Determination of phytosterol oxidation products in pharmaceutical liposomal formulations and plant vegetable oil extracts using novel fast liquid chromatography - Tandem mass spectrometric methods

Poudel, Asmita; Gachumi, George; Purves, Randy W.; Badea, Ildikó; El‐Aneed, Anas

doi:10.1016/j.aca.2021.339404

Cited by 6 publications

(8 citation statements)

References 47 publications

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“…There is clinical evidence that tocopherols, at an optimum dose, decrease susceptibility to oxidation of LDL, preventing the generation of oxidized LDL (ox-LDL), which is cytotoxic and accelerates atherosclerosis. , Thus, in addition to reducing LDL-C, our liposomal formulation containing tocopherols can potentially prevent the oxidation of LDL. While we demonstrated that POPs were reduced in liposomal PSs, the effect on serum LDL can only be confirmed by conducting in vitro or in vivo studies.…”

Section: Resultsmentioning

confidence: 72%

“…68,69 Thus, in addition to reducing LDL-C, our liposomal formulation containing tocopherols can potentially prevent the oxidation of LDL. While we demonstrated that POPs were reduced in liposomal PSs, 20 the effect on serum LDL can only be confirmed by conducting in vitro or in vivo studies.…”

Section: Determination Of Total-c Ldl-c and Vldl-cmentioning

confidence: 71%

“…Similarly to micelles, liposomes composed of PC can enhance the therapeutic efficacy of PSs due to their ability to accelerate micellar solubilization of bile salts, which is the mechanism of action of PSs. , Since PSs can undergo autoxidation generating PS oxidation products (POPs) that may impart a pro-atherogenic effect, , encapsulation in a delivery system could prevent the autooxidation of PSs and render PSs safe for consumption. Our recent work showed that liposomal entrapment maintained the oxidation stability of PSs, preventing the generation of POPs …”

Section: Introductionmentioning

confidence: 99%

“…Our recent work showed that liposomal entrapment maintained the oxidation stability of PSs, preventing the generation of POPs. 20 In addition to the formulation approach, the source of PSs can have an impact on their therapeutic effects. PSs, namely, campesterol, stigmasterol, and β-sitosterol, obtained from soybean and palm oils, are abundant in nature and have been tested for their efficacy in humans.…”

Section: Introductionmentioning

confidence: 99%

“…20,25,26 The liposomes were able to entrap PSs and tocopherols at an efficiency greater than 90% while maintaining oxidative stability. 20,25 This liposomal formulation, with optimal physicochemical properties and adequate stability, was used in this study to assess the LDL-cholesterol-lowering ability of the PS in comparison with a marketed PS-containing product in an animal model.…”

Section: Introductionmentioning

confidence: 99%

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Liposomal Phytosterols as LDL-Cholesterol-Lowering Agents in Diet-Induced Hyperlipidemia

et al. 2023

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The high blood level of low-density lipoprotein cholesterol (LDL-C) is a primary risk factor for cardiovascular disease. Plant sterols, known as phytosterols (PSs), can reduce LDL-C in a range of 8–14%. The extent of LDL-C reduction depends on its formulation. Encapsulation into liposomes is one formulation strategy to enhance the efficiency of PSs. PSs (campesterol, stigmasterol, and β-sitosterol) have frequently been assessed alone or in combination for their LDL-C-lowering ability. However, one naturally abundant PS, brassicasterol, has not yet been tested for its efficacy. We have previously developed a novel liposomal formulation containing the PS mixture present naturally in canola that is composed of brassicasterol, campesterol, and β-sitosterol. In this work, the efficacy of our novel liposomal PS formulation that includes brassicasterol was assessed in a hamster model. Animals were divided into five groups: (i) liposomal PS in orange juice, (ii) liposomal PS in water, (iii) marketed PS in orange juice, (iv) control orange juice, and (v) control water. The animals were fed a high-fat, cholesterol-supplemented (0.5%) diet to induce hypercholesterolemia. The treatment was administered orally once daily for 4 weeks. Fasting blood samples were collected at baseline, week 2, and week 4. The extent of the reduction of total cholesterol, LDL-C, high-density lipoprotein cholesterol (HDL-C), and triglycerides was compared among the groups. Liposomal PSs in both orange juice and water significantly reduced LDL-C compared to their controls. Furthermore, the liposomal PS was as effective as a marketed PS-containing product in reducing LDL-C. Liposomal PSs in both orange juice and water showed similar efficacy in LDL-C reduction, highlighting that these vehicles/food matrices do not affect the efficacy of PSs. The liposomal formulation of a natural PS mixture extracted from canola oil, with brassicasterol as a major component, exhibited a significant LDL-C reduction in a hamster model.

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