Chromatographic indexes on immobilized artificial membranes for the prediction of transdermal transport of drugs

Barbato, Francesco; Cappello, B; Miro, Agnese; Rotonda, M. L. La; Quaglia, Fabiana

doi:10.1016/s0014-827x(98)00082-2

Cited by 46 publications

(41 citation statements)

References 17 publications

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“…The systems include the immobilized artificial membrane (Barbato et al, 1998), biopartitioning micellar chromatography (Escuder-Gilabert et al, 2003;Waters et al, 2013), liposome electrokinetic chromatography (Wang et al, 2009), and keratin immobilized on the silica as a stationary phase (Turowski and Kaliszan, 1997). However, in respect to the optimization of the formulation destined for the administration onto the skin, the effects of various additives and carriers/vehicles on the drug penetration, these chromatographic systems exhibit a very limited potential and are therefore not further discussed in this review.…”

Section: Artificial In Vitro Skin Modelsmentioning

confidence: 99%

In vitro skin models as a tool in optimization of drug formulation

Flaten

Palac²,

Engesland

et al. 2015

European Journal of Pharmaceutical Sciences

178

135

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Abstract(Trans)dermal drug therapy is gaining increasing importance in the modern drug development. To fully utilize the potential of this route, it is important to optimize the delivery of active ingredient/drug into/through the skin. The optimal carrier/vehicle can enhance the desired outcome of the therapy therefore the optimization of skin formulations is often included in the early stages of the product development. A rational approach in designing and optimizing skin formulations requires well-defined skin models, able to identify and evaluate the intrinsic properties of the formulation. Most of the current optimization relies on the use of suitable ex vivo animal/human models.However, increasing restrictions in use and handling of animals and human skin stimulated the search for suitable artificial skin models. This review attempts to provide an unbiased overview of the most commonly used models, with emphasis on their limitations and advantages. The choice of the most applicable in vitro model for the particular purpose should be based on the interplay between the availability, easiness of the use, cost and the respective limitations.

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Section: Artificial In Vitro Skin Modelsmentioning

confidence: 99%

In vitro skin models as a tool in optimization of drug formulation

Flaten

Palac²,

Engesland

et al. 2015

European Journal of Pharmaceutical Sciences

178

135

View full text Add to dashboard Cite

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“…La Rotunda et al [27] reported that they could not find any correlation between k' and Kp values for the 12 drugs, although for 10 of the drugs they did find a correlation between log Kp and a parameter…”

Section: Rp-hplc and Mekc Datamentioning

confidence: 93%

“…Values of log PS were reasonably well correlated [44] as shown in Eq. ( 27), although there are too few data points to come to any very definite conclusions.…”

Section: Rp-hplc Datamentioning

confidence: 99%

“…More recently, La Rotonda et al [27] measured log k' values for 12 structurally varied drugs on an IAM column at with different acetonitrile / water mobile phases and extrapolated to 100 % water to obtain log k w values. La Rotunda et al [27] reported that they could not find any correlation between k' and Kp values for the 12 drugs, although for 10 of the drugs they did find a correlation between log Kp and a parameter…”

Section: Rp-hplc and Mekc Datamentioning

confidence: 99%

“…log PS = -1.21 + 0.77 R 2 -1.87 π 2 H -2.80 Σβ 2 H + 3.31 V x (27) It can be said, however, that the factors that influence rates of permeation from saline are quantitatively not the same as those that influence blood-brain distribution.…”

Section: Rp-hplc Datamentioning

confidence: 99%

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Connection between chromatographic data and biological data

Abraham

Gola

Kumarsingh

et al. 2000

Journal of Chromatography B: Biomedical Sciences and Applicatio

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There are no previous references to the direct use of GLC data in the correlation of biological processes, but we show that GLC retention data can be used in the correlation of several such processes involving gaseous solutes. There are a number of reports of RP-HPLC and MEKC data being used in the correlation of biological processes, but they are mostly restricted as to the number and type of solute studied.We show that if chromatographic data are used to obtain solvation descriptors for solutes, and if these descriptors are then used in the correlation of biological processes, that this indirect connection is a much more powerful and generally applicable method than is the direct connection between chromatographic data and biological data.

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Quantitative Retention‐Activity Relationship Studies by Liposome Electrokinetic Chromatography to Predict Skin Permeability

et al. 2008

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Liposome electrokinetic chromatography (LEKC) provides a simple and facile approach for drug membrane interactions using liposome as a pseudostationary phase. This study evaluated the potential of LEKC for high-throughput skin permeability profiled as an in vitro technique. A quantitative retention-activity relationship (QRAR) model for the estimation of skin permeability was proposed. For the 16 structurally diverse chemicals, lg k correlated well with permeability values (R 2 ＝0.886). The predictive ability of the model was evaluated by cross-validation. The result was compared to traditional quantitative structure-activity relationship, QSAR, models using some molecular descriptors and physicochemical parameters. Interestingly, a single LEKC retention parameter was capable of describing the skin permeability, while three variables in QSAR were needed to achieve a similar correlation (R 2 ＝0.704). The QRAR models developed in this paper may be a useful method to screening new chemicals and in the early stage of development and selection of chemicals.

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Chromatographic indexes on immobilized artificial membranes for the prediction of transdermal transport of drugs

Cited by 46 publications

References 17 publications

In vitro skin models as a tool in optimization of drug formulation

In vitro skin models as a tool in optimization of drug formulation

Connection between chromatographic data and biological data

Quantitative Retention‐Activity Relationship Studies by Liposome Electrokinetic Chromatography to Predict Skin Permeability

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