title: Tocol emulsions for drug solubilization and parenteral delivery.
abstract: Tocols represent a family of tocopherols, tocotrienols, and their derivatives, and are fundamentally derived from the simplest tocopherol, 6-hydroxy-2-methyl-2-phytylchroman, which is referred to as "tocol". The most common tocol is D-alpha-tocopherol, also known as vitamin E. Tocols can be excellent solvents for water insoluble drugs and are compatible with other cosolvents, oils and surfactants. This review highlights the major developments in the use of tocols in parenteral emulsions for drug delivery, with a focus on drug solubilization, physicochemical properties, and biopharmaceutical applications. Tocol emulsions offer an appealing alternative for the parenteral administration of poorly soluble drugs, including major chemotherapeutics such as paclitaxel. Data will be presented on solubilization of paclitaxel, a key chemotherapeutic agent, and its corresponding formulation development, toxicity, efficacy and pharmacokinetic studies in animal models and humans. The breadth of the utility of tocol-based emulsions will be discussed and examples of specific therapeutic drugs and applications will be provided. As these formulations progress further in the clinic, the therapeutic utility of tocol emulsions is anticipated to expand.
authors.affiliation: Morton Grove Pharmaceuticals, Vernon Hills, IL 60061-1590, USA. dkessler@sonuspharma.com
authors.forename: Panayiotis P
authors.initials: PP
authors.lastname: Constantinides
authors.forename: Alex
authors.initials: A
authors.lastname: Tustian
authors.forename: Dean R
authors.initials: DR
authors.lastname: Kessler
mesh_terms: D000638:Amiodarone / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002986:Clinical Trials as Topic; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry*; D005217:Fat Emulsions, Intravenous / Q000737:chemistry; D006801:Humans; D017239:Paclitaxel / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D024505:Tocopherols / Q000737:chemistry*; D024508:Tocotrienols / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D005217:Fat Emulsions, Intravenous; D024508:Tocotrienols; D000638:Amiodarone; D017239:Paclitaxel; D024505:Tocopherols