Accessibility navigation


Polymer structure and property effects on solid dispersions with haloperidol: poly(N-vinyl pyrrolidone) and poly(2-oxazolines) studies

Shan, X., Williams, A. C. and Khutoryanskiy, V. V. (2020) Polymer structure and property effects on solid dispersions with haloperidol: poly(N-vinyl pyrrolidone) and poly(2-oxazolines) studies. International Journal of Pharmaceutics, 590. 119884. ISSN 0378-5173

[img] Text - Accepted Version
· Restricted to Repository staff only until 18 September 2021.
· Available under License Creative Commons Attribution Non-commercial No Derivatives.

1MB

It is advisable to refer to the publisher's version if you intend to cite from this work. See Guidance on citing.

To link to this item DOI: 10.1016/j.ijpharm.2020.119884

Abstract/Summary

Poly(2-methyl-2-oxazoline) (PMOZ), poly(2-propyl-2-oxazoline) (PnPOZ) and poly(2-isopropyl-2-oxazoline) (PiPOZ) were synthesized by hydrolysis of 50 kDa poly(2-ethyl-2-oxazoline) (PEOZ) and subsequent reaction of the resulting poly(ethylene imine) with acetic, butyric and isobutyric anhydrides, respectively. These polymers were characterized by proton nuclear magnetic resonance, FTIR spectroscopy, powder X-ray diffraction, and differential scanning calorimetry. The poly(2-oxazolines) as well as poly(N-vinyl pyrrolidone) (PVP) were used to prepare solid dispersions with haloperidol, a model poorly soluble drug. Dispersions were investigated by powder X-ray diffractometry, differential scanning calorimetry and FTIR spectroscopy. Increasing the number of hydrophobic groups (-CH2- and -CH3) in the polymer resulted in greater inhibition of crystallinity of haloperidol in the order: PVP > PnPOZ=PEOZ > PMOZ. Interestingly, drug crystallization inhibition by PiPOZ was lower than with its isomeric PnPOZ because of the semi-crystalline nature of the former polymer. Crystallization inhibition was consistent with drug dissolution studies using these solid dispersions, with exception of PnPOZ, which exhibited lower critical solution temperature that affected the release of haloperidol.

Item Type:Article
Refereed:Yes
Divisions:Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) > NMR (CAF)
Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) > Thermal (CAF)
Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) > Xray (CAF)
Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Pharmaceutics Research Group
ID Code:93015
Publisher:Elsevier

University Staff: Request a correction | Centaur Editors: Update this record

Page navigation