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Phyto-phospholipid complexes (phytosomes): A novel strategy to improve the bioavailability of active constituents.

ABSTRACT: Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ''label-friendly" phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.

SUBMITTER: Lu M

PROVIDER: S-EPMC7032241 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Phyto-phospholipid complexes (phytosomes): A novel strategy to improve the bioavailability of active constituents.

Lu Mei M Qiu Qiujun Q Luo Xiang X Liu Xinrong X Sun Jing J Wang Cunyang C Lin Xiangyun X Deng Yihui Y Song Yanzhi Y

Asian journal of pharmaceutical sciences 20180727 3

Although active constituents extracted from plants show robust <i>in vitro</i> pharmacological effects, low <i>in vivo</i> absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ''label-friendly" phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phosp ...[more]

PMID: 32104457

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Project description:Luffa echinata Roxb. is one of the neglected medicinal plants. It is an important source of bioactive metabolites and used in several Ayurvedic formulations. In the present analysis, mature leaves and fruits were extracted with acetone, ethanol, acetonitrile, methanol and water. Phytochemicals like total phenolic (TPC), flavonoid (TFC), tannin (TTC), alkaloid (TAC) and terpenoid (TTEC) content were analysed. Further, antioxidant (AOX) activities like 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis-(3-ethyl) benzothiazoline-6-sulfonic acid (ABTS) radical scavenging, metal chelating activity (MC), ferric reducing antioxidant power (FRAP) and phosphomolybdenum assay (PMA) were studied. Highest TPC and TFC (189.57 ± 1.9 mg TAE/g extract, 30.48 ± 0.7 mg CE/g extract, respectively) were reported from acetone extract of the leaves. Ethanolic fruit extract showed the highest TTC (13.79 ± 0.2 mg CE/g extract). Acetone and acetonitrile fruit extract revealed maximum TTEC (602.79 ± 3.5 mg UAE/g extract) and moderate TAC (19.96 ± 0.9 mg GE/g extract), respectively. In AOX, highest DPPH (50.52 ± 0.03 mg AAE/g extract) and ABTS (26.78 ± 0.03 mg TE/g extract) radical scavenging reported in methanolic extract of fruit; however, acetone extract of leaf showed highest FRAP (376.89 ± 1.95 mg Fe(II)/g extract) and PMA (326.54 ± 4.73 mg AAE/g extract). In contrast, aqueous extract of leaf and fruit revealed highest metal chelating activity (41.67 ± 0.49 mg EDTA/g extract). In anti-diabetic studies, acetonitrile extract of leaves and fruits exhibited appreciable inhibition of α-amylase (83.33%) and α-glycosidase (77.42%) enzymes. Similarly, acetyl cholinesterase (AChE) inhibition was highest in water (88.91%) and acetone (81.87%) extracts of leaf and fruits. Fruit extracts showed potent anticancer activity against breast (MCF-7) and colon (HT-29) cancer cell lines (LC50 329.36 and 385.17 µg/mL, respectively). RP-HPLC analysis revealed highest cucurbitacin B (CuB) (196.24 ± 1.4 mg/g DW), followed by cucurbitacin I (CuI) and cucurbitacin E (CuE) in the fruits (57.14 ± 4.9 and 2.03 ± 0.03 mg/g DW, respectively). RP-HPLC analysis of extracts revealed presence of gallic acid (GA), catechin (CA), vanillic acid (VA), chlorogenic acid (CHLA) and coumaric acid (COA), in which highest GA found in the fruits (1.26 ± 0.07 mg/g DW). Liquid chromatography and mass spectrometry (LC-MS) and gas chromatography-mass spectrometry (GC-MS) analysis revealed presence of bioactive compounds from various groups. Based on the present findings, it was revealed that the fruit and leaf of L. echinata can be used as potent bioresource for natural antioxidants, anti-diabetic, and anticancer drug.

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Phyto-phospholipid complexes (phytosomes): A novel strategy to improve the bioavailability of active constituents.

Publications

Phyto-phospholipid complexes (phytosomes): A novel strategy to improve the bioavailability of active constituents.

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