Ex vivo and in situ approaches used to study intestinal absorption

Luo, Zhiqiang; Liu, Yang; Zhao, Baosheng; Tang, Mingmin; Dong, Honghuan; Zhang, Lei; Lv, Beiran; Li, Wei

doi:10.1016/j.vascn.2013.06.001

Cited by 81 publications

(57 citation statements)

References 78 publications

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“…The SPIP technique was applied as previously reported (Luo et al, 2013;Samiei et al, 2013). The male SpragueDawley rats were fasted for 24 h but allowed free access to water.…”

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

“…The absorption in the recirculating perfusion model will be increased just because it has a long retention time for the solution in the intestine (Cao et al, 2013). The single-pass perfusion is suitable for drugs that are rapidly absorbed, meanwhile it could have a comparatively absorption just by its slowly single-pass rate (Luo et al, 2013). Thus it is widely used for the research of the intestinal absorption.…”

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

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Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Lei

Cui

et al. 2014

Drug Delivery

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(2015) Enhanced oral bioavailability of piperine by selfemulsifying drug delivery systems: invitro,invivo and insitu intestinal permeability studies, Drug Delivery, 22:6, 740-747, DOI: 10.3109/10717544.2014 AbstractThe main purpose of this work was to develop and evaluate a self-emulsifying drug delivery system (SEDDS) of piperine to enhance its solubility and bioavailability. The formulation was optimized by solubility test and ternary phase diagrams. Then physiochemical properties and in vitro release of SEDDS were characterized. In vivo pharmacokinetics study and in situ singlepass intestinal perfusion were performed to investigate the effects of SEDDS on the bioavailability and intestinal absorption of piperine. The optimized formulation was composed of ethyl oleate, Tween 80 and Transcutol P (3:5.5:1.5, w/w), with the level of the piperine reached 2.5% (w/w). The in vitro dissolution rates of piperine SEDDS were significantly higher than the self-prepared capsules. In vivo pharmacokinetic study showed C max1 , C max2 and area under the curve of piperine after oral administration of SEDDS in rats were 3.8-, 7.2-and 5.2-fold higher than the self-prepared capsules, respectively, and the relative bioavailability of SEDDS was 625.74%. The in situ intestinal absorption study revealed that the effective permeability and the effective absorption rate values of piperine for SEDDS were significantly improved comparing to solutions (p50.01). So SEDDS formulation could improve the oral bioavailability and intestinal absorption of piperine effectively.

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“…The SPIP technique was applied as previously reported (Luo et al, 2013;Samiei et al, 2013). The male SpragueDawley rats were fasted for 24 h but allowed free access to water.…”

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Lei

Cui

et al. 2014

Drug Delivery

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“…The single-pass perfusion technique facilitates the study of rapid absorption and is suitable for drugs that are rapidly absorbed. In the recirculating perfusion model, the probability of absorption is considerably increased because of the longer retention time of the solution in the intestine (Grassi & Cadelli, 2001;Luo et al, 2013). Thus, it is recommended that drugs which are absorbed comparatively slowly as shown by single-pass perfusion techniques are reexamined using recirculating perfusion to magnify the concentration changes Luo et al, 2013;Singh et al, 2013).…”

Section: In Situ Absorption Evaluation Of Herbal Drug In Rat Intestinementioning

confidence: 99%

Self-emulsifying drug delivery system and the applications in herbal drugs

Zhang

et al. 2013

Drug Delivery

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Herbal drugs have been used for thousands of years in the east and have had a recent resurgence in popularity among consumers in the west. However, most of herbal drug are poorly soluble and have hydrophobic properties and poor distribution, leading to reduced bioavailability and hence decreased treatment efficacy, requiring repeated administration or increased dose. In the past few decades, considerable attention has been focused on the development of self-emulsifying drug delivery system (SEDDS) for herbal drugs. SEDDS is isotropic and thermodynamically stable solutions consisting of oil, surfactant, co-surfactant and drug that can spontaneously form oil-in-water micro/nanoemulsion when mixed with water under gentle stirring. The formulation can be a viable alternative to classical formulations to take advantage of their lipophilic nature and to solve their problems of poor solubility, poor bioavailability, low oral absorption and instability. The mechanism of self-emulsification, solubility studies, construction of phase diagram, optimization and characterization of herbal drugs-loaded SEDDS formulation and in situ absorption evaluation of herbal drugs in rat intestine are presented in our article.

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“…25 Unsurprisingly, in our study the intestine was mainly responsible for absorbing EDA. The intestinal absorption of EDA was clearly increased by loading EDA into NEEPN or CNE nanosystems.…”

Section: Neepn Absorption In Stomach and Intestinementioning

confidence: 49%

Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine–phospholipid nanocomplex

Hu¹,

Chen²,

Jiang³

et al. 2014

IJN

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Purpose The purpose of this study was to assess the improved absorption and in vivo kinetic characteristics of a novel water-in-oil nanoemulsion containing evodiamine–phospholipid nanocomplex (NEEPN) when administered orally. Methods NEEPN was fabricated by loading an evodiamine–phospholipid nanocomplex into a water-in-oil nanoemulsive system. The gastrointestinal absorption of NEEPN was investigated using an in situ perfusion method. The modified in vivo kinetic characteristics of evodiamine (EDA) in NEEPN were also evaluated. Results Compared with EDA or conventional nanoemulsions containing EDA instead of evodiamine–phospholipid complex, NEEPN with its favorable in vivo kinetic characteristics clearly enhanced the gastrointestinal absorption and oral bioavailability of EDA; for example, the relative bioavailability of NEEPN to free EDA was calculated to be 630.35%, and the effective permeability of NEEPN in the colon was 8.64-fold that of EDA. Conclusion NEEPN markedly improved the oral bioavailability of EDA, which was probably due to its increased gastrointestinal absorption. NEEPN also increased efficacy and reduced adverse effects for oral delivery of EDA. Such finding demonstrates great clinical significance as an ideal drug delivery system demands high efficacy and no adverse effects.

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Ex vivo and in situ approaches used to study intestinal absorption

Cited by 81 publications

References 78 publications

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Self-emulsifying drug delivery system and the applications in herbal drugs

Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine–phospholipid nanocomplex

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Ex vivo and in situ approaches used to study intestinal absorption

Cited by 81 publications

References 78 publications

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Self-emulsifying drug delivery system and the applications in herbal drugs

Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine&ndash;phospholipid nanocomplex

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Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine–phospholipid nanocomplex