Formation of stable nanocarriers by in situ ion pairing during block-copolymer-directed rapid precipitation.

ABSTRACT: We present an in situ hydrophobic salt forming technique for the encapsulation of weakly hydrophobic, ionizable active pharmaceutical ingredients (API) into stable nanocarriers (NCs) formed via a rapid precipitation process. Traditionally, NC formation via rapid precipitation has been difficult with APIs in this class because their intermediate solubility makes achieving high supersaturation difficult during the precipitation process and the intermediate solubility causes rapid Ostwald ripening or recrystallization after precipitation. By forming a hydrophobic salt in situ, the API solubility and crystallinity can be tuned to allow for NC formation. Unlike covalent API modification, the hydrophobic salt formation modifies properties via ionic interactions, thus circumventing the need for f

SUBMITTER: Pinkerton NM 

PROVIDER: S-EPMC3677719 | biostudies-literature | 2013 Jan

REPOSITORIES: biostudies-literature