Preparation and Characterization of Poly(2-oxazoline) Micelles for the Solubilization and Delivery of Water Insoluble Drugs

Natasha Vinod; Duhyeong Hwang; Salma H Azam; Amanda E D Van Swearingen; Elizabeth Wayne; Sloane Christian Fussell; Marina Sokolsky-Papkov; Chad V Pecot; Alexander V Kabanov

doi:10.21769/BioProtoc.3959

Preparation and Characterization of Poly(2-oxazoline) Micelles for the Solubilization and Delivery of Water Insoluble Drugs

Bio Protoc. 2021 Mar 20;11(6):e3959. doi: 10.21769/BioProtoc.3959.

Authors

Affiliations

¹ Center for Nanotechnology in Drug Delivery and Division of Pharmacoengineering and Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, NC, USA.
² Joint UNC/NC State Department of Biomedical Engineering, University of North Carolina, Chapel Hill, NC, USA.
³ Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
⁴ Department of Biology, Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
⁵ Division of Hematology & Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
⁶ Department of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
⁷ Laboratory of Chemical Design of Bionanomaterials, Faculty of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russia.

Abstract

Many new drug development candidates are highly lipophilic compounds with low water solubility. This constitutes a formidable challenge for the use of such compounds for cancer therapy, where high doses and intravenous injections are needed ( Di et al., 2012 ). Here, we present a poly(2-oxazoline) polymer (POx)-based nanoformulation strategy to solubilize and deliver hydrophobic drugs. POx micelles are prepared by a simple thin-film hydration method. In this method, the drug and polymer are dissolved in a common solvent and allowed to mix, following which the solvent is evaporated using mild heating conditions to form a thin film. The micelles form spontaneously upon hydration with saline. POx nanoformulation of hydrophobic drugs is unique in that it has a high drug loading capacity, which is superior to micelles of conventional surfactants. Moreover, multiple active pharmaceutical ingredients (APIs) can be included within the same POx micelle, thereby enabling the codelivery of binary as well as ternary drug combinations ( Han et al., 2012 ; He et al., 2016 ).

Keywords: Active pharmaceutical ingredients; Lipophilic; Nanoformulation; Poly(2-oxazoline); Polymeric micelles; Surfactants.

Abstract

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