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Biomolecules
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Transport Properties for Pharmaceutical Controlled-Release Systems
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Transport Properties for Pharmaceutical Controlled-Release Systems

A special issue of Biomolecules (ISSN 2218-273X).

Deadline for manuscript submissions: closed (1 October 2018) | Viewed by 24201

Special Issue Editors

Dr. Ana Cristina Faria Ribeiro

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Guest Editor
Department of Chemistry, University of Coimbra, 3004 - 535 Coimbra, Portugal
Interests: transport properties; thermodynamic properties; electrolytes; polyelectrolytes; polymers; carbohydrates; drugs
Special Issues, Collections and Topics in MDPI journals
Emeritus Prof. Miguel Angel Esteso

E-Mail Website
Guest Editor
1. Catholic University of Santa Teresa de Jesús de Ávila, 05005 Ávila, Spain
2. Department of Analytical Chemistry, Physical Chemistry and Chemical Engineering, University of Alcalá, 28805 Alcalá de Henares (Madrid), Spain
Interests: physical chemistry; (in)organic chemicals; drugs; wastewater treatment; food chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The development of controlled-release systems for the reliable and safe delivery of precise dosages of drugs continues to be an active area of research. For example, important results have been obtained by manipulating the rates of diffusion of carrier-drug complexes and thermodynamic binding constants. Despite considerable work, the transport behaviour of these systems is still poorly understood. Because this information is essential for the design of those systems, we propose this Special Issue describing comprehensive studies of the transport properties of drugs and carriers, with special emphasis on measuring in multicomponent chemical interdiffusion coefficients for solutions of drugs (e.g., ethambutol, l-dopa, xantines), and various carriers, including cyclodextrins and resorcinarenes. From such data, is it possible to obtain information, at a molecular level, on interactions that can occur and which may conceivably have application in pharmaceutical research.

Dr. Ana Cristina Faria Ribeiro
Prof. Dr. Miguel A. Esteso
Guest Editors

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomolecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • drugs
  • cyclodextrins
  • sulfonated resorcinares
  • transport properties

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Published Papers (4 papers)

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Research

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21 pages, 1078 KiB  
Article
Drug Delivery Systems: Study of Inclusion Complex Formation between Methylxanthines and Cyclodextrins and Their Thermodynamic and Transport Properties
by Cecília I. A. V. Santos, Ana C. F. Ribeiro and Miguel A. Esteso
Biomolecules 2019, 9(5), 196; https://doi.org/10.3390/biom9050196 - 20 May 2019
Cited by 23 | Viewed by 3566
Abstract
This paper presents an analysis of the molecular mechanisms involved in the formation of inclusion complexes together with some structural interpretation of drug–carrier molecule interactions in aqueous multicomponent systems comprising methylxanthines and cyclodextrins. The determination of apparent partial molar volumes ( [...] Read more.
This paper presents an analysis of the molecular mechanisms involved in the formation of inclusion complexes together with some structural interpretation of drug–carrier molecule interactions in aqueous multicomponent systems comprising methylxanthines and cyclodextrins. The determination of apparent partial molar volumes ( φ V ) from experimental density measurements, both for binary and ternary aqueous solutions of cyclodextrins and methylxanthines, was performed at low concentration range to be consistent with their therapeutic uses in the drug-releasing field. The estimation of the equilibrium constant for inclusion complexes of 1:1 stoichiometry was done through the mathematical modelling of this apparent molar property. The examination of the volume changes offered information about the driving forces for the insertion of the xanthine into the cyclodextrin molecule. The analysis on the volumes of transfer, Δ φ V , c , and the viscosity B-coefficients of transfer, ΔB, for the xanthine from water to the different aqueous solutions of cyclodextrin allowed evaluating the possible interactions between aqueous solutes and/or solute–solvent interactions occurring in the solution. Mutual diffusion coefficients for binary, and ternary mixtures composed by xanthine, cyclodextrin, and water were measured with the Taylor dispersion technique. The behavior diffusion of these multicomponent systems and the coupled flows occurring in the solution were analyzed in order to understand the probable interactions between cyclodextrin–xanthine by estimating their association constants and leading to clearer insight of these systems structure. The measurements were performed at the standard (298.15 ± 0.01) K and physiological (310.15 ± 0.01) K temperatures. Full article
(This article belongs to the Special Issue Transport Properties for Pharmaceutical Controlled-Release Systems)
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18 pages, 587 KiB  
Article
Cyclodextrins in Parkinson’s Disease
by Marisa C. F. Barros, Ana C. F. Ribeiro and Miguel A. Esteso
Biomolecules 2019, 9(1), 3; https://doi.org/10.3390/biom9010003 - 21 Dec 2018
Cited by 14 | Viewed by 3691
Abstract
Parkinson’s disease is a movement disorder characterized by a progressive degeneration of dopaminergic neurons that has been object of study by the scientific community through the last decades. However, nowadays there is still no treatment to cure it, although there are drugs available, [...] Read more.
Parkinson’s disease is a movement disorder characterized by a progressive degeneration of dopaminergic neurons that has been object of study by the scientific community through the last decades. However, nowadays there is still no treatment to cure it, although there are drugs available, with limited efficacy, to relieve the symptoms or replenish the cells with dopamine to supply the lack of dopaminergic neurons. This work was structured in two parts. In the first one, binary aqueous solutions of L-dopa and cyclodextrins were studied. In the second part, ternary aqueous solutions of L-dopa were studied with each of the selected cyclodextrins. In all cases, thermodynamic properties (density, partial molar volume and thermodynamic transfer functions for temperatures between 294.15 ± 0.01 K and 312.15 ± 0.01 K) and transport properties (mutual diffusion coefficients, viscosity, transfer viscosity at 298.15 ± 0.01 K and 310.15 ± 0.01 K) were studied. Using theoretical models to adjust the experimental data obtained for the diffusion coefficients and for the apparent molar volumes, in the ternary aqueous solutions, it was possible to estimate the values to the L-dopa-cyclodextrin association constant. For the aqueous ternary solutes, the partial molar volume of transfer of levodopa in the presence of the cyclodextrins, the partial molar expansibility at infinite dilution and from this, the Hepler constant, were determined. Also, the values of Gibbs free energy (ΔG0), enthalpy (ΔH0) and entropy (ΔS0) were determined. From the obtained information, it was possible to characterize the molecular interactions, as well as to identify some structural characteristics of the controlled drug delivery systems under study and to estimate the influence of the cyclodextrin substituent groups, and, also, the temperature effect in the interaction levodopa-cyclodextrin. It is our intent to attain information about the mechanism of possible new systems for controlled drug delivery systems, throughout an alternative perspective, which could allow to increase its effectiveness in the Parkinson’s treatment. Full article
(This article belongs to the Special Issue Transport Properties for Pharmaceutical Controlled-Release Systems)
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Review

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15 pages, 2220 KiB  
Review
Calixarenes: Generalities and Their Role in Improving the Solubility, Biocompatibility, Stability, Bioavailability, Detection, and Transport of Biomolecules
by Edilma Sanabria Español and Mauricio Maldonado Villamil
Biomolecules 2019, 9(3), 90; https://doi.org/10.3390/biom9030090 - 5 Mar 2019
Cited by 132 | Viewed by 12532
Abstract
The properties and characteristics of calix[n]arenes are described, as well as their capacity to form amphiphilic assemblies by means of the design of synthetic macrocycles with a hydrophilic head and a hydrophobic tail. Their interaction with various substances of interest in [...] Read more.
The properties and characteristics of calix[n]arenes are described, as well as their capacity to form amphiphilic assemblies by means of the design of synthetic macrocycles with a hydrophilic head and a hydrophobic tail. Their interaction with various substances of interest in pharmacy, engineering, and medicine is also described. In particular, the role of the calix[n]arenes in the detection of dopamine, the design of vesicles and liposomes employed in the manufacture of systems of controlled release drugs used in the treatment of cancer, and their role in improving the solubility of testosterone and anthelmintic drugs and the biocompatibility of biomaterials useful for the manufacture of synthetic organs is emphasized. The versatility of these macrocycles, able to vary in size, shape, functional groups, and hydrophobicity and to recognize various biomolecules and molecules with biological activity without causing cytotoxicity is highlighted. Full article
(This article belongs to the Special Issue Transport Properties for Pharmaceutical Controlled-Release Systems)
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10 pages, 1283 KiB  
Review
Transport Properties for Pharmaceutical Controlled-Release Systems: A Brief Review of the Importance of Their Study in Biological Systems
by Ana C. F. Ribeiro and Miguel A. Esteso
Biomolecules 2018, 8(4), 178; https://doi.org/10.3390/biom8040178 - 17 Dec 2018
Cited by 9 | Viewed by 3602
Abstract
The goal of this work was to comprehensive study the transport properties of controlled-release systems for the safe and reliable delivery of drugs. Special emphasis has been placed on the measurement of the diffusion of drugs, alone or in combination with carrier molecules [...] Read more.
The goal of this work was to comprehensive study the transport properties of controlled-release systems for the safe and reliable delivery of drugs. Special emphasis has been placed on the measurement of the diffusion of drugs, alone or in combination with carrier molecules for enhanced solubility and facilitated transport. These studies have provided detailed comprehensive information—both kinetic and thermodynamic—for the design and operation of systems for the controlled release and delivery of drugs. Cyclodextrins are among the most important carriers used in these systems. The basis for their popularity is the ability of these materials to solubilize poorly soluble drugs, generally resulting in striking increases in their water solubilities. The techniques used in these investigations include pulse voltammetry, nuclear magnetic resonance (NMR) and Raman spectroscopy, ultrasonic relaxation, and dissolution kinetics. Transport in these systems is a mutual diffusion process involving coupled fluxes of drugs and carrier molecules driven by concentration gradients. Owing to a strong association in these multicomponent systems, it is not uncommon for a diffusing solute to drive substantial coupled fluxes of other solutes, mixed electrolytes, or polymers. Thus, diffusion data, including cross-diffusion coefficients for coupled transport, are essential in order to understand the rates of many processes involving mass transport driven by chemical concentration gradients, as crystal growth and dissolution, solubilization, membrane transport, and diffusion-limited chemical reactions are all relevant to the design of controlled-release systems. While numerous studies have been carried out on these systems, few have considered the transport behavior for controlled-release systems. To remedy this situation, we decided to measure mutual diffusion coefficients for coupled diffusion in a variety of drug–carrier solutions. In summary, the main objective of the present work was to understand the physical chemistry of carrier-mediated transport phenomena in systems of controlled drug release. Full article
(This article belongs to the Special Issue Transport Properties for Pharmaceutical Controlled-Release Systems)
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