Abstract
Amorphous nanosuspensions (ANSs) enable rapid release and improved delivery of a poorly water-soluble drug; however, their preparation is challenging. Here, using hemoglobin (Hb) as a carrier, ANSs aggregated from paclitaxel (PTX)–Hb complexes were prepared to improve delivery of the hydrophobic anti-cancer agent. An affinity study demonstrated strong interaction between Hb and PTX. Importantly, the complexes could aggregate into <300 nm ANSs with high drug loading, which acidic condition facilitated their formation. Furthermore, the ANSs possessed improved cytotoxicity against cancer cells over the crystalline nanosuspensions. Taken together, ANSs aggregated from PTX–Hb complexes were developed, which could kill cancer cells with high efficiency.
Highlights
Over 40% of the marked products and approximately 90% of new drug candidates are poorly water-soluble compounds based on the biopharmaceutical classification system (BCS) [1]
In previous reports [12,13], using denatured soy protein isolate as a stabilizer, a nanosuspension formulation combining crystalline and amorphous drug was developed using a technique whereby the drug-protein complexes coated the nanocrystals of the insoluble drug
These results indicate that amorphous nanosuspensions (ANSs) possess improved cytotoxicity over LG-coated PTX nanocrystals (LPNs)
Summary
Over 40% of the marked products and approximately 90% of new drug candidates are poorly water-soluble compounds based on the biopharmaceutical classification system (BCS) [1]. In previous reports [12,13], using denatured soy protein isolate as a stabilizer, a nanosuspension formulation combining crystalline and amorphous drug was developed using a technique whereby the drug-protein complexes coated the nanocrystals of the insoluble drug. Inspired by these findings, we hypothesized that ANSs could be prepared via the aggregation of drug-protein complexes and were able to kill cancer cells with higher efficiency for rapid intracellular release post internalization. With the ability to bind with hydrophobic agent and high biocompatibility, Hb was used as the carrier to prepare drug–Hb complexes and ANSs with improved delivery of PTX
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