Route-Specific Challenges in the Delivery of Poorly Water-Soluble Drugs

Poor aqueous solubility of new chemical entities presents various challenges in the development of effective drug delivery systems for various delivery routes. Poorly soluble drugs that are delivered orally may commonly result in low bioavailability and are often subject to considerable food effects. In addition, poorly soluble drugs intended for parenteral delivery may also have to be solubilized with large amounts of cosolvents and surfactants, oftentimes resulting in adverse physiological reactions.

Other routes also offer unique opportunities for this class of drug molecules but also their own challenges. Ocular delivery of poorly soluble drugs is challenging due to the efficient absorption barriers and clearance mechanisms. Development of poorly soluble drugs administered mucosally through routes such as the nasal cavity, oral mucosa, and others may be restricted by the relatively small administered volume, the geometry of the administration site, and the excipients commonly used in these formulations.

Successful formulation design of poorly soluble drugs’ intended alternative routes of administration may be hindered by the limited number of excipients generally recognized as safe for this route of delivery and the anatomical and physiological clearance mechanisms found in these tissues. In summary, this chapter reviews the specific challenges faced in the delivery of poorly water-soluble drugs via oral, parenteral, and mucosal administration.

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This is a chapter of the bookFormulating Poorly Water Soluble Drugs“.

Book: Formulating Poorly Water Soluble Drugs

Warnken, Z., Smyth, H.D.C., Williams, R.O. (2022). Route-Specific Challenges in the Delivery of Poorly Water-Soluble Drugs. In: Williams III, R.O., Davis Jr., D.A., Miller, D.A. (eds) Formulating Poorly Water Soluble Drugs. AAPS Advances in the Pharmaceutical Sciences Series, vol 50. Springer, Cham.

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