ABSTRACT

The technical development and subsequent advancement of clinical

studies and ultimately commercial applications of various types of

nanoparticle drug formulations have accelerated over the last couple

of decades. These nanoparticle formulations have been pursued

as enabling technologies to achieve various modes of enhanced

drug delivery of therapeutic and diagnostic agents, including the

improved oral delivery of poorly water-soluble drugs in terms of

increased bioavailability, onset of action, and reduction of food

effects,1−3 improved targeted delivery of therapeutic agents,2−5 the reduction of toxicity, and enhancement in the efficacy of certain

agents2,3 and general improvements in dosing convenience and

compliance.1,2 In the field of drug delivery, the term nanoparticles encompasses a broad assortment of different types of nano-sized

particle structural motifs. Broadly speaking, the most common

nanoparticle structures used in oral drug delivery can be grouped

into two different categories: (i) pure drug nanoparticles consisting

of essentially 100% drug (with or without the addition of surface

stabilizers) in either a crystalline (nanocrystals)1,3 or noncrystalline

state6,7 and (ii) an assortment of different nano-sized structures in

which the drug is encapsulated or dispersed in a solid, semisolid, or

liquid state within a formulation matrix. In this latter category are

included polymeric nanoparticles,8 nanoemulsions,9 liposomes,10

and solid lipid nanoparticles,11 among others. Additional types of

nanostructured drug particles include dendrimers, quantum dots,

and various types of metal-based colloidal nanoparticles to which

a drug may be anchored via covalent or noncovalent mechanisms12

and which are outside the scope of this review.