Polymeric formulations for drug release prepared by hot melt extrusion: application and characterization

Drug Discovery Today

Volumn 20, Issue 7, 2015, Pages 812-823

  Stanković, Milica ^a,b   Frijlink, Henderik W ^a   Hinrichs, Wouter L J ^a  

^a UNIVERSITY OF GRONINGEN   (Netherlands)

^b RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH   (Austria)

Author keywords

[No Author keywords available]

Indexed keywords

ACETIC ACID; ALIPHATIC POLYESTER; CHITOSAN; ETHYLENE CO VINYL ACETATE; ETHYLENE VINYL ALCOHOL COPOLYMER; HYDROXYPROPYLCELLULOSE; HYDROXYPROPYLMETHYLCELLULOSE; LACTAM DERIVATIVE; MACROGOL; POLY(ORTHO ESTER); POLYACRYLIC ACID; POLYANHYDRIDE; POLYESTER; POLYMER; POLYURETHAN; POLYVINYL LACTAM POLYMER; PROPYLENE GLYCOL; STARCH; UNCLASSIFIED DRUG; XANTHAN; DELAYED RELEASE FORMULATION; DRUG; DRUG CARRIER;

ANALYTIC METHOD; ARTICLE; CRYSTAL STRUCTURE; DRUG DELIVERY SYSTEM; DRUG MANUFACTURE; DRUG RELEASE; HOT MELT EXTRUSION; MORPHOLOGY; POROSITY; SURFACE PROPERTY; SUSTAINED DRUG RELEASE; ANIMAL; BIOAVAILABILITY; CHEMISTRY; DELAYED RELEASE FORMULATION; DRUG ADMINISTRATION ROUTE; HEAT; HUMAN; MEDICINAL CHEMISTRY; PHARMACEUTICS; PROCEDURES; SOLUBILITY;

ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DELAYED-ACTION PREPARATIONS; DRUG ADMINISTRATION ROUTES; DRUG CARRIERS; HOT TEMPERATURE; HUMANS; PHARMACEUTICAL PREPARATIONS; POLYMERS; SOLUBILITY; TECHNOLOGY, PHARMACEUTICAL;

EID: 84936846994     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2015.01.012     Document Type: Review

References (138)

1. Görtz, H.H. (1992) Process for the preparation of solid pharmaceutical forms. EP 0240904 B1
2. J. Breitenbach Melt extrusion: from process to drug delivery technology Eur. J. Pharm. Biopharm. 54 2002 107 117
3. M.A. Repka Pharmaceutical applications of hot-melt extrusion: Part II Drug Dev. Ind. Pharm. 33 2007 1043 1057
4. M.A. Repka Applications of hot-melt extrusion in drug delivery Expert Opin. Drug Deliv. 5 2008 1357 1376
5. M.A. Repka Melt extrusion: process to product Expert Opin. Drug Deliv. 9 2012 105 125
6. S. Shah Melt extrusion with poorly soluble drugs Int. J. Pharm. 453 2013 233 252
7. D. Djuric, and P. Kleinebudde Impact of screw elements on continuous granulation with a twin-screw extruder J. Pharm. Sci. 97 2008 4934 4942
8. D. Treffer Hot melt extrusion as a continuous pharmaceutical manufacturing process M.A. Repka, Melt Extrusion. Materials, Technology and Drug Product Design Vol. 9 2013 Springer New York 363 396
9. J. Khinast Nano-extrusion: a one-step process for manufacturing of solid nanoparticle formulations directly from the liquid phase AAPS PharmSciTech 14 2013 601 604
10. S. Singhal Hot melt extrusion technique WebmedCentral Pharm. Sci. WMC001459 2 2011 1 20
11. H.F.J. Giles Extrusion: The Definitive Processing Guide 2005 William Andrew
12. L. Dierickx Co-extrusion as manufacturing technique for multilayer mini-matrices with dual drug release Eur. J. Pharm. Biopharm. 85 2013 1157 1163
13. A. Eitzlmayr Experimental characterization and modeling of twin-screw extruder elements for pharmaceutical hot melt extrusion AIChE J. 59 2013 4440 4450
14. A. Eitzlmayr Mechanistic modeling of modular co-rotating twin-screw extruders Int. J. Pharm. 474 2014 157 176
15. C. Rauwendaal Understanding Extrusion 2nd edn 2010 Hanser Publications
16. V. Taubner, and R. Shishoo Influence of processing parameters on the degradation of poly(l-lactide) during extrusion J. Appl. Polym. Sci. 79 2001 2128 2135
17. D.C. Hinz Process analytical technologies in the pharmaceutical industry: the FDA's PAT initiative Anal. Bioanal. Chem. 384 2006 1036 1042
18. J.A. Covas On-line rotational rheometry for extrusion and compounding operations J. Nonnewton. Fluid Mech. 148 2008 88 96
19. S.E. Barnes Process monitoring of polymer melts using in-line spectroscopy Trans. Inst. Meas. Control 29 2007 453 465
20. V.S. Tumuluri Off-line and on-line measurements of drug-loaded hot-melt extruded films using Raman spectroscopy Int. J. Pharm. 357 2008 77 84
21. D. Markl Supervisory control system for monitoring a pharmaceutical hot melt extrusion process AAPS PharmSciTech 14 2013 1034 1044
22. D. Treffer In-line implementation of an image-based particle size measurement tool to monitor hot-melt extruded pellets Int. J. Pharm. 466 2014 181 189
23. A. Gryczke Hot-melt extrusion process design using process analytical technology M.A. Repka, Melt Extrusion. Materials, Technology and Drug Product Design 2013 Springer 397 431
24. K. Kolter Hot-Melt Extrusion with BASF Pharma Polymers. Extrusion Compendium (2nd revised and enlarged edition) 2012 ISBN 978-3-00-039415-7
25. G. Sax, and G. Winter Mechanistic studies on the release of lysozyme from twin-screw extruded lipid implants J. Control. Release 163 2012 187 194
26. S.M. Aharoni Increased glass transition temperature in motionally constrained semicrystalline polymers Polym. Adv. Technol. 9 1998 169 201
27. S. Madan, and S. Madan Hot melt extrusion and its pharmaceutical applications Asian J. Pharm. Sci. 7 2012 123 133
28. S. Sejal, and M.A. Repka Melt extrusion in drug delivery: three decades of progress M.A. Repka, Melt Extrusion. Materials, Technology and Drug Product Design Vol. 9 2013 Springer New York
29. J.C. Middleton, and A.J. Tipton Synthetic biodegradable polymers as orthopedic devices Biomaterials 21 2000 2335 2346
30. L.S. Nair, and C.T. Laurencin Biodegradable polymers as biomaterials Prog. Polym. Sci. 32 2007 762 798
31. M. Vert Aliphatic polyesters: great degradable polymers that cannot do everything Biomacromolecules 6 2005 538 546
32. N. Saito Synthetic biodegradable polymers as drug delivery systems for bone morphogenetic proteins Adv. Drug Deliv. Rev. 57 2005 1037 1048
33. H. Seyednejad Functional aliphatic polyesters for biomedical and pharmaceutical applications J. Control. Release 152 2011 168 176
34. A-C. Albertsson, and I.K. Varma Aliphatic polyesters: synthesis, properties and applications Adv. Polym. Sci. 157 2002 1 40
35. R.A. Jain The manufacturing techniques of various drug loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices Biomaterials 21 2000 2475 2490
36. M. Labet, and W. Thielemans Synthesis of polycaprolactone: a review Chem. Soc. Rev. 38 2009 3484 3504
37. L. Cheng Characterization and in vitro release of praziquantel from poly(epsilon-caprolactone) implants Int. J. Pharm. 377 2009 112 119
38. Z. Ghalanbor Protein release from poly(lactide-co-glycolide) implants prepared by hot-melt extrusion: thioester formation as a reason for incomplete release Int. J. Pharm. 438 2012 302 306
39. Y. Lemmouchi Biodegradable polyesters for controlled release of trypanocidal drugs: in vitro and in vivo studies Biomaterials 19 1998 1827 1837
40. H. Tian Progress in polymer science biodegradable synthetic polymers: preparation, functionalization and biomedical application Prog. Polym. Sci. 37 2012 237 280
41. A. Göpferich Polymer bulk erosion Macromolecules 9297 1997 2598 2604
42. J. Heller, and J. Barr Poly(ortho esters) - from concept to reality Biomacromolecules 5 2004 1625 1632
43. J. Heller Poly(ortho esters) - their development and some recent applications Eur. J. Pharm. Biopharm. 50 2000 121 128
44. T.J. Johnson Segmented polyurethane intravaginal rings for the sustained combined delivery of antiretroviral agents dapivirine and tenofovir Eur. J. Pharm. Sci. 39 2010 203 212
45. F. Yao, and W.J. Kao Drug release kinetics and transport mechanisms of nondegradable and degradable polymeric delivery systems Expert Opin. Drug Deliv. 7 2011 429 444
46. Q. Guo Tailored drug release from biodegradable stent coatings based on hybrid polyurethanes J. Control. Release 137 2009 224 233
47. C.L. Stevenson Osmotic implantable delivery systems D. Wise, Handbook of Pharmaceutical Controlled Release Technology 2000 Dekker 225 254
48. B. Saad Development of degradable polyesterurethanes for medical applications: in vitro and in vivo evaluations J. Biomed. Mater. Res. 36 1997 65 74
49. J.P. Santerre Understanding the biodegradation of polyurethanes: from classical implants to tissue engineering materials Biomaterials 26 2005 7457 7470
50. A. Göpferich, and J. Tessmar Polyanhydride degradation and erosion Adv. Drug Deliv. Rev. 54 2002 911 931
51. K. Whitaker-Brothers, and K. Uhrich Poly(anhydride-ester) fibers: role of copolymer composition on hydrolytic degradation and mechanical properties J. Biomed. Mater. Res. A 70 2004 309 318
52. K. Kolter Properties and applications of polyvinyllactam polymers M.A. Repka, Melt Extrusion. Materials, Technology and Drug Product Design Vol. 9 2013 Springer New York 83 105
53. ® - the solid solution Drug Deliv. Technol. 10 2010 3
54. A. Almeida Ethylene vinyl acetate as matrix for oral sustained release dosage forms produced via hot-melt extrusion Eur. J. Pharm. Biopharm. 77 2011 297 305
55. M. Fukuda Floating hot-melt extruded tablets for gastroretentive controlled drug release system J. Control. Release 115 2006 121 129
56. Y. Zhu Influence of thermal processing on the properties of chlorpheniramine maleate tablets containing an acrylic polymer Pharm. Dev. Technol. 7 2002 481 489
57. M. Stanković Tailored protein release from biodegradable poly(ε-caprolactone-PEG)-b-poly(ε-caprolactone) multiblock-copolymer implants Eur. J. Pharm. Biopharm. 87 2014 329 337
58. M. Stanković Low temperature extruded implants based on novel hydrophilic multiblock copolymer for long-term protein delivery Eur. J. Pharm. Sci. 49 2013 578 587
59. M.A. Repka Influence of plasticizers and drugs on the physical-mechanical properties of hydroxypropylcellulose films prepared by hot melt extrusion Drug Dev. Ind. Pharm. 25 1999 625 633
60. E. Pinto, and T. Düring Cellulose ethers for extrusion application M.A. Repka, Melt Extrusion. Materials, Technology and Drug Product Design Vol. 9 2013 Springer New York 123 144
61. N.N. Mohammed Klucel™ EF and ELF polymers for immediate-release oral dosage forms prepared by melt extrusion technology AAPS PharmSciTech 13 2012 1158 1169
62. B. Rambali Itraconazole formulation studies of the melt-extrusion process with mixture design Drug Dev. Ind. Pharm. 29 2003 641 652
63. D.A. Miller Hot-melt extrusion for enhanced delivery of drug particles J. Pharm. Sci. 96 2007 361 376
64. M.A. Repka Characterization of cellulosic hot-melt extruded films containing lidocaine Eur. J. Pharm. Biopharm. 59 2005 189 196
65. C. De Brabander Development and evaluation of sustained release mini-matrices prepared via hot melt extrusion J. Control. Release 89 2003 235 247
66. D. Henrist, and J.P. Remon Influence of the process parameters on the characteristics of starch based hot stage extrudates Int. J. Pharm. 189 1999 7 17
67. B. Wolf Polysaccharide functionality through extrusion processing Curr. Opin. Colloid Interface Sci. 15 2010 50 54
68. Ghebremeskel, A.N. and Spada, L.T. (2012) Sustained release latanoprost implant. US 2012/0276186 A1
69. S.U. Schilling Influence of plasticizer type and level on the properties of Eudragit S100 matrix pellets prepared by hot-melt extrusion J. Microencapsul. 27 2010 521 532
70. N.R. Trivedi Pharmaceutical approaches to preparing pelletized dosage forms using the extrusion-spheronization process Crit. Rev. Ther. Drug Carr. Syst. 24 2007 1 40
71. J.O. Morales, and J.T. McConville Manufacture and characterization of mucoadhesive buccal films Eur. J. Pharm. Biopharm. 77 2011 187 199
72. Z. Ghalanbor Interdependency of protein-release completeness and polymer degradation in PLGA-based implants Eur. J. Pharm. Biopharm. 85 2013 624 630
73. S.S. Lee Biodegradable implants for sustained drug release in the eye Pharm. Res. 27 2010 2043 2053
74. J.C. Wright, and D.J. Burgess Long Acting Injections and Implants 2012 Springer Netherlands
75. M. Maniruzzaman Taste masking of paracetamol by hot-melt extrusion: an in vitro and in vivo evaluation Eur. J. Pharm. Biopharm. 80 2012 433 442
76. M.A. Repka Applications of hot-melt extrusion for drug delivery Expert Opin. Drug Deliv. 5 2008 1357 1376
77. A. Kalivoda Application of mixtures of polymeric carriers for dissolution enhancement of fenofibrate using hot-melt extrusion Int. J. Pharm. 429 2012 58 68
78. P. Srinarong Improved dissolution behavior of lipophilic drugs by solid dispersions: the production process as starting point for formulation considerations Expert Opin. Drug Deliv. 8 2011 1121 1140
79. T. Vasconcelos Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs Drug Discov. Today 12 2007 1068 1075
80. A. Forster Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis Int. J. Pharm. 226 2001 147 161
81. A. Forster Characterization of glass solutions of poorly water-soluble drugs produced by melt extrusion with hydrophilic amorphous polymers J. Pharm. Pharmacol. 53 2001 303 315
82. L.S. Ranzani Enhanced in vivo absorption of CB-1 antagonist in rats via solid solutions prepared by hot-melt extrusion Drug Dev. Ind. Pharm. 37 2011 694 701
83. F. Jijun Nimodipine (NM) tablets with high dissolution containing NM solid dispersions prepared by hot-melt extrusion Drug Dev. Ind. Pharm. 37 2011 934 944
84. H. He In vitro and in vivo evaluation of fenofibrate solid dispersion prepared by hot-melt extrusion Drug Dev. Ind. Pharm. 36 2010 681 687
85. K. Tahara Overall mechanism behind matrix sustained release (SR) tablets prepared with hydroxypropyl methylcellulose 2910 J. Control. Release 35 1995 59 66
86. S.U. Schilling Citric acid monohydrate as a release-modifying agent in melt extruded matrix tablets Int. J. Pharm. 361 2008 158 168
87. S. Fredenberg The mechanisms of drug release in poly(lactic-co-glycolic acid)-based drug delivery systems - a review Int. J. Pharm. 415 2011 34 52
88. M. Gosau, and B.W. Muller Release of gentamicin sulphate from biodegradable PLGA-implants produced by hot melt extrusion Pharmazie 65 2010 487 492
89. K. Rajagopal Trehalose limits BSA aggregation in spray-dried formulations at high temperatures: implications in preparing polymer implants for long-term protein delivery J. Pharm. Sci. 102 2013 2655 2666
90. Z. Ghalanbor Improved lysozyme stability and release properties of poly(lactide-co-glycolide) implants prepared by hot-melt extrusion Pharm. Res. 27 2010 371 379
91. D. Li PLA/PEG-PPG-PEG/dexamethasone implant prepared by hot-melt extrusion for controlled release of immunosuppressive drug to implantable medical devices. Part 2: In vivo evaluation Drug Deliv. 20 2013 134 142
92. L. Cheng In vitro and in vivo evaluation of praziquantel loaded implants based on PEG/PCL blends Int. J. Pharm. 387 2010 129 138
93. L.C. Li Polyanhydride implant for antibiotic delivery - from the bench to the clinic Adv. Drug Deliv. Rev. 54 2002 963 986
94. A. Rothen-Weinhold Release of BSA from poly(ortho ester) extruded thin strands J. Control. Release 71 2001 31 37
95. L.K. Fung, and W.M. Saltzman Polymeric implants for cancer chemotherapy Adv. Drug Deliv. Rev. 26 1997 209 230
96. J. Siepmann, and F. Siepmann Mathematical modeling of drug delivery Int. J. Pharm. 364 2008 328 343
97. H. Croxatto Progestin implants Steroids 65 2000 681 685
98. Shiah, J.-G. et al. (2011) Ocular implant made by a double extrusion process. US 8,034,366 B2
99. J.L. Bourges Intraocular implants for extended drug delivery: therapeutic applications Adv. Drug Deliv. Rev. 58 2006 1182 1202
100. J.I. Lim Visual and anatomic outcomes associated with posterior segment complications after ganciclovir implant procedures in patients with AIDS and cytomegalovirus retinitis Am. J. Ophthalmol. 127 1999 288 293
101. P.J. Kappel Outcomes associated with ganciclovir implants in patients with AIDS-related cytomegalovirus retinitis Ophthalmology 113 2006 673 683
102. A. Loxley Ethylene vinyl acetate intravaginal rings for the simultaneous delivery of the antiretroviral UC781 and contraceptive levonorgestrel Drug Deliv. Transl. Res. 1 2011 247 255
103. J.A.H. Van Laarhoven In vitro release properties of etonogestrel and ethinyl estradiol from a contraceptive vaginal ring Int. J. Pharm. 232 2002 163 173
104. K.M. Gupta Polyurethane intravaginal ring for controlled delivery of dapivirine, a nonnucleoside reverse transcriptase inhibitor of HIV-1 J. Pharm. Sci. 97 2008 4228 4239
105. J.T. Clark Quantitative evaluation of a hydrophilic matrix intravaginal ring for the sustained delivery of tenofovir J. Control. Release 163 2012 240 248
106. Darougar, D. and Darougar, S. (1982) Lacrisert Merc & Co. US Patent 4,343,787
107. A.P. Sam Controlled release contraceptive devices: a status report J. Control. Release 22 1992 35 46
108. J. Breitenbach, and J. Lewis Two concepts one technology: controlled-release and solid dispersions with Meltrex M.J. Rathbone, Modified Drug Release Technology 2nd edn 2008 Informa Healthcare 125 134
109. E. Cottam Effect of sterilisation by gamma irradiation on the ability of polycaprolactone (PCL) to act as a scaffold material Med. Eng. Phys. 31 2009 221 226
110. F. Hasanain Gamma sterilization of pharmaceuticals - a review of the irradiation of excipients, active pharmaceutical ingredients, and final drug product formulations PDA J. Pharm. Sci. Technol. 68 2014 113 137
111. C.C. Verheyen Evaluation of hydroxylapatite/poly(l-lactide) composites: mechanical behavior J. Biomed. Mater. Res. 26 1992 1277 1296
112. P. Puolakkainen The effect of sterilization on transforming growth factor beta isolated from demineralized human bone Transfusion 33 1993 679 685
113. W. Wang Instability, stabilization, and formulation of liquid protein pharmaceuticals Int. J. Pharm. 185 1999 129 188
114. L. Saerens Raman spectroscopy for the in-line polymer-drug quantification and solid state characterization during a pharmaceutical hot-melt extrusion process Eur. J. Pharm. Biopharm. 77 2011 158 163
115. G.P. Andrews Physicochemical characterization and drug-release properties of celecoxib hot-melt extruded glass solutions J. Pharm. Pharmacol. Pharmacol. 62 2010 1580 1590
116. A.M. Agrawal Characterization and performance assessment of solid dispersions prepared by hot melt extrusion and spray drying process Int. J. Pharm. 457 2013 71 81
117. J-B. Park New investigation of distribution imaging and content uniformity of very low dose drugs using hot-melt extrusion method Int. J. Pharm. 458 2013 245 253
118. S. Qi Characterisation of solid dispersions of paracetamol and EUDRAGIT E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis Int. J. Pharm. 354 2008 158 167
119. J. Djuris Preparation of carbamazepine-Soluplus solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting Eur. J. Pharm. Biopharm. 84 2013 228 237
120. J. Chesko Characterization of antigens adsorbed to anionic PLG microparticles by XPS and TOF-SIMS J. Pharm. Sci. 97 2008 1443 1453
121. M.A. Repka Production and characterization of hot-melt extruded films containing clotrimazole Drug Dev. Ind. Pharm. 29 2003 757 765
122. Z. Guo The utilization of drug-polymer interactions for improving the chemical stability of hot-melt extruded solid dispersions J. Pharm. Pharmacol. 66 2014 285 296
123. P. Srinarong Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tablets Pharm. Dev. Technol. 15 2010 460 468
124. L. Li Characterization of poly(ethylene oxide) as a drug carrier in hot-melt extrusion Drug Dev. Ind. Pharm. 32 2006 991 1002
125. S.J. Byard Studies on the crystallinity of a pharmaceutical development drug substance J. Pharm. Sci. 94 2005 1321 1335
126. S. Ozkan Multifunctional protein-encapsulated polycaprolactone scaffolds: fabrication and in vitro assessment for tissue engineering Biomaterials 30 2009 4336 4347
127. Z. Dong Evaluation of solid state properties of solid dispersions prepared by hot-melt extrusion and solvent co-precipitation Int. J. Pharm. 355 2008 141 149
128. Allergan Ozurdex Implant-Product Characteristics. OZURDEX 700 Micrograms Intravitreal Implant in Applicator 2010 Available at: http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/human/001140/WC500095499.pdf
129. AstraZeneca Zoladex (Goserelin Acetate Implant 3.6 mg) - Prescribing Information 2010 Available at: http://www.accessdata.fda.gov/drugsatfda-docs/label/2011/019726s054,020578s032lbl.pdf
130. J.A.H. Van Laarhoven Effect of supersaturation and crystallization phenomena on the release properties of a controlled release device based on EVA copolymer J. Control. Release 82 2002 309 317
131. E.M. Sherman, and J.G. Steinberg Heat-stable ritonavir tablets: a new formulation of a pharmacokinetic enhancer for HIV Expert Opin. Pharmacother. 12 2011 141 148
132. C.E. Klein The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect J. Acquir. Immune Defic. Syndr. 44 2007 401 410
133. Baert, L.E.C. et al. (2003) Antifungal compositions with improved bioavailability. US Patent 6,509,038 B2
134. ® (griseofulvin ultramicrosize) tablets, USP 125 mg; 250 mg. Available at: http://www.accessdata.fda.gov/drugsatfda-docs/label/2007/050475s053lbl.pdf
135. ® Monograph (Verapamil Hydrochloride) Extended-Release Tablets 2011
136. A. Gryczke Development and evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granules prepared by hot melt extrusion Colloids Surf. B: Biointerfaces 86 2011 275 284
137. Joshi, Y. et al. (2007) Formulation comprising metformin and vildagliptin. WO/2007/041053
138. ® (Azithromycin Tablets) 2013 Available at: http://www.labeling.pfizer.com/ShowLabeling.aspx?id=511