20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies

Pu, Yang; Zhang, Xitong; Zhang, Qi; Wang, Bing; Chen, Yuxi; Zang, Chuanqi; Wang, Yuqin; Dong, Tina Ting Xia; Zhang, Tong

doi:10.3390/molecules21101396

Cited by 25 publications

(12 citation statements)

References 61 publications

(72 reference statements)

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“…26 The phospholipid-active ingredient is responsible for the creation of a hydrogen connection between the polar head and the active ingredient's polar functionalities. 25,27 In summary, as presented in Figure 2, the hydroxyl groups of polyphenols can interact effectively with nitrate and phosphate groups of phospholipids.…”

Section: Phytosome Structure and Preparation Methodsmentioning

confidence: 93%

“…Many authors have stated that the hydrogen interactions are the main interactions in phytosome vesicles. 25 Phospholipids have an affinity for polyphenols and form supramolecular adducts that have a definite stoichiometry, which can be obtained from thermal analysis. Semalty et al tested this parameter and found that hydrogen bond formation or hydrophobic interactions were due to the interaction between the two molecules.…”

Section: Phytosome Structure and Preparation Methodsmentioning

confidence: 99%

“…Many authors have stated that the hydrogen interactions are the main interactions in phytosome vesicles. 25 …”

Section: Phytosome Structure and Preparation Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Phytosomes as Innovative Delivery Systems for Phytochemicals: A Comprehensive Review of Literature

Barani¹,

Sangiovanni²,

Angarano³

et al. 2021

IJN

137

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Nowadays, medicinal herbs and their phytochemicals have emerged as a great therapeutic option for many disorders. However, poor bioavailability and selectivity might limit their clinical application. Therefore, bioavailability is considered a notable challenge to improve bio-efficacy in transporting dietary phytochemicals. Different methods have been proposed for generating effective carrier systems to enhance the bioavailability of phytochemicals. Among them, nano-vesicles have been introduced as promising candidates for the delivery of insoluble phytochemicals. Due to the easy preparation of the bilayer vesicles and their adaptability, they have been widely used and approved by the scientific literature. The first part of the review is focused on introducing phytosome technology as well as its applications, with emphasis on principles of formulations and characterization. The second part provides a wide overview of biological activities of commercial and non-commercial phytosomes, divided by systems and related pathologies. These results confirm the greater effectiveness of phytosomes, both in terms of biological activity or reduced dosage, highlighting curcumin and silymarin as the most formulated compounds. Finally, we describe the promising clinical and experimental findings regarding the applications of phytosomes. The conclusion of this study encourages the researchers to transfer their knowledge from laboratories to market, for a further development of these products.

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Section: Phytosome Structure and Preparation Methodsmentioning

confidence: 93%

Section: Phytosome Structure and Preparation Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Phytosomes as Innovative Delivery Systems for Phytochemicals: A Comprehensive Review of Literature

Barani¹,

Sangiovanni²,

Angarano³

et al. 2021

IJN

137

View full text Add to dashboard Cite

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“…Each sample was placed on aluminum pans, and heated at a rate of 40 °C/min under an argon atmosphere was used from 40 to 600 °C. 18 Using Cu (1.54060 A) as a source of radiation, the P-XRD spectra for the same samples were recorded on a Shimadzu XRD 6000 diffractometer. The data was taken at a step size of 0.02 degrees and a time per step of 0.15 seconds throughout an angular range of 5 to 80 degrees.…”

Section: Predicted Intermolecular Hydrogen Bond Search With Data Anal...mentioning

confidence: 99%

Modified solid in oil nanodispersion containing vemurafenib-lipid complex-in vitro/in vivo study

2022

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Background: Vemurafenib (VEM) was a licensed drug for the treatment of skin melanoma and is available only in the market as oral tablets prescribed in huge doses (1920 mg/day). One reason for the high dose is vemurafenib's low oral bioavailability. Methods: VEM-lipid complex (DLC) was predicted based on Conquest and Mercury programs and prepared using the solvent evaporation method using the lipid (phosphatidylethanolamine). DLC was subjected to characterization (FT-IR, Raman spectroscopy, DSC, TGA, P-XRD, and FESEM) to confirm complexation. DLC was used to prepare solid in oil nanodispersion (DLC-SON) and subjected to in vitro, ex vivo, and in vivo evaluation in comparison to our recently prepared conventional SON (VEM-SON) and DLC-control. Results: Conquest and Mercury predict the availability of intermolecular hydrogen bonding between VEM and phosphatidylethanolamine (PE). All characterization tests of DLC ensure the complexation of the drug with PE. Ex vivo studies showed that the drug in DLC-SON has significantly (P<0.05) higher skin permeation than DLC-control but lower drug permeation than conventional SON but it has a higher % skin deposition (P<0.05) than others. The half-maximal inhibitory concentration (IC50) of the prepared DLC-SON is significantly high (P<0.05) in comparison to the conventional SON and pure VEM. In vivo permeation using confocal laser scanning microscopy (on the rat) results indicated that both conventional SON and DLC-SON can cross the SC and infiltrate the dermis and epidermis but DLC-SON has a higher luminance/gray value after 24 h in the dermis in comparison to the conventional SON. Conclusion: The novel lipid complex for VEM prepared using PE as a lipid and enclosed in SON showed higher anticancer activity and topical permeation as well as sustained delivery and good retention time in the dermis that localize the drug in a sufficient concentration to eliminate early diagnosed skin melanoma.

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“…10) Additionally, the favorable biocompatibility of phospholipid (PC) allows it to penetrate the cell membranes easily, and studies have reported that PC is capable of enhancing the solubility of drugs due to their amphiphilic nature, thereby improving their permeation and oral absorption. 11,12) For another, hydroxypropyl-β-cyclodextrin (HPCD) has already been confirmed as an excellent enhancer of drug solubility. 13) Meanwhile, the carrier formed by combinations of different carriers may exhibit the advantages of each single carrier, which have a synergistic effect on drug delivery.…”

Section: Introductionmentioning

confidence: 99%

Andrographolide/Phospholipid/Cyclodextrin Complex-Loaded Nanoemulsion: Preparation, Optimization, <i>in Vitro</i> and <i>in Vivo</i> Evaluation

Zou

Ding

Huang

et al. 2022

Biological & Pharmaceutical Bulletin

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Andrographolide (AG), a natural product with various pharmacological effects, exhibited low oral bioavailability owing to its poor solubility, stability, and low absorption. Previous studies have suggested that phospholipid (PC) and hydroxypropyl-β-cyclodextrin (HPCD) could improve the drug solubility and absorption. Moreover, nanoemulsion (NE) has been confirmed as an appropriate enhancer for oral bioavailability. Therefore, AG/HPCD/PC complex (AHPC) was synthesized, and AHPC-loaded nanoemulsion (AHPC-NE) was optimized and prepared using central composite design combined response surface methodology. The average droplet size and polydispersity index (PDI) were 116.50 5.99 and 0.29 0.03 nm, respectively. AHPC-NE with a loading capacity of 0.32 0.01% and an encapsulation efficiency of 96.43 2.27% appeared round and uniformly dispersed based on transmission electron microscopy. In vivo release studies demonstrated that AHPC-NE had good sustained-release effects. Further, AHPC-NE significantly enhanced the absorption of AG with a relative bioavailability of 550.71% compared to AG suspension. Such findings reveal AHPC-NE as a potential strategy for sustained-release and oral bioavailability enhancement.

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20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies

Cited by 25 publications

References 61 publications

Phytosomes as Innovative Delivery Systems for Phytochemicals: A Comprehensive Review of Literature

Phytosomes as Innovative Delivery Systems for Phytochemicals: A Comprehensive Review of Literature

Modified solid in oil nanodispersion containing vemurafenib-lipid complex-in vitro/in vivo study

Andrographolide/Phospholipid/Cyclodextrin Complex-Loaded Nanoemulsion: Preparation, Optimization, <i>in Vitro</i> and <i>in Vivo</i> Evaluation

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