71
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_6,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 6
Drug Delivery: Hydrophobic Drug Encapsulation into
Amphiphilic Block Copolymer Micelles
Angeliki Chroni, Varvara Chrysostomou, Athanasios Skandalis,
and Stergios Pispas
Abstract
Drug encapsulation into amphiphilic block copolymer micelles aims to increase drug solubility and minimize drug degradation upon administration, avoid undesirable side effects and ameliorate drug bioavailability. Drug encapsulation methodologies including thin-film hydration method and organic cosolvent
method are described in this chapter. Often, it is desirable to determine the most efficient solubilization
protocol leading to functional drug delivery nanovehicles in each case. The encapsulation of curcumin into
PEO-b-PPO-b-PEO (Pluronic F-127) polymeric micelles through thin-film hydration method presents
the most promising results. Indomethacin can be loaded successfully into the hydrophobic cores of PEOb- PCL amphiphilic block copolymer micelles following both encapsulation protocols.
Key words Drug delivery, Block copolymers, Curcumin, Indomethacin, Encapsulation processes,
Thin-film hydration, Organic solvent evaporation
1 Introduction
Polymer therapeutics paved the road for further innovations in the
field of drug delivery systems, by providing chemical stability,
improved drug solubilization, and controlled release of the drug
[1]. Hydrophobic drugs can be physically entrapped in the core of
biodegradable, biocompatible, amphiphilic block copolymer
micelles through encapsulation processes that exploit the selfassembly properties and solubilization of block copolymers in formulating efficient therapeutic delivery systems [2, 3]. Poly(ethylene
oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO-bPPO-b-PEO) block copolymer micelles have proved to be effective
nanocarriers for hydrophobic drugs, as they enhance the transport
of drugs across the blood-brain and intestinal barriers [4–7].
Various studies have verified the effective use of poly(ethylene
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_6,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 6
Drug Delivery: Hydrophobic Drug Encapsulation into
Amphiphilic Block Copolymer Micelles
Angeliki Chroni, Varvara Chrysostomou, Athanasios Skandalis,
and Stergios Pispas
Abstract
Drug encapsulation into amphiphilic block copolymer micelles aims to increase drug solubility and minimize drug degradation upon administration, avoid undesirable side effects and ameliorate drug bioavailability. Drug encapsulation methodologies including thin-film hydration method and organic cosolvent
method are described in this chapter. Often, it is desirable to determine the most efficient solubilization
protocol leading to functional drug delivery nanovehicles in each case. The encapsulation of curcumin into
PEO-b-PPO-b-PEO (Pluronic F-127) polymeric micelles through thin-film hydration method presents
the most promising results. Indomethacin can be loaded successfully into the hydrophobic cores of PEOb- PCL amphiphilic block copolymer micelles following both encapsulation protocols.
Key words Drug delivery, Block copolymers, Curcumin, Indomethacin, Encapsulation processes,
Thin-film hydration, Organic solvent evaporation
1 Introduction
Polymer therapeutics paved the road for further innovations in the
field of drug delivery systems, by providing chemical stability,
improved drug solubilization, and controlled release of the drug
[1]. Hydrophobic drugs can be physically entrapped in the core of
biodegradable, biocompatible, amphiphilic block copolymer
micelles through encapsulation processes that exploit the selfassembly properties and solubilization of block copolymers in formulating efficient therapeutic delivery systems [2, 3]. Poly(ethylene
oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO-bPPO-b-PEO) block copolymer micelles have proved to be effective
nanocarriers for hydrophobic drugs, as they enhance the transport
of drugs across the blood-brain and intestinal barriers [4–7].
Various studies have verified the effective use of poly(ethylene