Formulations containing natural and/or synthetic lipids can be confidently considered as a viable means for potentially enhancing the oral bioavailability and systemic exposure of poorly water soluble, highly lipophilic drug candidates. However, the flexibility of formulation design and the range of excipient choice for lipid-based systems decreases as compounds progress from discovery into clinical development. When evaluating formulation strategies, it is essential that the factors limiting drug exposure are initially identified in order to guide a rational formulation design program. As the co-administration of highly lipophilic drugs with lipids can influence their possible transport via the intestinal lymphatics, it is also prudent to consider whether lymphatic transport may contribute to oral bioavailability of highly lipophilic, poorly water soluble drugs.

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