Comparison of electrospun and extruded soluplus®-based solid dosage forms of improved dissolution

Journal of Pharmaceutical Sciences

Volumn 101, Issue 1, 2012, Pages 322-332

  Nagy, Zsombor K ^a   Balogh, Attila ^a   Vajna, Balázs ^a   Farkas, Attila ^a   Patyi, Gergo ^a   Kramarics, Áron ^b   Marosi, György ^a  

^a BUDAPEST UNIVERSITY OF TECHNOLOGY AND ECONOMICS   (Hungary)

^b EÖTVÖS LORÁND UNIVERSITY   (Hungary)

Author keywords

Electrospinning; Extrusion; Improved dissolution rate; Nanofibers; Nanotechnology; Oral drug delivery; Polymeric drug delivery; Raman microscopy; Solid dispersion; Solid solution

Indexed keywords

ALCOHOL; COPOLYMER; SOLUBILIZER; SOLUPLUS; SPIRONOLACTONE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG SOLUBILITY; ELECTROSPINNING; RAMAN SPECTROMETRY; SCANNING ELECTRON MICROSCOPY; X RAY DIFFRACTION;

EID: 82255179553     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22731     Document Type: Article

References (49)

1. Keseru GM, Makara GM. 2009. The influence of lead discovery strategies on the properties of drug candidates. Nat Rev Drug Discov 8:203-212.
2. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. 1997. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 23:3-25.
3. Lipinski CA. 2000. Drug-like properties and the causes of poor solubility and poor permeability. J Pharm Toxicol Methods 44:235-249.
4. Prentis R, Lis Y, Walker S. 1988. Pharmaceutical innovation by the seven UK-owned pharmaceutical companies (1964-1985). Br J Clin Pharmacol 25:387-396.
5. Amidon GL, Lennernäs H, Shah VP, Crison JR. 1995. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12:413-420.
6. Pouton CW. 2006. Formulation of poorly water-soluble drugs for oral administration: Physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci 29:278-287.
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. 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.
9. Yano H, Kleinebudde P. 2010. Improvement of dissolution behavior for poorly water-soluble drug by application of cyclodextrin in extrusion process: Comparison between melt extrusion and wet extrusion. AAPS Pharm Sci Tech 11:885-893.
10. 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.
11. 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.
12. 2-aided and conventional melt extrusion for enhancing the dissolution rate of an active pharmaceutical ingredient. Polym Adv Technol. In Press.
13. Windbergs M, Strachan CJ, Kleinebudde P. 2009. Influence of the composition of glycerides on the solid-state behaviour and the dissolution profiles of solid lipid extrudates. Int J Pharm 381:184-191.
14. Windbergs M, Gueres S, Strachan CJ, Kleinebudde P. 2010. Two-step solid lipid extrusion as a process to modify dissolution behavior. AAPS Pharm Sci Tech 11:2-8.
15. Breitenbach J. 2002. Melt extrusion: From process to drug delivery technology. Eur J Pharm Biopharm 54:107-117.
16. Lakshman JP, Cao Y, Kowalski J, Serajuddin ATM. 2008. Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug. Mol Pharm 5:994-1002.
17. Noyes AA, Whitney WR. 1897. The rate of solution of solid substances in their own solutions. J Am Chem Soc 19:930-934.
18. Hancock BC, Zografi G. 1997. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci 86:1-12.
19. Patterson JE, James MB, Forster AH, Lancaster RW, Butler JM, Rades T. 2005. The influence of thermal and mechanical preparative techniques on the amorphous state of four poorly soluble compounds. J Pharm Sci 94:1998-2012.
20. Guns S, Dereymaker A, Kayaert P, Mathot V, Martens JA, Van den Mooter G. 2011. Comparison between hot-melt extrusion and spray-drying for manufacturing solid dispersions of the graft copolymer of ethylene glycol and vinylalcohol. Pharm Res 28:673-682.
21. Ostwald W. 1900. Über die vermeintliche Isomerie des roten und gelben Quecksilberoxyds und die Oberflächenspannung fester Körper. Zeitschrift für Physikalische Chemie 34:495-503.
22. Freundlich H. 1909. Kapillarchemie. Vol. I. Leipzig: Akademische Verlagsgesellschaft GmbH.
23. Van Eerdenbrugh B, Vermant J, Martens JA, Froyen L, Van Humbeeck J, Van den Mooter G, Augustijns P. 2010. Solubility increases associated with crystalline drug nanoparticles: Methodologies and significance. Mol Pharm 7:1858-1870.
24. 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.
25. Marsac PJ, Rumondor ACF, Nivens DE, Kestur US, Stanciu L, Taylor LS. 2010. Effect of temperature and moisture on the miscibility of amorphous dispersions of felodipine and poly (vinyl pyrrolidone). J Pharm Sci 99:169-185.
26. Weuts I., Van Dycke F, Voorspoels J, De Cort S, Stokbroekx S, Leemans R, Brewster ME, Xu D, Segmuller B, Turner YTA, Roberts CJ, Davies MC, Qi S, Craig DQM, Reading M. 2010. Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: Etravirine. J Pharm Sci 100:260-274.
27. Brouwers J, Brewster ME, Augustijns P. 2009. Supersaturating drug delivery systems: The answer to solubility-limited oral bioavailability? J Pharm Sci 98:2549-2572.
28. Alonzo DE, Zhang GGZ, Zhou D, Gao Y, Taylor LS. 2010. Understanding the behavior of amorphous pharmaceutical systems during dissolution. Pharm Res 27:608-618.
29. Molnár K, Vas LM, Czigány T. 2011. Determination of tensile strength of electrospun single nanofibers through modeling tensile behavior of the nanofibrous mat. Comp. Part B:Engin. In Press.
30. Kostakova E, Meszaros L, Gregr J. 2009. Composite nanofibers produced by modified needleless electrospinning. Materials Lett 63:2419-2422.
31. 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.
32. Thakur RA, Florek CA, Kohn J, Michniak BB. 2008. Electrospun nanofibrous polymeric scaffold with targeted drug release profiles for potential application as wound dressing. Int J Pharm 364:87-93.
33. Rho KS, Jeong L, Lee G, BM, Park YJ, Hong SD, Roh S, Cho JJ, Park WH, Min BM. 2006. Electrospinning of collagen nanofibers: effects on the behavior of normal human keratinocytes and early-stage wound healing. Biomaterials 27:1452-1461.
34. Kolacna L, Bakesova J, Varga F, Kostakova E, Planka L, Necas A, Lukas D, Amler E, Pelouch V. 2007. Biochemical and biophysical aspects of collagen nanostructure in the extracellular matrix. Physiol Res 56:51-60.
35. Schnell E, Klinkhammer K, Balzer S, Brook G, Klee D, Dalton P, Mey J. 2007. Guidance of glial cell migration and axonal growth on electrospun nanofibers of poly-ε-caprolactone and a collagen/poly-ε-caprolactone blend. Biomaterials 28:3012-3025.
36. 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.
37. Yu DG, Zhang XF, Shen XX, Brandford-White C, Zhu LM. 2009. Ultrafine ibuprofen loaded polyvinylpyrrolidone fiber mats using electrospinning. Polymer Int 58:1010-1013.
38. 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.
39. Nagy ZK, Nyúl K, Wagner I, Molnár K, Marosi G. 2010. Electrospun water soluble polymer mat for ultrafast release of Donepezil HCl. Express Polym Lett 4:763-772.
40. Fathi-Azarbayjaniand A, Chan SY. 2010. Single and multi-layered nanofibers for rapid and controlled drug delivery. Chem Pharm Bull 58:143-146.
41. Yu DG, Branford-White C, White K, Li XL, Zhu LM. 2010. Dissolution improvement of electrospun nanofiber-based solid dispersions for acetaminophen. AAPS PharmSciTech 11:809-817.
42. Vasconcelos T, Sarmento B, Costa P. 2007. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today 12:1068-1075.
43. Hardung H, Djuric D, Ali S. 2010. Combining HME & solubilization: Soluplus®-The solid solution. Drug Deliv Technol 10:20-27.
44. Doggrell SA, Brown L. 2001. The spironolactone renaissance. Expert Opin Invest Drugs 10:943-954.
45. Patyi G, Bódis 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 Thermal Anal Calorimetry 102:349-355.
46. Shenoy SL, Bates WD, Frisch HL, Wnek GE. 2005. Role of chain entanglements on fiber formation during electrospinning of polymer solutions: Good solvent, non-specific polymer-polymer interaction limit. Polymer 46:3372-3384.
47. Liu YY, Li QW, Hu QX, Jing CJ, Wang QG. 2011. A new spurts controllable electrospinning collecting device designed basing on advanced motion control. Applied Mechanics Mater 44:1698-1702.
48. Vajna B, Farkas I, Szabó A, Zsigmond Z, Marosi G. 2010. Raman microscopic evaluation of technology dependent structural differences in tablets containing imipramine model drug. J Pharm Biomed Anal 51:30-38.
49. Rajabi O, Tayyari F, Salari R, Tayyari SF. 2008. Study of interaction of spironolactone with hydroxypropyl-[beta]-cyclodextrin in aqueous solution and in solid state. J Mol Structure 878:78-83.