Developments in Methods for Measuring the Intestinal Absorption of Nanoparticle-Bound Drugs

Liu, Wei; Pan, Hao; Zhang, Caiyun; Zhao, Lei; Zhao, Rongqin; Zhu, Yongtao; Pan, Weisan

doi:10.3390/ijms17071171

Cited by 53 publications

(30 citation statements)

References 95 publications

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“…Caco-2 (human colon carcinoma) cell line is grown normally as a monolayer on polycarbonate membrane in transwell chambers. In this system, the apical and basolateral culture fluids are separated allowing the transport of molecules from one culture fluid to the other (Liu et al, 2016). This model is useful to quantify compound absorption across the monolayer, determine apparent permeability coefficient (P app ) and analyze uptake mechanisms (e.g.…”

Section: Intestinal Epithelial Monolayer Assays (Cellular Uptake)mentioning

confidence: 99%

“…In situ experiments include intestinal loop, intestinal perfusion and intestinal vascular cannulation models. They typically refer to experiments on whole animals, providing intact intestinal mucosa, complete blood supply and nerve domination, together with expression of enzymes and transporters (Liu et al, 2016). However, sophisticated surgical procedures and instrumentation are required.…”

Section: In Situ and Ex Vivomentioning

confidence: 99%

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Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Gonçalves

Martins

Duarte

et al. 2018

Trends in Food Science & Technology

193

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Background: Aiming at the enhancement of food products' nutritional and health value, the incorporation of nutraceuticals has attracted increasing interest in the last years. However, they often exhibit low water solubility and stability, limiting their direct incorporation into food products. Also, they show very low bioavailability due to limited bioaccessibility, poor absorption and/or chemical transformation within the gastrointestinal tract. This renders their health benefits extremely difficult to be realized by the consumers. Scope and approach: In the present review the recent innovations regarding the formulation and design of biobased micro and nano-delivery systems to encapsulate nutraceuticals is discussed; it also gives an overview of the challenges associated to their development; and highlights some strategies to enhance nutraceuticals' bioavailability. An insight about delivery systems' potential toxicity (in particular at nano-scale) is also provided. Key findings and conclusions: Recent developments in the design of bio-based delivery systems offer the possibility of stabilizing and enhancing nutraceuticals' functionality within food products. In fact, different strategies can be used to enhance nutraceuticals' bioavailability: i) nano-delivery systems, besides showing a huge potential for the protection of valuable nutraceuticals during food processing/digestion, can be used to increase their bioavailability; ii) absorption enhancement technologies have been successfully used to increase nutraceuticals' membrane permeation; and iii) excipient foods have been shown to improve nutraceuticals' biological activity. However, the application of these enabling technologies to food is hindered by very pertinent issues that can be summarized in the effective preservation/maximization of the nutraceuticals' bioactivity and safety, once inside the human body.

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Section: Intestinal Epithelial Monolayer Assays (Cellular Uptake)mentioning

confidence: 99%

Section: In Situ and Ex Vivomentioning

confidence: 99%

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Gonçalves

Martins

Duarte

et al. 2018

Trends in Food Science & Technology

193

View full text Add to dashboard Cite

show abstract

“…In this study, we evaluated the permeation capacity and the effect of SOD_Cl, GliSOD_P51 and GliSOD_P61 on the paracellular transport of fluorescein isothiocyanate (FITC)-Dextran in rat small intestine using the in vitro non everted rat intestine sac model. We used this method since it has been widely used to predict in vivo absorption of drugs in humans with low cost and greater simplicity [ 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Gliadin Peptide Facilitates FITC Dextran Transport across the Non Everted Gut Sac of Rat Small Intestine

et al. 2018

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Superoxide dismutase (SOD) is an antioxidant protein. When administered orally, it has low bioavailability due to its low permeation. In a previous study we fused gliadin peptide P51 (LGQQQPFPPQQPYPQPQPF) and gliadin peptide P61 (QQPYPQPQPF) with SOD Citrus limon (SOD_Cl), namely GliSOD_P51 and GliSOD_P61 to increase permeation of SOD_Cl through intestine. In this work, the permeation of fluorescein isothiocyanate (FITC)-Dextran 10 kDa, FD10 and 40 kDa, FD40 as paracellular transport markers across excised rat intestinal wall was investigated with the presence of GliSOD_P51 and GliSOD_P61. A permeability study was performed using non-everted rat intestine by incubating FD10 or FD40 with SOD_Cl, and GliSOD_P61. The presence of SOD_Cl, GliSOD_P51 or GliSOD_P61 inside intestine (apical) and outside intestine (basolateral) was analyzed by protein electrophoresis. The concentration of FD that penetrated to the basolateral solution was analyzed by spectrofluorometry. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis revealed the presence of GliSOD_P51 and GliSOD_P61 but not SOD_Cl in basolateral compartment. The percentage of FD10 but not FD40 and SOD_Cl that penetrated to the basolateral solution significantly increased with the presence of gliadin in GliSOD_P51 and GliSOD_P61. GliSOD_P51 and GliSOD_P61 are able to penetrate the rat intestinal epithelial membrane and the gliadin peptides facilitate FD10 to penetrate the epithelial.

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“…The studies were done in triplicate. The whole process was repeated by replacing the solid SEDDS F1 with bambuterol hydrochloride dissolved in distilled water [29] . The amount of the drug permeating across the membrane/intestine for the drug in solution and the solid SEDD system was compared.…”

Section: Resultsmentioning

confidence: 99%

Formulation and Evaluation of Solid Self-emulsifying Drug Delivery System of Bambuterol Hydrochloride

Saggar¹,

Upadayay²,

Goswami³

2019

pharmaceutical-sciences

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Self-emulsifying drug delivery system (SEDDS) refers to a formulation comprising an isotropic mixture of natural and synthetic oils with hydrophilic or lipophilic surfactants and co solvents, which spontaneously emulsifies when exposed to gastrointestinal fluid to form oil-in-water emulsion [1-4]. The emulsion so produced is a clear dispersion in which the particle size of the dispersed phase ranges from nanometers to several microns. According to Đekić and Primorac, microemulsions are isotropic, transparent systems, which contain spherical droplets of water phase or oil phase, with diameter of average size from 10 to 100 nm, dispersed in a continuous oil or water phase, respectively whereas nanoemulsions are oil-in-water or water-in-oil emulsions with droplet size in the range of 50-1000 nm (preferably from 100 to 500 nm) [5]. The main difference between microemulsions and nanoemulsions is regarding their physical stability, appearance, and microstructure [5]. Pouton et al. reported that SEDDS can be dispensed in either soft gelatin or hard gelatin capsules. Upon oral administration, these systems form fine emulsions (or microemulsions) in the gastro-intestinal tract (GIT) with mild agitation provided by gastric mobility [6,7]. The difference between a SEDDS and self-micro emulsifying drug delivery system is that the former when diluted results in a droplet size between 100 and 300 nm and the later results in a droplet size of less than 50 nm [8]. SEDDS can overcome the problems associated with various drugs falling in various BCS classes, in case of BCS class III drugs, SEDDS can overcome the problem of enzymatic degradation, gut wall efflux and bioavailability [9]. On ingestion of SEDDS, it is initially acted upon by the gastric lipase in the stomach, which digests the lipid part of the formulation and further the gastric emptying enables the emulsification process before

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Developments in Methods for Measuring the Intestinal Absorption of Nanoparticle-Bound Drugs

Cited by 53 publications

References 95 publications

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Gliadin Peptide Facilitates FITC Dextran Transport across the Non Everted Gut Sac of Rat Small Intestine

Formulation and Evaluation of Solid Self-emulsifying Drug Delivery System of Bambuterol Hydrochloride

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