Impact of emulsion-based drug delivery systems on intestinal permeability and drug release kinetics

Buyukozturk, Fulden; Benneyan, James C.; Carrier, Rebecca L.

doi:10.1016/j.jconrel.2009.10.005

Cited by 175 publications

(100 citation statements)

References 32 publications

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“…Previous studies have shown that the use of surfactants may lead to increased, decreased, or unchanged membrane permeability (31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42). It is important to note that surfactants may increase intestinal membrane permeability for drugs with inherently low-permeability and high aqueous solubility (i.e., BCS class III compounds), e.g., through the disruption of membrane integrity to increase paracellular transport (e.g., tight junction opening, which may induce potentially toxic effects) and/or the inhibition of efflux transporters (36,39,(42)(43)(44)(45). However, for lipophilic drugs with inherently high transcellular membrane permeability (e.g., BCS class II), surfactants can decrease the free fraction of drug which results in decreased intestinal membrane permeability (31,35,(39)(40)(41)(42).…”

Section: S-p Interplay From Surfactant-based Systemsmentioning

confidence: 99%

The Solubility–Permeability Interplay and Its Implications in Formulation Design and Development for Poorly Soluble Drugs

Dahan

Miller

2012

AAPS J

228

132

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Abstract. While each of the two key parameters of oral drug absorption, the solubility and the permeability, has been comprehensively studied separately, the relationship and interplay between the two have been largely ignored. For instance, when formulating a low-solubility drug using various solubilization techniques: what are we doing to the apparent permeability when we increase the solubility? Permeability is equal to the drug's diffusion coefficient through the membrane times the membrane/aqueous partition coefficient divided by the membrane thickness. The direct correlation between the intestinal permeability and the membrane/aqueous partitioning, which in turn is dependent on the drug's apparent solubility in the GI milieu, suggests that the solubility and the permeability are closely associated, exhibiting a certain interplay between them, and the current view of treating the one irrespectively of the other may not be sufficient. In this paper, we describe the research that has been done thus far, and present new data, to shed light on this solubility-permeability interplay. It has been shown that decreased apparent permeability accompanies the solubility increase when using different solubilization methods. Overall, the weight of the evidence indicates that the solubility-permeability interplay cannot be ignored when using solubility-enabling formulations; looking solely at the solubility enhancement that the formulation enables may be misleading with regards to predicting the resulting absorption, and hence, the solubility-permeability interplay must be taken into account to strike the optimal solubility-permeability balance, in order to maximize the overall absorption.

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Section: S-p Interplay From Surfactant-based Systemsmentioning

confidence: 99%

The Solubility–Permeability Interplay and Its Implications in Formulation Design and Development for Poorly Soluble Drugs

Dahan

Miller

2012

AAPS J

228

132

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“…These findings are in agreement with earlier studies that showed similar relationships between the emulsification times and the various concentrations of oil and surfactant mixtures. For example, Buyukozturk et al 45 revealed a strong relationship between the mean droplet size of emulsions which contained surfactants with high levels of HLB and the changes in the oil-to-surfactant ratio. Bachynsky et al 46 found that the self-emulsification properties are affected even with low amounts of oil in the system.…”

Section: Evaluation Of Swietenia Oil Self-nanoemulsifying Systemsmentioning

confidence: 99%

The preparation and evaluation of self-nanoemulsifying systems containing Swietenia oil and an examination of its anti-inflammatory effects

Eid¹,

El‐Enshasy²,

Aziz³

et al. 2014

IJN

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There is an increasing trend among pharmaceutical industries to use natural bioactive materials as medicinal agents and to use new technologies such as self-nanoemulsifying systems. The solubility and bioavailability of poorly soluble drugs can be enhanced by self-nanoemulsifying systems. Swietenia oil is frequently used because of its antimicrobial, antimutagenic, and anticancer bioactive medical properties. This study was conducted to develop self-nanoemulsifying systems for Swietenia oil that will enhance the anti-inflammatory activity of the oil. The self-emulsifying systems developed for Swietenia oil in this study were constructed using ternary phase diagrams and contained the nonionic surfactants Labrasol ® , Tween 20, Capmul ® , and Labrafil ® . The effect of these surfactants on the formulation was examined. The mean droplet size of Swietenia oil as well as their distribution, appearance, viscosity, and spreading times were studied to find the optimum formula, which contained droplets that were less than 200 nm. The next step was to test the anti-inflammatory properties of the optimum formula using a carrageenan-induced rat paw edema test. The results from this test were compared to the oil solution. Different oil/surfactants mixtures had various emulsification properties that were related to the size of their droplets. Tween 20 is a good surfactant to use in self-emulsifying systems because it produces droplets of nano-size. Mixtures of Capmul/Labrasol at a ratio of 2:1 and Labrafil/Tween 20 at a ratio of 1:2 were able to produce self-nanoemulsifying formulations containing Swietenia oil concentrations that ranged from 20%–50%. Nanoemulsion occurred when the size of the droplets fell below 200 nm with low size distribution (<0.3) after being gently mixed with water. It was found that the hydrophilic/lipophilic balance value affected the ternary phase diagram behavior of Swietenia oil and surfactants. In addition, the anti-inflammatory properties of Swietenia oil were greater in the self-nanoemulsifying systems than in the oil solution.

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“…The literature offers only very limited information regarding in vitro drug permeability and absorption following the digestion of LBDDS. The effects of some formulation parameters (oil structure, surfactant HLB, lipid/ surfactant ratio) on the intestinal permeability and drug release kinetics from LBDDS were investigated by Buyukozturk et al (80) and the effect of SMEDDS on tight junctions was evaluated by Sha et al (81). Using Caco-2 cell line monolayers the studies revealed useful considerations for the design of LBDDS, including the potential toxicity of these formulations towards Caco2-cell lines, as evident from the observed disruption of the tight junctions.…”

Section: Permeability Studies With Lbddsmentioning

confidence: 99%

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

Thomas

Holm

Rades

2012

AAPS J

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Abstract. Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application.KEY WORDS: in vitro digestion; in vitro lipolysis models; lipid-based drug delivery systems; poorly soluble drugs; self-nanoemulsifying drug delivery systems (SNEDDS).

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Impact of emulsion-based drug delivery systems on intestinal permeability and drug release kinetics

Cited by 175 publications

References 32 publications

The Solubility–Permeability Interplay and Its Implications in Formulation Design and Development for Poorly Soluble Drugs

The Solubility–Permeability Interplay and Its Implications in Formulation Design and Development for Poorly Soluble Drugs

The preparation and evaluation of self-nanoemulsifying systems containing Swietenia oil and an examination of its anti-inflammatory effects

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

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