Simvastatin nanolipid carriers decreased hypercholesterolemia induced cholesterol inclusion and phosphatidylserine exposure on human erythrocytes

Harisa, Gamaleldin I.; Badran, Mohamed M.

doi:10.1016/j.molliq.2015.04.005

Cited by 29 publications

(16 citation statements)

References 49 publications

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“…Herein, incubation of erythrocytes with cholesterol enriches plasma increased cholesterol inclusion into erythrocytes. Similar results were documented in several previous studies (Uydu et al, 2012, Harisa and Badran, 2015). In contrary, CS prevents cholesterol deposition into erythrocyte membranes; similarly, it has been reported that cholesterol lowering therapy decreases erythrocytes membrane cholesterol (Uydu et al, 2012).…”

Section: Discussionsupporting

confidence: 93%

Chitosan treatment abrogates hypercholesterolemia-induced erythrocyte’s arginase activation

Harisa

Attia

Zoheir

et al. 2017

Saudi Pharmaceutical Journal

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This study aimed to evaluate the protective effect of chitosan (CS) against hypercholesterolemia (HC) induced arginase activation and disruption of nitric oxide (NO) biosynthesis using erythrocytes as cellular model. Human erythrocytes were isolated and classified into eight groups. Next, cells were treated with l-arginine (l-ARG), N-nitro-l-arginine methyl ester (l-NAME), CS or CS + l-ARG in the presence of normal plasma or cholesterol enriches plasma. Then, erythrocytes were incubated at 37 °C for 24 h. The present results revealed that, HC induced significant increase of cholesterol inclusion into erythrocytes membrane compared to control. Moreover, HC caused significant decrease in nitric oxide synthase (NOS) activity similar to l-NAME; however, arginase activity and arginase/NOS ratio significantly increased compared to control. On contrast, treatment of HC with, l-arginine, CS or CS plus l-arginine prevents HC induced cholesterol loading into erythrocytes membrane, NOS inhibition and arginase activation. This study suggested that CS could be protective agent against HC induced disruption of erythrocyte's oxidative status and arginase activation.

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Section: Discussionsupporting

confidence: 93%

Chitosan treatment abrogates hypercholesterolemia-induced erythrocyte’s arginase activation

Harisa

Attia

Zoheir

et al. 2017

Saudi Pharmaceutical Journal

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“…For the bioavailability enhancement, parenteral routes are preferred because SMV is a prodrug, hence oral administration is the only preferred route for this drug and hepatic metabolism cannot be avoided. On the other hand, the solubility of SMV can be enhanced by incorporating it into a nano-carrier [5].…”

Section: Introductionmentioning

confidence: 99%

Chemical engineering of a lipid nano-scaffold for the solubility enhancement of an antihyperlipidaemic drug, simvastatin; preparation, optimization, physicochemical characterization and pharmacodynamic study

Alam

Ahmed

Nikita

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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This project was designed to extract anti-hyperlipidaemic activity of simvastatin for the longer duration of time and the solubility enhancement of this BCS class II drug was also sought by preparing nanostructured lipid carrier (NLC). The method for NLC preparation involved melt-emulsification followed by ultrasonication. The developed formulation was optimized by 3-level, 3-factor Box-Behnken design. The independent variables were % lipid mixture, % surfactant and sonication time (minutes). The responses selected were particle size, PDI and entrapment efficiency. The optimized formulation had particle size 114.62 ± 5.65, PDI 0.210 ± 0.034 and entrapment efficiency 85.20 ± 7.98%. The optimized formulation was further characterized by TEM and SEM. Spherical shape and nano size distribution of the optimized formulation were confirmed by SEM and TEM, respectively. The DSC of optimized formulation hints for the loss of crystalline nature of drug whereas the FT-IR spectra reveal that there is no interaction between drug and excipients when incorporated in NLC. The drug release from the NLC was biphasic (burst release was followed by sustained release). The kinetic of drug release followed Fickian diffusion with Korsmeyer-Peppas model. When the antihyperlipidaemic activity of SMV-NLC was compared with SMVsuspension, it was found that SMV-NLC significantly decreased the total cholesterol and triglyceride level by 2.77 and threefolds, respectively.

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“…reported that GMS used in the formulation of carvedilol-loaded NLCs resulted in particles with negative ZP. In addition, the used liquid lipid, Miglyol ® 812N, carry negative charge at the carboxylic groups imparting a negative surface charge (Harisa & Badran, 2015 ). These results are in agreement with those obtained in a previous study by Hou et al.…”

Section: Resultsmentioning

confidence: 99%

Lipid-based nano-formulation platform for eplerenone oral delivery as a potential treatment of chronic central serous chorioretinopathy: in-vitro optimization and ex-vivo assessment

2021

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Purpose Eplerenone (EPL) is a selective mineralocorticoid receptor antagonist used for treatment of chronic central serous chorioretinopathy which characterized by accumulation of subretinal fluid causing a localized area of retinal detachment. unfortunately, EPL suffers from poor oral bioavailability due to poor aqueous solubility in addition to high hepatic first pass metabolism. Method Aiming to improve its oral bioavailability, EPL-loaded nanostructured lipid carriers (NLCs) were prepared by the emulsification solvent evaporation method and in-vitro evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). A D-optimal design was used for study the effect of liquid lipid to solid lipid ratio, surfactant type and percentage on PS, PDI, EE%, and for data optimization. The optimized EPL-loaded NLCs system was further evaluated using in-vitro drug release and ex-vivo permeation studies through rabbit intestine in comparison to EPL aqueous suspension. The physicochemical properties of the drug in the optimized system were further examined using FT-IR and X-ray diffraction studies. Results The resultant NLCs showed small PS (100.85–346.60 nm), homogenous distribution (0.173–0.624), negatively charged particles (ZP −20.20 to −36.75 mV), in addition to EE% (34.31–70.64%). The optimized EPL-loaded NLCs system with a desirability value of 0.905 was suggested through the Design expert ® software, containing liquid to solid lipid ratio (2:1) in presence of 0.43%w/v Pluronic ® F127 as a surfactant. The optimized EPL-loaded NLCs system showed a PS of 134 nm and PDI of 0.31, in addition to high EE% (76 ± 6.56%w/w), and ZP (-32.37 mV). The ex-vivo permeation study showed two-fold higher drug permeation through rabbit intestine compared to that from the aqueous drug suspension after 24 h, confirming the ability of optimized EPL-loaded NLCs system as successful oral targeting delivery carrier. Conclusion Our results pave the way for a new oral nanotherapeutic approach toward CSCR treatment. In-vivo study is currently under investigation.

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Simvastatin nanolipid carriers decreased hypercholesterolemia induced cholesterol inclusion and phosphatidylserine exposure on human erythrocytes

Cited by 29 publications

References 49 publications

Chitosan treatment abrogates hypercholesterolemia-induced erythrocyte’s arginase activation

Chitosan treatment abrogates hypercholesterolemia-induced erythrocyte’s arginase activation

Chemical engineering of a lipid nano-scaffold for the solubility enhancement of an antihyperlipidaemic drug, simvastatin; preparation, optimization, physicochemical characterization and pharmacodynamic study

Lipid-based nano-formulation platform for eplerenone oral delivery as a potential treatment of chronic central serous chorioretinopathy: in-vitro optimization and ex-vivo assessment

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