Water-in-oil microemulsions for effective transdermal delivery of proteins

Expert Opinion on Drug Delivery

Volumn 8, Issue 4, 2011, Pages 537-546

  Russell Jones, Gregory ^a   Himes, Roy ^b  

^a Mentor Pharmaceutical Consulting Pty Ltd   (Australia)

^b UNIVERSITY OF WOLLONGONG   (Australia)

Author keywords

GHRP 6; IGF I; insulin; microemulsion; transdermal; vaccine delivery; weight loss

Indexed keywords

ADALIMUMAB; ALUMINUM POTASSIUM SULFATE; APOMORPHINE; ATD; CLIMIRA; CLONIDINE; CYCLOSPORIN; DESMOPRESSIN; ESTRADIOL; ETANERCEPT; FENTANYL; GLUCOSE; GLYCERYL TRINITRATE; HISTIDYL DEXTRO TRYPTOPHYLALANYLTRYPTOPHYL DEXTRO PHENYLALANYLLYSINAMIDE; IMMUNOGLOBULIN G; INFLIXIMAB; INSULIN; IODINE 125; LIDOCAINE; METHOTREXATE; NICOTINE; OXYBUTYNIN; PASSPORT; SCOPOLAMINE; SOMATOMEDIN C; TESTOSTERONE; TETANUS TOXOID; UMBELLIFERONE; UNCLASSIFIED DRUG; WATER IN OIL MICROEMULSION; WATER OIL CREAM;

ANTIBODY RESPONSE; DENDRITIC CELL; DIFFUSION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG PENETRATION; FOOT DISEASE; GLUCOSE BLOOD LEVEL; HUMAN; IMMUNOGLOBULIN BLOOD LEVEL; INFLAMMATION; LYMPH VESSEL; MICROEMULSION; NONHUMAN; OBESITY; REVIEW; SKIN BLOOD FLOW; SKIN PERMEABILITY; TOPICAL TREATMENT; TRANSDERMAL DRUG ADMINISTRATION; TRANSDERMAL PATCH; VACCINATION;

ADMINISTRATION, CUTANEOUS; ANIMALS; BIOLOGICAL TRANSPORT; DRUG CARRIERS; DRUG STABILITY; EMULSIONS; HUMANS; PEPTIDES; PROTEINS; SKIN; SKIN ABSORPTION;

EID: 79952926478     PISSN: 17425247     EISSN: None     Source Type: Journal    
DOI: 10.1517/17425247.2011.559458     Document Type: Review

References (86)

1. Subedi RK, Oh SY, Chun MK, et al. Recent advances in transdermal drug delivery. Arch Pharm Res 2010;33(3):339-51
2. Williams AC, Barry BW. Penetration enhancers. Adv Drug Deliv Rev 2004;56:603-18 (Pubitemid 38326936)
3. Walker RB, Smith EW. The role of percutaneous penetration enhancers. Adv Drug Deliv Rev 1996;18:295-301 (Pubitemid 26063305)
4. Cevce G. Lipid vesicles and other colloids as drug carriers on the skin. Adv Drug Deliv Rev 2004;56:675-711
5. Leichtnam ML, Rolland H, Wuthrich P, et al. Formulation and evaluation of a testosterone transdermal spray. J Pharm Sci 2006;95:1693-702 (Pubitemid 44229576)
6. Ainbinder D, Touitou E. Testosterone ethosomes for enhanced transdermal delivery. Drug Deliv 2005 12:297-303 (Pubitemid 41356186)
7. Gooren LJG, Bunck MCM. Transdermal testosterone delivery: Testosterone patch and gel. World J Urol 2003;21:316-19 (Pubitemid 44175245)
8. El-Kamel AH, Al-Fagih IM, Alsarra I. Testosterone solid lipid microparticles for transdermal drug delivery. Formulation and physicochamical characterization. J Microencapsul 2007;24(5):457-75 (Pubitemid 46995432)
9. Fang J-Y, Yu S-Y, Wu P-C, et al. In vitro skin permeation of estradiol from various proniosome formulations. Int J Pharm 2001;215:91-9 (Pubitemid 32206607)
10. Ghafourian T, Fooladi S. The effect of structural QSAR parameters on skin penetration. Int J Pharm 2001;217:1-11 (Pubitemid 32268628)
11. CeveCevc G, Blume G, Schatzlein A, et al. The skin: A pathway for systemic treatment with patches and lipid-based agent carriers. Adv Drug Deliv Rev 1996;18:349-78 (Pubitemid 26063309)
12. Choi MJ, Maiback HI. Liposomes and niosomes as topical drug delivery systems. Skin Pharmacol Physiol 2005;18:209-19 (Pubitemid 41159952)
13. Mezei M, Gulasekharam V. Liposomes - a selective drug delivery system for the topical route administration. I. Lotion dosage forms. Life Sci 1980;26:1473-7 (Pubitemid 10042852)
14. Mezei M, Gulasekharam V. Liposomes - a selective drug delivery system for the topical route administration: Gel dosage form. J Pharm Pharmacol 1982;34:473-4 (Pubitemid 12082555)
15. Jain S, Jain P, Umamaheshwari RB, et al. Transfersomes - A novel vesicular carrier for enhanced transdermal delivery: Development, characterization, and performance evaluation. Drug Dev Ind Pharm 2003;29:1013-26 (Pubitemid 37346103)
16. Walters KA. Penetration enhancers and their use in transdermal therapeutic systems. In: Hadgraft J, Guy RH, editors, Transdermal drug delivery, developmental issues and research initiatives, Marcel Dekker, New York; 1989. p. 197-246
17. Langer R. Transdermal drug delivery; past progress, current status, and future prospects. Adv Drug Deliv Rev 2004;56:S57-8
18. Denet A-R, Vanbever R, Preat V. Skin electroporation for transdermal and topical delivery. Adv Drug Deliv Rev 2004;56(5):659-74 (Pubitemid 38326938)
19. Kalia YN, Naik A, Garrison J, et al. Iontophoretic drug delivery. Adv Drug Deliv Rev 2004;56:619-58 (Pubitemid 38326937)
20. Giudice EL, Campbell JD. Needle-free vaccine delivery. Adv Drug Deliv Rev 2006;58:68-89
21. Krestos K, Kasting GB. Dermal capillary clearance: Physiology and model. Skin Pharmacol Physiol 2005;18:55-74 (Pubitemid 40522773)
22. Aukland K, Reed RK. Interstitial-lymphatic mechanisms in the control of extracellular fluid volume. Physiol Rev 1993;73:1-78 (Pubitemid 23065433)
23. Ikomi F, Hunt J, Hanna G, et al. Interstitial fluid, plasma protein, colloid, and leukocyte uptake into initial lymphatics. J Appl Physiol 1996;81:2060-7 (Pubitemid 26384534)
24. Reed RK, Ishibashi M, Townsley MI, et al. Blood-to-tissue clearance vs. lymph analysis in determining capillary transport characteristics for albumin in skin. Am J Physiol 1993;264:H1394-401
25. Renkin EM, Wiig H. Limits to steady-state lymph flow rates derived from plasma-to-tissue uptake measurements. Microvasc Res 1994;47:318-22
26. Schmid-Schonbein GW. Microlymphatics and lymph flow. Physiol Rev 1990;70:987-1028 (Pubitemid 20364821)
27. Leu AJ, Husmann JW, Held T, et al. Measurement of the lymphatic clearance of the human skin using a fluorescent tracer. J Vasc Res 2001;38(5):423-31 (Pubitemid 34701455)
28. Uren RF, Howard-Giles R, Thompson JF. Patterns of lymphatic drainage in the skin of patients with melanoma. J Nucl Med 2003;44:570-82 (Pubitemid 39663425)
29. Russell-Jones GJ, Ey PL, Reynolds BL. Inhibition of cutaneous anaphylaxis and arthus reactions in the mouse by antigen-specific IgA. Int Arch Allergy Appl Immunol 1981;66:316-25 (Pubitemid 12233816)
30. Russell-Jones GJ, Lee SR, McMenigall K, et al. Topical delivery of proteins using microemulsions. Proceedings of 34th International Symposium on Controlled Release of Bioactive Materials held in Los Angeles, CA; 2007
31. Russell-Jones GJ, Luke MR, Himes SR. Transdermal Delivery of Pharmaceutical Agents. WO2007070983; 2007. USP 2007/0243132. (Priority Date 22/12/05), Eu, Au (PCT 2006/001999)
32. de Wilt JH, Thompson JF, Uren RF, et al. Correlation between preoperative lymphoscintigraphy and metastatic nodal disease sites in 362 patients with cutaneous melanomas of the head and neck. Ann Surg 2004;239(4):544-52 (Pubitemid 38372771)
33. Uren RF, Howman-Giles RB, Chung D, et al. Role of lymphoscintigraphy for selective sentinel lymphadenectomy. Cancer Treat Res 2005;127:15-38
34. Uren RF, Thompson JF, Howman-Giles R, et al. The role of lymphoscintigraphy in the detection of lymph node drainage in melanoma. Surg Oncol Clin N Am 2006;15(2):285-300
35. Uren RF, Howman-Giles R, Chung DK, et al. The reproducibility in routine clinical practice of sentinel lymph node identification by pre-operative lymphoscintigraphy in patients with cutaneous melanoma. Ann Surg Oncol 2007;14(2):899-905 (Pubitemid 46175341)
36. Thompson JF, Uren RF. Lymphatic mapping in management of patients with primary cutaneous melanoma [review]. Lancet Oncol 2005;6(11):877-85 (Pubitemid 41614800)
37. Thompson JF, Uren RF, Saw RP, et al. Internal mammary node metastasis from primary cutaneous melanoma on the anterior chest. ANZ J Surg 2005;75(8):723-5 (Pubitemid 41648207)
38. Reynolds HM, Smith NP, Uren RF, et al. Three-dimensional visualization of skin lymphatic drainage patterns of the head and neck. Head Neck 2009;31(10):1316-25
39. Reynolds HM, Walker CG, Dunbar PR, et al. Functional anatomy of the lymphatics draining the skin: A detailed statistical analysis. J Anat 2010;216(3):344-55
40. Mills PC, Cross SE. Transdermal drug delivery: Basic principles for the veterinarian. Vet J 2006;172:218-33 (Pubitemid 44138698)
41. Mills PC, Magnusson BM, Cross SE. The effects of vehicle and region of application on in vitro penetration of testosterone through canine skin. Vet J 2006;171:276-80 (Pubitemid 43257231)
42. Russell-Jones GJ, Lee SR, McMenigall K, et al. Topical delivery of proteins using microemulsions. Recent advances in drug delivery systems. Salt Lake City, Utah; 2007; Elsevier, Georgia
43. Himes R, Lee S, McMenigall K, Russell-Jones GJ. Reduction in inflammation in the footpad of carrageenan treated mice following the topical administration of anti-TNF molecules formulated in a Microemulsion. JCR J Control Release 2010;145(3):210-13
44. Constantinedes PP, Scalart J-P, Lancaster C, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium chain glycerides. Pharm Res 1994;11:1385-90 (Pubitemid 24339642)
45. Paul BK, Moulik SP. Uses and applications of microemulsions. Curr Sci 2001;80:990-1001 (Pubitemid 33620215)
46. Prince LM, editor, Microemulsions, theory and practice. Academic Press, New York; 1977
47. Schulman JH, Stoeckenius W, Prince LM. Mechanism of formation and structure of microemulsions by electron microscopy. J Phys Chem 1959;63:1677-80
48. Kumar P, Mittal KL, editors, Handbook of microemulsion science and technology. CRC, Dekker, New York; 1999
49. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev 2002;54:S77-98 (Pubitemid 35379956)
50. Kreilgaard M, Pedersen EJ, Jaroszewski JW. NMR characterisation and transdermal drug delivery potential of microemulsion systems. J Control Release 2000;69:421-33
51. Kreilgaard M, Kemme MJB, Burggraaf J, et al. Influence of a microemulsion vehicle on cutaneous bioequivalence of a lipophilic model drug assessed by microdialysis and pharmacodynamics. Pharm Res 2001;18:593-9 (Pubitemid 32595786)
52. Kemken J, Ziegler A, Muller BW. Investigations into the pharmacodynamic effects of dermally administered microemulsions containing beta-blockers. J Pharm Pharmacol 1991;43:679
53. Kemken J, Ziegler A, Muller BW. Pharmacodynamic effects of transdermal bupranolol and timolol in vivo: Comparison of microemulsion and matrix patches as vehicle. Methods Find Exp Clin Pharmacol 1991;13:361-5
54. Kemken J, Ziegler A, Muller BW. Influence of supersaturation on the pharmacodynamic effect of bupranolol after dermal administration using microemulsions as vehicle. Pharm Res 1992;9:554-8
55. Sintov AC, Shapiro L. New microemulsion vehicle facilitates precutaneous penetration in vitro and cutaneous drug bioavailability in vivo. JCR 2004;95:173-83 (Pubitemid 38230033)
56. Sintov AC, Krymberk I, Gavrilov V, et al. Transdermal delivery of paracetamol for pediatric use: Effects of vehicle formulations on the percutaneous penetration. J Pharm Pharmacol 2003;55:911-19 (Pubitemid 36916681)
57. Delgado-Charro MB, Iglesias-Vilas G, Blanco-Mendez J, et al. Delivery of a hydrophilic solute through the skin from novel microemulsion systems. Eur J Pharm Biopharm 1997;43:37-42 (Pubitemid 28298808)
58. Schmalfuss U, Neubert R, Wohlrab W. Modification of drug penetration into human skin using microemulsions. J Control Release 1997;46:279-85 (Pubitemid 27132852)
59. Rhee Y-S, Choi J-G, Park E-S, et al. Transdermal delivery of ketoprofen using microemulsions. Int J Pharm 2001;228:161-70 (Pubitemid 32905375)
60. Valenta C, Schultz K. Influence of carrageenan on the rheology and skin permeation of microemulsion formulations. JCR 2004;95:257-65 (Pubitemid 38230040)
61. Shukla A, Krause A, Neubert RHH. Microemulsions as colloidal vehicle systems for dermal drug delivery. IV. Investigation of microemulsion systems based on a eutectic mixture of lidocaine and prilocaine as the colloidal phase by dynamic light scattering. J Pharm Pharmacol 2003;55:741-8 (Pubitemid 36752717)
62. Ambade KW, Jadhav SL, Gambhire MN, et al. Formulation and evaluation of flurbiprofen microemulsion. Curr Drug Deliv 2008;5:32-41 (Pubitemid 351225632)
63. Kantarci G, Ozguney I, Karasulu HY, et al. Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies. AAPS PharmSciTech 2007;2:E91-8
64. Osborne DW, Ward AJ, O'Neill KJ. Microemulsions as topical drug delivery vehicles. Part 1. Characterization of a model system. Drug Dev Ind Pharm 1988;14:1202-19
65. Osborne DW, Ward AJ, O'Neill KJ. Microemulsions as topical drug delivery vehicles: In vitro transdermal studies of a model hydrophilic drug. J Pharm Pharmacol 1991;43:450-4
66. Alvarez-Figueroa MJ, Blanco-Mendez J. Transdermal delivery of methotrexate: Ionophoretic delivery from hydrogels and passive delivery from microemulsions. Int J Pharm 2001;215:57-65 (Pubitemid 32206604)
67. Baroli B, Lopez-Quintela MA, Delgado-Charro MB, et al. Microemulsions for topical delivery of 8-methoxsalen. J Control Release 2000;69:209-18
68. Getie M, Wohlrab J, Neubert RHH. Dermal delivery of desmopressin actetate using colloidal carrier systems. J Pharm Pharmacol 2005;57:423-7 (Pubitemid 40515863)
69. Goebel A, Neubert RHH. Dermal peptide delivery using colloidal carrier systems. Skin Pharmacol Physiol 2008;21:3-9
70. Steinman RM, Pope M. Exploiting dendritic cells to improve vaccine efficiency. J Clin Invest 2002;109:1519-26 (Pubitemid 34663511)
71. Gupta PN, Mishra V, Rawat A, et al. Non-invasive vaccine delivery in transferosomes, niosomes, and liposomes: A comparative study. Int J Pharm 2005;293:73-82 (Pubitemid 40381082)
72. Ruiz-Torres A, Soares M, Kirzner M. Ageing and Longevity are related to Growth Hormon/insulin-like growth factor-1 secretion. Gerontology 2002;48:401-7 (Pubitemid 36152992)
73. Scacchi M, Pincelli AI, Cavagnini F. Growth hormone in obesity. Int J Obese Relat Metab Disord 1999;23:260-71 (Pubitemid 29118856)
74. Yang L, Morriello G, Patchett AA, et al. 1-[2(R)-(2-Amino-2- methylpropionylamino)- 3-(1H-indol-3- yl)propionyl]-3- benzylpiperidine-3(S)- carboxylic Acid Ethyl Ester (L-163,540): A potent, orally bioavailable, and short-duration growth hormone secretagogue. J Med Chem 1998;41:2439-41
75. Hillier TA, Fryburg DA, Jahn LA, et al. Extreme hyperinsulinemia unmasks insulin's effect to stimulate protein synthesis in human forearm. Am J Physiol 1998;274:E1067-74
76. Chow LS, Albright RC, Bigelow ML, et al. Mechanism of insulin's anabolic effect on muscle: Measurements of muscle protein synthesis and breakdown using aminoacyl-tRNA and other surrogate measures. Am J Physiol Endocrin Metab 2006;291:E729-36 (Pubitemid 44484914)
77. Nygren F, Nair KS. Differential regulation of protein dynamics in splanchnic and skeletal muscle beds by insulin and amino acids in healthy human subjects. Diabetes 2003;52:1377-85 (Pubitemid 36666191)
78. Fujita S, Rasmussen BB, Cadenas JG, et al. Aerobic exercise overcomes the age-related insulin resistance of muscle protein metabolism by improving endothelial function and Akt/mammalian target of rapamycin signaling. Diabetes 2007;56:1615-22 (Pubitemid 46842620)
79. Garvey WT, Olefsky JM, Marshall S. Insulin receptor down-regulation is linked to an insulin-induced postreceptor defect in the glucose transport system in rat adipocytes. J Clin Invest 1985;76:22-30 (Pubitemid 15240413)
80. Berhanu P, Kolterman OG, Baron A, et al. Insulin receptors in isolated human adipocytes: Characterization by photaffinity labeling and evidence for interanlization and cellular processing. J Clin Invest 1983;72:1958-70 (Pubitemid 14224401)
81. Knutson VP, Donnelly PV, Balba Y, et al. Insulin resistance is mediated by a proteolytic fragment of the insulin receptor. JBC 1995;270:24972-40
82. Torossian K, Nower P, Schwartz T, et al. Phorbol esters inhibit insulin-induced receptor down-regulation in cultured human lymphocytes: Association with diminished insulin receptor autophosphorylation. Biochem J 1993;290:151-8 (Pubitemid 23081213)
83. Kawakami K, Yoshikawa T, Hayashi T, et al. Microemulsion formulation for enhanced absorption of poorly soluble drugs. II. In vivo study. J Control Release 2002;81:75-82 (Pubitemid 34454851)
84. Kawakami K, Yoshikawa T, Moroto Y, et al. Microemulsion formulation for enhanced absorption of poorly soluble drugs. I. Prescription design. J Control Release 2002;81:65-74 (Pubitemid 34454850)
85. Lee PJ, Langer R, Shastri VP. Novel microemulsion enhancer formulation for simultaneous transdermal delivery of hydrophilic and hydrophobic drugs. Pharm Res 2003;20:264-9 (Pubitemid 36269734)
86. Hosmer J, Reed R, Bentley MV, et al. Microemulsions containing medium-chain glycerides as transdermal delivery systems for hydrophilic and hydrophobic drugs. AAPS PharmSciTech 2009;10(2):589-96