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Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)

Reading School of Pharmacy, University of Reading, Whiteknights, P.O. Box 224, Reading RG6 6AD, UK
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Academic Editor: Wouter L. J. Hinrichs
Pharmaceutics 2021, 13(5), 659; https://doi.org/10.3390/pharmaceutics13050659
Received: 14 March 2021 / Revised: 22 April 2021 / Accepted: 28 April 2021 / Published: 4 May 2021
Poly(N-vinyl pyrrolidone) (PVP), poly(2-methyl-2-oxazoline) (PMOZ), poly(2-ethyl-2-oxazoline) (PEOZ), poly(2-n-propyl-2-oxazoline) (PnPOZ), and poly(2-isopropyl-2-oxazoline) (PiPOZ) were used to prepare solid dispersions with ibuprofen (IB), a model poorly-water soluble drug. Dispersions, prepared by solvent evaporation, were investigated using powder X-ray diffractometry, differential scanning calorimetry, and FTIR spectroscopy; hydrogen bonds formed between IB and all polymers in solid dispersions. PMOZ, the most hydrophilic polymer, showed the poorest ability to reduce or inhibit the crystallinity of IB. In contrast, the more hydrophobic polymers PVP, PEOZ, PnPOZ, and PiPOZ provided greater but similar abilities to reduce IB crystallinity, despite the differing polymer hydrophobicity and that PiPOZ is semi-crystalline. These results indicate that crystallinity disruption is predominantly due to hydrogen bonding between the drug molecules and the polymer. However, carrier properties affected drug dissolution, where PnPOZ exhibited lower critical solution temperature that inhibited the release of IB, whereas drug release from other systems was consistent with the degree of ibuprofen crystallinity within the dispersions. View Full-Text
Keywords: solid dispersions; hydrogen bonding; hydrophobicity; poly(N-vinyl pyrrolidone); poly(2-oxazolines); crystallinity; hydrophobic drug; amorphous; ibuprofen solid dispersions; hydrogen bonding; hydrophobicity; poly(N-vinyl pyrrolidone); poly(2-oxazolines); crystallinity; hydrophobic drug; amorphous; ibuprofen
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MDPI and ACS Style

Shan, X.; Moghul, M.A.; Williams, A.C.; Khutoryanskiy, V.V. Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines). Pharmaceutics 2021, 13, 659. https://doi.org/10.3390/pharmaceutics13050659

AMA Style

Shan X, Moghul MA, Williams AC, Khutoryanskiy VV. Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines). Pharmaceutics. 2021; 13(5):659. https://doi.org/10.3390/pharmaceutics13050659

Chicago/Turabian Style

Shan, Xiaoning; Moghul, Maryam A.; Williams, Adrian C.; Khutoryanskiy, Vitaliy V. 2021. "Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)" Pharmaceutics 13, no. 5: 659. https://doi.org/10.3390/pharmaceutics13050659

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