Development of an Oral Compound Pickering Emulsion Composed of Nanocrystals of Poorly Soluble Ingredient and Volatile Oils from Traditional Chinese Medicine

Zhang, Jifen; Zhang, Jiao; Wang, Shuai; Yi, Tao

doi:10.3390/pharmaceutics10040170

Cited by 26 publications

(37 citation statements)

References 39 publications

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“…However, many of the bioactive ingredients of traditional Chinese Pharmaceutics 2020, 12, 216 2 of 18 medicine (TCM) are poorly soluble, which leads to low oral bioavailability and delivery problems. This makes the efficacies of TCM decrease or administration doses increase [13][14][15]. Consequently, oral formulations with improved absorption of Pur have attracted widespread attention.…”

Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

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Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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“…The C max reached up to 7.267 ± 0.432 mg/L, which is more than three times higher than that of water group. The relative bioavailability was calculated as 323%, which is higher than that of the previously reported NSSPE [ 23 ] and SMEDDS [ 24 ] methods.…”

Section: Resultsmentioning

confidence: 57%

“…Efforts have been devoted into the improvement of the solubility and bioavailability of Pueraria flavones. Zhang et al [ 23 ] developed an oral drug nanocrystal self-stabilized Pickering emulsion (NSSPE) and investigated the oral bioavailability of PUE NSSPE. The results showed that the C max of PUE was increased from 634.17 ng/mL to 3226.14 ng/mL.…”

Section: Introductionmentioning

confidence: 99%

Screening, Optimization, and Bioavailability Research of Natural Deep Eutectic Solvent Extracts from Radix Pueraria

Huang

Yang

et al. 2021

Molecules

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Natural deep eutectic solvent (NaDES) is generally considered as a greener alternative to fossil solvent, with great potential in various areas. In the present work, 25 different NaDESs were screened for the extraction of puerarin (PUE) and its two natural derivatives from Radix Pueraria (RP). As the main isoflavone in RP, PUE has a wide range of biological activities. However, its application is restricted due to its poor solubility in water and low oral bioavailability. In this study, the extraction of PUE with NaDESs showed significant advantages compared with traditional solvents. While using L-Pro-Maa (L-proline-malic acid) under optimal conditions, the optimized yields of PUE, 3-MPR and PRX were 98.7 mg/g, 16.3 mg/g and 9.9 mg/g, respectively, which were 2.2-, 2.9- and 3.4-fold higher than that of water. Furthermore, the oral bioavailability of PUE in NaDES extracts was comparatively investigated in rats with HPLC-MS technique. Pharmacokinetic analysis revealed that the relative bioavailability of PUE in L-Pro-Maa extract is 323%. The result indicated that NaDES is not only a sustainable ionic liquid with higher extraction efficiency, but also an enhancer of oral bioavailability of specific natural products.

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“…A novel liquid Pickering emulsion with a unique composition and microstructure, i.e., drug nanocrystals self-stabilized Pickering emulsion (NSSPE) has been developed to orally deliver poorly water-soluble drugs. In NSSPE, nanocrystals of poorly water-soluble drugs, which acted as the therapeutic substance as well as the stabilizer of emulsion, were adsorbed at the oil-water interface, forming a unique core-shell structure with a core of oil saturated with drug and a shell of drug nanocrystals [ 1 , 2 ]. Consequently, NSSPE could significantly enhance the oral bioavailability of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

“…Consequently, NSSPE could significantly enhance the oral bioavailability of poorly water-soluble drugs. Pharmacokinetics studies showed NSSPE improved AUC of silybin and puerarin to 4.6 times and 2.6 times compared with crude material, respectively [ 1 , 2 ], suggesting great application potential for oral administration of poorly water-soluble drugs. NSSPE also has the higher drug loading and safety than traditional emulsions [ 3 , 4 ].…”

Section: Introductionmentioning

confidence: 99%

A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers

Zhang

Wang

et al. 2021

Molecules

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A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.

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Development of an Oral Compound Pickering Emulsion Composed of Nanocrystals of Poorly Soluble Ingredient and Volatile Oils from Traditional Chinese Medicine

Cited by 26 publications

References 39 publications

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Screening, Optimization, and Bioavailability Research of Natural Deep Eutectic Solvent Extracts from Radix Pueraria

A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers

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