FTIR, dissolution and anti-viral activity of nevirapine co-crystals

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dc.contributor.authorSamsodien, Halima
dc.contributor.authorBapoo, Rafik
dc.contributor.authorDoms, T.I.
dc.contributor.authorHarneker, Z.
dc.contributor.authorLouw, A.S.
dc.contributor.authorScheepers, I.C.
dc.contributor.authorSonday, A.B.
dc.contributor.authorGeldenhuys, B.
dc.date.accessioned2017-11-14T13:47:12Z
dc.date.available2017-11-14T13:47:12Z
dc.date.issued2017
dc.description.abstractThe study uses Fourier Transform Infrared (FTIR) spectroscopy to identify five Nevirapine (NV) co-crystals, determines the dissolution profile of the co-crystals and the antiviral activity comparative to pure NV. Hot stage microscopy measured the purity and integrity of each co-crystal. FTIR analysis was used to identify the co-crystals to make recommendations regarding the future use of the technique to identify the NV co-crystals. Dissolution studies of the NV co-crystals prepared with maleic acid, salicylic acid and glutaric acid (NVMLE, NVSLI and NVGLT, respectively) were completed using the rotating basket method. Assays were conducted using High Performance Liquid Chromatography and compared to pure NV and the five NV: co-former mixtures. The antiviral activity was tested to determine whether the co-crystals had an improved activity against HIV-1 compared to pure NV. All co-crystals, except NVTTA (a NV co-crystal prepared with rac-tartaric acid), were pure and maintained their integrity for approximately one year. NVGLT, NVMLE and NVTTA, 1:1 molar ratio co-crystals were identified by FTIR. The C=O stretching frequency of the carboxylic acid groups of NV and GLT were observed at 1638.15 cm-1 and 1719.23 cm-1 in the NVGLT co-crystal which corresponded with spectra of NVMLE and NVTTA. In NVMLE the C=O stretching frequency of the C=O of NV and MLE were observed at 1640.58 cm-1 and 1694.10 cm-1 and in NVTTA it was at 1637.25 cm-1 and 1708.50 cm-1, suggesting the presence of both parent molecules in the new phase for NVGLT, NVMLE and NVTTA. Dissolution studies suggested that NVGLT was the only co-crystal that yielded better results than both NV and its physical mixture. The antiviral activity of the NVSC (an NV co-crystal prepared with saccharin) and NVSLI cocrystals in DMSO was significantly different to pure NV, demonstrating an improvement in anti-viral activity.en_US
dc.identifier.citationSamsodien, H., et al. (2017). FTIR, dissolution and anti-viral activity of nevirapine cocrystals. Pharmaceautica Analytica Acta, 8(9): 561en_US
dc.identifier.issn2153-2435
dc.identifier.urihttp://dx.doi.org/10.4172/2153-2435.1000561
dc.identifier.urihttp://hdl.handle.net/10566/3269
dc.language.isoenen_US
dc.privacy.showsubmitterFALSE
dc.publisherOMICS Internationalen_US
dc.rights© 2017 Samsodien H, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
dc.status.ispeerreviewedTRUE
dc.subjectCo-crystalsen_US
dc.subjectNevirapineen_US
dc.subjectDissolution rateen_US
dc.subjectScale-upen_US
dc.subjectAntiviral activityen_US
dc.subjectFTIRen_US
dc.subjectSolubilityen_US
dc.titleFTIR, dissolution and anti-viral activity of nevirapine co-crystalsen_US
dc.typeArticleen_US

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