Impacts of particle shapes on the oral delivery of drug nanocrystals: Mucus permeation, transepithelial transport and bioavailability

Guo, Meng; Wei, Mengdi; Li, Wen; Guo, Meichen; Guo, Chunlin; Ma, Minchao; Wang, Yu; Yang, Zhiman; Li, Mo; Fu, Qiang; Yang, Li; Zhang, He

doi:10.1016/j.jconrel.2019.06.015

Cited by 76 publications

(34 citation statements)

References 46 publications

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“…Bafilomycin A1 is an inhibitor of endosomal acidification. Brefeldin A can prevent the transport of NPs from the ER to the Golgi complex, and monensin can block transport from the Golgi complex to the plasma membrane [49,50].…”

Section: Evaluation Of Model Nps Permeation In Monolayer Cellsmentioning

confidence: 99%

Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Guo

Liu

et al. 2021

J Nanobiotechnol

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Background The use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs. In this study—with the premise of controlling single variables—we prepared model nanoparticles with different particle sizes, surface charges, and surface hydrophobicity/hydrophilicity. The two key stages of intestinal nanoparticles (NPs) absorption—the intestinal mucus layer penetration stage and the trans-intestinal epithelial cell stage—were decoupled and analyzed. The intestinal absorption of each group of model NPs was then investigated. Results Differences in the behavioral trends of NPs in each stage of intestinal absorption were found to result from differences in particle properties. Small size, low-magnitude negative charge, and moderate hydrophilicity helped NPs pass through the small intestinal mucus layer more easily. Once through the mucus layer, an appropriate size, positive surface charge, and hydrophobic properties helped NPs complete the process of transintestinal epithelial cell transport. Conclusions To achieve high drug bioavailability, the basic properties of the delivery system must be suitable for overcoming the physiological barrier of the gastrointestinal tract.

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Section: Evaluation Of Model Nps Permeation In Monolayer Cellsmentioning

confidence: 99%

Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Guo

Liu

et al. 2021

J Nanobiotechnol

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“…Another study proposed that particle diffusion through the mucus layer increases the absorption of aprepitant ( Roos et al, 2018b ). Particle diffusion through the mucus layer has also been reported to increase the bioavailability of other drugs ( Guo et al, 2019 ).…”

Section: Resultsmentioning

confidence: 99%

Enabling formulations of aprepitant: in vitro and in vivo comparison of nanocrystalline, amorphous and deep eutectic solvent based formulations

Palmelund

Eriksen

Bauer‐Brandl

et al. 2021

International Journal of Pharmaceutics: X

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A deep eutectic solvent (DES) is a eutectic system consisting of hydrogen bond donor and acceptor has been suggested as a promising formulation strategy for poorly soluble drugs. A DES consisting of choline chloride and levulinic acid in a 1:2 molar ratio was used to formulate a liquid solution of the model drug aprepitant. This formulation was tested in vitro (drug release and permeability) and in vivo (rat model) and compared with the performance of amorphous aprepitant and the commercial aprepitant nanocrystalline formulation. In this study a DES formulation is compared for the first time directly to other established enabling formulations. The in vitro drug release study demonstrated that the DES formulation and the amorphous form both were able to induce an apparent supersaturation followed by subsequent drug precipitation. To mitigate the risk of precipitation, HPMC was predissolved in the dissolution medium, which successfully reduced the degree of precipitation. In line with the results from the release study, an in vitro permeation study showed superior permeation of the drug from the DES formulation and from the amorphous form compared to the nanocrystalline formulation. However, the promising in vitro findings could not be directly translated into an increased in vivo performance in rats compared to the nanocrystalline formulation. Whilst the DES formulation (34 ± 4%) showed a higher oral bioavailability compared to amorphous aprepitant (20 ± 4%), it was on par with the oral bioavailability obtained from the nanocrystalline formulation (36 ± 2%).

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“…A biomimetic virus-like or charge reversible nanoparticles are able to improve the oral insulin delivery by overcoming mucus barriers 154 . In addition, particle geometry can affect the mucus-penetrating ability significantly by micromovement 155 . It has been revealed that the nanorods diffused across mucus layer rapidly by rotation 156 .…”

Section: Current Strategies Towards Enhancement Of the Oral Absorption Of Ppsmentioning

confidence: 99%

Oral delivery of proteins and peptides: Challenges, status quo and future perspectives

Zhu

Chen

Paul

et al. 2021

Acta Pharmaceutica Sinica B

127

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Proteins and peptides (PPs) have gradually become more attractive therapeutic molecules than small molecular drugs due to their high selectivity and efficacy, but fewer side effects. Owing to the poor stability and limited permeability through gastrointestinal (GI) tract and epithelia, the therapeutic PPs are usually administered by parenteral route. Given the big demand for oral administration in clinical use, a variety of researches focused on developing new technologies to overcome GI barriers of PPs, such as enteric coating, enzyme inhibitors, permeation enhancers, nanoparticles, as well as intestinal microdevices. Some new technologies have been developed under clinical trials and even on the market. This review summarizes the history, the physiological barriers and the overcoming approaches, current clinical and preclinical technologies, and future prospects of oral delivery of PPs.

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Impacts of particle shapes on the oral delivery of drug nanocrystals: Mucus permeation, transepithelial transport and bioavailability

Cited by 76 publications

References 46 publications

Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Enabling formulations of aprepitant: in vitro and in vivo comparison of nanocrystalline, amorphous and deep eutectic solvent based formulations

Oral delivery of proteins and peptides: Challenges, status quo and future perspectives

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