Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems

Journal of Pharmaceutical Sciences

Volumn 102, Issue 2, 2013, Pages 508-517

  Nagy, Zsombor Kristóf ^a   Balogh, Attlia ^a   Drávavölgyi, Gábor ^a   Ferguson, James ^b   Pataki, Hajnalka ^a   Vajna, Balázs ^a   Marosi, György ^a  

^a BUDAPEST UNIVERSITY OF TECHNOLOGY AND ECONOMICS   (Hungary)

^b UNIVERSITY OF EDINBURGH   (United Kingdom)

Author keywords

Amorphous; Continuous pharmaceutical manufacturing; Electrospun nanofibers; Enhanced dissolution rate; Extrusion; Melt electrospinning; Oral drug delivery; Solid dispersion; Solid solution

Indexed keywords

ALCOHOL; CARVEDILOL; EUDRAGIT; POLYMER;

ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; ELECTROSPINNING; INFRARED SPECTROMETRY; MELT ELECTROSPINNING; SCANNING ELECTRON MICROSCOPY; X RAY DIFFRACTION;

EID: 84872500180     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23374     Document Type: Article

References (57)

1. Weinberg BD, Blanco E, Gao J. 2008. Polymer implants for intratumoral drug delivery and cancer therapy. J Pharm Sci 97:1681-1702.
2. Kretlow JD, Klouda L, Mikos AG. 2007. Injectable matrices and scaffolds for drug delivery in tissue engineering. Adv Drug Deliv Rev 59:263-273.
3. Boateng JS, Matthews KH, Stevens HNE, Eccleston GM. 2008. Wound healing dressings and drug delivery systems: A review. J Pharm Sci 97:2892-2923.
4. Higuchi T. 1963. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 52:1145-1149.
5. Kállai N, Luhn O, Dredan J, Kovacs K, Lengyel M, Antal I. 2010. Evaluation of drug release from coated pellets based on isomalt, sugar, and microcrystalline cellulose inert cores. AAPS Pharm Sci Tech 11:383-391.
6. Luhn O, Kallai N, Nagy ZK, Kovacs K, Fritzsching B, Klebovich I, Antal I. 2012. Dissolution profile of novel composite pellet cores based on different ratios of microcrystalline cellulose and isomalt. J Pharm Sci 101:2675-2680.
7. Sugano K, Okazaki A, Sugimoto S, Tavornvipas S, Omura A, Mano T. 2007. Solubility and dissolution profile assessment in drug discovery. Drug Metab Pharmacokinet 22:225-254.
8. Keseru GM, Makara GM. 2009. The influence of lead discovery strategies on the properties of drug candidates. Nat Rev Drug Discov 8:203-212.
9. Lipinski CA. 2000. Drug-like properties and the causes of poor solubility and poor permeability. J Pharm Toxicol Methods 44:235-249.
10. Van den Mooter G. 2011. The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate. Drug Discov Today 9:79-85.
11. Szuts A, Lang P, Ambrus R, Kiss L, Deli MA, Szabo-Revesz P. 2011. Applicability of sucrose laurate as surfactant in solid dispersions prepared by melt technology. Int J Pharm 410:107-110.
12. Vajna B, Farkas I, Farkas A, Pataki H, Nagy ZK, Madarasz J, Marosi G. 2011. Characterization of drug-cyclodextrin formulations using Raman mapping and multivariate curve resolution. J Pharm Biomed Anal 56:38-44.
13. Rodier E, Lochard H, Sauceau M, Letourneau JJ, Freiss B, Fages J. 2005. A three step supercritical process to improve the dissolution rate of Eflucimibe. Eur J Pharm Sci 26:184-193.
14. Allesu M, Chieng N, Rehder S, Rantanen J, Rades T, Aaltonen J. 2009. Enhanced dissolution rate and synchronized release of drugs in binary systems through formulation: Amorphous naproxen-cimetidine mixtures prepared by mechanical activation. J Control Release 136:45-53.
15. Alonzo DE, Gao Y, Zhou D, Mo H, Zhang GGZ, Taylor LS. 2011. Dissolution and precipitation behavior of amorphous solid dispersions. J Pharm Sci 100:3316-3331.
16. Verreck G, Six K, Van den Mooter G, Baert L, Peeters J, Brewster ME. 2003. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion-Part I. Int J Pharm 251:165-174.
17. Breitenbach J. 2002. Melt extrusion: From process to drug delivery technology. Eur JPharm Biopharm 54:107-117.
18. Patyi G, Bodis A, Antal I, Vajna B, Nagy ZK, Marosi G. 2010. Thermal and spectroscopic analysis of inclusion complex of spironolactone prepared by evaporation and hot melt methods. J Therm Anal Calorim 102:349-355.
19. Patyi G, Nagy Z, Vajna B, Anna P, Marosi G. 2012. Interfaces in multiphase polymers and nanomedicines. Materials Sci Forum 714:211-215.
20. Sauceau M, Fages J, Common A, Nikitine C, Rodier E. 2011. New challenges in polymer foaming: A review of extrusion processes assisted by supercritical carbon dioxide. Progr Polym Sci 36:749-766.
21. Verreck G, Decorte A, Heymans K, Adriaensen J, Cleeren D, Jacobs A, Liu D, Tomasko D, Arien A, Peeters J. 2005. The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64. Eur J Pharm Sci 26:349-358.
22. 2-aided and conventional melt extrusion for enhancing the dissolution rate of an active pharmaceutical ingredient. Polym Adv Technol 23:909-918.
23. Vajna B, Pataki H, Nagy Z, Farkas I, Marosi G. 2011. Characterization of melt extruded and conventional Isoptin formulations using Raman chemical imaging and chemometrics. Int J Pharm 419:107-113.
24. Verreck G, Chun I, Peeters J, Rosenblatt J, Brewster ME. 2003. Preparation and characterization of nanofibers containing amorphous drug dispersions generated by electrostatic spinning. Pharm Res 20:810-817.
25. Yu DG, Zhang XF, Shen XX, Brandford-White C, Zhu LM. 2009. Ultrafine ibuprofen loaded polyvinylpyrrolidone fiber mats using electrospinning. Polym Int 58:1010-1013.
26. Yu DG, Shen XX, Branford-White C, White K, Zhu LM, Bligh S. 2009. Oral fast-dissolving drug delivery membranes prepared from electrospun polyvinylpyrrolidone ultrafine fibers. Nanotechnology 20:055104.
27. Yu DG, Yu JH, Chen L, Williams GR, Wang X. 2012. Modified coaxial electrospinning for the preparation of high-quality ketoprofen-loaded cellulose acetate nanofibers. Carbohydr Polym 90:1016-1023.
28. Nagy ZK, Nyul K, Wagner I, Molnar K, Marosi G. 2010. Electrospun water soluble polymer mat for ultrafast release of Donepezil HCl. Express Polym Lett 4:763-772.
29. Yu DG, Branford-White C, White K, Li XL, Zhu LM. 2010. Dissolution improvement of electrospun nanofiber-bsed solid dispersions for acetaminophen. AAPS PharmSciTech 11:809-817.
30. Nagy ZK, Balogh A, Vajna B, Farkas A, Patyi G, Kramarics Á, Marosi G. 2012. Comparison of electrospun and extruded soluplus-based solid dosage forms of improved dissolution. J Pharm Sci 101:322-332.
31. Nagy ZK, Patyi G, Bodzay B, Vajna B, Marosi G. 2011. Prüfungen und Herstellungsverfahren von Composites bis zu Nanomedikamenten. Gummi Fasern Kunststoffe 64:100-104.
32. Molnar K, Vas LM, Czigany T. 2012. Determination of tensile strength of electrospun single nanofibers through modeling tensile behavior of the nanofibrous mat. Composites B Eng 43:15-21.
33. Lukas D, Sarkar A, Martinova L, Vodsedalkova K, Lubasova D, Chaloupek J, Pokorny P, Mikes P, Chvojka J, Komarek M. 2009. Physical principles of electrospinning (electrospinning as a nano-scale technology of the twenty-first century). Textile Progr 41:59-140.
34. Yu D, Branford-White C, White K, Chatterton N, Zhu L, Huang L, Wang B. 2011. A modified coaxial electrospinning for preparing fibers from a high concentration polymer solution. Express Polym Lett 5:732-741.
35. Kostakova E, Meszaros L, Gregr J. 2009. Composite nanofibers produced by modified needleless electrospinning. Mater Lett 63:2419-2422.
36. Huang F, Wang Q, Wei Q, Gao W, Shou H, Jiang S. 2010. Dynamic wettability and contact angles of poly (vinylidene fluoride) nanofiber membranes grafted with acrylic acid. Express Polym Lett 4:551-558.
37. Rosic R, Kocbek P, Baumgartner S, Kristl J. 2011. Electro-spun hydroxyethyl cellulose nanofibers: The relationship between structure and process. J Drug Deliv Sci Technol 21:229-236.
38. Sun K, Li Z. 2011. Preparations, properties and applications of chitosan based nanofibers fabricated by electrospinning. Express Polym Lett 5:342-361.
39. Rampichova M, Martinova L, Kostakova E, Filova E, Mickova A, Buzgo M, Michalek J, Pradny M, Necas A, Lukas D. 2012. A simple drug anchoring microfiber scaffold for chondrocyte seeding and proliferation. J Mater Sci 23:555-563.
40. Hutmacher DW, Dalton PD. 2011. Melt electrospinning. Chemistry 6:44-56.
41. Larrondo L, St John Manley R. 1981. Electrostatic fiber spinning from polymer melts. I. Experimental observations on fiber formation and properties. J Polym Sci Polym Phys Ed 19:909-920.
42. Zhou H, Green TB, Joo YL. 2006. The thermal effects on electrospinning of polylactic acid melts. Polymer 47:7497-7505.
43. Kim SJ, Jang DH, Park WH, Min BM. 2010. Fabrication and characterization of 3-dimensional PLGA nanofiber/microfiber composite scaffolds. Polymer 51:1320-1327.
44. Detta N, Brown TD, Edin FK, Albrecht K, Chiellini F, Chiellini E, Dalton PD, Hutmacher DW. 2010. Melt electrospinning of polycaprolactone and its blends with poly (ethylene glycol). Polym Int 59:1558-1562.
45. Ogata N, Shimada N, Yamaguchi S, Nakane K, Ogihara T. 2007. Melt-electrospinning of poly (ethylene terephthalate) and polyalirate. J Appl Polym Sci 105:1127-1132.
46. Wang X, Huang Z. 2010. Melt-electrospinning of PMMA. Chinese J Polym Sci 28:45-53.
47. Mitchell S, Sanders J. 2006. A unique device for controlled electrospinning. J Biomed Mater Res A 78:110-120.
48. Lyons J, Li C, Ko F. 2004. Melt-electrospinning part I: Processing parameters and geometric properties. Polym 45:7597-7603.
49. Malakhov S, Khomenko AY, Belousov S, Prazdnichnyi A, Chvalun S, Shepelev A, Budyka A. 2009. Method of manufacturing nonwovens by electrospinning from polymer melts. Fibre Chem 41:355-359.
50. Niu H, Lin T. 2012. Fiber generators in needleless electrospinning. J Nanomater 2012:13. doi:10.1155/2012/725950
51. Fang J, Zhang L, Sutton D, Wang X, Lin T. 2012. Needleless melt-electrospinning of polypropylene nanofibres. J Nanomater 2012:9. doi:10.1155/2012/382639
52. Wu JX, Yang M, Berg F, Pajander J, Rades T, Rantanen J. 2011. Influence of solvent evaporation rate and formulation factors on solid dispersion physical stability. Eur J Pharm Sci 44:610-620.
53. Rosic R, Pelipenko J, Kocbek P, Baumgartner S, Bester-Rogac M, Kristl J. 2012. The role of rheology of polymer solutions in predicting nanofiber formation by electrospinning. Eur Polym J 48:1374-1384.
54. Pataki H, Csontos I, Nagy ZK, Vajna B, Molnar M, Katona L, Marosi GJ. 2012. Implementation of Raman signal feedback to perform controlled crystallization of carvedilol. Org Process Res Dev [Epub ahead of print.] DOI: 10.1021/op300062t.
55. Pokharkar VB, Mandpe LP, Padamwar MN, Ambike AA, Mahadik KR, Paradkar A. 2006. Development, characterization and stabilization of amorphous form of a low Tg drug. Powder Technol 167:20-25.
56. Billes F, Pataki H, Unsalan O, Mikosch H, Vajna B, Marosi G. 2012. Solvent effect on the vibrational spectra of Carvedilol. Spectrochim Acta A Mol Biomol Spectrosc 95:148-164.
57. Patterson JE, James MB, Forster AH, Lancaster RW, Butler JM, Rades T. 2007. Preparation of glass solutions of three poorly water soluble drugs by spray drying, melt extrusion and ball milling. Int J Pharm 336:22-34.