Polymer-based nanoparticulate solid dispersions prepared by a modified electrospraying process
Deng-Guang Yu, Gareth R. Williams, Xia Wang, Jun-He Yang, Xiao-Yan Li, Wei Qian, Ying Li
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DOI: 10.4236/jbise.2011.412091   PDF    HTML     6,249 Downloads   12,352 Views   Citations

Abstract

A modified electrospraying process is exploited to enhance the dissolution profiles of a poorly water-soluble drug. With polyvinylpyrrolidone (PVP) as a hydrophilic polymer matrix and ketoprofen (KET) as a model drug, polymer-drug composites in the form of nanoparticles were prepared and characterized. The surface morphologies, the physical status of the drug, and the drug-polymer interactions were studied using FESEM, DSC, XRD, and ATR-FTIR. FESEM observations demonstrated that the nanoparticles gradually decreased in size from 640 ± 350, to 530 ± 320, 460 ± 200 and 320 ± 160 nm as the KET content increased from 0, to 9.1%, 16.7% and 33.3% w/w, respectively. Results from DSC and XRD suggested that KET was distributed in the PVP matrix in an amorphous manner at the molecular level. This is thought to be due to their compatibility, arising through hydrogen bonding as demonstrated by ATR- FTIR spectra. In vitro dissolution tests showed that the nanoparticles released the incorporated KET within 1 min, evidencing markedly improved dissolution over pure KET and a KET-PVP physical mixture. Electrospraying can hence offer a facile route to develop new polymer composites for biomedical applications, in particular for improving dissolution rate of poorly water-soluble drugs.

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Yu, D. , Williams, G. , Wang, X. , Yang, J. , Li, X. , Qian, W. and Li, Y. (2011) Polymer-based nanoparticulate solid dispersions prepared by a modified electrospraying process. Journal of Biomedical Science and Engineering, 4, 741-749. doi: 10.4236/jbise.2011.412091.

Conflicts of Interest

The authors declare no conflicts of interest.

References

[1] Vasconcelos, T., Sarmento, B. and Costa, P. (2007) Solid dispersions as strategy to improve oral bioavailability of poor water-soluble drugs. Drug Discovery Today, 12, 1068-1075. doi:10.1016/j.drudis.2007.09.005
[2] Nagy, Zs. K., Nyú, K., Wagner, I., Molnár, K. and Marosi, Gy. (2010) Electrospun water soluble polymer mat for ultrafast release of Donepezil HCl. eXPRESS Polymer Letters, 4, 763-772.
[3] Blagden, N., De Matas, M., Gavan, P. T. and York, P. (2007) Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Advanced Drug Delivery Reviews, 59, 617-630. doi:10.1016/j.addr.2007.05.011
[4] Yu, D.G., Branford-White, C., White, K., Annie Bligh, S.W., Williams, G., Zhu, L. M. and Chatterton, N.P. (2011) Self-assembled liposomes from amphiphilic electrospun nanofibers. Soft Matter, 7, 8239-8247. doi:10.1039/c1sm05961k
[5] Rasenack, N. and Muller, B.W. (2002) Dissolution rate enhancement by in situ micronization of poorly water-soluble drugs. Pharmaceutical Research, 19, 1894-1900. doi:10.1023/A:1021410028371
[6] Farokhzad, O.C. and Langer, R. (2009) Impact of nano- technology on drug delivery. ACS Nano, 2009, 3, 16-20. doi:10.1021/nn900002m
[7] Moshfeghi, A.A. and Peyman, G.A. (2005) Micro- and nano-particulates. Advanced Drug Delivery Reviews, 57, 2047- 2052. doi:10.1016/j.addr.2005.09.006
[8] Nagy, Z.K., Balogh, A., Vajna, B., Farkas, A., Patyi, G., Kramarics, á. and Marosi, G. (2011) Comparison of electrospun and extruded soluplus-based solid dosage forms of improved dissolution. Journal of Pharmaceutical Sciences, 100, 322-332. doi:10.1002/jps.22731
[9] Farokhzad, O.C. (2008) Nanotechnology for drug delivery: the perfect partnership. Expert Opinion on Drug Delivery, 5, 927-929. doi:10.1517/17425247.5.9.927
[10] Fini, A., Cavallari, C., Ospitali F. and Gonzalez-Rodriguez, M.L. (2011) Theophylline-loaded compritol microspheres prepared by ultrasound-assisted atomization. Journal of Pharmaceutical Sciences, 100, 743-757. doi:10.1002/jps.22312
[11] Al-Obaidi, H., Brocchini, S. and Buckton, G. (2009) Anomalous properties of spray dried solid dispersions. Journal of Pharmaceutical Sciences, 98, 4724-4737. doi:10.1002/jps.21782
[12] Moneghini, M., Bellich, B., Baxa, P. and Princivalle, F. (2008) Microwave generated solid dispersions containing ibuprofen. International Journal of Pharmaceutics, 361, 125-130. doi:10.1016/j.ijpharm.2008.05.026
[13] Patel, R. and Patel, P. (2008) Preparation, characterization, and dissolution behavior of a solid dispersion of simvastatin with polyethylene glycol 4000 and polyvinyl- pyrrolidone K30. Journal of Dispersion Science and Technology, 29, 193-204. doi:10.1080/01932690701706946
[14] Lee, J. and Yu, C. (2006) Critical freezing rate in freeze drying nanocrystal dispersions. Journal of Controlled Release, 111, 185-192. doi:10.1016/j.jconrel.2005.12.003
[15] Pasquali, I., Bettini, R. and Giordano, F. (2008) Supercritical fluid technologies: An innovative approach for manipulating the solid-state of pharmaceuticals. Advanced Drug Delivery Reviews, 60, 399-410. doi:10.1016/j.addr.2007.08.030
[16] Sun, N.Y., Wei, X.L., Wu, B. J., Chen, J., Lu Y. and Wu, W. (2007) Enhanced dissolution of silymarin/polyvi- nylpyrrolidone solid dispersion pellets prepared by a one-step fluid-bed coating technique. Powder Technology, 182, 72-80. doi:10.1016/j.powtec.2007.05.029
[17] Ivanisevic, I. (2010) Physical stability studies of miscible amorphous solid dispersions. Journal of Pharmaceutical Sciences, 99, 4005-4012. doi:10.1002/jps.22247
[18] Yu, D. G., Shen, X.X., Branford-White, C., White, K., Bligh, S.W.A. and Zhu, L.M. (2009) Oral fast-dissolving drug delivery membranes prepared from electrospun PVP ultrafine fibers. Nanotechnology, 20, 055104(9).
[19] Yu, D.G., White, K, Yang J.H., Wang, X., Qian, W. and Li, Y. (2012) PVP nanofibers prepared using co-axial electrospinning with salt solution as sheath fluid. Materials Letters, 67, 78-80. doi:10.1016/j.matlet.2011.09.035
[20] Yu, D.G., Lu, P., Branford-White, C., Yang, J.H. and Wang, X. (2011) Polyacrylonitrile nanofibers prepared using co- axial electrospinning with LiCl solution as sheath fluid. Nanotechnology, 22, 435301(7).
[21] Yu, D.G., Yang, J.M., Branford-White, C., Lu P., Zhang, L. and Zhu L.M. (2010) Third generation solid dispersions of ferulic acid in electrospun composite nanofibers. International Journal of Pharmaceutics, 400, 158-164.
[22] Salata, O.V. (2005) Tools of nanotechnology: Electrospray. Current Nanoscience, 1, 25-33. doi:10.2174/1573413052953192
[23] Yu, D.G., Gao L.D., White, K., Branford-White, C., Lu, W.Y. and Zhu, L.M. (2010) Multicomponent composite nanofibers electrospun from hot aqueous solutions of a poorly soluble drug. Pharmaceutical Research, 27, 2466- 2477. doi:10.1007/s11095-010-0239-y
[24] Yu, D.G., Williams, G.R., Yang, J.H., Wang, X., Yang, J.M. and Li, X.Y. (2011) Solid lipid nanoparticles self-assembled from electrosprayed polymer-based micoparticles. Journal of Material Chemistry, 21, 15957-15961. doi:10.1039/c1jm12720a
[25] Chakraborty, S., Liao, I. C., Adler, A. and Leong, K.W. (2009) Electrohydrodynamics: Afacile technique to fabricate drug delivery systems. Advanced Drug Delivery Reviews, 61, 1043-1054. doi:10.1016/j.addr.2009.07.013
[26] Wu, Y. and Clark, R.L. (2008) Electrohydrodynamic atomization: A versatile process for preparing materials for biomedical applications. Journal of Biomaterials Science, Polymer Edition, 19, 573-601. doi:10.1163/156856208784089616
[27] Heikkila, P. and Harlin, A. (2009) Electrospinning of polyacrylonitrile (PAN) solution:Effect of conductive additive and filler on the process. eXPRESS Polymer Letters, 3, 437-445.
[28] Ding, L., Lee, T. and Wang, C.H. (2005) Fabrication of monodispersed taxol-loaded particles using electrohydrodynamic atomization. Journal of Controlled Release, 102, 395-413. doi:10.1016/j.jconrel.2004.10.011
[29] Chang, M.W., Stride, E. and Edirisinghe, M. (2010) A new method for the preparation of monoporous hollow microspheres. Langmuir, 26, 5115-5121. doi:10.1021/la903592s
[30] Enayati, M., Ahmad, Z., Stride, E. and Edirisinghe, M. (2010) One step electrohydrodynamic production of drug- loaded micro- and nano-particles. Journal of the Royal Society Interface, 7, 667-675. doi:10.1098/rsif.2009.0348
[31] Stride, E. and Edirisinghe, M. (2008) Novel microbubble preparation technologies. Soft Matter, 4, 2350-2359.
[32] Qian, F., Huang, J. and Hussain, M.A. (2010) Drug-polymer solubility and miscibility: Stability consideration and practical challenges in amorphous solid dispersion development. Journal of Pharmaceutical Sciences, 99, 2941-2947. doi:10.1002/jps.22074
[33] Guedes, F. L., de Oliveira, B.G., Hernandes, M.Z., De Simone, C.A., Veiga, F.J., de Lima, Mdo C., Pitta, I.R., Galdino, S.L. and Neto, P.J. (2011) Solid dispersions of imidazolidinedione by PEG and PVP polymers with potential antischistosomal activities. AAPS PharmSciTech, 12, 401-410. doi:10.1208/s12249-010-9556-z
[34] Wu, K., Li, J., Wang, W. and Winstead, D.A. (2009) Formation and characterization of solid dispersions of piroxicam and polyvinylpyrrolidone using spray drying and precipitation with compressed antisolvent. Journal of Pharmaceutical Sciences, 98, 2422-2431. doi:10.1002/jps.21598
[35] Wang, C., Chien, H. S., Hsu, C. H., Wang, Y.C., Wang, C.T. and Lu, H.A. (2007) Electrospinning of polyacrylonitrile solutions at elevated temperatures. Macromolecules, 40, 7973-7983. doi:10.1021/ma070508n
[36] Xie, J., Lim, L.K., Phua, Y., Hua, J. and Wang, C.H. (2006) Electrohydrodynamic atomization for biodegradable polymeric particle production. Journal of Colloid and Interface Science, 302, 103-112. doi:10.1016/j.jcis.2006.06.037
[37] Pareta, R. and Edirisinghe, M.J. (2006) A novel method for the preparation of biodegradable microspheres for protein drug delivery. Journal of the Royal Society Interface, 3, 573-582. doi:10.1098/rsif.2006.0120
[38] Di Martino, P., Joiris, E., Gobetto, R., Masic, A., Palmieri, G.F. and Martelli, S. (2004) Ketoprofen-poly (vinylpyrrolidone) physical interaction. Journal of Crystal Growth, 265, 302-308. doi:10.1208/pt0802037
[39] Manna, L., Banchero, M., Sola, D., Ferri, A., Ronchetti, S. and Sicardi, S. (2007) Impregnation of PVP microparticles with ketoprofen in the presence of supercritical CO2. The Journal of Supercritical Fluids, 42, 378-384. doi:10.1016/j.supflu.2006.12.002
[40] Sancin, P., Caputo, O., Cavallari, C., Passerini, N., Rodriguez, L., Cini, M. and Fini, A. (1999) Effects of ultrasound-assisted compaction on ketoprofen/Eudragit S100 mixtures. European Journal of Pharmaceutical Sciences, 7, 207-213. doi:10.1016/S0928-0987(98)00022-0
[41] Rawlinson, C.F., Williams, A.C., Timmins, P. and Grimsey, I. (2007) Polymer-mediated disruption of drug crystallinity. International Journal of Pharmaceutics, 336, 42- 48. doi:10.1016/j.ijpharm.2006.11.029
[42] Merisko-Liversidge, E., Liversidge, G.G. and Cooper, E.R. (2003) Nanosizing: A formulation approach for poorly- water-soluble compounds. European Journal of Pharma-ceutical Sciences, 18, 113-120. doi:10.1016/S0928-0987(02)00251-8
[43] Demir, M.M. (2010) Investigation on glassy skin formation of porous polystyrene fibers electrospun from DMF. eXPRESS Polymer Letters, 4, 2-8.
[44] Kumari, A., Yadav, S.K. and Yadav, S.C. (2010) Biodegradable polymeric nanoparticles based drug delivery systems. Colloids and Surfaces B: Biointerfaces, 75, 1-18. doi:10.1016/j.colsurfb.2009.09.001

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