Development of an oral microemulsion formulation of alendronate: Effects of oil and co-surfactant type on phase behaviour

Journal of Microencapsulation

Volumn 25, Issue 5, 2008, Pages 315-323

  Karamustafa, Fulya ^a   Ćelebi, Nevin ^a  

^a GAZI UNIVERSITY   (Turkey)

Author keywords

Alendronate; In vitro release; Microemulsion; Phase diagrams; Physical stability

Indexed keywords

ALENDRONIC ACID; COSURFACTANT; DYE; OIL; PHOSPHATIDYLCHOLINE; PROPYLENE GLYCOL; WATER;

ARTICLE; CENTRIFUGATION; CONDUCTANCE; DIALYSIS; DRUG FORMULATION; DRUG RELEASE; DRUG STABILITY; FLOW KINETICS; MICROEMULSION; PHASE SEPARATION; PHYSICAL CHEMISTRY; REFRACTION INDEX; TEMPERATURE; TURBIDITY; VISCOMETER; VISCOSITY;

ADMINISTRATION, ORAL; ALCOHOLS; ALENDRONATE; BIOCOMPATIBLE MATERIALS; BONE DENSITY CONSERVATION AGENTS; DIFFUSION; DRUG DELIVERY SYSTEMS; EMULSIONS; LECITHINS; OILS; POLYMERS; PROPYLENE GLYCOLS; RHEOLOGY; STRESS, MECHANICAL; SURFACE-ACTIVE AGENTS; TEMPERATURE;

EID: 47749117267     PISSN: 02652048     EISSN: 14645246     Source Type: Journal    
DOI: 10.1080/02652040801977045     Document Type: Article

References (46)

1. Aboofazeli, R., Lawrence, CB, Wicks, SR and Lawrence, MJ (1994) Investigations into the formation and characterization of phospholipid microemulsions. III. Pseudo-ternary phase diagrams of systems containing water-lecithin-isopropyl myristate and either an alkanoic acid, amine, alkanediol, polyethylene glycol alkyl ether or alcohol as cosurfactant. Int J Pharm, 111, pp. 63-72.
2. Angelico, R., Palazzo, G., Colafemmina, G., Cirkel, PA, Giustini, M. and Ceglie, A. (1998) Water diffusion and head group mobility in polymer-like reverse micelles: Evidence of a sphere-to-rod-to-sphere transition. J Phys Chem B, 102, pp. 2883-2889.
3. Bagwe, RP, Kanicky, JR, Palla, BJ, Patanjali, PK and Shah, DO (2001) Improved drug delivery using microemulsions: Rationale, recent progress, and new horizons. Crit Rev Ther Drug Carr Sys, 18, pp. 77-140.
4. Binks, BP, Espert, A., Fletcher, PDI and Soubiran, L. (2003) Phase behaviour of microemulsions stabilized by double chain cationic surfactants and alcohol co-surfactants. Colloids Surf A Physicochem Eng Aspec, 212, pp. 135-145.
5. Bone, HG, Adami, S., Rizzoli, R., Favus, M., Ross, PD, Santora, A., Prahalada, S., Daifotis, A., Orloff, J. and Yates, J. (2000) Weekly administration of alendronate: Rationale and plan for clinical assessment. Clin Ther, 22, pp. 15-28.
6. Borgstrom, B. (1980) Importance of phospholipids, pancreatic phospholipase A2 and fatty acid for the digestion of dietary fat. Gastroenterology, 78, pp. 954-962.
7. Carey, MC, Small, DM and Bliss, CM (1983) Lipid digestion and absorption. Annu Rev Physiol, 45, pp. 651-677.
8. Cilek, A., Celebi, N. and Tirnaksiz, F. (2006) Lecithin-based microemulsion of a peptide for oral administration: Preparation, characterization, and physical stability of the formulation. Drug Deliv, 13, pp. 19-24.
9. Constantinides, PP (1995) Lipid microemulsions for improving drug dissolution and oral absorption: Physical and biopharmaceutical aspects. Pharm Res, 12, pp. 1561-1572.
10. Constantinides, PP, Lancaster, CM, Marcello, J., Chiossone, D., Orner, D., Hidalgo, I., Smith, PL, Sarkahian, AB, Yiv, SH and Owen, AJ (1995) Enhanced intestinal absorption of an RGD peptide from water-in-oil microemulsions of different composition and particle size. J Control Rel, 34, pp. 109-116.
11. Constantinides, PP and Scalart, JP (1997) Formulation and physical characterization of water-in-oil microemulsions containing long-versus medium-chain glycerides. Int J Pharm, 158, pp. 57-68.
12. Constantinides, PP, Scalart, JP, Lancaster, C., Marcello, J., Marks, G., Ellens, H. and Smith, PL (1994) Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Re, 11, pp. 1385-1390.
13. Cornell, BA, Middlehurst, J. and Separovic, F. (1986) Small unilamellar phospholipids vesicles and the theory of membrane formation. Faraday Disc Chem Soc, 81, pp. 163-167.
14. De Marco, J., Biffar, SE, Reed, DG and Brooks, MA (1989) The determination of 4-amino-1-hydroxybutane-1,1-diphosphonic acid monosodium salt trihydrate in pharmaceutical dosage forms by high-performance liquid chromatography. J Pharm Biomed Anal, 7, pp. 1719-1727.
15. Fletcher, PDI and Morris, JS (1995) Turbidity of oil-in-water microemulsion droplets stabilized by nonionic surfactants. Colloids Surf A: Physicochemi Engi Aspects, 98, pp. 147-154.
16. Garcia-Celma, MJ, Azemar, N., Pes, MA and Solans, C. (1994) Solubilization of antifungal drugs in water/POE (20) sorbitan monooleate/ oil systems. Int J Pharm, 105, pp. 77-81.
17. Gasco, MR, Gallarate, M., Trotta, M., Bauchiero, L., Gremmo, E. and Chiappero, O. (1989) Microemulsions as topical delivery vehicles: Ocular administration of timolol. J Pharm Biomed Anal, 7, pp. 433-439.
18. Gertz, BJ, Holland, SD, Kline, WF, Matuszewski, BK, Freeman, A., Quan, H., Lasseter, KC, Mucklow, JC and Porras, AG (1995) Studies of the oral bioavailability of alendronate. Clin Pharmacol Ther, 58, pp. 288-298.
19. Graham, DY, Malaty, HM and Goodgame, R. (1997) Primary amino-bisphosphonates: A new class of gastrotoxic drugs-comparison of alendronate and aspirin. Am J Gastroenterol, 92, pp. 1322-1325.
20. Hoar, TP and Schulman, JH (1943) Transparent water-in-oil dispersions: the oleopathic hydro-micelle. Nature, 152, p. 102.
21. Kawakami, K., Yoshikawa, T., Moroto, Y., Kanaoka, E., Takahashi, K., Nishihara, Y. and Kazuyoshi, M. (2002) Microemulsion formulation for enhanced absorption of poorly soluble drugs I. Prescription design. J Contr Rel, 81, pp. 65-74.
22. Ke, W-T, Lin, S-Y, Ho, H-O and Sheu, M-T (2005) Physical characterization of microemulsion systems using tocopheryl polyethylene glycol 1000 succinate (TPGS) as a surfactant for the oral delivery of protein drugs. J Contr Rel, 102, pp. 489-507.
23. Kim, SK, Lee, EH, Vaishali, B., Lee, S., Lee, Y-K, Kim, C-Y, Moon, HT and Byun, Y. (2005) Tricaprylin microemulsion for oral delivery of low molecular weight heparin conjugates. J Contr Rel, 105, pp. 32-42.
24. Kirk, JK and Spangler, JG (1996) Alendronate: A bisphosphonate for treatment of osteoporosis. Clin Pharmacol, 54, pp. 2053-2060.
25. Kristis, G. (1990) A viscosity study on oil-in water microemulsion. Int J Pharm, 61, pp. 213-218.
26. Lawrence, MJ (1994) Microemulsions as drug delivery vehicles. Curr Opin Colloid Interface Sci, 1, pp. 826-832.
27. Lawrence, MJ and Rees, GD (2000) Microemulsion-based media as novel drug delivery systems. Adv Drug Del Rev, 45, pp. 89-121.
28. Leung, R. and Shah, DO (1989) Microemulsions: An evolving technology for pharmaceutical applications. Controlled release of drugs: Polymers and aggregate systems, pp. 85-215. VCH, New York
29. Lin, JH, Chen, I-W, Deluna, FA and Hichens, M. (1993) Role of calcium in plasma protein binding and renal handling of alendronate in hypo-and hypercalcemic rats. J Pharmacol Exp Ther, 267, pp. 670-675.
30. Mehta, SK, Kavaljit, XX and Bala, K. (1999) Phase behaviour, structural effects, volumetric and transport properties in nonaqueous microemulsions. Phys Rev E, 59, pp. 4317-4325.
31. Osborne, DW, Middleton, CA and Rogers, RL (1988) Alcohol-free microemulsions., 9, pp. 415-423.
32. Patil, P., Joshi, P. and Paradkar, A. (2004) Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen. AAPS PharmSciTech, 5, pp. 1-8.
33. Pattarino, F., Marengo, E., Gasco, MR and Carpignano, R. (1993) Experimental design and partial least squares in the study of complex mixtures: Microemulsions as drug carriers. Int J Pharm, 91, pp. 157-165.
34. Porras, AG, Holland, SD and Gertz, BJ (1999) Pharmacokinetics of alendronate. Clin Pharmacokinet, 36, pp. 315-328.
35. Ritschel, WA (1991) Microemulsions for improved peptide absorption from the gastrointestinal tract. Meth Find Exp Clin Pharmacol, 13, pp. 205-220.
36. Saag, KG, Emkey, R., Schnitzer, TJ, Brown, JP, Hawkins, F., Goemaere, S., Thamsborg, G., Liberman, UA, Delmas, PD, Malice, M-P, Czachur, M. and Daifotis, AG (1998) Alendronate for the prevention and treatment of glucocorticoid-induced osteoporosis. N Engl J Med, 339, pp. 292-299.
37. Schurtenberger, P., Peng, Q., Leser, ME and Luisi, PL (1993) Structure and phase behaviour of lecithin-based microemulsions: A study of chain length dependence. J Colloid Interface Sci, 156, pp. 43-51.
38. Sharpe, M., Noble, S. and Spencer, CM (2001) Alendronate an update of its use in osteoporosis. Drugs, 61, pp. 999-1039.
39. Siebenbrodt, I. and Kiepert, S. (1993) Poloxamer-systems as potential ophtyhalmics II. Micromemulsions. Eur J Pharm Biopharm, 39, pp. 25-30.
40. Tenjarla, S. (1999) Microemulsions: An overview and pharmaceutical applications. Crit Rev Ther Drug Carr Sys, 16, pp. 461-521.
41. Trotta, M., Cavalli, R., Ugazio, E. and Gasco, MR (1996) Phase behaviour of microemulsion systems containing lecithin and lysolecithin as surfactants. Int J Pharm, 143, pp. 67-73.
42. Turkyilmaz, A., Celebi, N., Gonul, B. and Alkan-Onyuksel, H. (1997) Physical characterization and stability of microemulsion for oral administration of a peptide. Biomedical science and technology, recent developments in the pharmaceutical and medical sciences, pp. 65-72. Plenum Press, New York
43. Warisnoicharoen, W., Lansley, AB and Lawrence, MJ (2000) Nonionic oil-in-water microemulsions: The effect of oil type on phase behaviour. Int J Pharm, 198, pp. 7-27.
44. Yaghmur, A., Aserin, A. and Garti, N. (2002) Phase behavior of microemulsions based on food-grade nonionic surfactants: Effect of polyols and short-chain alcohols. Colloids Surf A Physicochem Eng Aspec, 209, pp. 71-81.
45. Yetkin, G., Celebi, N., Ozer, C, Gonul, B. and Ozoǧul, C. (2004) The healing effect of TGF-α on gastric ulcer induced by acetylsalicylic acid in rats. Int J Pharm, 277, pp. 163-172.
46. Zhang, XC, Jackson, JK and Burt, HM (1996) Development of amphiphilic diblock copolymers as micellar carriers of taxol. Int J Pharm, 132, pp. 195-206.