Formulation optimization and the absorption mechanisms of nanoemulsion in improving baicalin oral exposure

Wu, Lei; Bi, Yujie; Wu, Hongfei

doi:10.1080/03639045.2017.1391831

Cited by 28 publications

(11 citation statements)

References 34 publications

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“…And it reaches the maximum emulsification area when the K m (the ratio of Tween‐80 and PEG‐400) is 2 : 1. Studies have shown that the formulation of SMEDDS is required to achieve better self‐emulsifying effect with a lower amount of emulsifier and needs to be emulsified at a fast speed and stably . The above results indicated that the optimal ratio of solvents is Tween‐80 : PEG‐400 : IPM = 14 : 7 : 9.…”

Section: Resultsmentioning

confidence: 88%

The preparation and investigation of spinosin–phospholipid complex self-microemulsifying drug delivery system based on the absorption characteristics of spinosin

Song

Lai

Xie

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives The aim of this research was to investigate the intestinal absorption characteristics and mechanisms of spinosin (SPI), and a new dosage form was prepared to increase the intestinal absorption of SPI. Methods In this study, the intestinal absorption characteristics and mechanisms of SPI were first investigated using in situ absorption model and Caco‐2 monolayer model. Subsequently, the phospholipid complex (PLC) loaded with SPI was prepared followed by a self‐microemulsifying drug delivery system (SMEDDS) technique for developing a more efficient formulation. Key findings The results showed that the absorption rate constant (0.02 h−1) and absorption percentage (10%) of SPI were small. Paracellular and active transport pathways mainly mediated the intestinal absorption of SPI. Moreover, SPI‐PLC‐SMEDDS showed a nanoscale particle size and excellent dispersibility in vitro. The cellular uptake and transportation properties of SPI‐PLC‐SMEDDS in the Caco‐2 cell model were improved significantly. Besides, a statistically dramatically higher oral bioavailability (almost fivefold) was observed following the oral administration of SPI‐PLC‐SMEDDS than free SPI on the basis of pharmacokinetic experiment results. Furthermore, the SPI‐PLC‐SMEDDS exhibited certain immunization. Conclusions SPI‐PLC‐SMEDDS could be a promising oral drug delivery system to improve the absorption of SPI.

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Section: Resultsmentioning

confidence: 88%

The preparation and investigation of spinosin–phospholipid complex self-microemulsifying drug delivery system based on the absorption characteristics of spinosin

Song

Lai

Xie

et al. 2019

Journal of Pharmacy and Pharmacology

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“…The co-surfactants can reduce the surface tension of nanoemulsion and adjust the flexibility of interfacial films. 9 This study investigated the effects of three co-surfactants (DEGEE, propylene glycol, ethanol) on the area of nanoemulsion regions. The phase diagrams formed by EL35 (K m =1:1), triacetin, and three different co-surfactants were shown in Fig.…”

Section: Pseudo Ternary Phase Diagramsmentioning

confidence: 99%

“…Nanoemulsion is a transparent homogeneous dispersion system which is spontaneously formed by water, oil, surfactants and co-surfactants, with a particle size of 1−100nm. 9 As a new type of drug delivery system, nanoemulsion presents various forms of drug delivery according to its structure types and drug characteristics, and it has significant effects in targeted drug delivery, sustained release, and solubilization. Its mechanisms to improve the bioavailability mainly include: improving drug intestinal permeability, 10 increasing drug lymphatic transport, 9 preventing the recognition and efflux of proteins, 11 and improving drug solubility and stability.…”

Section: Introductionmentioning

confidence: 99%

Nanoemulsion for Improving the Oral Bioavailability of Hesperetin: Formulation Optimization and Absorption Mechanism

Zeng

Wang

Tian

et al. 2021

Journal of Pharmaceutical Sciences

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This study aimed to prepare a nanoemulsion vehicle to improve the oral bioavailability of hesperetin. The pseudo-ternary phase diagrams and the RSM were used to optimize nanoemulsion parameters. Compared with hesperetin suspension, the AUC 0-t and C max of nanoemulsion were increased by 5.67-fold and 2.64-fold, respectively. The proportion of lymphatic transport reached 87.72%, the cumulative absorption amount of jejunum, ileum, and duodenum increased by 1.1-fold, 1.92-fold, and 1.5-fold, respectively. The results implied that hesperetin nanoemulsion could effectively improve the bioavailability of hesperetin by increasing lymphatic transport and enhancing intestinal permeability. Therefore, nanoemulsion is a potential method to improve the bioavailability of hesperetin, which has strong practicability.

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“…Despite its low solubility, the bioavailability of baicalein is still superior to that of baicalin when administered at equivalent doses in rats, when measuring the baicalin plasma concentration [196]. Many technological attempts have been made to improve the bioavailability of baicalein or baicalin: preparation of micelles with different excipients [194,197]; co-crystal formation with theophylline [198], nicotinamide [199], or other compounds [200]; co-precipitates with polyvinylpyrrolidone [201]; nanocrystals for oral or pulmonary administration [56,202,203,204]; nanoemulsions [205,206,207,208]; nanosuspensions [209]; nanoliposomes [210,211] and nanostructure lipid carriers [212,213]; self-assembled nanoparticles [214]; solid lipid nanoparticles [215]; solid dispersions with different excipients [216,217,218,219]; preparation of complexes with cyclodextrins [220]; and self-microemulsifying systems [221].…”

Section: Bioavailabilitymentioning

confidence: 99%

Pharmacokinetics of B-Ring Unsubstituted Flavones

et al. 2019

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B-ring unsubstituted flavones (of which the most widely known are chrysin, baicalein, wogonin, and oroxylin A) are 2-phenylchromen-4-one molecules of which the B-ring is devoid of any hydroxy, methoxy, or other substituent. They may be found naturally in a number of herbal products used for therapeutic purposes, and several have been designed by researchers and obtained in the laboratory. They have generated interest in the scientific community for their potential use in a variety of pathologies, and understanding their pharmacokinetics is important for a grasp of their optimal use. Based on a comprehensive survey of the relevant literature, this paper examines their absorption (with deglycosylation as a preliminary step) and their fate in the body, from metabolism to excretion. Differences among species (inter-individual) and within the same species (intra-individual) variability have been examined based on the available data, and finally, knowledge gaps and directions of future research are discussed.

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Formulation optimization and the absorption mechanisms of nanoemulsion in improving baicalin oral exposure

Abstract: Based on the results, optimal nanoemulsion might be promising nanosystems for oral delivery of baicalin to satisfy clinical requirements.

Cited by 28 publications

References 34 publications

The preparation and investigation of spinosin–phospholipid complex self-microemulsifying drug delivery system based on the absorption characteristics of spinosin

The preparation and investigation of spinosin–phospholipid complex self-microemulsifying drug delivery system based on the absorption characteristics of spinosin

Nanoemulsion for Improving the Oral Bioavailability of Hesperetin: Formulation Optimization and Absorption Mechanism

Pharmacokinetics of B-Ring Unsubstituted Flavones

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