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. 2019 Aug 8;11(8):398.
doi: 10.3390/pharmaceutics11080398.

In Vitro and Ex Vivo Evaluation of Tablets Containing Piroxicam-Cyclodextrin Complexes for Buccal Delivery

Affiliations

In Vitro and Ex Vivo Evaluation of Tablets Containing Piroxicam-Cyclodextrin Complexes for Buccal Delivery

Eleni Kontogiannidou et al. Pharmaceutics. .

Abstract

In the current study, the development of mucoadhesive tablets for buccal delivery of a non-steroidal anti-inflammatory drug was investigated. Binary complexes with piroxicam and cyclodextrins (β-cyclodextrin (β-CD), methylated-β-cyclodextrin (Me-β-CD), and hydroxypropyl-β-cyclodextrin (HP-β-CD)) were prepared by the co-evaporation method. All formulations were characterized by means of differential scanning calorimetry, infrared spectroscopy and powder X-ray diffractometry. Mucoadhesive tablets of binary systems were formulated by direct compression using chitosan as mucoadhesive polymer. The in vitro release profiles of tablets were conducted in simulated saliva and, the drug permeation studies, across porcine buccal mucosa. The results suggest that the rank order effect of cyclodextrins for the drug release was Me-β-CD > HP-β-CD > β-CD, whereas the ex vivo studies showed that the tablets containing chitosan significantly increased the transport of the drug compared to their free complexes. Finally, histological assessment revealed loss of the superficial cell layers, which might be attributed to the presence of cyclodextrins.

Keywords: cyclodextrins; ex vivo buccal permeation; in vitro studies.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The water uptake capacity of tablets (n = 3).
Figure 2
Figure 2
DSC thermograms of pure compounds and binary systems.
Figure 3
Figure 3
XRD patterns of pure compounds and binary systems.
Figure 4
Figure 4
FTIR spectra of pure components and binary systems.
Figure 5
Figure 5
In vitro release studies of pure piroxicam and binary systems in tablet form (n = 3).
Figure 6
Figure 6
Cumulative transport of piroxicam across buccal mucosa (a) in free complexes and (b) in tablet form.
Figure 7
Figure 7
Light micrographs of (a) porcine buccal mucosa (untreated); (b) free complex with β-CD); (c) free complex with Me-β-CD; and (d) free complex with HP-β-CD. Bar represents 500 μm.
Figure 8
Figure 8
Light micrographs of tablet with (a) chitosan as control (without complexes); (b) β-CD; (c) Me-β-CD; and (d) HP-β-CD. Bar represents 500 μm.

References

    1. Nicolazzo J.A., Reed B.L., Finnin B.C. Buccal penetration enhancers—How do they really work? J. Control. Release. 2005;105:1–15. doi: 10.1016/j.jconrel.2005.01.024. - DOI - PubMed
    1. Marxen E., Jacobsen J., Hyrup B., Janfelt C. Permeability Barriers for Nicotine and Mannitol in Porcine Buccal Mucosa Studied by High-Resolution MALDI Mass Spectrometry Imaging. Mol. Pharm. 2018;15:519–526. doi: 10.1021/acs.molpharmaceut.7b00891. - DOI - PubMed
    1. Kontogiannidou E., Andreadis D.A., Zografos A.L., Nazar H., Klepetsanis P., van der Merwe S.M., Fatouros D.G. Ex vivo buccal drug delivery of ropinirole hydrochloride in the presence of permeation enhancers: The effect of charge. Pharm. Dev. Technol. 2017;22:1017–1021. doi: 10.3109/10837450.2015.1135343. - DOI - PubMed
    1. Nazari K., Kontogiannidou E., Ahmad R.H., Gratsani A., Rasekh M., Arshad M.S., Sunar B.S., Armitage D., Bouropoulos N., Chang M.W., et al. Development and characterisation of cellulose based electrospun mats for buccal delivery of non-steroidal anti-inflammatory drug (NSAID) Eur. J. Pharm. Sci. 2017;102:147–155. doi: 10.1016/j.ejps.2017.02.033. - DOI - PubMed
    1. Patel V.F., Liu F., Brown M.B. Modeling the oral cavity: In vitro and in vivo evaluations of buccal drug delivery systems. J. Control. Release. 2012;161:746–756. doi: 10.1016/j.jconrel.2012.05.026. - DOI - PubMed