Effectiveness of various drug carriers in controlled release formulations of raloxifene HCl prepared by melt mixing

Current Drug Delivery

Volumn 6, Issue 5, 2009, Pages 425-436

  Bikiaris, Dimitrios ^a   Karavelidis, Vassilios ^a   Karavas, Evangelos ^b  

^a ARISTOTLE UNIVERSITY OF THESSALONIKI   (Greece)

^b Pharmaceutical Industry   (Greece)

Author keywords

Aliphatic polyesters; Biocompatible polymers; Gelucire; Melt mixing; PEG; Raloxifene HCl

Indexed keywords

DRUG CARRIER; GELUCIRE; MACROGOL; POLY(ETHYLENE SUCCINATE); POLY(PROPYLENE ADIPATE); POLY(PROPYLENE SUCCINATE); POLYESTER; POLYLACTIDE; RALOXIFENE; UNCLASSIFIED DRUG;

ARTICLE; BODY TEMPERATURE; CELL VIABILITY; CONTROLLED RELEASE FORMULATION; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SOLUBILITY; ENDOTHELIUM CELL; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; INFRARED SPECTROSCOPY; MELTING POINT; PARTICLE SIZE; PHYSICAL CHEMISTRY; POLYMERIZATION; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; THERMOSTABILITY; X RAY DIFFRACTION;

ADIPIC ACIDS; CELL SURVIVAL; CELLS, CULTURED; DELAYED-ACTION PREPARATIONS; DRUG CARRIERS; DRUG STABILITY; ENDOTHELIAL CELLS; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MICROSCOPY, ELECTRON, SCANNING; NANOPARTICLES; PARTICLE SIZE; POLYESTERS; POLYETHYLENES; POLYPROPYLENES; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; SUCCINATES; TRANSITION TEMPERATURE; X-RAY DIFFRACTION;

EID: 72149089570     PISSN: 15672018     EISSN: None     Source Type: Journal    
DOI: 10.2174/156720109789941632     Document Type: Article

References (52)

1. 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, 1323-1339.
2. McGinity, J.W.; Zhang, F.; Repka, M.A.; Koleng, J.J. Hot-melt extrusion as a pharmaceutical process. Am. Pharm. Rev., 2001, 4, 25-36.
3. Zhang, F.; McGinity, J.W. Properties of sustained release tablets prepared by hot-melt extrusion. Pharm. Dev. Technol., 1999, 4, 241-50.
4. Verhoeven, E.; De Beer, T.R.M.; Van den Mooter, G.; Remon, J.P.; Vervaet, C. Eur. J. Pharm. Biopharm., 2008, 69, 312-319.
5. De Brabander, C.; Vervaet, C.; Remon, J.P. Development and evaluation of sustained release mini-matrices prepared via hot melt extrusion, J. Control. Release, 2003, 89, 235-247.
6. Nakamichi, K.; Nakano, T.; Yasuura, H.; Izumi, S.; Kawashima, Y. The role of the kneading paddle and the effects of screw revolution speed and water content on the preparation of solid dispersions using a twin-screw extruder. Int. J. Pharm., 2002, 241, 203-211.
7. Nakamichi, K.; Nakano, T.; Yasuura, H.; Izumi, S.; Kawashima, Y. Stabilization of sodium guaiazulene sulfonate in granules for tableting prepared using a twin-screw extruder. Eur. J. Pharm. Biopharm., 2003, 56, 347-354.
8. Van Melkebeke, B.; Vermeulen, B.; Vervaet, C.; Remon, J.P. Melt granulation using a twin-screw extruder: a case study. Int. J. Pharm., 2006, 326, 89-93.
9. Young, C.R.; Koleng, J.J.; McGinity, J.W. Production of spherical pellets by a hot-melt extrusion and spheronization process. Int. J. Pharm., 2002, 242, 87-92.
10. Folloniers, N.; Doelker, E.; Cole, E.T. Various ways of modulating the release of diltiazem hydrochloride from hot-melt extruded sustained release pellets prepared using polymeric materials. J. Control. Release, 1995, 36, 243-50.
11. Bruce, L.D.; Shah, N.A.; Malick, A.W.; Infeld, M.H.; McGinity, J.W. Properties of hot-melt extruded tablet formulations for colonic delivery of 5-amino salicylic acid. Eur. J. Pharm. Biopharm., 2005, 59, 85-97.
12. Repka, M.A.; Gutta, K.; Prodduturi, S.; Munjal, M.; Stodghill, S.P. Characterization of cellulose hot-melt extruded films containing lidocaine. Eur. J. Pharm. Biopharm., 2005, 59, 189-196.
13. Repka, M.A.; Gerding, T.G.; Repka, S.L.; McGinity, J.W. Influence of plasticizers and drugs on the physical-mechanical properties of hydroxypropylcellulose films prepared by hot-melt extrusion. Drug Dev. Ind. Pharm., 1999, 25, 625-33.
14. Repka, M.A.; McGinity, J.W.; Physical-mechanical, moisture absorption and bioadhesive properties of hydroxypropylcellulose hot-melt extruded films. Biomaterials. 2000, 21, 1509-17.
15. Crowley, M.M.; Zhang, F.; Koleng, J.J.; McGinity, J.W. Stability of polyethylene oxide in matrix tablets prepared by hot-melt extrusion. Biomaterials, 2002, 23, 4241-4248.
16. Zhang, F.; McGinity, J.W. Properties of hot-melt extruded theophylline tablets containing poly (vinyl acetate). Drug Dev. Ind. Pharm., 2000, 26, 931-42.
17. Aitken-Nichol, C.; Zhang, F.; McGinity, J.W. Hot-melt extrusion of acrylic films. Pharm. Res., 1996, 13, 804-808.
18. Verhoeven, E.; Vervaet, C.; Remon, J.P. Xanthan gum to tailor drug release of sustained-release ethylcellulose mini-matrices prepared via hot-melt extrusion: in vitro and in vivo evaluation. Eur. J. Pharm. Biopharm., 2006, 63, 320-330.
19. Chasin, M.; Langer R. Biodegradable polymers as drug delivery systems. Marcel Dekker INC: New York, 1990.
20. Delmas, P.D.; Bjarnason, N.H.; Mitlak, B.H.; Ravoux, A.C.; Shah, A.S.; Huster, W.J.; Draper, M.; Christiansen, C.N. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N. Engl. J. Med., 1997, 337, 1641-1647.
21. Hol, T.; Cox, M.B.; Bryant, H.U.; Draper, M.W. Selective estrogen receptor modulators and postmenopausal women's health. J. Womens Health, 1997, 6, 523-531.
22. Hardman, J.G.; Limbird L.E.; Gilman, A.G. Eds., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10th ed., McGraw Hill: New York, 2001.
23. Teeter, J.S.; Meyerhoff, R.D. Environmental fate and chemistry of raloxifene hydrochloride. Environ. Toxicol. Chem., 2002, 21, 729-36.
24. Roupakias, C.; Bikiaris, D.; Karayannidis, G. Synthesis, thermal characterization, and tensile properties of alipharomatic polyesters derived from 1,3-propanediol and terephthalic, isophthalic, and 2,6- naphthalenedicarboxylic acid. J. Polym. Sci., Part A. Polym. Chem., 2005, 43, 3998-4011.
25. Bikiaris, D.N.; Papageorgiou, G.Z.; Achilias, D.S. Synthesis and comparative biodegradability studies of three poly(alkylene succinate) s. Polym. Degrad. Stab., 2006, 91, 31-43.
26. Zorba, T.; Chrissafis, K.; Paraskevopoulos, K.M.; Bikiaris, D.N. Synthesis, characterization and thermal degradation mechanism of three poly(alkylene adipate)s: Comparative study. Polym. Degrad. Stab., 2007, 92, 222-230.
27. Papageorgiou, G.Z.; Bikiaris, D.N. Crystallization and melting behavior of three biodegradable poly(alkylene succinates). A comparative study. Polymer, 2005, 46, 12081-12092.
28. Athanasiou, K.A.; Niederauer, G.G.; Agrawal, C.M. Sterilization, toxicity, biocompatibility, and clinical applications of polylactic acid/polyglycolic acid copolymers. Biomaterials, 1996, 17, 93-102.
29. Sinha, V. R.; Bansal, K.; Kaushik, R.; Kumria, R.; Trehan, A. Poly-ε-Caprolactone Microspheres and Nanospheres: An overview. Int. J. Pharmaceut., 2004, 278, 1-23.
30. Papageorgiou, G.Z.; Bikiaris, D.; Karavas, E.; Politis, S.; Docoslis, A.; Park, Y.; Stergiou, A.; Georgarakis, E. Effect of physical state and particle size distribution on dissolution enhancement of Nimodipine/ PEG solid dispersions prepared by melt mixing and solvent evaporation. AAPS J., 2006, 8(4), E623-E631.
31. Wang, L.; Cui, F.D.; Sunada, H. Preparation and evaluation of solid dispersions of nitrendipine prepared with fine silica particles using the melt-mixing method. Chem. Pharm. Bull., 2006, 54, 37-43.
32. Six, K.; Berghmans, H.; Leuner, C.; Dressman, J.; Van Werde, K.; Mullens, J.; Benoist, L.; Thimon, M.; Meublat, L.; Verreck, G.; Peeters, J.; Brewster, M.; Van den Mooter, G. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, part II. Pharm. Res., 2003, 20, 1047-1054.
33. Bruce, L.D.; Shah, N.H.; Malick, A.W.; Infeld, M.H.; McGinity, J.W. Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid. Eur. J. Pharm. Biopharm., 2005, 59, 85-97.
34. Chrissafis, K.; Paraskevopoulos, K.M.; Bikiaris, D.N. Thermal degradation mechanism of poly(ethylene succinate) and poly(butylene succinate): Comparative study. Thermochim. Acta, 2005, 435, 142-150.
35. Chrissafis, K.; Paraskevopoulos, K.M.; Bikiaris, D.N. Thermal degradation kinetics of the biodegradable aliphatic polyester, poly(propylene succinate). Polym. Degrad. Stab., 2006, 91, 60-68.
36. Chrissafis, K.; Paraskevopoulos, K.M.; Bikiaris, D.N. Effect of molecular weight on thermal degradation mechanism of the biodegradable polyester poly(ethylene succinate). Thermochim. Acta, 2006, 440, 166-175.
37. Leuner, C.; Dressman, J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm., 2000, 50, 47-60.
38. Karavas, E.; Georgarakis, M.; Docoslis, A.; Bikiaris, D. Combining SEM, TEM, and micro-Raman techniques to differentiate between the amorphous molecular level dispersions and nanodispersions of a poorly-water soluble drug within a polymer matrix. Int. J. Pharm., 2007, 340, 76-83.
39. Passerini, N.; Perissutti, B.; Moneghini, M.; Voinovich, D.; Albertini, B.; Cavallari, C.; Rodriguez, L. Characterization of carbamazepine-Gelucire 50/13 microparticles prepared by a spraycongealing process using ultrasounds. J. Pharm. Sci., 2002, 91, 699-707.
40. Kanaze, F.I.; Kokkalou, E.; Niopas, I.; Georgarakis, M.; Stergiou, A.; Bikiaris, D. Novel drug delivery systems for flavonoid compounds with enhanced solubility based on solid dispersions with polyvinypyrolidone and polyethyleneglycol. J. Appl. Polym. Sci., 2006, 102, 460-471.
41. Bikiaris, D.; Papageorgiou, G.Z.; Stergiou, A.; Pavlidou, E.; Karavas, E.; Kanaze, F.; Georgarakis, M. Physicochemical studies on solid dispersions of poorly-water soluble drugs. Evaluation of capabilities and limitations of thermal analysis. Thermochim. Acta, 2005, 439, 58-67.
42. Karavas, E.; Georgarakis, E.; Bikiaris, D. Felodipine nanodispersions as active core for predictable pulsatile chronotherapeutics using PVP/HPMC blends as coating layer. Int. J. Pharm., 2006, 313, 189-197.
43. Fini, F.; Moyano, J.R.; Ginés, J.M.; Perez-Martinez, J.I.; Rabasco, A.M. Diclofenac salts, II. Solid dispersions in PEG6000 and Gelucire 50/13. Eur. J. Pharm. Biopharm., 2005, 60, 99-111.
44. Ge, H.; Hu, Y.; Yang, S.; Jiang, X.; Yang, C. Preparation, Characterization and Drug Release Behaviors of Drug-Loaded ε-Caprolactone/ L-lactide Copolymer Nanoparticles. J. Appl. Polym. Sci., 2000, 75, 874-882.
45. Chawla, J.S.; Amiji, M.M. Biodegradable poly(ε-caprolactone) nanoparticles for tumor targeted delivery of tamoxifene. Int. J. Pharm., 2002, 249, 127-137.
46. Zhang, Y.; Wang, C.; Yang, W.; Shi, B.; Fu, S. Tri-component diblock copolymers of poly(ethylene glycol)-poly(ε-caprolactoneco-lactide): synthesis, characterization and loading captothecin. Colloid. Polym. Sci., 2005, 283, 1246-1252.
47. Broman, E.; Khoo C.; Taylor, L.S. A comparison of alternative polymer excipients and processing methods for making solid dispersions of a poorly water-soluble drug. Int. J. Pharm., 2001, 222, 139-151.
48. Karavas, E.; Georgarakis, E.; Sigalas, M.P.; Avgoustakis, K.; Bikiaris, D. Investigation of the release mechanism of a sparingly water-soluble drug from solid dispersions in hydrophilic carriers based on physical state of drug, particle size distribution and drug-polymer interactions. Eur. J. Pharm. Biopharm., 2007, 66, 334-347.
49. Galal, S.; EL Massik, M.A.; Abdallah, O.Y.; Daabis, N.A. Study of In-Vitro Release Characteristics of Carbamazepine Extended Release Semisolid Matrix Filled Capsules Based on Gelucires. Drug Dev. Ind. Pharm., 2005, 30, 817-829.
50. Esquisabel, A.; San Vicente, A.; Igartua, M.; Hernandez, R.M.; Gascon, A.R.; Calvo, M.B.; Pedraz, J.L. Influence of melting point and hydrophilic/lipophilic balance on the release of salbutamol sulfate from lipid matrixes. Pharm. Sci., 1996, 6, 365-369.
51. Chien, N.; Nguyen, J.; Christensen, M.; Ayres, J,W. Formulation of Sustained-Release Verapamil HCl and Diltiazem HCl Semisolid Matrix Capsules. Pharm. Dev. Technol., 2008, 13, 115-125.
52. Harland, R.S.; Gazzaniga, A.; Sangali, E.M.; Colombo P.; Peppas, N.A. Drug/polymer matrix swelling and dissolution. Pharm. Res., 1988, 5, 488-494.