Nanostructured lipid carriers for improved oral delivery and prolonged antihyperlipidemic effect of simvastatin

Fathi, Heba A.; Allam, Ayat; Elsabahy, Mahmoud; Fetih, Gihan; El-Badry, Mahmoud

doi:10.1016/j.colsurfb.2017.11.064

Cited by 106 publications

(57 citation statements)

References 53 publications

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“…This micrograph showed that the NLC was homogeneous as a uniform round population. Consistent with studies conducted by Fathi et al (), Pinto et al (), and Patwekar et al (), the TEM images demonstrated that the NLC with bioactive components had the same morphology, which was a round shape on a nanosize scale as confirmed by zetasizer instruments.…”

Section: Resultssupporting

confidence: 89%

Application of Response Surface Methodology for the Optimization of β‐Carotene‐Loaded Nanostructured Lipid Carrier from Mixtures of Palm Stearin and Palm Olein

Rohmah

Raharjo

Hidayat

et al. 2019

J Americ Oil Chem Soc

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The main purpose of this study was to optimize a β-carotene-loaded nanostructured lipid carrier (βC-NLC) using the lipid matrix of palm stearin and palm olein and Tween 80 as a surfactant. The NLC was prepared by using the high shear homogenization method. Box-Behnken Design (BBD) response surface methodology (RSM) was applied to optimize the process and formulation. A three-factor experimental model was used to optimize the combination of palm stearin ratio (A, %w/w), lipid:surfactant ratio (B, %w/w), and (lipid+surfactant):water ratio (C, %w/w). The formulations were evaluated for their responses on particle size (Y1), polydispersity index (Y2), zeta potential (Y3), and encapsulation efficiency (Y4). Subsequently, Fourier-transform infrared spectroscopy (FTIR), thermal (DT-TGA), x-ray diffraction (XRD), transmission electron microscopy (TEM), and in vitro release (Franz diffusion cell) analyses were utilized to observe the resulting optimum formulation. The optimum formulation was obtained at a combination of A (5.5:4.5), B (1:4.9), and C (24:76) %w/w. This resulted in βC-NLC having a particle size of 166 nm, polydispersity index of 0.35, zeta potential of −26.9 mV, and an encapsulation efficiency of 91.2%. No strong interaction between different NLC components was observed based on FTIR, DT-TGA, and XRD profiles. Round-shaped NLC particles were observed under TEM.Franz diffusion cell observation resulted in diffusion profile of β-carotene of 110.6 μg cm −2 with a flux of 1.06 (μg cm −2 hour −1 ). This indicates that palm stearin and palm olein can be prospectively developed as βC-NLC.Keywords β-Carotene Á Nanostructured lipid carriers Á Response surface methodology Á Box-Behnken design J Am Oil Chem Soc (2020) 97: 213-223.

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Section: Resultssupporting

confidence: 89%

Application of Response Surface Methodology for the Optimization of β‐Carotene‐Loaded Nanostructured Lipid Carrier from Mixtures of Palm Stearin and Palm Olein

Rohmah

Raharjo

Hidayat

et al. 2019

J Americ Oil Chem Soc

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“…Several studies have indicated that the NLC formulation has a promising perspective to improve the oral bioavailability of poorly soluble drugs [33,34]. In the current study, plasma concentration time profiles and the corresponding pharmacokinetic parameters after oral administration of 10% TMS, TMS-pNLCs, TMS-lNLCs, and TMS-sNLCs in broilers at a single TMS dose of 25 mg/kg are presented in Figure 9 and Table 1, respectively.…”

Section: In Vivo Pharmacokinetic Studymentioning

confidence: 85%

Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation

et al. 2020

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This study aimed to develop nanostructured lipid carriers (NLCs) for improved oral absorption of tilmicosin (TMS) in broilers. Thus, palmitic acid, lauric acid, and stearic acid were selected as solid lipids to formulate TMS-pNLCs, TMS-lNLCs, and TMS-sNLCs, respectively. They showed similar physicochemical properties and meanwhile possessed excellent storage and gastrointestinal stability. The TMS interacted with the lipid matrix and was encapsulated efficiently in NLCs in an amorphous structure. NLCs could enhance oral absorption of TMS compared to 10% tilmicosin phosphate solution in broilers, among which the TMS-sNLCs were the most efficient drug delivery carriers, with a relative oral bioavailability of 203.55%. NLCs could inhibit the efflux of P-glycoprotein (P-pg) toward TMS, which may be involved with improved oral absorption. Taken together, these types of solid lipids influenced the enhanced level of NLCs toward oral bioavailability of TMS, and the sNLCs proved to be the most promising oral delivery carriers of TMS.

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“…Tween 80 was added to maintain sink conditions (Muthu, Kulkarni, Raju, & Feng, 2012;Zhang et al, 2010). Samples were taken at predetermined time intervals (1, 2, 4, 6, 8, and 24 hr) (Fathi, Allam, Elsabahy, Fetih, & El-Badry, 2018), and release media was replaced with the fresh one for maintenance of sink conditions. The experiment was carried out in triplicate.…”

Section: Physicochemical Characterizationmentioning

confidence: 99%

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Alavi

Akhlaghi

Dadashzadeh

et al. 2019

Journal of Food Science

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This study was aimed to develop a novel nanocarrier for coenzyme Q10 (CoQ10) by a green process that prevented the use of surfactants and organic solvents. Triglyceride/phospholipid‐based nanocarriers were developed through high‐pressure homogenization (an industrial feasible process), and a 25‐1 fractional factorial design was adopted to assess the influences of formulation variables on the considered responses, including vesicle size, entrapment efficiency, loading capacity, and solubility of the vehicles in simulated gastrointestinal fluids. The optimized formulation was further in‐depth characterized in terms of morphology, release behavior, biocompatibility (Caco‐2 cell cytotoxicity and histological examination), thermal behavior, and Fourier transform infrared analysis. Optimal nanocarriers were found to have mean particle size of 75 nm, narrow particle distribution, and CoQ10 entrapment of 95%. The optimized formulation was stable upon incubation in simulated gastrointestinal fluids without considerable leakage of cargo, which was in agreement with their sustained release behavior. Microscopic observations also confirmed nanosized nature of the vesicles and revealed their spherical shape. Moreover, toxicity evaluations at the cellular and tissue levels revealed their nontoxic nature. In conclusion, triglyceride/phospholipid‐based nanocarriers proved to be a green safe vehicle for delivery of CoQ10 with industrial‐scale production capability and could provide a new horizon for delivery of hydrophobic nutraceuticals. Practical application Green nanostructure formulation approaches have recently gained tremendous attraction for their safe profile especially when it comes to supplements, which are generally recommended for daily use. However, their sufficient association with cargoes and industrial‐scale production have remained considerable challenges. This study focuses on the development of lipid‐based nanocarriers for CoQ10 by an industrial feasible process that prevents the use of any surfactants or organic solvents.

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Nanostructured lipid carriers for improved oral delivery and prolonged antihyperlipidemic effect of simvastatin

Cited by 106 publications

References 53 publications

Application of Response Surface Methodology for the Optimization of β‐Carotene‐Loaded Nanostructured Lipid Carrier from Mixtures of Palm Stearin and Palm Olein

Application of Response Surface Methodology for the Optimization of β‐Carotene‐Loaded Nanostructured Lipid Carrier from Mixtures of Palm Stearin and Palm Olein

Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

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