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Novel polyvinylpyrrolidones to improve delivery of poorly water- soluble drugs: from design to synthesis and evaluation

journal contribution
posted on 2023-06-26, 07:15 authored by Anna I Niemczyk, Adrian C Williams, Clare F Rawlinson-Malone, Wayne Hayes, Barnaby GreenlandBarnaby Greenland, David Chappell, Olga Khutoryanskaya, Peter Timmins
Polyvinylpyrrolidone is widely used in tablet formulations with the linear form acting as a wetting agent and disintegrant, whereas the cross-linked form is a superdisintegrant. We have previously reported that simply mixing the commercial cross-linked polymer with ibuprofen disrupted drug crystallinity with consequent improvements in drug dissolution behavior. In this study, we have designed and synthesized novel cross-linking agents containing a range of oligoether moieties that have then been polymerized with vinylpyrrolidone to generate a suite of novel excipients with enhanced hydrogen-bonding capabilities. The polymers have a porous surface and swell in the most common solvents and in water, properties that suggest their value as disintegrants. The polymers were evaluated in simple physical mixtures with ibuprofen as a model poorly water-soluble drug. The results show that the novel PVPs induce the drug to become “X-ray amorphous”, which increased dissolution to a greater extent than that seen with commercial cross-linked PVP. The polymers stabilize the amorphous drug with no evidence for recrystallization seen after 20 weeks of storage.

History

Publication status

  • Published

File Version

  • Published version

Journal

Molecular Pharmaceutics

ISSN

1543-8384

Publisher

American Chemical Society

Issue

8

Volume

9

Page range

2237-2247

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2017-10-31

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