In vitro and in vivo evaluation of a water-in-oil microemulsion system for enhanced peptide intestinal delivery

AAPS Journal

Volumn 15, Issue 1, 2013, Pages 288-298

  Liu, Dongyun ^a   Kobayashi, Taku ^b,c   Russo, Steven ^b,c   Li, Fengling ^b,c   Plevy, Scott E ^b,c   Gambling, Todd M ^b   Carson, Johnny L ^b   Mumper, Russell J ^a,c  

^a University of North Carolina at Chapel Hill   (United States)

^b UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^c UNIVERSITY OF NORTH CAROLINA   (United States)

Author keywords

intestinal delivery; oral; peptide; water in oil microemulsion

Indexed keywords

5 CARBOXYTETRAMETHYLRHODAMINE; 6 CARBOXYTETRAMETHYLRHODAMINE; HUMAN IMMUNODEFICIENCY VIRUS PROTEIN; MIGLYOL; OCTANOIN; OIL; PEPTIDE; PLACEBO; POLYSORBATE 80; PROTEIN; TETRAMETHYLRHODAMINE; TRANSACTIVATOR PROTEIN; UNCLASSIFIED DRUG; WATER;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CHEMICAL LABELING; COLON; CONDUCTANCE; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG STABILITY; DUODENUM; FEEDING; FEMALE; FLUORESCENCE; FLUORESCENCE MICROSCOPY; ILEUM; IN VITRO STUDY; IN VIVO STUDY; INJECTION; INTESTINE; INTESTINE FLUID; JEJUNUM; MICROEMULSION; MOUSE; NONHUMAN; PARTICLE SIZE; VISCOSITY; WATER IN OIL MICROEMULSION;

ANIMALS; DRUG DELIVERY SYSTEMS; DRUG STABILITY; ELECTRIC CONDUCTIVITY; EMULSIONS; FEMALE; INTESTINAL ABSORPTION; INTESTINES; MICE; MICE, INBRED C57BL; PEPTIDES; RHODAMINES; TAT GENE PRODUCTS, HUMAN IMMUNODEFICIENCY VIRUS; VISCOSITY;

EID: 84871960343     PISSN: 15507416     EISSN: None     Source Type: Journal    
DOI: 10.1208/s12248-012-9441-7     Document Type: Article

References (38)

1. Antosova Z, Mackova M, Kral V, Macek T. Therapeutic application of peptides and proteins: parenteral forever? Trends Biotechnol. 2009;27(11):628-35.
2. Sarciaux JM, Acar L, Sado PA. Using microemulsion formulations for oral drug delivery of therapeutic peptides. Int J Pharm. 1995;120(2):127-36.
3. Wang J, Chow D, Heiati H, Shen W-C. Reversible lipidization for the oral delivery of salmon calcitonin. J Control Release. 2003;88(3):369-80. (Pubitemid 36331879)
4. Kipnes M, Dandona P, Tripathy D, Still JG, Kosutic G. Control of postprandial plasma glucose by an oral insulin product (HIM2) in patients with type 2 diabetes. Diabetes Care. 2003;26(2):421-6. (Pubitemid 36929066)
5. Russell-Jones GJ. Use of targeting agents to increase uptake and localization of drugs to the intestinal epithelium. J Drug Target. 2004;12(2):113-23. (Pubitemid 38801449)
6. Goldberg M, Gomez-Orellana I. Challenges for the oral delivery of macromolecules. Nat Rev Drug Discov. 2003;2(4):289-95. (Pubitemid 37361687)
7. Lowman AM, Morishita M, Kajita M, Nagai T, Peppas NA. Oral delivery of insulin using pH-responsive complexation gels. J Pharm Sci. 1999;88(9):933-7. (Pubitemid 29438959)
8. Ma Z, Lim TM, Lim L-Y. Pharmacological activity of peroral chitosan-insulin nanoparticles in diabetic rats. Int J Pharm. 2005;293(1-2):271-80. (Pubitemid 40381099)
9. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev. 2000;45(1):89-121.
10. Cheng M-B, Wang J-C, Li Y-H, Liu X-Y, Zhang X, Chen D-W, et al. Characterization of water-in-oil microemulsion for oral delivery of earthworm fibrinolytic enzyme. J Control Release. 2008;129(1):41-8.
11. Constantinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Res. 1994;11(10):1385-90. (Pubitemid 24339642)
12. Ritschel WA. Microemulsion technology in the reformulation of cyclosporine: the reason behind the pharmacokinetic properties of Neoral. Clin Transplant. 1996;10(4):364-73. (Pubitemid 26300748)
13. Lyons KC, Charman WN, Miller R, Porter CJH. Factors limiting the oral bioavailability of N-acetylglucosaminyl-N-acetylmuramyl dipeptide (GMDP) and enhancement of absorption in rats by delivery in a water-in-oil microemulsion. Int J Pharm. 2000;199(1):17-28. (Pubitemid 30224501)
14. Kim SK, Lee EH, Vaishali B, Lee S, Lee Y-k, Kim C-Y, et al. Tricaprylin microemulsion for oral delivery of low molecular weight heparin conjugates. J Control Release. 2005;105(1-2):32-42. (Pubitemid 40805473)
15. Constantinides PP. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm Res. 1995;12(11):1561-72. (Pubitemid 26005509)
16. Kompella UB, Lee VHL. Delivery systems for penetration enhancement of peptide and protein drugs: design considerations. Adv Drug Deliv Rev. 2001;46(1-3):211-45. (Pubitemid 33653423)
17. Dave SH, Tilstra JS, Matsuoka K, Li F, Karrasch T, Uno JK, et al. Amelioration of chronic murine colitis by peptide-mediated transduction of the IκB kinase inhibitor NEMO binding domain peptide. J Immunol. 2007;179(11):7852-9.
18. Product information: MIGLYOL® 810, 812, 818, 829, 840 neutral oils for pharmaceuticals and cosmetics. Sasol Germany GmbH. 2004. http://abstracts.aapspharmaceutica.com/expoaaps07/Data/EC/Event/Exhibitors/263/ cb63fb76-28f4-4948-a6d0-ae249dae9c30.pdf. Accessed 19 Sept 2012.
19. ABITEC Corporation. Technical data: Capmul MCM, NF. ABITEC Corporation. 2009. http://www.abiteccorp.com/product-lines/capmul. Accessed 19 Sept 2012.
20. Inactive ingredient search for approved drug products. FDA/Center for Drug Evaluation and Research. 2012. http://www.accessdata.fda.gov/scripts/cder/ iig/index.cfm. Accessed 19 Sept 2012.
21. Tilstra J, Rehman KK, Hennon T, Plevy SE, Clemens P, Robbins PD. Protein transduction: identification, characterization and optimization. Biochem Soc Trans. 2007;35(Part 4):811-5. (Pubitemid 47310374)
22. Scott Swenson E, Curatolo WJ. (C) Means to enhance penetration: (2) Intestinal permeability enhancement for proteins, peptides and other polar drugs: mechanisms and potential toxicity. Adv Drug Deliv Rev. 1992;8(1):39-92.
23. Constantinides PP, Lancaster CM, Marcello J, Chiossone DC, Orner D, Hidalgo I, et al. Enhanced intestinal absorption of an RGD peptide from water-in-oil microemulsions of different composition and particle size. J Control Release. 1995;34(2):109-16.
24. Constantinides PP, Welzel G, Ellens H, Smith PL, Sturgis S, Yiv SH, et al. Water-in-oil microemulsions containing medium-chain fatty acids/salts: formulation and intestinal absorption enhancement evaluation. Pharm Res (New York). 1996;13 Suppl 9:S219.
25. Mehta SK, Bala K. Tween-based microemulsions: a percolation view. Fluid Phase Equilibr. 2000;172(2):197-209. (Pubitemid 32475905)
26. Lang J, Lalem N, Zana R. Quaternary water in oil microemulsions. 1. Effect of alcohol chain length and concentration on droplet size and exchange of material between droplets. J Phys Chem. 1991;95(23):9533-41.
27. Constantinides PP, Scalart JP. Formulation and physical characterization of water-in-oil microemulsions containing long- versus medium-chain glycerides. Int J Pharm. 1997;158(1):57-68. (Pubitemid 27504474)
28. Constantinides PP, Yiv SH. Particle size determination of phase-inverted water-in-oil microemulsions under different dilution and storage conditions. Int J Pharm. 1995;115(2):225-34.
29. Spernath A, Aserin A. Microemulsions as carriers for drugs and nutraceuticals. Adv Colloid Interface Sci. 2006;128-130:47-64. (Pubitemid 46215528)
30. Patel A, Vavia P. Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate. AAPS J. 2007;9(3):E344-E52. (Pubitemid 351801762)
31. Grunwald J, Rejtar T, Sawant R, Wang Z, Torchilin VP. TAT peptide and its conjugates: proteolytic stability. Bioconjug Chem. 2009;20(8):1531-7.
32. Chauhan A, Tikoo A, Kapur AK, Singh M. The taming of the cell penetrating domain of the HIV Tat: myths and realities. J Control Release. 2007;117(2):148-62. (Pubitemid 46172502)
33. Guo L, Ma E, Zhao H, Long Y, Zheng C, Duan M. Preliminary evaluation of a novel oral delivery system for rhPTH1-34: In vitro and in vivo. Int J Pharm. 2011;420(1):172-9.
34. Cole ET, Cadé D, Benameur H. Challenges and opportunities in the encapsulation of liquid and semi-solid formulations into capsules for oral administration. Adv Drug Deliv Rev. 2008;60(6):747-56.
35. Fan Y, Li X, Zhou Y, Fan C, Wang X, Huang Y, et al. Improved intestinal delivery of salmon calcitonin by water-in-oil microemulsions. Int J Pharm. 2011;416(1):323-30.
36. Coco R, Plapied L, Pourcelle V, Jérôme C, Brayden DJ, Schneider Y-J, et al. Drug delivery to inflamed colon by nanoparticles: comparison of different strategies. Int J Pharm. 2012. doi: 10.1016/j.ijpharm. 2012.07.017.
37. Hong S, Yum S, Yoo H-J, Kang S, Yoon J-H, Min D, et al. Colon-targeted cell-permeable NFκB inhibitory peptide is orally active against experimental colitis. Mol Pharmaceutics. 2012;9(5):1310-9.
38. Yoshitomi HNT, Frederick G, Dillsaver M, Higuchi T. Effect of triglyceride on small intestinal absorption of cefoxitin in rats. J Pharm Pharmacol. 1987;39(11):887-91. (Pubitemid 18048637)