of TQ directly depended upon the plasma concentration, F9 and F12 could be more effective than TQ suspension in clinical experiments.…”

Section: Pharmacokinetic Parameters Of Tqmentioning

confidence: 92%

Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

et al. 2015

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Abstract. Thymoquinone (TQ), obtained from black cumin (Nigella sativa), is a natural product with antioxidant, anti-inflammatory, and hepatoprotective effects but unfortunately with poor bioavailability. Aiming to improve its poor oral bioavailability, TQ-loaded nanostructured lipid carriers (NLCs) were prepared by high-speed homogenization followed by ultrasonication and evaluated in vitro. Bioavailability and pharmacodynamic studies were also performed. The resultant NLCs showed poor physical homogeneity in Compritol 888 ATO Pluronic F127 system which consequently produced larger particle size and polydispersity index, smaller zeta potential values, and lower short-term (30 days) physical stability than other systems. Encapsulation efficiency percentage (EE%) lied between 84.6±5% and 96.2±1.6%. TQ AUC 0-t values were higher in animals treated with NLCs, with a relative bioavailability of 2.03-and 3.97-fold (for F9 and F12, respectively) higher than TQ suspension, indicating bioavailability enhancement by NLC formulation. Hepatoprotective effects of F12 showed significant (P<0.05) decrease in both serum alanine amino transferase and aspartate amino transferase to reach 305.0±24.88 and 304.7±23.55 U/ml, respectively, when compared with untreated toxic group. Anti-oxidant efficacy of F12 showed significant (P<0.05) decline of malondialdehyde and elevation of reduced glutatione. This improvement was also confirmed histopathologically.

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Section: Pharmacokinetic Parameters Of Tqmentioning

confidence: 92%

Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

et al. 2015

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“…This stage was followed by slower release phase lasting up to 10 h as a result of slow diffusion of drug from lipid matrix (Ravi et al, 2014). By applying kinetic fit, AT release from NLC-1 in pH 6.8 was most appropriately fitted to Higuchi diffusion model (r ¼ 0.9829) indicating lipid matrix erosion.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

et al. 2017

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Atorvastatin (AT) is a widely used lipid-regulating drug to reduce cholesterol and triglycerides. Its poor aqueous solubility and hepatic metabolism require development of drug delivery systems able to improve its solubility and bypass hepatic effect. For this purpose, atorvastatin nanostructured lipid carriers (AT-NLCs) were prepared and characterized. AT-NLCs were prepared by emulsification using high-speed homogenization followed by ultrasonication. The prepared NLCs showed particle size between 162.5 ± 12 and 865.55 ± 28 nm while zeta potential values varied between À34 ± 0.29 and À23 ± 0.36 mV. They also showed high encapsulation efficiency (>87%) and amorphous state of the drug in lipid matrix. Pharmacokinetic parameters of optimized formulation (NLC-1; composed of 2% Gelucire V R 43/01, 8% Capryol V R PGMC, 2% Pluronic V R F68 and 0.5% lecithin) revealed 3.6-and 2.1-fold increase in bioavailability as compared to atorvastatin suspension and commercial product (Lipitor V R ), respectively. Administration of NLC-1 led to significant reduction (p < .05) in the rats' serum levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL) and significant increase in highdensity lipoprotein (HDL). This improvement was confirmed histologically by minimizing the associated hepatic steatosis. These investigations demonstrated the superiority of NLCs for improvement of oral bioavailability and in vivo performance of AT. ARTICLE HISTORY

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“…Currently, there are two seemingly contradictory theories on the mechanisms of enhanced oral absorption by lipid nanoparticles. The first purported that lipid nanoparticles, either SLNs or NLCs, could be internalized by intestinal epithelia and suggested a mechanism of endocytosis, more specifically, clathrin-or caveolae-mediated endocytosis (Beloqui et al, 2013;Chen et al, 2013;Ravi et al, 2014;Zhang et al, 2010Zhang et al, , 2012. However, these findings are significantly weakened by the fact that all of the conclusions are based on observations in Caco-2 cell lines.…”

Section: Introductionmentioning

confidence: 86%

Comparison of the oral bioavailability of silymarin-loaded lipid nanoparticles with their artificial lipolysate counterparts: implications on the contribution of integral structure

Shangguan

Lü

et al. 2015

International Journal of Pharmaceutics

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Lipid nanoparticles for oral delivery of raloxifene: Optimization, stability, in vivo evaluation and uptake mechanism

Cited by 116 publications

References 34 publications

Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

Comparison of the oral bioavailability of silymarin-loaded lipid nanoparticles with their artificial lipolysate counterparts: implications on the contribution of integral structure

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