Paclitaxel is one of most significant anticancer agents, whose clinical usefulness is limited by its unfavorable pharmacokinetic and physical properties. Different approaches have been attempted in the effort to develop alternative formulations, reducing its side effects and increasing aqueous solubility, selectivity and potency. A macromolecular drug-delivery system is a complex system in which the drug is attached to a carrier molecule. An ideal drug carrier must be biochemically inert and non-toxic; while protecting the drug until it reaches the desired site of action, and then it must then release it. Proteins such as albumin and antibodies, carbohydrate polymers such as hyaluronic acid or chitosan, synthetic polymers such as polyethylene glycols or N-(2-hydroxypropyl) methacrylamide, polyaminoacids and dendrimers have all been used to obtain soluble macromolecular prodrugs or nanomolecular medicines. Macromolecules are widely employed to carry paclitaxel or other taxanes, and remarkable progress has been made and notable results are now available. This chapter describes, evaluates and compares these approaches, and focuses on the more recent advanced and promising systems as well as on future developments. Particular emphasis is placed on macromolecular paclitaxel drug delivery systems that have entered clinical trials.
Macromolecules as Paclitaxel Carriers: From Chemical Considerations to Clinical Applications
DOSIO, Franco;GASTALDI, Daniela
2011-01-01
Abstract
Paclitaxel is one of most significant anticancer agents, whose clinical usefulness is limited by its unfavorable pharmacokinetic and physical properties. Different approaches have been attempted in the effort to develop alternative formulations, reducing its side effects and increasing aqueous solubility, selectivity and potency. A macromolecular drug-delivery system is a complex system in which the drug is attached to a carrier molecule. An ideal drug carrier must be biochemically inert and non-toxic; while protecting the drug until it reaches the desired site of action, and then it must then release it. Proteins such as albumin and antibodies, carbohydrate polymers such as hyaluronic acid or chitosan, synthetic polymers such as polyethylene glycols or N-(2-hydroxypropyl) methacrylamide, polyaminoacids and dendrimers have all been used to obtain soluble macromolecular prodrugs or nanomolecular medicines. Macromolecules are widely employed to carry paclitaxel or other taxanes, and remarkable progress has been made and notable results are now available. This chapter describes, evaluates and compares these approaches, and focuses on the more recent advanced and promising systems as well as on future developments. Particular emphasis is placed on macromolecular paclitaxel drug delivery systems that have entered clinical trials.
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