Pharmaceutical plasticizers for drug delivery systems

Current Drug Delivery

Volumn 9, Issue 2, 2012, Pages 148-163

  El Gendy, Nashwa A ^a,b  

^a UNIVERSITY OF KANSAS   (United States)

^b Beni Suef University   (Egypt)

Author keywords

Controlled release; Drug delivery; Plasticizers; Polymer

Indexed keywords

ACETYLTRIBUTYL CITRATE; ACETYLTRIETHYL CITRATE; ADIPIC ACID; CARBON DIOXIDE; CHLORPHENIRAMINE MALEATE; CITRIC ACID; CITRIC ACID TRIBUTYL ESTER; CITRIC ACID TRIETHYL ESTER; ETHYLENE VINYL ACETATE COPOLYMER; GELUCIRE; GLYCEROL; GLYCEROL BEHENATE; HYDROXYPROPYLMETHYLCELLULOSE; IBUPROFEN; MACROGOL; METHYL PARABEN; PECTIN; PHOSPHATIDYLCHOLINE; PHTHALIC ACID; PHTHALIC ACID DIBUTYL ESTER; PHTHALIC ACID DIETHYL ESTER; PLASTICIZER; PROPYLENE GLYCOL; SEBACIC ACID DIBUTYL ESTER; SEBACIC ACID DIETHYL ESTER; SORBITOL; STEARIC ACID; TRIACETIN; TRIMELLITATE; UNCLASSIFIED DRUG;

CONCENTRATION (PARAMETERS); DIFFERENTIAL SCANNING CALORIMETRY; DIFFUSION COEFFICIENT; DISPERSION; DRUG DELIVERY SYSTEM; DRUG DIFFUSION; DRUG DOSAGE FORM; DRUG GRANULATION; DRUG RELEASE; EMULSION; EVAPORATION; GLASS TRANSITION TEMPERATURE; HUMIDITY; HYDROGEN BOND; HYDROPHILICITY; HYDROPHOBICITY; HYPERBARISM; IN VITRO STUDY; LOW TEMPERATURE; MELTING POINT; MOLECULAR WEIGHT; MUCOADHESION; NANOPHARMACEUTICS; PARTICLE SIZE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; REVIEW; SCANNING ELECTRON MICROSCOPY; TENSILE STRENGTH; VAPORIZATION; VISCOSITY; X RAY DIFFRACTION;

EID: 84857847854     PISSN: 15672018     EISSN: 18755704     Source Type: Journal    
DOI: 10.2174/156720112800234602     Document Type: Review

References (92)

1. Repka, M. A.; McGinity, J. W. Influence of Vitamin E TPGS on the properties of hydrophilic films produced by hot-melt extrusion. Int. J. Pharm. 2000, 202 (1-2), 63-70.
2. Flößer, A.; Kolter, K.; Reich, H. B.; Schepky, G. Variation of composition of an enteric formulation based on Kollicoat MAE 30 D. Drug Dev. Ind. Pharm. 2000, 26 (2), 177-187.
3. Wang, C. C.; Zhang, G. Influence of plasticizers on the mechanical properties of pellets containing Eudragit RS 30 D. Int. J. Pharm. 1997, 152 (2), 153-163.
4. Zhu, Y.; Shah, N. H.; Malick, A. W.; Infeld, M. H.; McGinity, J. W. Solid-state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate. Int. J. Pharm. 2002, 241 (2), 301-310.
5. Verreck, G.; Decorte, A.; Heymans, K.; Adriaensen, J.; Cleeren, D.; Jacobs, A.; Liu, D.; Tomasko, D.; Arien, A.; Peeters, J. 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. 2005, 26 (3-4), 349-358.
6. Tatavarti, A. S.; Dollimore, D.; Alexander, K. S. A thermogravimetric analysis of non-polymeric pharmaceutical plasticizers: Kinetic analysis, method validation, and thermal stability evaluation. AAPS J. 2002, 4 (4), 231-242.
7. Wu, C.; McGinity, J. W. Non-traditional plasticization of polymeric films. Int. J. Pharm. 1999, 177 (1), 15-27.
8. G. Handbook of Plasticizers, Chem Tee: Onairo, Canada, 1999; pp. 437-439.
9. Gutierrez-Rocca, J. C.; McGinity, J. W. Influence of water soluble and insoluble plasticizers on the physical and mechanical properties of acrylic resin copolymers. Int. J. Pharm. 1994, 103 (3), 293-301.
10. Repka, M. A.; McGinity, J. W. Physical-mechanical, moisture absorption and bioadhesive properties of hydroxypropylcellulose hot-melt extruded films. Biomaterials 2000, 21 (14), 1509-1517.
11. G. S. Film coating theory and practice. J. Pharm. Sci. 1966, 55 (1), 81-89.
12. Repka, M. A.; Majumdar, S.; Kumar Battu, S.; Srirangam, R.; Upadhye, S. B. Applications of hot-melt extrusion for drug delivery. Expert Opin. Drug Deliv. 2008, 5 (12), 1357-1376.
13. Baiardo, M.; Frisoni, G.; Scandola, M.; Rimelen, M.; Lips, D.; Ruffieux, K.; Wintermantel, E. Thermal and mechanical properties of plasticized poly (L lactic acid). J. Appl. Polym. Sci. 2003, 90 (7), 1731-1738.
14. Lin, A.; Muhammad, N.; Pope, D.; Augsburger, L. Effect of curing and storage conditions on drug release from pellets coated with Eudragit NE30D. AAPS Pharm. Sci. 2000, 2 (4).
15. Mehuys, E.; Vervaet, C.; Remon, J. P. Hot-melt extruded ethylcellulose cylinders containing a HPMC-Gelucire core for sustained drug delivery. J. Control. Release 2004, 94 (2-3), 273-280.
16. Verreck, G.; Decorte, A.; Li, H.; Tomasko, D.; Arien, A.; Peeters, J.; Rombaut, P.; Van den Mooter, G.; Brewster, M. E. The effect of pressurized carbon dioxide as a plasticizer and foaming agent on the hot melt extrusion process and extrudate properties of pharmaceutical polymers. J. Supercrit. fluids 2006, 38 (3), 383-391.
17. Chamarthy, S. P.; Pinal, R. Plasticizer concentration and the performance of a diffusion-controlled polymeric drug delivery system. Colloid Surface A 2008, 331 (1-2), 25-30.
18. Coleman, N. J.; Craig, D. Q. M. Modulated temperature differential scanning calorimetry: a novel approach to pharmaceutical thermal analysis. Int. J. Pharm. 1996, 135 (1-2), 13-29.
19. Ferrero, M.; Velasco, M.; Ford, J.; Rajabi-Siahboomi, A.; Muñoz, A.; Jiménez-Castellanos, M. Determination of the glass transition temperatures of some new methyl methacrylate copolymers using modulated temperature differential scanning calorimetry (MTDSC). Pharm. Res. 1999, 16 (9), 1464-1469.
20. nd ed.; Wiley&Sons: London, 1999.
21. Raloff, J. Girls may face risks from phthalates. Sciences. 2000, 158 (11), 165-165.
22. th ed.; Taylor and Francis group: Boca Raton, Fl., 2007; pp. 104-110.
23. Siepmann, J.; Lecomte, F.; Bodmeier, R. Diffusion-controlled drug delivery systems: calculation of the required composition to achieve desired release profiles. J. Control. Release 1999, 60 (2-3), 379-389.
24. R. D. Polymeric plasticizers for higher performance flexible PVC applications. J. Vinyl Technol. 1991, 13 (3), 130-133.
25. Ghebremeskel, A. N.; Vemavarapu, C.; Lodaya, M. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: Selection of polymer-surfactant combinations using solubility parameters and testing the processability. Int. J. Pharm. 2007, 328 (2), 119-129.
26. Follonier, N.; Doelker, E.; Cole, E. T. Evaluation of hot-melt extrusion as a new technique for the production of polymer-based pellets for sustained release capsules containing high loadings of freely soluble drugs. Drug Dev. Ind. Pharm. 1994, 20 (8), 1323-1339.
27. Ghebre-Selassie, I.; Martin, C. Pharmaceutical Extrusion Technology, CRC Press: 2003.
28. Zhang, F.; McGinity, J. W. Properties of sustained-release tablets prepared by hot-melt extrusion. Pharm. Dev. Technol. 1999, 4 (2), 241-250.
29. Tate, S.; Chiba, S.; Tani, K. Melt viscosity reduction of poly (ethylene terephthalate) by solvent impregnation. Polymer 1996, 37 (19), 4421-4424.
30. Frohoff-Hulsmann, M. A.; Schmitz, A.; Lippold, B. C. Aqueous ethyl cellulose dispersions containing plasticizers of different water solubility and hydroxypropyl methylcellulose as coating material for diffusion pellets:I. Drug release rates from coated pellets. Int. J. Pharm. 1999, 177 (1), 69-82.
31. Skultety, P. F.; Sims, S. M. Evaluation of the loss of propylene glycol during aqueous film coating. Drug Dev. Ind. Pharm. 1987, 13 (12), 2209-2219.
32. Wu, C.; McGinity, J. W. Influence of methylparaben as a solid-state plasticizer on the physicochemical properties of Eudragit RS PO hot-melt extrudates. Eur. J. Pharm. Biopharm. 2003, 56 (1), 95-100.
33. Schilling, S. U.; Shah, N. H.; Malick, A. W.; Infeld, M. H.; McGinity, J. W. Citric acid as a solid state plasticizer for Eudragit RS PO. J. Pharm. Pharmacol. 2007, 59 (11), 1493-1500.
34. Desai, D. Solid-State Plasticizers for Melt Extrusion. PhD Thesis, The University of Rhode Island, 2008.
35. O'Donnell, P. B.; Wu, C.; Wang, J.; Wang, L.; Oshlack, B.; Chasin, M.; Bodmeier, R.; McGinity, J. W. Aqueous pseudolatex of zein for film coating of solid dosage forms. Eur. J. Pharm. Biopharm. 1997, 43 (1), 83-89.
36. Wu, C.; McGinity, J. W. Influence of relative humidity on the mechanical and drug release properties of theophylline pellets coated with an acrylic polymer containing methylparaben as a non-traditional plasticizer. Eur. J. Pharm. Biopharm. 2000, 50 (2), 277-284.
37. Wu, C.; McGinity, J. W. Influence of ibuprofen as a solid-state plasticizer in Eudragit RS 30 D on the physicochemical properties of coated beads. AAPS Pharm. Sci. Tech. 2001, 2 (4), 35-43.
38. ® 100 matrices for the controlled release of lobenzarit disodium. Drug Dev. Ind. Pharm. 1999, 25 (2), 229-233.
39. Palmieri, G. F.; Lovato, D.; Martelli, S. New controlled-release ibuprofen tablets. Drug Dev. Ind. Pharm. 1999, 25 (5), 671-677.
40. Sanghavi, N.; Bijlani, C.; Kanath, P.; Sarwade, V. Matrix tablets of salbutamol sulphate. Drug Dev. Ind. Pharm. 1990, 16 (12), 1955-1961.
41. Lachman, L.; Lieberman, H. A.; Kanig, J. L. The Theory and Practice of Industrial Pharmacy, 3rd ed.; Lea & Febiger: Philadelphia, 1986.
42. th ed.; Lippincott Williams &Wilkins: Baltimore, MD, 2000.
43. Sears, J. K.; Darby, J. R. The Technology of Plasticizers, Wiley and Sons: New York, 1982.
44. A. S. Plasticizers: Principles and Practice, Institute of Materials: Philadelphia, PA., 1995; pp. 45-50.
45. Bruce, L. D.; Petereit, H. U.; Beckert, T.; McGinity, J. W. Properties of enteric coated sodium valproate pellets. Int. J. Pharm. 2003, 264 (1-2), 85-96.
46. rd ed.; Feton, L. A.; McGinity, J. W., Eds. Informa Healthcare: New York, 2008.Vol. 4, pp: 112-115.
47. Djuric, D.; Karl, M.; Kolter, K.; Maschke, A.; Nalawade, S. Suitability of Plasticized Polymers for Hot Melt Extrusion. 2010.
48. Bose, S.; Bogner, R. H. Solventless pharmaceutical coating processes: a review. Pharm. Dev. Technol. 2007, 12 (2), 115-131.
49. Luo, Y.; Zhu, J.; Ma, Y.; Zhang, H. Dry coating, a novel coating technology for solid pharmaceutical dosage forms. Int. J. Pharm. 2008, 358 (1-2), 16-22.
50. Kibria, G.; Roni, M. A.; Absar, M. S.; Jalil, R. Effect of plasticizer on release kinetics of diclofenac sodium pellets coated with Eudragit RS 30 D. AAPS Pharm. Sci. Tech. 2008, 9 (4), 1240-1246.
51. Felton, L.; Haase, M.; Shah, N.; Zhang, G.; Infeld, M.; Malick, A.; McGinity, J. Physical and enteric properties of soft gelatin capsules coated with Eudragit L 30 D-55. Int. J. Pharm. 1995, 113 (1), 17-24.
52. Shah, P. S.; Zatz, J. L. Plasticization of cellulose esters used in the coating of sustained release solid dosage forms. Drug Dev. Ind. Pharm. 1992, 18 (16), 1759-1772.
53. Vesey, C. F.; Farrell, T.; Rajabi-Siahboomi, A. R. Evaluation of alternative plasticizers for surelease, an aqueous ethylcellulose dispersion for modified release film-coating. DEP 2005, 67, 20.5.
54. Rohera, B. D.; Parikh, N. H. Influence of plasticizer type and coat level on Surelease film properties. Pharm. Dev. Technol. 2002, 7 (4), 407-420.
55. Hagesaether, E.; Arne Sande, S. Effect of pectin type and plasticizer on in vitro mucoadhesion of free films. Pharm. Dev. Technol. 2008, 13 (2), 105-114.
56. Tymes, N. W.; Shah, V. P.; Skelly, J. P. In vitro release profile of estradiol transdermal therapeutic systems. J. Pharm. Sci. 1990, 79 (7), 601-602.
57. Shin, S. C.; Lee, H. J. Controlled release of triprolidine using ethylene-vinyl acetate membrane and matrix systems. Eur. J. Pharm. Biopharm. 2002, 54 (2), 201-206.
58. L. L. Determination of in vivo and in vitro release of theophylline aminoisobutanol in a prolonged action system. J. Pharm. Sci. 1965, 54 (3), 457-458.
59. Coutel-Egros, A.; Maitani, Y.; Veillard, M.; Machida, Y.; Nagai, T. Combined effects of pH, cosolvent and penetration enhancers on the in vitro buccal absorption of propranolol through excised hamster cheek pouch. Int. J. Pharm. 1992, 84 (2), 117-128.
60. Donbrow, M.; Friedman, M. Enhancement of permeability of ethyl cellulose films for drug penetration. J. Pharm. Pharmacol. 1975, 27 (9), 633-646.
61. Michaels, A. S.; Bixler, H. J. Flow of gases through polyethylene. J. Polym. Sci. 1961, 50 (154), 413-439.
62. G. Design and evaluation of transdermal drug delivery system of valsartan using glycerine as plasticizer. Inter. J. Pharm. Tech. Res. 2011, 3 (2), 185-192.
63. El-Gendy, N. A.; Sabry, N. A.; El-Attar, M.; Omar, E.; Mahmoud, M. Transdermal delivery of salbutamol sulphate: Formulation and evaluation. Pharm. Dev. Technol. 2009, 14 (2), 216-225.
64. Mundada, A. S.; Avari, J. G. Evaluation of gum copal as rate controlling membrane for transdermal application: effect of plasticizers. Acta Pharm. Sci. 2010, 52, 31-38.
65. El-Gendy, N.; Abdelbary, G.; El-Komy, M.; Saafan, A. Design and Evaluation of a bioadhesive patch for topical delivery of gentamicin sulphate. Curr. Drug Del. 2009, 6 (1), 50-57.
66. R. Tableting of coated pellets. Eur. J. Pharm. Biopharm. 1997, 43 (1), 1-8.
67. Amighi, K.; Möes, A. Influence of plasticizer concentration and storage conditions on the drug release rate from Eudragit RS30D film-coated sustained-release theophylline pellets. Eur. J. Pharm. Biopharm. 1996, 42 (1), 29-35.
68. Hamed, E.; Sakr, A. Effect of curing conditions and plasticizer level on the release of highly lipophilic drug from coated multiparticulate drug delivery system. Pharm. Dev. Technol. 2003, 8 (4), 397-407.
69. Zhu, Y.; Mehta, K. A.; McGinity, J. W. Influence of plasticizer level on the drug release from sustained release film coated and hot-melt extruded dosage forms. Pharm. Dev. Technol. 2006, 11 (3), 285-294.
70. Bodmeier, R.; Paeratakul, O. Propranolol HCl release from acrylic films prepared from aqueous latexes. Int. J. Pharm. 1990, 59 (3), 197-204.
71. Colombo, P.; Bettini, R.; Massimo, G.; Catellani, P. L.; Santi, P.; Peppas, N. A. Drug diffusion front movement is important in drug release control from swellable matrix tablets. J. Pharm Sci 1995, 84 (8), 991-997.
72. R. Influence of hydrophilic character of plasticizer and polymer on certain film properties. Int. J. Pharm. 1982, 11 (1), 1-9.
73. Johnson, K.; Hathaway, R.; Leung, P.; Franz, R. Effect of triacetin and polyethylene glycol 400 on some physical properties of hydroxypropyl methylcellulose free films. Int. J. Pharm. 1991, 73 (3), 197-208.
74. Lin, S. Y.; Lee, C. J.; Lin, Y. Y. The effect of plasticizers on compatibility, mechanical properties, and adhesion strength of drug-free Eudragit E films. Pharm. Res. 1991, 8 (9), 1137-1143.
75. Lippold, B. C.; Lippold, B. H.; Sutter, B. K.; Gunder, W. Properties of Aqueous, Plastic Izer-Containing Ethyl Cellulose Dispersions and Prepared Films in Respect to the Production of oral Extended Release Formulations. Drug Dev. Ind. Pharm. 1990, 16 (11), 1725-1747.
76. Entwistle, C.; Rowe, R. Plasticization of cellulose ethers used in the film coating of tablets. J. Pharm. Pharmacol. 1979, 31 (1), 269-272.
77. Eckersley, S.; Rudin, A. The effect of plasticization and pH on film formation of acrylic latexes. J. Appl. Polym. Sci. 1993, 48 (8), 1369-1381.
78. Shailaja, D.; Yaseen, M. Controlled release from PVC matrices: effect of four phthalate plasticizers on diffusion of THF. Eur. Polym. J. 1992, 28 (11), 1321-1324.
79. Bodmeier, R.; Paeratakul, O. The effect of curing on drug release and morphological properties of ethylcellulose pseudolatex-coated beads. Drug Dev. Ind. Pharm. 1994, 20 (9), 1517-1533.
80. Sinko, C. M.; Amidon, G. L. Plasticizer-induced changes in the mechanical rate of response of film coatings: an approach to quantitating plasticizer effectiveness. Int. J. Pharm. 1989, 55 (2-3), 247-256.
81. Seow, C.; Cheah, P.; Chang, Y. Antiplasticization by Water in Reduced Moisture Food Systems. J. Food Sci. 1999, 64 (4), 576-581.
82. Marzec, A.; Lewicki, P. P. Antiplasticization of cereal-based products by water. Part I. Extruded flat bread. J. Food Eng. 2006, 73 (1), 1-8.
83. Gondek, E.; Lewicki, P. P. Antiplasticization of cereal-based products by water. Part II: Breakfast cereals. J. Food Eng. 2006, 77 (3), 644-652.
84. A. Some relations between molecular structure and plasticizing effect. J. Appl. Phys. 1940, 11 (4), 255-261.
85. Gondaliya, D.; Pundarikakshudu, K. The fabrication and evaluation of the formulation variables of a controlled-porosity osmotic drug delivery system with diltiazem hydrochloride. Pharm. Technol. 2003, 27 (9), 58-68.
86. Chiou, J.; Barlow, J. W.; Paul, D. Plasticization of glassy polymers by CO2. J. Appl. Polym. Sci. 1985, 30 (6), 2633-2642.
87. Wesseling, M.; Kuppler, F.; Bodmeier, R. Tackiness of acrylic and cellulosic polymer films used in the coating of solid dosage forms. Eur. J. Pharm. Biopharm. 1999, 47 (1), 73-78.
88. Nakagami, H.; Keshikawa, T.; Matsumura, M.; Tsukamoto, H. Application of aqueous suspensions and latex dispersions of water-insoluble polymers for tablet and granule coatings. Chem. Pharm. Bull. 1991, 39 (7), 1837-1842.
89. Thoma, K.; Bechtold, K. Influence of aqueous coatings on the stability of enteric coated pellets and tablets. Eur. J. Pharm. Biopharm. 1999, 47 (1), 39-50.
90. Arwidsson, H.; Hjelstuen, O.; Ingason, D.; Graffner, C. Properties of ethyl cellulose films for extended release. II: Influence of plasticizer content and coalescence conditions when using aqueous dispersions. Acta Pharm. Nordica 1991, 3 (2), 65-70.
91. Bodmeier, R.; Paeratakul, O. Leaching of water-soluble plasticizers from polymeric films prepared from aqueous colloidal polymer dispersions. Drug Dev. Ind. Pharm. 1992, 18 (17), 1865-1882.
92. Heng, P. W. S.; Chan, L.; Ong, K. Influence of storage conditions and type of plasticizers on ethylcellulose and acrylate films formed from aqueous dispersions. J. Pharm. Pharm. Sci. 2003, 6 (3), 334-344.