Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
Abstract
:1. Introduction
- The swelling of zein-matrices was studied by image analysis in a nearly-continuous mode: We utilized a USB-microscope connected to a PC to automatically collect images of the swelling tablets over 20 h, at a frequency of one frame every 10 min. Image sequences were then binarized using image analysis software, so to enable the calculation of the percentages of total tablet swelling, as well as the extent of swelling in the axial and radial directions, over time. The facile image analysis method developed here, functioned as a direct readout of tablet swelling.
- With the broader aim to underpin the unique matrix-forming ability of zein, the performance of zein tablets was compared to that of HPMC and EC tablets, as reference controls of purely hydrophilic/swellable and insoluble matrices, respectively. Indeed, all throughout the study, swelling measurements of zein/co-excipients matrices were systematically compared with those of HPMC/co-excipients and EC/co-excipients matrices.
2. Materials and Methods
2.1. Materials
2.2. Methods
2.2.1. Preparation of Tablets
2.2.2. Swelling Studies
2.2.3. Drug Release Studies
3. Results and Discussion
3.1. Swelling and Drug Release of Matrices of Pure Polymers
3.2. Swelling and Drug Release of Matrices Containing Diluents
3.2.1. Swelling
3.2.2. Drug Release
3.3. Swelling and Drug Release of Matrices containing PVP and SLS
3.3.1. Swelling
3.3.2. Drug Release
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Conflicts of Interest
References
- Demir, M.; Ramos-Rivera, L.; Silva, R.; Nazhat, S.N.; Boccaccini, A.R. Zein-based composites in biomedical applications. J. Biomed. Mater. Res. Part A 2017, 105, 1656–1665. [Google Scholar] [CrossRef] [PubMed]
- Paliwal, R.; Palakurthi, S. Zein in controlled drug delivery and tissue engineering. J. Control. Release 2014, 189, 108–122. [Google Scholar] [CrossRef] [PubMed]
- Zhang, Y.; Cui, L.; Che, X.; Zhang, H.; Shi, N.; Li, C.; Chen, Y.; Kong, W. Zein-based films and their usage for controlled delivery: Origin, classes and current landscape. J. Control. Release 2015, 206, 206–219. [Google Scholar] [CrossRef] [PubMed]
- Zhang, Y.; Cui, L.; Li, F.; Shi, N.; Li, C.; Yu, X.; Chen, Y.; Kong, W. Design, fabrication and biomedical applications of zein-based nano/micro-carrier systems. Int. J. Pharm. 2016, 513, 191–210. [Google Scholar] [CrossRef] [PubMed]
- Berardi, A.; Bisharat, L.; AlKhatib, H.S.; Cespi, M. Zein as a Pharmaceutical Excipient in Oral Solid Dosage Forms: State of the Art and Future Perspectives. AAPS PharmSciTech 2018, 19, 2009–2022. [Google Scholar] [CrossRef] [PubMed]
- Bisharat, L.; Berardi, A.; Perinelli, D.R.; Bonacucina, G.; Casettari, L.; Cespi, M.; AlKhatib, H.S.; Palmieri, G.F. Aggregation of zein in aqueous ethanol dispersions: Effect on cast film properties. Int. J. Biol. Macromol. 2017, 106, 360–368. [Google Scholar] [CrossRef] [PubMed]
- Georget, D.M.R.; Barker, S.A.; Belton, P.S. A study on maize proteins as a potential new tablet excipient. Eur. J. Pharm. Biopharm. 2008, 69, 718–726. [Google Scholar] [CrossRef]
- Guo, H.X.; Shi, Y.P. A novel zein-based dry coating tablet design for zero-order release. Int. J. Pharm. 2009, 370, 81–86. [Google Scholar] [CrossRef]
- Raza, A.; Shen, N.; Li, J.; Chen, Y.; Wang, J.-Y. Formulation of zein based compression coated floating tablets for enhanced gastric retention and tunable drug release. Eur. J. Pharm. Sci. 2019, 132, 163–173. [Google Scholar] [CrossRef]
- Berardi, A.; Bisharat, L.; Cespi, M.; Basheti, I.A.; Bonacucina, G.; Pavoni, L.; AlKhatib, H.S. Controlled release properties of zein powder filled into hard gelatin capsules. Powder Technol. 2017, 320, 703–713. [Google Scholar] [CrossRef]
- Bouman, J.; Belton, P.; Venema, P.; van der Linden, E.; de Vries, R.; Qi, S. The development of direct extrusion-injection moulded zein matrices as novel oral controlled drug delivery systems. Pharm. Res. 2015, 32, 2775–2786. [Google Scholar] [CrossRef] [PubMed]
- Bouman, J.; Belton, P.; Venema, P.; Van Der Linden, E.; De Vries, R.; Qi, S. Controlled release from zein matrices: Interplay of drug hydrophobicity and pH. Pharm. Res. 2016, 33, 673–685. [Google Scholar] [CrossRef] [PubMed]
- Berardi, A.; Bisharat, L.; Bonacucina, G.; Casettari, L.; Logrippo, S.; Cespi, M.; AlKhatib, H.S.; Palmieri, G.F. Formulation, swelling and dissolution kinetics study of zein based matrix tablets. Powder Technol. 2017, 310, 241–249. [Google Scholar] [CrossRef]
- Shukla, R.; Cheryan, M. Zein: The industrial protein from corn. Ind. Crops Prod. 2001, 13, 171–192. [Google Scholar] [CrossRef]
- Dabbagh, M.A.; Ford, J.L.; Rubinstein, M.H.; Hogan, J.E. Effects of polymer particle size, compaction pressure and hydrophilic polymers on drug release from matrices containing ethylcellulose. Int. J. Pharm. 1996, 140, 85–95. [Google Scholar] [CrossRef]
- Ford, J.L. Design and Evaluation of Hydroxypropyl Methylcellulose Matrix Tablets for Oral Controlled Release: A Historical Perspective. In Hydrophilic Matrix Tablets for Oral Controlled Release; Springer: Berlin/Heidelberg, Germany, 2014; pp. 17–51. ISBN 1493915185. [Google Scholar]
- Tapia-Hernández, J.A.; Del-Toro-Sánchez, C.L.; Cinco-Moroyoqui, F.J.; Ruiz-Cruz, S.; Juárez, J.; Castro-Enríquez, D.D.; Barreras-Urbina, C.G.; López-Ahumada, G.A.; Rodríguez-Félix, F. Gallic Acid-Loaded Zein Nanoparticles by Electrospraying Process. J. Food Sci. 2019, 84, 818–831. [Google Scholar] [CrossRef]
- Alehosseini, A.; Gómez-Mascaraque, L.G.; Ghorani, B.; López-Rubio, A. Stabilization of a saffron extract through its encapsulation within electrospun/electrosprayed zein structures. LWT 2019, 113, 108280. [Google Scholar] [CrossRef]
- Teklehaimanot, W.H.; Emmambux, M.N. Foaming properties of total zein, total kafirin and pre-gelatinized maize starch blends at alkaline pH. Food Hydrocoll. 2019, 97, 105221. [Google Scholar] [CrossRef]
- Díaz-Gómez, L.J.; Ortíz-Martínez, M.; Aguilar, O.; García-Lara, S.; Castorena-Torres, F. Antioxidant Activity of Zein Hydrolysates from Zea Species and Their Cytotoxic Effects in a Hepatic Cell Culture. Molecules 2018, 23, 312. [Google Scholar] [CrossRef]
- Rowe, R.C.; Sheskey, P.J.; Quinn, M.E.; Association, A.P.; Press, P. Handbook of Pharmaceutical Excipients; Pharmaceutical Press: London, UK, 2009; Volume 6. [Google Scholar]
- Casettari, L.; Bonacucina, G.; Morris, G.A.; Perinelli, D.R.; Lucaioli, P.; Cespi, M.; Palmieri, G.F. Dextran and its potential use as tablet excipient. Powder Technol. 2015, 273, 125–132. [Google Scholar] [CrossRef] [Green Version]
- Berardi, A.; Bisharat, L.; Blaibleh, A.; Pavoni, L.; Cespi, M. A simple and inexpensive image analysis technique to study the effect of disintegrants concentration and diluents type on disintegration. J. Pharm. Sci. 2018, 107, 2643–2652. [Google Scholar] [CrossRef] [PubMed]
- Bisharat, L.; AlKhatib, H.S.; Muhaissen, S.; Quodbach, J.; Blaibleh, A.; Cespi, M.; Berardi, A. The influence of ethanol on superdisintegrants and on tablets disintegration. Eur. J. Pharm. Sci. 2019, 129, 140–147. [Google Scholar] [CrossRef] [PubMed]
- Amayreh, R.; Bisharat, L.; Cespi, M.; Palimieri, G.F.; Berardi, A. Evaluation of the Disintegration Action of Soy Polysaccharide by Image Analysis. AAPS PharmSciTech 2019, 20, 265. [Google Scholar] [CrossRef] [PubMed]
- Chen, Y.Y.; Hughes, L.P.; Gladden, L.F.; Mantle, M.D. Quantitative Ultra-Fast MRI of HPMC Swelling and Dissolution. J. Pharm. Sci. 2010, 99, 3462–3472. [Google Scholar] [CrossRef] [PubMed]
- Rajabi-Siahboomi, A.R.; Bowtell, R.W.; Mansfield, P.; Henderson, A.; Davies, M.C.; Melia, C.D. Structure and behaviour in hydrophilic matrix sustained release dosage forms: 2. NMR-imaging studies of dimensional changes in the gel layer and core of HPMC tablets undergoing hydration. J. Control. Release 1994, 31, 121–128. [Google Scholar] [CrossRef]
- Roberts, M.; Cespi, M.; Ford, J.L.; Dyas, A.M.; Downing, J.; Martini, L.G.; Crowley, P.J. Influence of ethanol on aspirin release from hypromellose matrices. Int. J. Pharm. 2007, 332, 31–37. [Google Scholar] [CrossRef]
- Gao, P.; Meury, R.H. Swelling of Hydroxypropyl Methylcellulose Matrix Tablets. 1. Characterization of Swelling Using a Novel Optical Imaging Method. J. Pharm. Sci. 1996, 85, 725–731. [Google Scholar] [CrossRef]
- Tajarobi, F.; Abrahmsén-Alami, S.; Carlsson, A.S.; Larsson, A. Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging—Effect of solubility of additives on HPMC matrix tablets. Eur. J. Pharm. Sci. 2009, 37, 89–97. [Google Scholar] [CrossRef]
- Tran, P.H.L.; Tran, T.T.D.; Park, J.B.; Lee, B.J. Controlled release systems containing solid dispersions: Strategies and mechanisms. Pharm. Res. 2011, 28, 2353–2378. [Google Scholar] [CrossRef]
- Gustafsson, C.; Bonferoni, M.C.; Caramella, C.; Lennholm, H.; Nyström, C. Characterisation of particle properties and compaction behaviour of hydroxypropyl methylcellulose with different degrees of methoxy/hydroxypropyl substitution. Eur. J. Pharm. Sci. 1999, 9, 171–184. [Google Scholar] [CrossRef]
- Nokhodchi, A.; Rubinstein, M.H.; Ford, J.L. The effect of particle size and viscosity grade on the compaction properties of hydroxypropylmethylcellulose 2208. Int. J. Pharm. 1995, 126, 189–197. [Google Scholar] [CrossRef]
- Oh, Y.K.; Flanagan, D.R. Diffusional properties of zein membranes and matrices. Drug Dev. Ind. Pharm. 2010, 36, 497–507. [Google Scholar] [CrossRef] [PubMed]
- Gao, P.; Skoug, J.W.; Nixon, P.R.; Ju, T.R.; Stemm, N.L.; Sung, K.C. Swelling of hydroxypropyl methylcellulose matrix tablets. 2. Mechanistic study of the influence of formulation variables on matrix performance and drug release. J. Pharm. Sci. 1996, 85, 732–740. [Google Scholar] [CrossRef] [PubMed]
- Palmieri, G.F.; Joiris, E.; Bonacucina, G.; Cespi, M.; Mercuri, A. Differences between eccentric and rotary tablet machines in the evaluation of powder densification behaviour. Int. J. Pharm. 2005, 298, 164–175. [Google Scholar] [CrossRef] [PubMed]
- Cespi, M.; Misici-Falzi, M.; Bonacucina, G.; Ronchi, S.; Palmieri, G.F. The effect of punch tilting in evaluating powder densification in a rotary tablet machine. J. Pharm. Sci. 2008, 97, 1277–1284. [Google Scholar] [CrossRef]
- Skelbæk-Pedersen, A.; Vilhelmsen, T.; Wallaert, V.; Rantanen, J. Quantification of Fragmentation of Pharmaceutical Materials after Tableting. J. Pharm. Sci. 2019, 108, 1246–1253. [Google Scholar] [CrossRef]
- Markl, D.; Yassin, S.; Wilson, D.I.; Goodwin, D.J.; Anderson, A.; Zeitler, J.A. Mathematical modelling of liquid transport in swelling pharmaceutical immediate release tablets. Int. J. Pharm. 2017, 526, 1–10. [Google Scholar] [CrossRef]
- Quodbach, J.; Moussavi, A.; Tammer, R.; Frahm, J.; Kleinebudde, P. Tablet Disintegration Studied by High-Resolution Real-Time Magnetic Resonance Imaging. J. Pharm. Sci. 2014, 103, 249–255. [Google Scholar] [CrossRef]
- Sinha, T.; Bharadwaj, R.; Curtis, J.S.; Hancock, B.C.; Wassgren, C. Finite element analysis of pharmaceutical tablet compaction using a density dependent material plasticity model. Powder Technol. 2010, 202, 46–54. [Google Scholar] [CrossRef]
- Diarra, H.; Mazel, V.; Busignies, V.; Tchoreloff, P. Investigating the effect of tablet thickness and punch curvature on density distribution using finite elements method. Int. J. Pharm. 2015, 493, 121–128. [Google Scholar] [CrossRef]
- Laity, P.R.; Cameron, R.E. Synchrotron X-ray microtomographic study of tablet swelling. Eur. J. Pharm. Biopharm. 2010, 75, 263–276. [Google Scholar] [CrossRef] [PubMed]
- Barba, A.A.; d’Amore, M.; Chirico, S.; Lamberti, G.; Titomanlio, G. Swelling of cellulose derivative (HPMC) matrix systems for drug delivery. Carbohydr. Polym. 2009, 78, 469–474. [Google Scholar] [CrossRef]
- Ruso, J.M.; Deo, N.; Somasundaran, P. Complexation between Dodecyl Sulfate Surfactant and Zein Protein in Solution. Langmuir 2004, 20, 8988–8991. [Google Scholar] [CrossRef] [PubMed]
- Deo, N.; Jockusch, S.; Turro, N.J.; Somasundaran, P. Surfactant Interactions with Zein Protein. Langmuir 2003, 19, 5083–5088. [Google Scholar] [CrossRef]
- Nokhodchi, A.; Norouzi-Sani, S.; Siahi-Shadbad, M.-R.; Lotfipoor, F.; Saeedi, M. The effect of various surfactants on the release rate of propranolol hydrochloride from hydroxypropylmethylcellulose (HPMC)-Eudragit matrices. Eur. J. Pharm. Biopharm. 2002, 54, 349–356. [Google Scholar] [CrossRef]
Abbreviation | Components (% w/w) | ||||||||
---|---|---|---|---|---|---|---|---|---|
Propranolol HCl | Zein | Lac | DCP | MCC | PVP | SLS | Magnesium Stearate | ||
Zein | - | 99.5 | - | - | - | - | - | 0.5 | |
Zein 10%D | 10.0 | 89.5 | - | - | - | - | - | 0.5 | |
Binary mixtures | Zein 20%Lac | - | 79.5 | 20.0 | - | - | - | - | 0.5 |
Zein 50%Lac | - | 49.5 | 50.0 | - | - | - | - | 0.5 | |
Zein 20%DCP | - | 79.5 | - | 20.0 | - | - | - | 0.5 | |
Zein 50%DCP | - | 49.5 | - | 50.0 | - | - | - | 0.5 | |
Zein 10%MCC | - | 89.5 | - | - | 10.0 | - | - | 0.5 | |
Zein 40%MCC | - | 59.5 | - | - | 40.0 | - | - | 0.5 | |
Zein 1%PVP | - | 98.5 | - | - | - | 1.0 | - | 0.5 | |
Zein 5%PVP | - | 94.5 | - | - | - | 5.0 | - | 0.5 | |
Zein 1%SLS | - | 98.5 | - | - | - | - | 1.0 | 0.5 | |
Zein 3%SLS | - | 96.5 | - | - | - | - | 3.0 | 0.5 | |
Ternary mixtures | Zein L Lac 10%D | 10.0 | 71.5 | 18.0 | - | - | - | - | 0.5 |
Zein H Lac 10%D | 10.0 | 44.52 | 44.98 | - | - | - | - | 0.5 | |
Zein L DCP 10%D | 10.0 | 71.5 | - | 18.0 | - | - | - | 0.5 | |
Zein H DCP 10%D | 10.0 | 44.52 | - | 44.98 | - | - | - | 0.5 | |
Zein L MCC 10%D | 10.0 | 80.5 | - | - | 9.0 | - | - | 0.5 | |
Zein H MCC 10%D | 10.0 | 53.52 | - | - | 35.98 | - | - | 0.5 | |
Zein L PVP 10%D | 10.0 | 88.60 | - | - | - | 0.9 | - | 0.5 | |
Zein H PVP 10%D | 10.0 | 85.0 | - | - | - | 4.5 | - | 0.5 | |
Zein L SLS 10%D | 10.0 | 88.6 | - | - | - | - | 0.9 | 0.5 | |
Zein H SLS 10%D | 10.0 | 86.80 | - | - | - | - | 2.7 | 0.5 |
Abbreviation | Components (% w/w) | |||||||||
---|---|---|---|---|---|---|---|---|---|---|
Propranolol HCl | HPMC | Lac | DCP | MCC | PVP | SLS | TiO2 | Magnesium Stearate | ||
HPMC | - | 99.0 | - | - | - | - | - | 0.5 | 0.5 | |
HPMC 10%D | 10 | 89.0 | - | - | - | - | - | 0.5 | 0.5 | |
Binary mixtures | HPMC 20%Lac | - | 79.0 | 20.0 | - | - | - | - | 0.5 | 0.5 |
HPMC 50%Lac | - | 49.0 | 50.0 | - | - | - | - | 0.5 | 0.5 | |
HPMC 20%DCP | - | 79.0 | - | 20.0 | - | - | - | 0.5 | 0.5 | |
HPMC 50%DCP | - | 49.0 | - | 50.0 | - | - | - | 0.5 | 0.5 | |
HPMC 10%MCC | - | 89.0 | - | - | 10.0 | - | - | 0.5 | 0.5 | |
HPMC 40%MCC | - | 59.0 | - | - | 40.0 | - | - | 0.5 | 0.5 | |
HPMC 1%PVP | - | 98.0 | - | - | - | 1.0 | - | 0.5 | 0.5 | |
HPMC 5%PVP | - | 94.0 | - | - | - | 5.0 | - | 0.5 | 0.5 | |
HPMC 1%SLS | - | 98.0 | - | - | - | - | 1.0 | 0.5 | 0.5 | |
HPMC 3%SLS | - | 96.0 | - | - | - | - | 3.0 | 0.5 | 0.5 |
Abbreviation | Components (% w/w) | ||||||||
---|---|---|---|---|---|---|---|---|---|
Propranolol HCl | EC | Lac | DCP | MCC | PVP | SLS | Magnesium Stearate | ||
EC | - | 99.5 | - | - | - | - | - | 0.5 | |
EC 10%D | 10 | 89.5 | - | - | - | - | - | 0.5 | |
Binary mixtures | EC 20%Lac | - | 79.5 | 20.0 | - | - | - | - | 0.5 |
EC 50%Lac | - | 49.5 | 50.0 | - | - | - | - | 0.5 | |
EC 20%DCP | - | 79.5 | - | 20.0 | - | - | - | 0.5 | |
EC 50%DCP | - | 49.5 | - | 50.0 | - | - | - | 0.5 | |
EC 10%MCC | - | 89.5 | - | - | 10.0 | - | - | 0.5 | |
EC 40%MCC | - | 59.5 | - | - | 40.0 | - | - | 0.5 | |
EC 1%PVP | - | 98.5 | - | - | - | 1.0 | - | 0.5 | |
EC 5%PVP | - | 94.5 | - | - | - | 5.0 | - | 0.5 | |
EC 1%SLS | - | 98.5 | - | - | - | - | 1.0 | 0.5 | |
EC 3%SLS | - | 96.5 | - | - | - | - | 3.0 | 0.5 |
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Berardi, A.; Abdel Rahim, S.; Bisharat, L.; Cespi, M. Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients. Pharmaceutics 2019, 11, 513. https://doi.org/10.3390/pharmaceutics11100513
Berardi A, Abdel Rahim S, Bisharat L, Cespi M. Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients. Pharmaceutics. 2019; 11(10):513. https://doi.org/10.3390/pharmaceutics11100513
Chicago/Turabian StyleBerardi, Alberto, Safwan Abdel Rahim, Lorina Bisharat, and Marco Cespi. 2019. "Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients" Pharmaceutics 11, no. 10: 513. https://doi.org/10.3390/pharmaceutics11100513
APA StyleBerardi, A., Abdel Rahim, S., Bisharat, L., & Cespi, M. (2019). Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients. Pharmaceutics, 11(10), 513. https://doi.org/10.3390/pharmaceutics11100513