Nanoformulation strategies for improving intestinal permeability of drugs: A more precise look at permeability assessment methods and pharmacokinetic properties changes

Babadi, Delaram; Dadashzadeh, Simin; Osouli, Mahraz; Daryabari, Maryam Sadat; Haeri, Azadeh

doi:10.1016/j.jconrel.2020.02.041

Cited by 64 publications

(35 citation statements)

References 213 publications

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“…A large number of studies have shown that appropriate nano system selection and fine-tuning of the physical and chemical properties of the system can enhance drug absorption. In addition to preventing degradation by enzymes and acids in the gastrointestinal tract and increasing the solubility of drugs in the lumen, delivery carriers can also enhance transport through the gastrointestinal barrier [15][16][17].…”

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confidence: 99%

“…From a physiological point of view, the gastrointestinal barrier is designed to protect our bodies from foreign compounds. The therapeutic agent must first diffuse through the mucous layer, and then enter the blood or lymph circulation through the epithelial cell barrier under the mucosa [15,25]. However, thorough research on the actual outcomes for NPs in the digestive tract remains limited [11].…”

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confidence: 99%

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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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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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“…In addition, the liposomal structure is not resistant to the acidic environment of the stomach. In the same manner as various nanoparticles, it is difficult for the intact liposomes to permeate freely across intestinal barriers due to their relatively large size [52]. One of the biggest limitations of liposomes as a drug delivery system has been the difficulty in continuous mass production and quality control because the liposomal system is very complex [8,14].…”

Section: Biocompatibility Physical Instability In Liquid State Versatmentioning

confidence: 99%

Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

Lee

2020

Pharmaceutics

155

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It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability in the GI tract and poor permeability across intestinal epithelia because of its relatively large size. In addition, there have been no liposomal formulations approved for oral use to date, despite the success of parenteral liposomes. Nevertheless, liposomal oral delivery has resurged with the rapid increase of published studies in the last decade. However, it is discouraging that most of this research has been in vitro studies only and there have not been many water-insoluble drugs with in vivo data. The present review focused on the in vivo evidence for the improved BA of water-insoluble drugs using liposomes to resolve doubts raised concerning liposomal oral delivery and attempted to provide insight by highlighting the approaches used for in vivo achievements.Pharmaceutics 2020, 12, 264 2 of 30 However, there have been several drawbacks to be overcome, such as instability in the GI tract and poor permeability across the intestinal epithelia because of liposomes' relatively large size [8]. Moreover, it seemed that liposomal oral delivery was faltering during 1980s due to some disappointing results for insulin [9]. However, liposomal oral delivery resurged with a rapid increase in the number of papers published, as shown in Pubmed search results, mainly due to various advanced modification technologies, even though liposomal oral delivery-related papers account for only 5-6% of the total number of liposomes-related studies (Figure 1). In addition, there was an encouraging meta-analysis report in which phospholipid-based solid formulations were analyzed as being effective for BA enhancement [10]. Although liposomal delivery does not seem to achieve satisfactory improvement of oral BA for peptides and protein drugs yet, it looks more promising for oral delivery of hydrophobic drugs because liposomes can solubilize poorly water-soluble drugs, protect the drug from degradation in the GI tract and enhance permeability through the epithelial cell membrane, consequently increasing oral BA. However, most published papers performed in vitro studies only, thus lacking in vivo pharmacokinetic results. The present review focuses on the in vivo evidence for the improved BA of water-insoluble drugs and highlights the approaches used for in vivo achievements.

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“…Over the past decades, various nanomaterials have been widely employed as either the drug carriers or the functional agents for drug delivery, tissue engineering, and theranostics, due largely to their unique physicochemical properties and the convenience for functionalization 1‐5 . The advantages, modification strategies, potential delivery routes, and also challenges of nanomaterial systems have already been well documented 6‐8 . It is commonly acknowledged that oral administration is the most preferred route for drug delivery due to its great convenience and patient compliance 9,10 .…”

Section: Introductionmentioning

confidence: 99%

Protein corona formed in the gastrointestinal tract and its impacts on oral delivery of nanoparticles

Zhu

Qian

et al. 2020

Medicinal Research Reviews

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The interaction of nanoparticles (NPs) with proteins and the formation of protein corona in the biological fluids are of great interest and significance for drug delivery. In the past decade, the corona formation in the blood and its impacts on the in vitro and in vivo fate of NPs has been well investigated and reviewed. Recently, more and more attention is paid to the nano–protein interactions taking place in the gastrointestinal tract (GIT) between the orally administered NPs and the digestive enzymes. The enzyme corona formed in the GIT can significantly affect the properties, gastrointestinal transit, and oral absorption of NPs. Since oral delivery is the most preferred delivery route, comprehensively understanding the corona formation in the GIT and its impacts on oral delivery NPs are of great importance. Herein, we aim to summarize the recent updates on the nano–protein interactions between NPs and digestive enzymes, and launch an interesting discussion on the potentials of using the digestive enzyme corona for the colon targeted delivery.

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Nanoformulation strategies for improving intestinal permeability of drugs: A more precise look at permeability assessment methods and pharmacokinetic properties changes

Cited by 64 publications

References 213 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

Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

Protein corona formed in the gastrointestinal tract and its impacts on oral delivery of nanoparticles

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