Cyclodextrins in delivery systems: Applications

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Abstract

Cyclodextrins (CDs) are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. CD molecules are relatively large with a number of hydrogen donors and acceptors and, thus in general, they do not permeate lipophilic membranes. In the pharmaceutical industry, CDs have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs and to increase their bioavailability and stability. CDs are used in pharmaceutical applications for numerous purposes, including improving the bioavailability of drugs. Current CD-based therapeutics is described and possible future applications are discussed. CD-containing polymers are reviewed and their use in drug delivery is presented. Of specific interest is the use of CD-containing polymers to provide unique capabilities for the delivery of nucleic acids. Studies in both humans and animals have shown that CDs can be used to improve drug delivery from almost any type of drug formulation. Currently, there are approximately 30 different pharmaceutical products worldwide containing drug/CD complexes in the market.

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Most cited references 76

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Industrial Applications of Cyclodextrins.

Allan R. Hedges (1998)

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Cyclodextrin-based controlled drug release system.

F Hirayama (1999)

Because of their bioadaptability and multi-functional characteristics, cyclodextrins (CDs) are capable of alleviating the undesirable properties of drug molecules in various routes of administration through the formation of inclusion complexes. This article outlines the current application of natural and chemically modified CDs in the design of advanced dosage forms. In an oral drug delivery system (DDS), the hydrophilic and ionizable CDs can serve as potent drug carriers in the immediate release- and delayed release-formulations, respectively, while the release rate of water-soluble drugs can be retarded by hydrophobic CDs. Since CDs are able to extend the function of pharmaceutical additives, the combination of molecular encapsulation with other carrier materials will become effective and a valuable tool in the improvement of drug formulation. Moreover, the most desirable attribute for the drug carrier is its ability to deliver a drug to a targeted site; conjugates of a drug with CDs can be a versatile means of constructing a new class of colon-targeting prodrugs. On the basis of this knowledge, the advantages and limitations of CDs in DDS are addressed.

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Mechanisms by which cyclodextrins modify drug release from polymeric drug delivery systems.

D. Bibby, N M Davies, I G Tucker (2000)

For many drug candidates a modified in vivo drug release is desired to improve efficacy, sustain effect or minimise toxicity. Polymeric delivery systems, such as microspheres, nanospheres and polymeric films, have been extensively researched in an attempt to achieve modified drug release. Cyclodextrins offer an alternative approach. These cyclic oligosaccharides have the ability to form non-covalent complexes with a number of drugs and in so doing alter their physicochemical properties. In addition, the primary and secondary hydroxyl groups of the native (alpha, beta, gamma-) cyclodextrins are potential sites for chemical modification. It follows that the incorporation of these agents into polymeric drug delivery systems, as physical mixtures, covalently bound conjugates or cross-linking agents, frequently permits a greater degree of control of drug release. This paper reviews the incorporation of various cyclodextrins into polymeric formulations. The mechanisms by which cyclodextrin/polymer formulations act to modify drug release are considered.

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Author and article information

Journal

Journal ID (nlm-ta): J Pharm Bioallied Sci

Journal ID (publisher-id): JPBS

Title: Journal of Pharmacy and Bioallied Sciences

Publisher: Medknow Publications Pvt Ltd (India )

ISSN (Print): 0976-4879

ISSN (Electronic): 0975-7406

Publication date (Print): Apr-Jun 2010

Volume: 2

Issue: 2

Pages: 72-79

Affiliations

[1]Jaipur National University, Jagatpura, Jaipur, Rajasthan, India

[1 ]Department of pharmaceutics, Pranveer Singh Institute of Technology, Kalpi Road, Bhauti, Kanpur 208020, Uttar Pradesh, India

Author notes

Address for correspondence: Mr. Gaurav Tiwari, E-mail: tiwari_mpharm@ 123456rediffmail.com

Article

Publisher ID: JPBS-2-72

DOI: 10.4103/0975-7406.67003

PMC ID: 3147107

PubMed ID: 21814436

SO-VID: 43340caa-a2a8-407a-b164-4857bf1d77e6

License:

This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

History

Date received : 20 March 2010

Date revision received : 26 March 2010

Date accepted : 13 April 2010

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