Approaches for the development of solid self-emulsifying drug delivery systems and dosage forms

Asian Journal of Pharmaceutical Sciences

Volumn 4, Issue 4, 2009, Pages 240-253

  Katteboina, Suman ^a   Chandrasekhar P, V S R ^b   Balaji, S ^c  

^a BAPATLA COLLEGE OF PHARMACY   (India)

^b HINDU COLLEGE OF PHARMACY   (India)

^c ANDHRA UNIVERSITY   (India)

Author keywords

Excipient; Lipid formulation classification system; Lipid based formulation; Self dispersion; Self emulsifying drug delivery system; Surfactant

Indexed keywords

5 [5 [2,6 DICHLORO 4 (4,5 DIHYDRO 2 OXAZOLYL)PHENOXY]PENTYL] 3 METHYLISOXAZOLE; ALPHA TOCOPHEROL; ALPHA TOCOTRIENOL; AMPRENAVIR; CARMUSTINE; CARVEDILOL; CHINESE DRUG; CLOZAPINE; CYCLOSPORIN A; DIAZEPAM; DICLOFENAC; DRUG CARRIER; EXCIPIENT; EZETIMIBE; FLUOROURACIL; GENTAMICIN; GLYCYRRHIZIC ACID; INDOMETACIN; KETOPROFEN; LABRASOL; PACLITAXEL; PHENACETIN; PRAZIQUANTEL; PROGESTERONE; SIMVASTATIN; SOLID LIPID NANOPARTICLE; SOYBEAN OIL EMULSION; SURFACTANT; UBIDECARENONE; UNCLASSIFIED DRUG; ZEDOARY TURMERIC OIL;

ADSORPTION; AQUEOUS SOLUTION; AREA UNDER THE CURVE; BRAIN TUMOR; CONTROLLED DRUG RELEASE; DRUG BIOAVAILABILITY; DRUG CAPSULE; DRUG COATING; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG GRANULATION; DRUG HALF LIFE; DRUG IMPLANT; DRUG PELLET; DRUG RELEASE; DRUG SOLUBILITY; EMULSION; GASTROINTESTINAL HEMORRHAGE; HUMAN; LIPID COMPOSITION; LIVER DISEASE; MAXIMUM PLASMA CONCENTRATION; MICELLE; MICROEMULSION; NONHUMAN; POWDER; REVIEW; SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM; SPHERONIZATION; SPRAY DRYING; TABLET FORMULATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 77953453032     PISSN: 18180876     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (88)

1. C. Lipinski, Poor aqueous solubility an industry wide problem in drug discovery. Am. Pharm. Rev., 2002: 82-85.
2. G. L. Amidon, H. Lennernas, V. P. Shah, et al. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res., 1995, 12: 413-420.
3. M. G. Wakerly, C .W. Pouton, B. J. Meakin. Evaluation of the self-emulsifying performance of a non-ionic surfactant-vegetable oil mixture. J Pharm Pharmacol., 1987, 39:6.
4. M. G. Wakerly, C. W. Pouton, B. J. Meakin, et al. Self-emulsification of vegetable oil non- ionic surfactant mixtures. ACS Symp Ser., 1986, 242-255.
5. S. A. Charman, W. N. Charman, M. C. Rogge, et al. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm Res., 1992, 9: 87-93.
6. N. H. Shah, M. T. Carvagal, C. L. Patel, et al. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm., 1994, 106: 15-23.
7. R. Neslihan Gursoy, Simon Benita. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs, Biomedecine & Pharmacotherapy Volume 58, Issue 3, April 2004, Pages 173-182.
8. P. P. Constantinides Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm Res., 1995, 12: 1561-1572.
9. C. W. Pouton. Lipid formulations for oral administration of drugs: nonemulsifying, self-emulsifying and self-microemulsifying drug delivery systems. Eur. J. Pharm. Sci., 2000, 11: S93-S98.
10. C. W. Pouton. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the Lipid Formulation Classification System, Eur. J. Pharm. Sci., 2006, 29: 278-287.
11. P. J. Carrigan, T. R. Bates. Biopharmaceutics of drugs administered in lipid-containing dosage forms: GI absorption of griseofulvin from an oil in water emulsion in the rat. J. Pharm. Sci., 1973, 62: 1476-1479.
12. R. A. Myers, V. J. Stella, Systemic bioavailability of penclomedine (NSC-338720) from oil-in-water emulsions administered intraduodenally to rats, Int. J. Pharm., 1992, 78: 217-226.
13. C. W. Pouton. Formulation of self-emulsifying drug delivery systems, Adv. Drug Deliver. Rev., 1997, 25: 47-58. (Pubitemid 27107790)
14. C.W. Pouton. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. Int. J. Pharm., 1985, 27: 335-348.
15. J. F. Cuine, C. L. McEvoy, W. N. Charman, et al. Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs, J. Pharm. Sci., 2008, 97: 993-1010.
16. T. Gershanik, S. Benita. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs, Eur. J. Pharm. Sci. Biopharm., 2000, 50: 179-188.
17. S. A. Charman, W. N. Charman, M. C. Rogge, Self-emulsifying drug delivery systems: formulation and evaluation of an investigational lipophilic compound, Pharm. Res., 1992, 9: 87-93.
18. A. K. Trull, K. K. C. Tan, L. Tan, et al. Enhanced absorption of new oral cyclosporin microemulsion formulation, Neoral, in liver transplant recipients with external biliary diversion. Transplant. Proc., 1994, 26: 2977-2978.
19. E. A. Mueller, J. M. Kovarik, J. B. Van Bree, et al. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm. Res., 1994, 11: 301-304.
20. J. M. Kovarik, E. A. Mueller, J. B. Van Bree, et al. Reduced inter- and intra individual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J. Pharm.Sci., 1994, 83: 444-446. (Pubitemid 24224228)
21. D. J. Hauss, S. E. Fogal, J. V. Ficorilli, et al. Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor. J. Pharm. Sci., 1998, 87: 164-169.
22. T. Julianto, K. H. Yuen, A. Mohammad Noor. Improved bioavailability of vitamin E with a self emulsifying formulation. Int. J. Pharm., 2000, 200: 53-57.
23. T. R. Kommuru, B. Gurley, M. A. Khan, et al. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int. J. Pharm., 2001, 212: 233-246.
24. B. K. Kang, J. S. Lee, S. K. Chon, et al. Development of self-micro emulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm., 2004, 274: 65-73.
25. L. Wei, P. Sun, S. Nie, et al. Preparation and evaluation of SEDDS and SMEDDS containing carvedilol. Drug Dev. Ind. Pharm., 2005, 31: 785-794.
26. S. P. Yap, K. H. Yuen. Influence of lipolysis and droplet size on tocotrienol absorption from self emulsifying formulations, Int. J. Pharm., 2004, 281: 67-78.
27. C. K. Kim, Y. J. Cho, Z. G. Gao. Preparation and evaluation of biphenyl dimethyl dicarboxylate microemulsions for oral delivery. J. Control. Release, 2001, 70: 149-155.
28. J. Y. Kim, Y. S. Ku. Enhanced absorption of indomethacin after oral or rectal administration of a self emulsifying system containing indomethacin to rats. Int. J. Pharm., 2000, 194: 81-89.
29. R.G. Strickley, Solubilizing excipients in oral and injectable formulations, Pharm. Res., 2004, 21: 201-230.
30. C.W. Pouton, Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system, Eur. J. Pharm. Sci., 2006, 29: 278-287.
31. L. Rodriguez, N. Passerini, C. Cavallari, et al. Description and preliminary evaluation of a new ultrasonic atomizer for spray-congealing process. Int. J. Pharm., 1999, 183: 133-143.
32. N. Passerini, B. Albertini, B. Perissuti, et al. Evaluation of melt granulation and ultrasonic spray congealing as techniques to enhance the dissolution of praziquantel, Int. J. Pharm., 2006, 318: 92-102.
33. C. Cavallari, L. Rodriguez, B. Albertini, et al. Thermal and fractal analysis of diclofenac/Gelucire 50/13 microparticles obtained by ultrasound-assisted atomization. J. Pharm. Sci., 2005, 94.
34. T. Yi, J. L. Wan, H. B. Xu, et al. A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs. Eur. J. Pharm. Biopharm., 2008, 70: 439-444.
35. Y. Ito, T. Kusawake, M. Ishida, et al. Oral solid gentamicin preparation using emulsifier and adsorbent. J. Control. Release, 2005, 105: 23-31.
36. C. Fabio, C. Elisabetta. Pharmaceutical composition comprising a water/oil/ water double microemulsion incorporated in a solid support. WO2003/013421.
37. L. Boltri. Enhancement and modification of etoposide release from crospovidone particles loaded with oil-surfactant blends. Pharm. Dev. Technol., 1997, 2: 373-381.
38. N. Venkatesan, J. Yoshimitsu, Y. Ito, et al. Liquid filled nanoparticles as a drug delivery tool for protein therapeutics. Biomaterials, 2005, 26: 7154-7163.
39. A. Seo, P. Holm, H. G. Kristensen, et al. The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer. Int. J. Pharm., 2003, 259: 161-171.
40. M. K. Gupta, D. Goldman, R. H. Bogner, et al. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm. Dev. Technol., 2001, 6: 563-572.
41. M. K. Gupta, Y. C. Tseng, D. Goldman, et al. Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules. Pharm. Res., 2002, 19: 1663-1672.
42. V. Jannin, J. Musakhanian, D. Marchaud. Approaches for the development of solid and semi-solid lipid-based formulations. Adv. Drug. Deliv. Rev., 2008, 60: 734-746.
43. G. Verreck, M. E. Brewster. Melt extrusion-based dosage forms: excipients and processing conditions for pharmaceutical formulations. Bull. Tech. Gattefosse., 2004, 97: 85-95.
44. S. Nazzal, M. Nutan, A. Palamakula, et al. Optimization of a self-nanoemulsified tablet dosage form of Ubiquinone using response surface methodology: effect of formulation ingredients. Int. J. Pharm., 2002, 240: 103-114.
45. E. Mehuys, J. P. Remon Human bioavailability of propranolol from a matrix-in-cylinder system with a HPMC-GelucireR core. J. Control. Release, 2005, 107: 523-536.
46. S. Hulsmann, T. Backensfeld, S. Keitel, et al. Melt extrusion-an alternative method for enhancing the dissolution rate of 17-bestradiol hemihydrate. Eur. J. Pharm. Biopharm., 2000, 49: 237-242.
47. A. Abdalla and K. Mader Preparation and characterization of a self-emulsifying pellet formulation. Eur. J. Pharm. Biopharm., 2007, 66: 220-226.
48. T. Iosio, D. Voinovich., M. Grassi, et al. Bi-layered self-emulsifying pellets prepared by co-extrusion and spheronization: influence of formulation variables and preliminary study on the in vivo absorption. Eur. J. Pharm. Biopharm., 10.1016/j.ejpb., 2007,11.014.
49. C. Thies, I. Ribeiro Dos Santos, J. Richard, et al. A supercritical fluid-based coating technology. 1: process considerations, J. Microencapsul., 2003, 20: 87-96.
50. I. Ribeiro Dos Santos, C. Thies, J. Richard, et al. A supercritical fluid bases coating technology. 2: solubility considerations. J. Microencapsul., 2003, 20: 97-109.
51. S. Sethia, E. Squillante. Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. J. Pharm. Sci., 2002, 91: 1948-1957.
52. S. Sethia, E. Squillante. Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods, Int. J. Pharm., 2004, 272: 1-10.
53. S. Sethia, E. Squillante. In vitro-in vivo evaluation of supercritical processed solid dispersions: permeability and viability assessment in Caco-2 cells. J. Pharm. Sci., 2004, 93: 2985-2993.
54. L. D. Hu, X. Tang, F. Cui. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs, J. Pharm. Pharmacol., 2004, 56: 1527-1535.
55. Y. Wang, Y. Deng, S. Mao, et al. Characterization and body distribution of beta-elemene solid lipid nanoparticles (SLN). Drug Dev. Ind. Pharm., 2005, 31: 769-778.
56. E. Gavini, V. Sanna, R. Sharma, et al. Solid lipid microparticles (SLM) containing juniper oil as anti-acne topical carriers: preliminary studies. Pharm. Dev. Technol., 2005, 10: 479-487.
57. M. Ricci, C. Puglia, F. Bonina, C. D. Di Giovanni, et al. Evaluation of indomethacin percutaneous absorption from nanostructured lipid carriers (NLC): in vitro and in vivo studies, J. Pharm. Sci., 2005, 94: 1149-1159.
58. R. Sivaramakrishnan, C. Nakamura, W. Mehnert, et al. Glucocorticoid entrapment into lipid carriers. Characterisation by parelectric spectroscopy and influence on dermal uptake. J. Control. Release, 2004, 97: 493-502.
59. E. B. Souto, S. A. Wissing, C. M. Barbosa, et al. Comparative study between the viscoelastic behaviors of different lipid nanoparticle formulations. J. Cosmet. Sci., 2004, 55: 463-471.
60. E. B. Souto, R. H. Muller. SLN and NLC for topical delivery of ketoconazole. J. Microencapsul., 2005, 22: 501-510.
61. Veerawat Teeranachaideekul, B. Eliana, H. Souto Rainer Muller. Cetyl palmitate-based NLC for topical delivery of Coenzyme Q10-development, physicochemical characterization and in vitro release studies European J. Pharm. Biopharm., 2007, 67: 141-148.
62. Kopparam Manjunath, Vobalaboina Venkateswarlu. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J. Control. Release, 2005, 107: 215-228.
63. S. L. Myers, M. L. Shively. Preparation and characterization of emulsifiable glasses: oil-in-water and water-in-oil-in-water emulsion. J. Colloid Interface Sci., 1992, 149: 271-278.
64. J. Bamba, G. Cavé, Y. Bensouda, et al. Cryoprotection of emulsions in freeze-drying: freezing process analysis. Drug. Dev. Ind. Pharm., 1995, 21: 1749-1760.
65. K. L. Christensen, G. P. Pedersen, H. G. Kristensen Technical optimization of redispersible dry emulsions. Int. J. Pharm., 2001, 212: 195-202.
66. T. Hansen, P. Holm, K. Schultz. Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid. Int. J. Pharm., 2004, 287: 55-66.
67. D. J. Jang, E. J. Jeong, H. M. Lee, et al. Improvement of bioavailability and photostability of amlodipine using redispersible dry emulsion. Eur. J. Pharm. Sci., 2006, 28: 405-411.
68. E. Toorisaka, M. Hashida, N. Kamiya, et al. An enteric-coated dry emulsion formulation for oral insulin delivery. J. Control Release, 2005, 107: 91-96.
69. P. Gao, W. Morozowich. Development of supersaturatable selfemulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs. Expert. Opin. Drug. Discov., 2006, 3: 97-110.
70. P. Gao, B. D. Rush, W. P. Pfund, et al. Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability. J. Pharm. Sci., 2003, 92: 2386-2398.
71. S. Nazzal, and M.A. Khan, Controlled release of a self-emulsifying formulation from a tablet dosage form: stability assessment and optimization of some processing parameters. Int. J. Pharm., 2006, 315: 110-121.
72. P. Patil, P. Joshi, A. Paradkar Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen. AAPS Pharm. Sci. Tech., 10.1208/pt050342 http://www.aapspharmscitech.org/articles/pt0503/pt050342/pt050342.pdf.
73. S. Joseph. Solid self-emulsifying dosage form for improved delivery of poorly soluble hydrophobic compounds and the process for preparation thereof. US Pat 20030072798.
74. L. L. Wei. Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol. Drug. Dev. Ind. Pharm., 2007, 33: 990-998.
75. R. Gandhi, C. Lal Kaul, R. Panchagnula. Extrusion and spheronization in the development of oral controlled-release dosage forms. PSTT, 1999, 2: 160-170. (Pubitemid 29195749)
76. M. Serratoni, S. Newton, A. Booth, Clarke. Controlled drug release from pellets containing water insoluble drugs dissolved in a self-emulsifying system. Eur. J. Pharm. Biopharm., 2007, 65: 94-98.
77. J. Hamdani, A.J. Moes, K. Anighi Physical and thermal characterizations of Precirol and Compritol as lipophilic glycerides used for the preparation of controlled-release matrix pellets. Int. J. Pharm., 2003, 260: 47-57.
78. A. T. M. Serajuddin. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci., 1999, 88: 1058-1066.
79. M. Vasanthavada, A. T. M. Serajuddin. Lipid-based self-emulsifying solid dispersions. In oral lipid-based formulations: enhancing bioavailability of poorly water-soluble drugs (Hauss, D. J., ed.), pp. Informa Healthcare, 2007, 149-184.
80. A. T. Serajuddin, P. C. Sheen, D. Mufson, et al. Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions. J. Pharm. Sci., 1998, 77: 414-417.
81. S. M. Khoo, C. J. H. Porter, W. N. Charman. The formulation of halofantrine as either non-solubilising PEG 6000 or solubilising lipid based solid dispersions: physical stability and absolute bioavailability assessment. Int. J. Pharm., 2000, 205: 65-78.
82. P. Patil, A. Paradkar. Porous polystyrene beads as carriers for self-emulsifying system containing loratadine. AAPS Pharm. Sci. Tech., 2006, 10.1208/0pt07012 http://www.aaps-pharm-scitech.org/articles/pt0701/pt070128/ pt070128.pdf.
83. J. You. Study of the preparation of sustained-release microspheres containing zedoary turmeric oil by the emulsion-solvent-diffusion method and evaluation of the self-emulsification and bioavailability of the oil. Colloid. Surf. B., 2006, 48: 35-41.
84. A. A. Attama, M. O. Nkemnele. In vitro evaluation of drug release from self micro-emulsifying drug delivery systems using a biodegradable homolipid from Capra hircus. Int. J. Pharm., 2005, 304: 4-10.
85. Y. X. Hu. Preparation and evaluation of 5-FU/PLGA/gene nanoparticles. Key Eng. Mat., 2005, 288-289: 147-150.
86. W. J. Trickler, A. A. Nagvekar, A. K. Dash. A novel nanoparticle formulation for sustained paclitaxel delivery. AAPS Pharm. Sci. Tech., 2008, 10.1208/s12249-008-9063-9067
87. J. Y. Kim, Y.S. Ku. Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats. Int. J. Pharm., 2000, 194: 81-89
88. G. S. Chae, J. S. Lee, S. H. Kim, et al. Enhancement of the stability of BCNU using self-emulsifying drug delivery systems (SEDDS) and in vitro antitumor activity of self-emulsified BCNU-loaded PLGA wafer. Int. J. Pharm., 2005, 301: 6-14.