Biopharmaceutical challenges associated with drugs with low aqueous solubility-The potential impact of lipid-based formulations

Advanced Drug Delivery Reviews

Volumn 60, Issue 6, 2008, Pages 617-624

  O'Driscoll, C M ^a   Griffin, B T ^a  

^a UNIVERSITY COLLEGE CORK   (Ireland)

Author keywords

Bioactive excipients; In vitro in vivo correlations; Lipid based formulations; Solubility

Indexed keywords

DRUG DELIVERY; LIPIDS; PHYSICAL CHEMISTRY; SOLUBILITY;

BIOACTIVE EXCIPIENTS; IN VITRO-IN VIVO CORRELATIONS; LIPID-BASED FORMULATIONS;

DRUG PRODUCTS;

ALPHA (3,5 DI TERT BUTYL 4 HYDROXYBENZYLIDENE) GAMMA BUTYROLACTONE; CHLORPHENOTANE; CLOFAZIMINE; CREMOPHOR; CYCLOSPORIN A; EXCIPIENT; LIPID; RITONAVIR; SAQUINAVIR;

CORRELATION ANALYSIS; DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG METABOLISM; DRUG SOLUBILITY; GASTROINTESTINAL TRACT; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; LIPID SOLUBILITY; NONHUMAN; PRIORITY JOURNAL; REVIEW;

ADMINISTRATION, ORAL; ANIMALS; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; DRUG DESIGN; GASTROINTESTINAL TRACT; HUMANS; LIPIDS; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; WATER;

EID: 39149126301     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.addr.2007.10.012     Document Type: Review

References (38)

1. Amidon G.L., Lennernäs H., Shah V.P., and Crison J.R. A theoretical basis for a biopharmaceutic drug classification: the correlation in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12 (1995) 413-420
2. Dressman J.B., Amidon G.L., Reppas C., and Shah V.P. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res. 15 (1998) 11-22
3. Horter D., and Dressman J.B. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv. Drug Deliv. Rev. 46 (2001) 75-87
4. Pouton C.W. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur. J. Pharm. Sci. 11 Supp. 2 (2000) S93-S98
5. O'Driscoll C.M. Lipid based formulations for intestinal lymphatic delivery. Eur. J. Pharm. Sci. 15 (2002) 405-415
6. Porter C.J.H., Trevaskis N.L., and Charman W.N. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nature Rev. Drug Disc. 6 (2007) 231-248
7. Charman W.N. Lipids, lipophilic drugs, and oral drug delivery-some emerging concepts. J. Pharm. Sci. 89 (2000) 967-978
8. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23 (1997) 3-25
9. Wu C.Y., and Benet L.Z. Predicting drug disposition via application of BCS: Transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm. Res. 22 (2005) 11-23
10. Yazdanian M., Briggs K., Jankovsky C., and Hawi A. The "high solubility" definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm. Res. 21 (2004) 293-299
11. Lennernäs H. Intestinal drug absorption and bioavailability: beyond involvement of single transport function. J. Pharm. Pharmacol. 55 (2003) 429-433
12. Constantinides P.P., and Wasan K.M. Lipid formulation strategies for enhancing intestinal transport and absorption of P-glycoprotein (P-gp) substrate drugs: in vitro/in vivo case studies. J. Pharm. Sci. 96 (2007) 235-248
13. Fleisher D., Li C., Zhou Y., Pao L.H., and Karim A. Drug, meal and formulation interactions influencing drug absorption after oral administration-clinical implications. Clin. Pharmacokin. 36 (1999) 233-254
14. Khoo S.M., Shackleford D.M., Porter C.J.H., Edwards G.A., and Charman W.N. Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs. Pharm. Res. 20 (2003) 1460-1465
15. Williams G.C., and Sinko P.J. Oral absorption of the HIV protease inhibitors: a current update. Adv. Drug Deliv. Rev. 39 (1999) 211-238
16. Mouly S.J., Paine M.F., and Watkins P.B. Contributions of CYP3A4, P-glycoprotein, and serum protein binding to the intestinal first-pass extraction of saquinavir. J. Pharmacol. Exp. Ther. 308 (2004) 941-948
17. Meaden E.R., Hoggard P.G., Newton P., Tjia J.F., Aldam D., Cornforth D., Lloyd J., Williams I., Back D.J., and Khoo S.H. P-glycoprotein and MRP1 expression and reduced ritonavir and saquinavir accumulation in HIV-infected individuals. J. Antimicrob. Chemother. 50 (2002) 583-588
18. Park S., and Sinko P.J. P-glycoprotein and multidrug resistance-associated proteins limit the brain uptake of Saquinavir in mice. J. Pharmacol. Exp. Ther. 312 (2005) 1249-1256
19. Griffin B.T., and O'Driscoll C.M. An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat. Pharm. Res. (2007) 10.1007/s11095-007-9473-3
20. Gursoy R.N., and Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed. Pharmacother. 58 (2004) 173-182
21. Seeballuck F., Lawless E., Ashford M.B., and O'Driscoll C.M. Stimulation of triglyceride-rich lipoprotein secretion by Polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model. Pharm. Res. 21 (2004) 2320-2326
22. Seeballuck F., Ashford M.B., and O'Driscoll C.M. The effects of Pluronic (R) block copolymers and Cremophor (R) EL on intestinal lipoprotein processing and the potential link with P-glycoprotein in Caco-2 cells. Pharm. Res. 20 (2003) 1085-1092
23. Woodcock D.M., Linsenmeyer M.E., Chojnowski G., Kriegler A.B., Nink V., Webster L.K., and Sawyer W.H. Reversal of multidrug resistance by surfactants. Br. J. Cancer 66 (1992) 62-68
24. Nerurkar M.M., Burton P.S., and Borchardt R.T. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux system. Pharm. Res. 13 (1996) 528-534
25. O'Driscoll C.M. Intestinal lymphatic targeting of drugs. STP Pharma Sci. 13 (2003) 17-25
26. Porter C.J.H., and Charman W.N. Intestinal lymphatic drug transport: an update. Adv. Drug Deliv. Rev. 50 (2001) 61-80
27. Perry C.M., and Noble S. Saquinavir soft-gel capsule formulation. A review of its use in patients with HIV infection. Drugs 55 (1998) 461-486
28. Griffin B.T., and O'Driscoll C.M. A comparison of intestinal lymphatic transport and systemic bioavailability of saquinavir from three lipid-based formulations in the anaesthetised rat model. J. Pharm. Pharmacol. 58 (2006) 917-925
29. Karpf D.M., Holm R., Garafalo C., Levy E., Jacobsen J., and Müllertz A. Effect of different surfactants in biorelevant medium on the secretion of a lipophilic compound in lipoproteins using Caco-2 cell culture. J. Pharm. Sci. 95 (2006) 45-55
30. Cuine J.F., Charman W.N., Pouton C.W., Edwards G.A., and Porter C.J.H. Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs. Pharm. Res. 24 (2007) 748-757
31. Porter C.J.H. Using In Vitro Data to Guide and Explain In Vivo Performance: Case Studies in AAPS Spring Workshop on Effective Utilization of Lipid Based Systems to Enhance the Delivery of Poorly Soluble Drugs: Physiochemical, Biopharmaceutical and Product Development Considerations (2007)
32. Cao X.H., Gibbs S.T., Fang L.Y., Miller H.A., Landowski C.P., Shin H.C., Lennernäs H., Zhong Y.Q., Amidon G.L., Yu L.X., and Sun D.X. Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat models. Pharm. Res. 23 (2006) 1675-1686
33. Chiou W.L., Jeong H.Y., Chung S.M., and Wu T.C. Evaluation of using dog as an animal model to study the fraction of oral dose absorbed of 43 drugs in humans. Pharm. Res. 17 (2000) 135-140
34. Kararli T.T. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory-animals. Biopharm. Drug Dispos. 16 (1995) 351-380
35. Davis S.S., Illum L., and Hinchcliffe M. Gastrointestinal transit of dosage forms in the pig. J. Pharm. Pharmacol. 53 (2001) 33-39
36. Goh L.B., Spears K.J., Yao D.G., Ayrton A., Morgan P., Wolf C.R., and Friedberg T. Endogenous drug transporters in in vitro and in vivo models for the prediction of drug disposition in man. Biochem. Pharmacol. 64 (2002) 1569-1578
37. Petri N., Bergman E., Forsell P., Hedeland M., Bondesson U., Knutson L., and Lennernäs H. First-pass effects of Verapamil on the intestinal absorption and liver disposition of fexofenadine in the porcine model. Drug Metab. Dispos. 34 (2006) 1182-1189
38. Tannergren C., Evilevitch L., Pieyzynowski S., Piedra J.V., Westrom B., Erlwanger K., Tatara M., and Lennernäs H. The effect of pancreatic and biliary depletion on in vivo pharmacokinetics of Digoxin in pigs. Eur. J. Pharm. Sci. 29 (2006) 198-204