File(s) under permanent embargo
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 TimminsPolyvinylpyrrolidone 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 PharmaceuticsISSN
1543-8384Publisher
American Chemical SocietyPublisher URL
Issue
8Volume
9Page range
2237-2247Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes