Preparation of a nanoscale dihydromyricetin-phospholipid complex to improve the bioavailability: in vitro and in vivo evaluations

Zhao, Xinyuan; Shi, Chunyu; Zhou, Xiya; Lin, Tong; Gong, Yusheng; Yin, Mingxing; Fan, Li; Wang, Wenqing; Fang, Jianguo

doi:10.1016/j.ejps.2019.104994

Cited by 50 publications

(24 citation statements)

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“…Phospholipid complexes, also named phytosomes, are a novel drug delivery system formed by non-covalent bonds (electrostatic interaction, van der Waals force, hydrogen bond and etc.) between phospholipids and drugs [32].The structure of phospholipid complexes is similar to that of liposomes, with the major difference being that in phospholipid complexes, the drug is mainly connected with the phospholipid polar head, whereas in liposomes, the drug is encapsulated in its cavity or phospholipid bilayer [33]. Drug-phospholipid complexes possess amphiphilic characteristics, which makes them more readily soluble in GIT and more easily absorbed through amphiphilic cell membrane and lymphatic system, thereby improving the bioavailability of drugs.…”

Section: Introductionmentioning

confidence: 99%

Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes

et al. 2021

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Breviscapine (BVP), a flavonoid compound, is widely used in the treatment of cardiovascular and cerebrovascular diseases; however, the low oral bioavailability and short half-life properties limit its application. The aim of this study was to investigate the three preparations for improving its oral bioavailability: nanosuspensions (BVP-NS), liposomes (BVP-LP) and phospholipid complexes (BVP-PLC). In vitro and in vivo results suggested that these three could all significantly improved the cumulative released amount and oral bioavailability compared with physical mixture, in which BVP-PLC was the most optimal preparation with the relative bioavailability and mean retention time of 10.79 ± 0.25 (p < 0.01) and 471.32% (p < 0.01), respectively. Furthermore, the influence of drug-lipid ratios on the in vitro release and pharmacokinetic behavior of BVP-PLC was also studied and the results showed that 1:2 drug-lipid ratio was the most satisfactory one attributed to the moderate-intensity interaction between drug and phospholipid which could balance the drug loading and drug release very well.

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Section: Introductionmentioning

confidence: 99%

Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes

et al. 2021

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“…In 2018, Dong et al proposed a mechanism of action concerning the hepatoprotective activity of H. dulcis fruit extract, and a further study of the same authors elucidated the direct involvement of DHM in the metabolism of acetaminophen endowing the use of fruits as an herbal remedy for preventing acetaminophen-induced liver injury [22,23]. The potential application of DHM as a drug or active component in food supplements is limited by its poor chemical stability and poor bioavailability [24]; however, in the last decade, new drug delivery systems have been proposed to overcome these disadvantages [25][26][27][28][29][30][31]. DHM is responsible for other pharmacological activities not related to H. dulcis, and thus that are not discussed in this paper [32].…”

Section: Phytochemistrymentioning

confidence: 99%

Hovenia dulcis Thumberg: Phytochemistry, Pharmacology, Toxicology and Regulatory Framework for Its Use in the European Union

et al. 2021

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Hovenia dulcis Thunberg is an herbal plant, belonging to the Rhamnaceae family, widespread in west Asia, USA, Australia and New Zealand, but still almost unknown in Western countries. H. dulcis has been described to possess several pharmacological properties, such as antidiabetic, anticancer, antioxidant, anti-inflammatory and hepatoprotective, especially in the hangover treatment, validating its use as an herbal remedy in the Chinese Traditional Medicine. These biological properties are related to a variety of secondary metabolites synthesized by the different plant parts. Root, bark and leaves are rich of dammarane-type triterpene saponins; dihydrokaempferol, quercetin, 3,3′,5′,5,7-pentahydroflavone and dihydromyricetin are flavonoids isolated from the seeds; fruits contain mainly dihydroflavonols, such as dihydromyricetin (or ampelopsin) and hovenodulinol, and flavonols such as myricetin and gallocatechin; alkaloids were found in root, barks (frangulanin) and seeds (perlolyrin), and organic acids (vanillic and ferulic) in hot water extract from seeds. Finally, peduncles have plenty of polysaccharides which justify the use as a food supplement. The aim of this work is to review the whole scientific production, with special focus on the last decade, in order to update phytochemistry, biological activities, nutritional properties, toxicological aspect and regulatory classification of H. dulcis extracts for its use in the European Union.

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“…Stability at extreme temperatures (>room temperature) could not be achieved because phospholipid will deteriorate at higher temperatures. [40] The optimized CCAEL formulation was evaluated for EE, vesicle size, and ζ potential. According to the data [ Table 5], after a period of 4 weeks, formulations were stored at refrigeration temperature showed higher EE when compared to the room temperature.…”

Section: In Vitro Intestinal Permeation Studymentioning

confidence: 99%

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Aim: A chitosan-coated liposomes of standardized Centella asiatica extract (CAE) was developed with the aim of improving the solubility of its phytoconstituents for the oral route with the intention to treat Alzheimer's disease. Materials and Methods: The CAE was obtained by the soxhletion process. The formulation was optimized using design-expert software, solvent evaporation, and ionotropic gelation method was adopted to prepare CAE liposome (CAEL) and chitosan-coated CAE liposomes (CCAEL), respectively. The prepared CCAEL was characterized for its vesicle size, entrapment efficiency, polydispersity index, drug content analysis, Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), transmission electron microscopy (TEM), atomic force microscopy (AFM), in vitro drug release, in vitro antioxidant study, ex vivo permeation study, and stability study. Results and Discussion: The proper amalgamation of drug and chitosan-phospholipid mixture was confirmed by FTIR and DSC. The surface morphology of the prepared formulation was examined by TEM and AFM. The in vitro rate of drug release pattern was analyzed where CAE showed less rate of release of 35.34 ± 0.30% in about 10 h due to poor solubility, while approximately 58.6 ± 0.42% release was observed from optimized CCAEL. In vitro antioxidant study demonstrated that free radical scavenging activity of CAE was retained even after intricate it with the phospholipid, that is, % inhibition of 2,2-diphenyl-1-picrylhydrazyl at 50 µg/ml was found 73.84% whereas 74.4% CAE. In vitro intestinal study proved that the permeation rate increases due to the encapsulation of chitosan-phospholipid complex. Stability study showed that chitosan coated liposomes were stable due to compact chitosan coating layer. Conclusion: The outcome of the current study is quite encouraging, shows better solubility and permeability. Further detailed preclinical studies are required to be conducted to ensure better product development.

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Preparation of a nanoscale dihydromyricetin-phospholipid complex to improve the bioavailability: in vitro and in vivo evaluations

Cited by 50 publications

References 50 publications

Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes

Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes

Hovenia dulcis Thumberg: Phytochemistry, Pharmacology, Toxicology and Regulatory Framework for Its Use in the European Union

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