Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization
TL;DR: The effects of substitution on various cyclodextrins properties and the forces involved in the drug-cyclodextrin complex formation are discussed, and methods which are useful in the optimization of complexation efficacy are reviewed.
About: This article is published in Journal of Pharmaceutical Sciences.The article was published on 1996-10-01. It has received 2124 citations till now. The article focuses on the topics: Cyclodextrin & Inclusion compound.
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TL;DR: Cyclodextrins are a family of cyclic oligosaccharides composed of α-(1,4) linked glucopyranose subunits.
2,917 citations
Cites background or methods from "Pharmaceutical Applications of Cycl..."
...Several techniques are used to form cyclodextrin complexes[32,45]....
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...These forces include van der Waals interactions, hydrogen bonding, hydrophobic interactions, release of ring strain in the cyclodextrin molecule and changes in solvent-surface tensions [45]....
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TL;DR: The historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions, as well as the production, the different carriers and the methods used for the characterization of solid dispersion are outlined.
2,695 citations
2,057 citations
TL;DR: This review is intended to give a general background to the use of cyclodextrin as solubilizers as well as highlight kinetic and thermodynamic tools and parameters useful in the study of drug Solubilization bycyclodextrins.
1,674 citations
TL;DR: Of specific interest is the use of cyclodextrin-containing polymers to provide unique capabilities for the delivery of nucleic acids.
Abstract: Cyclodextrins are cyclic oligomers of glucose that can form water-soluble inclusion complexes with small molecules and portions of large compounds. These biocompatible, cyclic oligosaccharides do not elicit immune responses and have low toxicities in animals and humans. Cyclodextrins are used in pharmaceutical applications for numerous purposes, including improving the bioavailability of drugs. Current cyclodextrin-based therapeutics are described and possible future applications discussed. Cyclodextrin-containing polymers are reviewed and their use in drug delivery presented. Of specific interest is the use of cyclodextrin-containing polymers to provide unique capabilities for the delivery of nucleic acids.
1,650 citations
Cites background from "Pharmaceutical Applications of Cycl..."
..., and are specific to the circumstance — that is, the specific physicochemical issues that have to be overcome and the administration rout...
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References
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TL;DR: On the basis of the assumed theory the rate of the observed reaction is directly proportional to the concentration of the enzyme-substrate compound, where (E:l = (ES).
Abstract: On the basis of the assumed theory the rate of the observed reaction is directly proportional to the concentration of the enzyme-substrate compound, (ES), a t all values of the concentration of the substrate, (S). It is proportional to (S) only a t low values of (S). The numerical value of the dissociation constant is given by the substrate concentration a t half-maximum velocity, where (E:l = (ES). The equilibrium in equation 1 may be heterogeneous or homogeneous. Hitchcock'\" has pointed
11,349 citations
Book•
01 Jan 1994
TL;DR: The Handbook of Pharmaceutical Excipients is internationally recognised as the authoritative source of information on pharmaceutical excipients giving a comprehensive guide to uses, properties and safety.
Abstract: Since 1986, the "Handbook of Pharmaceutical Excipients" has been the essential reference for those involved in the development, production, control, or regulation of pharmaceutical preparations. Published jointly by the American Pharmacists Association and the Pharmaceutical Press, a division of the Royal Pharmaceutical Society of Great Britain, London, UK, this new edition is a comprehensive guide to the uses, properties, and safety of pharmaceutical excipients.
7,329 citations
TL;DR: As cyclodextrins catalyze several chemical reactions they and their functionalized derivatives provide useful enzyme models and can be used to advantage in the production of pharmaceuticals, pesticides, foodstuffs, and toilet articles.
Abstract: α-, β-, and γ-Cyclodextrins are cyclic oligosaccharides consisting of six, seven, or eight glucose units, which can be obtained on a large scale from starch. They form inclusion compounds with smaller molecules which fit into their 5—8 A cavity. These (crystalline) complexes are of interest for scientific research as, contrary to the classical clathrates, they exist in aqueous solution and can be used to study the hydrophobic interactions which are so important in biological systems. Cyclodextrins also serve as models both for polymeric starch and, in the form of their polyiodide complexes, for “blue iodine-starch”. As cyclodextrins catalyze several chemical reactions they and their functionalized derivatives provide useful enzyme models. Cyclodextrins can be used to advantage in the production of pharmaceuticals, pesticides, foodstuffs, and toilet articles—the (micro-encapsulated) active and aromatic substances enclosed within them are protected from the effects of light and atmosphere and can be easily handled and stored in powder from. Substances which are not very soluble in water become more soluble in the presence of cyclodextrins—creams and emulsions can be stabilized, and the growth and yield of grain harvests can be increased. Cyclodextrins can be chemically modified for many different purposes; polymerized cyclodextrin or cyclodextrin bound to a polymer carrier have already been employed in gel inclusion and affinity chromatography.
1,817 citations
TL;DR: Current methodology to stabilize proteins is presented, including additives, excipients, chemical modification, and the use of site-directed mutagenesis to produce a more stable protein species.
Abstract: Recombinant DNA technology has now made it possible to produce proteins for pharmaceutical applications Consequently, proteins produced via biotechnology now comprise a significant portion of the drugs currently under development Isolation, purification, formulation, and delivery of proteins represent significant challenges to pharmaceutical scientists, as proteins possess unique chemical and physical properties These properties pose difficult stability problems A summary of both chemical and physical decomposition pathways for proteins is given Chemical instability can include proteolysis, deamidation, oxidation, racemization, and β-elimination Physical instability refers to processes such as aggregation, precipitation, denaturation, and adsorption to surfaces Current methodology to stabilize proteins is presented, including additives, excipients, chemical modification, and the use of site-directed mutagenesis to produce a more stable protein species
1,247 citations
Book•
30 Nov 1993
TL;DR: The present study focused on the development and application of Cyclodextrin Inclusion Compounds in Various Drug Formulations, as well as their applications in Pharmaceutical Applications and Legal Aspects.
Abstract: Preface. Introduction: Historical Developments Cyclodextrins and their Effects on Drugs. 1. Cyclodextrins. 2. CD Derivatives. 3. Interaction between CDs and Biological Systems. 4. Interaction between Drugs and CDs in Aqueous Systems. 5. Interaction between Drugs and CDs in Solid State. 6. Preparations of Cyclodextrin Inclusion Compounds. 7. CDs in Various Drug Formulations. 8. Stabilization of Drugs. 9. Pharmacokinetical and Biopharmaceutical Consequences of Complexation. 10. Various Pharmaceutical Applications. 11. Pharmaceutical-Technological Aspects of CDs in the Drug Formulation. 12. CD-Complexed Drugs. 13. Legal Aspects. References. Index.
533 citations