Skip to main content
Have a personal or library account? Click to login
Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs Cover

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Acta Pharmaceutica
Volume 63 (2013): Issue 4 (December 2013)
By: ,  ,   and    
Open Access
|Dec 2013
References

References

  1. 1. J. M. Custodio, C. Y. Wu and L. Z. Benet, Predicting drug disposition, absorption/elimination/ transporter interplay and the role of food on drug absorption, Adv. Drug Deliver. Rev.(2008) 717-733; DOI: 10.1016/j.addr.2007.08.043.
    Open DOISearch in Google Scholar
  2. 2. A. Chaudhary, U. Nagaich, N. Gulati, V. K. Sharma and R. L. Khosa, Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review, J. Adv. Pharm. Educ. Res.(2012) 32-67.
    Search in Google Scholar
  3. 3. K. Kohli, S. Chopra, D. Dhar, S. Arora and R. K. Khar, Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability, Drug Discov. Today(2010) 958-965; DOI: 10.1016/ j.drudis.2010.08.007.
    Search in Google Scholar
  4. 4. Y. Kawabata, K. Wada, M. Nakatani, S. Yamada and S. Onoue, Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications, Int. J. Pharm.(2011) 1-10; DOI: 10.1016/j.ijpharm.2011.08.032.
    Open DOISearch in Google Scholar
  5. 5. T. Loftsson, E. M. Brewater and M. Masson, Role of cyclodextrins in improving oral drug delivery, Am. J. Drug Deliv.(2004) 261-275; DOI: 10.2165/00137696-200402040-00006.
    Open DOISearch in Google Scholar
  6. 6. S. B. Murdandea and M. J. Gumkowskia, Development of a self-emulsifying formulation that reduces the food effect for torcetrapib: An overview, Int. J. Pharm.(2008) 15-22; DOI: 10. 1016/j.ijpharm.2007.09.015.
    Search in Google Scholar
  7. 7. J. Parul, A. Geeta and K. Amanpreet, Bioavailability enhancement of poorly soluble drugs by SMEDDS: A review, J. Drug Deliv. Ther.(2013) 98-109.
    Search in Google Scholar
  8. 8. S. Saroy, D. A. Baby and M. Sabitha, Current trends in lipid based delivery systems and its applications in drug delivery, Asian J. Pharm. Clin. Res.(2012) 4-9.
    Search in Google Scholar
  9. 9. H. J. C. Porter, L. N. Trevaskis and W. N. Charman, Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs, Nat. Rev. Drug Discov.(2007) 231-248; DOI: 10. 1038/nrd2197.
    Open DOISearch in Google Scholar
  10. 10. B. K. Nanjwade, D. J. Patel, R. A. Udhani and F. V. Manvi, Function of lipids for enhancement of oral bioavailability of poorly water-soluble drugs, Sci. Pharm.(2011) 705-727; DOI: 10.3797/ scipharm.1105-09.
    Open DOISearch in Google Scholar
  11. 11. W. C. Pouton and J. H. C. Porter, Formulation of lipid-based delivery systems for oral administration: Materials, methods and strategies, Adv. Drug Deliver. Rev.(2008) 625-637; DOI: 10. 1016/j.addr.2007.10.010.
    Open DOISearch in Google Scholar
  12. 12. W. C. 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) 278-287; DOI: 10.1016/j.ejps.2006.04.016.
    Open DOISearch in Google Scholar
  13. 13. V. Jannin, J. Musakhanian and D. Marchaud, Approaches for the development of solid and semi-solid lipid-based formulations, Adv. Drug Deliver. Rev.(2008) 734-746; DOI: 10.1016/j. addr.2007.09.006.
    Search in Google Scholar
  14. 14. B. V. Rajesh, T. K. Reddy, G. Srikanth, V. Mallikarjun and P. Nivethithai, Lipid based self-emulsifying drug delivery system (SEDDS) for poorly water-soluble drugs: A review, J. Glob. Pharma Technol.(2010) 47-55.
    Search in Google Scholar
  15. 15. R. N. Gupta, R. Gupta and R. G. Singh, Enhancement of oral bioavailability of lipophilic drugs from self-microemulsifying drug delivery systems (SMEDDS), Int. J. Drug Dev. Res.(2009) 10-18.
    Search in Google Scholar
  16. 16. K. Mohsin, A. A. Shahba and F. K. Alanazi, Lipid based self-emulsifying formulations for poorly water soluble drugs- an excellent opportunity, Ind. J. Pharm. Edu. Res.(2012) 88-96.
    Search in Google Scholar
  17. 17. P. Gao and W. Morozowich, Development of supersaturatable self-emulsifying drug delivery system formulation for improving the oral absorption of poorly soluble drugs, Expert Opin. Drug Del.(2006) 97-110; DOI: 10.1517/17425247.3.1.97.
    Open DOISearch in Google Scholar
  18. 18. B. D. Tarr and S. H. Yalkowsky, Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size, Pharm. Res.(1989), 40-43; DOI: 10.1023/A:10158435 17762.
    Search in Google Scholar
  19. 19. B. Singh, S. Bandopadhyay, R. Kapil, R. Singh and O. Katare, Self-emulsifying drug delivery systems (SEDDS): Formulation development, characterization, and applications, Crit. Rev. Ther. Drug(2009) 427-521.
    Search in Google Scholar
  20. 20. J. H. Lin, W. Chen and J. King, The effect of dosage form on oral absorption of L-365, 260, a potent CCK receptor antagonist in dogs, Pharm. Res.(1991) 272.
    Search in Google Scholar
  21. 21. M. J. Groves and D. A. Degalindez, The self-emulsifying action of mixed surfactants in oil, Acta Pharm. Suec.(1976) 361-372.
    Search in Google Scholar
  22. 22. S. M. Khoo, A. J. Humberstone, C. J. H. Porter, G. A. Edwards and W. N. Charman, Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine, Int. J. Pharm.(1998) 155-164; DOI: 10.1016/S0378-5173(98)00054-4.
    Open DOISearch in Google Scholar
  23. 23. K. J. Palin and C. G. Wilson, The effect of different oils on the absorption of probucol in the rat, J. Pharm. Pharmacol.(1984) 641-643; DOI: 10.1111/j.2042-7158.1984.tb04919.
    Search in Google Scholar
  24. 24. J. Rao and D. J. McClements, Formation of flavor oil microemulsions, nanoemulsions and emulsions: influence of composition and preparation method, J. Agric. Food Chem.(2011) 5026-5035; DOI: 10.1021/jf200094m.
    Open DOISearch in Google Scholar
  25. 25. M. Stuchlik and S. @ák, Lipid-based vehicle for oral drug delivery, Biomed. Pap.(2001) 17-26.
    Open DOISearch in Google Scholar
  26. 26. P. Constantinides, Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects, Pharm. Res.(1995) 1561-1572; DOI: 10.1023/A: 1016268311867.
    Search in Google Scholar
  27. 27. M. Kimura, M. Shizuki, K. Miyoshi, T. Sakai, H. Hidaka, H. Takamura and T. Matoba, Relationship between the molecular structures and emulsification properties of edible oils, Biosci. Biotech. Bioch.(1994) 1258-1261; DOI: 10.1271/bbb.58.1258.
    Open DOISearch in Google Scholar
  28. 28. M. Grovea and A. Mullertzb, Bioavailability of seocalcitol II: development and characterisation of self-microemulsifying drug delivery systems (SMEDDS) for oral administration containing medium and long chain triglycerides, Eur. J. Pharm. Sci.(2006) 233-234; DOI: 10.1016/j.ejps.2006.02.005.
    Open DOISearch in Google Scholar
  29. 29. C. J. Porter, A. M. Kaukonen and B. J. Boyd, Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation, Pharm. Res.(2004) 1405-1412; DOI: 10.1023/B:PHAM.0000036914.22132.cc.
    Open DOISearch in Google Scholar
  30. 30. H. N. Prajapati, M. D. Dalrymple and T. M. A. Serajuddin, A comparative evaluation of mono-, di- and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development, Pharm. Res.(2012) 285-305; DOI: 10.1007/s11095-011-0541-3.
    Open DOISearch in Google Scholar
  31. 31. K. Bolko, A. Zvonar and M. Ga{perlin, Mixed lipid phase SMEDDS as an innovative approach to enhance resveratrol solubility, Drug Dev. Ind. Pharm. 2013, in press; DOI: 10.3109/03639045. 2012.749888.
    Search in Google Scholar
  32. 32. P. P. Constantinides and J. P. Scalart, Formulation and physical characterization of water-in-oil microemulsions containing long- versus medium-chain glycerides, Int. J. Pharm.(1997) 57-68; DOI: 10.1016/S0378-5173(97)00248-2.
    Open DOISearch in Google Scholar
  33. 33. D. M. Small, Surface and bulk interactions of lipids and water with a classification of biologically active lipids based on these interactions, Fed. Proc.(1970) 1320-1326.
    Search in Google Scholar
  34. 34. W. C. Pouton, Properties and uses of common formulation lipids, surfactants and cosolvents, in AAPS, Workshop, March 2007.
    Search in Google Scholar
  35. 35. N. H. Shah, M. T. Carvajal, C. I. Patel, M. H. Infeld and A. W. Malick, Self-emulsifying drug delivery systems (SEDDS) with polyglycolized glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs, Int. J. Pharm.(1994) 15-23.
    Open DOISearch in Google Scholar
  36. 36. Pharmaceutical Excipients, Product Reference Quick Guide, Gattefosse, Version VIII, April 2012; http://www.drug-dev.com/Media/MarketPlaceMedia/2012%20GUSA%20PHARMA%20EXCIPIENT %20GUIDE%204.16.12.pdf; access date December 12, 2012.
    Search in Google Scholar
  37. 37. J. B. Cannon, Strategies to formulate lipid-based drug delivery systems, Am. Pharm. Rev.(2011) 4.
    Search in Google Scholar
  38. 38. A. Zvonar, M. Ga{perlin and J. Kristl, Samo(mikro)emulgirajo~i sistemi - alternativen pristop za izbol{anje biolo{ke uporabnosti lipofilnih u~inkovin = Self(micro)emulsifying systems - alternative approach for improving bioavailability of lipophilic drugs, Farm. Vestn.(2008), 263-268.
    Search in Google Scholar
  39. 39. S. Charman, Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound, Pharm. Res.(1992) 87-93; DOI: 10.1023/A: 1018987928936.
    Search in Google Scholar
  40. 40. R. Neslihan Gursoy and S. Benita, Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs, Biomed. Pharmacother.(2004) 173-182; DOI: 10.1016/j. biopha.2004.02.001.
    Search in Google Scholar
  41. 41. E. S. Swenson, W. B. Milisen and W. Curatolo, Intestinal permeability enhancement: efficacy, acute local toxicity and reversibility, J. Pharm. Res.(1994) 1132-1142; DOI: 10.1023/A:1018984731584.
    Open DOISearch in Google Scholar
  42. 42. T. G. Mason, J. N. Wilking, K. Meleson, C. B. Chang and S. M. Graves, Nanoemulsions: formation, structure and physical properties, J. Phys-Condens. Mat.(2006) 635-666; DOI: 10.1088/ 0953-8984/18/41/R01.
    Search in Google Scholar
  43. 43. H. D. Oh, H. J. Kang, W. D. Kim, J. B. Lee, O. J. Kim, S. C. Yong and G. H. Choi, Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier, Int. J. Pharm.(2011) 412-418; DOI: 10.1016/j.ijpharm.2011.
    Search in Google Scholar
  44. 44. K. B. Kang, J. S. Lee and S. K. Chon, Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs, Int. J.Pharm.(2004) 65-73; DOI: 10.1016/j.ijpharm.2003.12.028.
    Open DOISearch in Google Scholar
  45. 45. S. Nazzal, I. SmalyukhI, O. D. Lavrentovich and M. A. Khan, Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: mechanism and progress of emulsion formation, Int. J. Pharm.(2002) 247-65;DOI: 10.1016/S0378-5173(02)00003-0.
    Open DOISearch in Google Scholar
  46. 46. C. W. Pouton, Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying drug delivery systems, Eur. J. Pharm. Sci.(2000) 93-98; DOI: 10.1016/S0928-0987(00)00167-6.
    Open DOISearch in Google Scholar
  47. 47. N. Anton and T. F. Vandamme, Nano-emulsions and micro-emulsions: Clarifications of the critical differences, Pharm. Res.(2011) 978-985; DOI: 10.1007/s11095-010-0309-1.
    Open DOISearch in Google Scholar
  48. 48. P. K. Suresh and S. Sharma, Formulation and in vitro characterization of self-nanoemulsifying drug delivery system of cinnarizine, Int. J. Compr. Pharm. 2011. ISSN 0976-8157.
    Search in Google Scholar
  49. 49. D. Ghai and V. R. Sinha, Nanoemulsions as self-emulsified drug delivery carriers for enhanced permeability of the poorly water-soluble selective b1-adrenoreceptor blocker Talinolol, Nanomed.- Nanotechnol.(2012) 618-626; DOI: 10.1016/j.nano.2011.08.015.
    Open DOISearch in Google Scholar
  50. 50. S. Tenjarla, Microemulsions: an overview and pharmaceutical applications, Crit. Rev. Ther. Drug.(1999) 461-521.
    Search in Google Scholar
  51. 51. P. V. Chavda, Are SMEDDs and SNEDDs same? A gimmick or pharmaceutically relevant, Mintage J. Pharm. Med. Sci.(2012) 7-10.
    Search in Google Scholar
  52. 52. D. J. McClements and J. Rao, Food-grade nanoemulsions: Formulation, fabrication, properties, performance, biological fate and potential toxicity, Crit. Rev. Food Sci.(2011) 285-330; DOI: 10.1080/10408398.2011.559558.
    Open DOISearch in Google Scholar
  53. 53. A. Martin, Physical Pharmacy, 4th ed., Lea&Febriger, London 1993, pp.127-128.
    Search in Google Scholar
  54. 54. H. Araya, M. Tomita and M. Hayashi, The novel formulation design of O/W microemulsion for improving the gastrointestinal absorption of poorly water soluble compounds, Int. J. Pharm.(2005) 61-74; DOI: 10.1016/j.ijpharm.2002.08.022.
    Search in Google Scholar
  55. 55. J. M. Lawrence, Microemulsions as drug delivery vehicles, Colloid Interface Sci.(1996) 826-832; DOI: 10.1016/S1359-0294(96)80087-2.
    Open DOISearch in Google Scholar
  56. 56. P. Solans, J. Nolla and N. Azemar, Nanoemulsions, Curr. Opin. Colloid In.(2005) 102-110; DOI: 10.1016/j.cocis.2005.06.004.
    Open DOISearch in Google Scholar
  57. 57. M. Antonietti and K. Landfester, Polyreactions in miniemulsions, Prog. Polym. Sci.(2002) 689-757; DOI: 10.1016/S0079-6700(01)00051-X.
    Open DOISearch in Google Scholar
  58. 58. T. Tadros, P. Izquierdo, J. Esquena and C. Solans, Formation and stability of nanoemulsions, Colloid Interface Sci.(2004) 303-318; DOI: 10.1016/j.cis.2003.10.023.
    Open DOISearch in Google Scholar
  59. 59. V. Sadtler, M. Rondon-Gonzales, A. Acrement, A. Choplin and E. Marie, PEO-covered nanoparticles by emulsion. Inversion point (EIP) method, Macromol. Rapid Comm.(2010) 998-1002; DOI: 10.1002/marc.200900835.
    Open DOISearch in Google Scholar
  60. 60. I. Sole, A. Maestro, C. Gonzales, C. Solans and J. M. Gutierrez, Optimization of nano-emulsion preparation by low-energy methods in an ionic surfactant system, Langmuir(2006) 8326-8332; DOI: 10.1021/Ia0613676.
    Search in Google Scholar
  61. 61. P. Shah, D. Bhalodia and P. Shelat, Nanoemulsion: A pharmaceutical review, Syst. Rev. Pharm.(2010) 24-32; DOI: 10.4103/0975-8453.59509.
    Open DOISearch in Google Scholar
  62. 62. E. Mohajeri and G. D. Noudeh, Effect of temperature on the critical micelle concentration and micellization thermodynamic of nonionic surfactants: polyoxyethylene sorbitan fatty acid esters, E. J. Chem.(2012) 2268-2274; DOI: 10.1155/2012/961739.
    Open DOISearch in Google Scholar
DOI: https://doi.org/10.2478/acph-2013-0040 | Journal eISSN: 1846-9558 | Journal ISSN: 1330-0075
Journal RSS Feed
Language: English
Page range: 427 - 445
Published on: Dec 31, 2013
Published by: Croatian Pharmaceutical Society
In partnership with: Paradigm Publishing Services
Keywords:
lipid-based drug delivery systems (LBDDS),
self-emulsifying drug delivery systems (SEDDS),
self-microemulsifying drug delivery systems (SMEDDS),
self-nanoemulsifying drug delivery systems (SNEDDS),
microemulsions,
nanoemulsions
Related subjects:
Pharmacy,
Pharmacy, other

© 2013 Katja Čerpnjak, Alenka Zvonar, Mirjana Gašperlin, Franc Vrečer, published by Croatian Pharmaceutical Society
This work is licensed under the Creative Commons License.

Volume 63 (2013): Issue 4 (December 2013)
Next article