Abstract: Methods are provided that for producing aqueous formulations of pharmaceutical agents having low aqueous solubility. The methods also provide a simple means of producing the formulation as a sterile product. The drug is physically entrapped by a spatially stabilized matrix comprising a hydrophilic or hydrophilic-hydrophobic block polymer, without being covalently bound to the polymer. The drug formulation is a nanoparticle or sub-nanoparticle in size. In a preferred embodiment the nanoparticles are anisotropic, being much longer than they are wide.

Abstract: Pharmaceutical formulations are provided that increase the systemic bioavailability of camptotheca derivatives; preferably, the camptothecin derivative is 7-ethyl-10-hydroxyl camptothecin, SN-38. The drug is complexed with a stabilizing agent, but is not covalently bound thereto. Anionic or neutral lipids and/or polymers are used as the stabilizing agent, and secondary stabilizing agents and/or other excipients may be incorporated into the formulation as well. Therapeutic methods are also provided, wherein a formulation of the invention is administered to a patient to treat a condition, disorder, or disease that is responsive to camptothecin derivatives. Generally, administration is oral or parenteral.