Current status of delivery systems to improve target efficacy of oligonucleotides

Current Pharmaceutical Design

Volumn 10, Issue 7, 2004, Pages 785-796

  Shoji, Yoko ^a   Nakashima, Hideki ^a  

^a ST MARIANNA UNIVERSITY SCHOOL OF MEDICINE   (Japan)

Author keywords

Delivery system; Gene based medicine; Oligonucleotides

Indexed keywords

1,3 PROPANEDIOL; ALKYL GROUP; ANION; ANTISENSE OLIGONUCLEOTIDE; APTAMER; AVIDIN; CATION; CHOLESTEROL; DENDRIMER; DRUG VEHICLE; ESTER DERIVATIVE; GERANIOL; GLYCOPROTEIN P; LIPOFECTIN; LIPOSOME; MEMBRANE PROTEIN; MESSENGER RNA; METHYLPHOSPHONIC ACID; MORPHOLINE DERIVATIVE; MYC PROTEIN; OLIGONUCLEOTIDE; PEPTIDE NUCLEIC ACID; PHOSPHOROTHIOIC ACID DERIVATIVE; POLYETHYLENEIMINE; POLYLYSINE; POLYMER; RAS PROTEIN; RIBOZYME; STEROID; UNINDEXED DRUG;

ANALYTICAL ERROR; CELL TYPE; CHEMICAL MODIFICATION; CLINICAL TRIAL; CONCENTRATION RESPONSE; DATA ANALYSIS; DOSE RESPONSE; DRUG ADMINISTRATION ROUTE; DRUG EFFICACY; DRUG HALF LIFE; DRUG RESEARCH; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ELECTRICITY; GENE DELIVERY SYSTEM; GENE THERAPY; GENE VECTOR; GENETIC CODE; HUMAN; HUMAN GENOME; IMMUNOPATHOLOGY; IN VITRO STUDY; IN VIVO STUDY; INTERNALIZATION; KERATINOCYTE; MOLECULAR SIZE; NONHUMAN; NONVIRAL GENE DELIVERY SYSTEM; PRIORITY JOURNAL; RETINITIS; REVIEW; THROMBOCYTOPENIA; TISSUE TYPES; TREATMENT FAILURE; VIRUS CARCINOGENESIS;

ANIMALS; ANTINEOPLASTIC AGENTS; BRAIN; DELAYED-ACTION PREPARATIONS; DRUG DELIVERY SYSTEMS; DRUG DESIGN; HUMANS; OLIGONUCLEOTIDES, ANTISENSE;

EID: 1442301081     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/1381612043453009     Document Type: Review

References (125)

1. Zamecnif PC, Stephenson ML. Inhibition of Rous sarcoma virus replication and cell transformation by a specific oligodeoxynucleotide. Proc Natl Acad Sci USA 1978; 78: 280-284.
2. Goodchild J. Conjugates of oligonucleotides and modified oligonucleotides: a review of their synthesis and properties. Bioconjug Chem 1990; 1: 165-187.
3. Zon G. Oligonucleotide analogues as potential chemotherapeutic agents. Pharm Res 1998; 5: 539-549.
4. Nielsen PE. DNA analogues with nonphosphodiester backbones. Annu Rev Biophys Biomol Struct 1995; 24: 167-183.
5. Manoharan M. Review: Oligonucleotide conjugate as potential antisense drug with improved uptake, biodistribution, targeted delivery, and mechanism of action. Antisense Nucleic Acid Drug Dev 2002; 12: 103-128.
6. Stein CA. How to design an antisense oligodeoxynucleotide experiment: A consensus approach. Antisense Nucleic Acid Drug Dev 1998; 8: 129-132.
7. DeFife KM, Wong-Staal F. Integrated approaches to therapeutic target gene discovery. Curr Opin Drug Discov Devel 2002; 5: 683-689.
8. Somia N, Verma IM. Gene therapy: trials and tribulations. Nat Rev Genet 2000; 1: 91-99.
9. Turturro F. Recombinant adenovirus-mediated cytotoxic gene therapy of lymphoproliferative disorders: is CAR important for the vector to ride? Gene Ther 2003; 10: 100-104.
10. de Smet MD, Meenken CJ, van den Horn GJ. Fomivirsen - a phosphorothioate oligonucleotide for the treatment of CMV retinitis. Ocul Immunol Inflamm 1999; 7: 189-198.
11. Orr RM. Technology evaluation: fomivirsen, Isis Pharmaceuticals Inc/CIBA vision. Curr Opin Mol Ther 2001; 3: 288-294.
12. Webb MS, Zon G. Preclinical and clinical experience of antisense therapy for solid tumors. Curr Opin Mol Ther 1999; 1: 458-463.
13. Wang H, Prasad G, Buolamwini JK, Zhang R. Antisense anticancer oligonucleotide therapeutics. Curr Cancer Drug Targets 2001; 1: 177-196.
14. Cho-Chung YS. Antisense DNAs as targeted therapeutics for cancer: no longer a dream. Curr Opin Investig Drugs 2002; 3: 934-939.
15. Opalinska JB, Gewirtz AM. Nucleic-acid therapeutics: basic principles and recent applications. Nat Rev Drug Discov 2002; 1: 503-514.
16. Summerton J, Weller D. Morpholino antisense oligomers: design, preparation, and properties. Antisense Nucleic Acid Drug Dev 1997; 7: 187-195.
17. Henry SP, Novotny W, Leeds J, Auletta C, Kornburst DJ. Inhibition of coagulation by a phosphorothioate oligonucleotide. Antisense Nucleic Acid Drug Dev 1997; 7: 503-510.
18. Krieg AM, Yi AK, Matson S, Waldscmidt TJ, Bishop GA, Teasdale R, et al. CpG motifs in bacterial DNA trigger direct B-cell activation. Nature 1995; 374: 546-549.
19. Sarmiento UM, Perez JR, Becker JM, Narayanan R. In vivo toxicological effects of rel A antisense phosphorothioates in CD-1 mice. Antisense Res Dev 1994; 4: 99-107.
20. Kanamaru T, Takagi T, Takakura Y, Hashida. Biological effects and cellular uptake of c-myc antisense oligonucleotides ahd their cationic liposome complexes. J Drug Target 1998; 5: 235-246.
21. Nakai D, Seita T, Terasaki T, Iwasa S, Shoji Y, Mizushima Y, et al. Cellular uptake mechanism for oligonucleotides: involvement of endocytosis in the uptake of phosphodiester oligonucleotides by a human colorectal adenocarcinoma cell line, HCT-15. J Pharmacol Exp Ther 1996; 278: 1362-1372.
22. Shoji Y, Shimada J, Mizushima Y, Iwasawa A, Nakamura Y, Inouye K, et al Cellular uptake and biological effects of antisense oligodeoxynucleotide analogs targeted to herpes simplex virus. Antimicrob Agents Chemother 1996; 40: 1670-1675.
23. Laktinov PP, Dazard JE, Vives E, Rykova EY, lette J, Vlassov VV, et al. Characterisation of membrane oligoncueltoide-binding proteins and oligonucleotide uptake in keratinocytes. Nucleic Acid Res 1999; 27: 2315-2324.
24. Akhtar S, Juliano RL. Cellular uptake and intracellular fate of antisense oligonucleotides. TICB 1992; 2: 139-144.
25. Yakubov LA, Deeva EA, Zarytova VF, Ivanova EM, Ryte AS, Yurchenko V, et al. Mechanism of oligonucleotide uptake by cells: involvement of specific receptors? Proc Natl Acad Sci USA 1989; 86: 6454-6458.
26. Stein CA, Tonkinson JL, Zhang LM, Yakubov LA, Gervasoni J, Taub R, et al. Dynamics of the internalization of phosphodiester oligodeoxynucleotides in HL60 cells. Biochemistry 1993; 32: 4855-4861.
27. Beltinger C, Saragovi HU, Smith RM, LeSauteur L, Shah N, DeDionisio L, et al. Binding, uptake and intracellular trafficking of phosphorothioate-modified oligodeoxynucleotides. J Clin Invest 1995; 95: 1814-1823.
28. Benimetskaya L, Loike JD, Kahangir K, Like G, Silverstein S, Cao L, et al. Mac-1 (CD11b/CD18) is an oligodeoxynucleotide binding protein. Nat Med 1997; 3: 414-420.
29. Budker V, Budker T, Zhang G, Subbotin V, Loomis, Wolff JA. Hypothesis: a naked plasmid DNA is taken up cells in vivo by a receptor-mediated process. J Gene Med 2000; 2: 76-88.
30. Loke SL, Stein C, Zhang X, Avigan M, Cohen J, Neckers LM. Delivery of c-myc antisense phosphorothioate oligodeoxynucleotides to hematopoietic-cells in culture by liposome fusion - specific reduction in c-myc protein expression correlates with inhibition of cell-growth and DNS synthesis. Curr Top Microbiol Immunol 1988; 14: 282-289.
31. Islam A, Handley SL, Thompson KSJ, Akhtar S. Studies on uptake, sub-cellular trafficking and efflux of antisense oligodeoxynucleotides in glioma cells using self-assembling cationic lipoplexe as delivery systems. J Drug Targeting 2000; 7: 373-382.
32. Iversen PL, Zhu S, Meyer A, Zon G. Cellular uptake and subcellular distribution of phosphorothioate oligonucleotide into cultured cells. Antisense Res Dev 1992; 2: 211-222.
33. Alahari SK, Dean NM, Fisher MH, Delong R, Manoharan M, Tivel KL, et al. Inhibition of expression of the multidrug resistance-associated P-glycoprotein by phosphorothioate and 5′ cholesterol-conjugated antisense phosphorothioate oligonucleotides. Mol Pharmacol 1996; 50: 808-819.
34. Shoji Y, Ishige H, Tamura N, Iwatani W, Morimatsu M, Shimada J, et al. Enhancement of anti-herpetic activity of antisense phosphorothioate oligonucleotides 5′ end modified with geraniol. J Drug Targeting 1998; 5: 261-273.
35. Boffa LC, Scarfi S, Mariani MR, Damonte G, Alfrey VG, Benatti U, et al. Dihydrotestosterone as a selective cellular/nuclear localization vector for anti-gene peptide nucleic acid in prostatic carcinoma cells. Cancer Res 2000; 60: 2258-2262.
36. Kobylanska A, Pluskota E, Swiatkowska M, Wojcik M, Cierniewska-Cieslak A, Krakowiak A, et al. Inhibition of plasminogen activator inhitor release in endothelial cell cultures by antisense oligodeoxyriobnucleotides with a 5′-end lipophilic modification. Acta Biochim Pol 1999; 46: 679-691.
37. Pandolfi D, Rauzi F, Capobianco ML. Evaluation of different types of end-capping modifications on the stability of oligonucleotides toward 3′ and 5′-exonucleases. Nucleosides Nucleotides 1999; 18:2051-2069.
38. Vlassov VV, Balakireva LA, Yakubov LA'. Transport of oligonucleotide across natural and model membranes. Biochim Biophys Acta 1994; 1197: 95-108.
39. de Smidt PC, Le Doan T, de Falco S, van Berkel TU. Association of antisense oligonucleotides with lipoprotein prolongs the plasma half-life and modifies tissue distribution. Nucleic Acid Res 1991; 19: 4695-4700.
40. Felgner TL, Ringold GM. Cationic liposome-mediated transfection. Nature 19891 337: 387-388.
41. Zelphati O, Szoka FC. Intracellular distribution and mechanism of delivery of oligonucleotides mediated by cationic lipids. Pharmacol Res 1996; 13: 1367-1372.
42. Marcusson EG, Balkrishnan B, Manoharn M, Bennet CF., Dean NM. Phosphorothioate oligodeoxyribonucleotides dissociate from cationic lipids before entering the nucleus. Nucleic Acids Res 1998; 26: 2016-2023.
43. Garcia-Chaumont C, Seksek O, Grzybowska J, Borowski E, Bolard J. Delivery systems of antisense oligonucelotides. Pharmacol Ther 2000; 87: 255-277.
44. Arima A, Aramaki Y, Tsuchiya S. Effects of oligodeoxynucleotides on the physicochemical characteristics and cellular uptake of liposomes. J Pharm Sci 1997; 86: 438-442.
45. Peir P, Simoes S, Nir S, Gaspar R, Duzgunes N, deLima MCP. Interaction of cationic liposomes and their DNA complexes with monocytic leukemia cells. Biochim Bhiophys Acta 1999; 1418: 71-84.
46. Lewis JG, Lin K-Y, Kothavale A, Flanagan WM, Matteucci MD, DePrince RB, et al. Serum-resistant cytofectin for cellular delivery of antisense oligodeoxynucleotides and plasmid DNA. Proc Natl Acad Sci USA 1996; 93: 3176-3181.
47. Zelphati O, Uyechi LS, Barron LG, Szoka FC. Effect of serum components on the physico-chemical properties of cationic lipid/oligonucleotide complexes and on their interactions with cells. Biochem Biophys Acta 1998; 1390: 119-133.
48. Yoo H, Juliano RL. Enhanced delivery of antisense oligonucleotide with fluorophore-conjugated PAMAM dedrimers. Nucleic Acid Res 2000; 28: 4225-4231.
49. Bielinska A, Kukowska-latallo JF, Johnson J, Tomalia DA, Baker JR Jr. Regulation of in vitro gene expression using antisense oligonucleotides or antisense expression plasmids transfected using starburst PAMAM dendrimers. Nucleic Acids Res 1996; 24: 2176-2182.
50. Delong R, Stephenson K, Loftus T, Fisher M, Alahari S, Nolting A, et al. Characterization of complexes of oligonucleotides with polyamidoamine starburst dendrimers and effects on intracellular delivery. J Pharm Sci 1997; 86: 762-764.
51. Kukowska-Latallo JF, Bielinska AU, Johnson J, Spindler R, Tomalia DA, Baker JR Jr. Efficient transfer of genetic material into mammalian cells using Starburst polyamidoamine dendrimers. Proc Natl Acad Sci USA 1996; 93: 4897-4902.
52. Boussif O, Lezoualc'h F, Zanta MA, Mergny MD, Scherman D, Demeneix B, et al. A versatile vector for gene and oligonucleotide transfer into cells in culture and in vivo: polyethylenimine. Proc Natl Acad Sci USA 1995; 92: 7297-7301.
53. Dheur S, Dias N, van Aerschot A, Herdewijin P, Bettinger T, Remy JS, et al. Polyethylenimine but not cationic lipid improves antisense activity of 3′-capped phosphodiester oligonucleotides. Nucleic Acid Drug Dev 1999; 9: 515-525.
54. Boado RJ, Pardridge WM Complete inactivation of target mRNA by biotinylated antisense oligodeoxynucleotide-avidin conjugates. Bioconjug Chem 1994; 5: 406-410.
55. Stewart AJ, Pichon C, Meunier L, Midoux P, Monsigny M, Roche AC. Enhanced biological activity of antisense oligonucleotides complexed with glycosylated poly-L-lysine. Mol Pharmacol 1996; 50: 1487-1494.
56. Gonzalez FM, Tillman L, Hardee G, Bodmeier R. Characterization of complexes of an antisense oligonucleotide with protamine and poly-L-lysine salts. J Control Release 2001; 73: 381-390.
57. Fattal E, Vauthier C, Aynie I, Nakada Y, Lambert G, Malvy C, et al. Biodegradable polyalkylcyanoacrylate nanoparticles for the delivery of oligonucleotides. J Control Release 1998; 53: 137-143.
58. Chavany C, Ledoan T, Couvreur P, Puisieux F, Helene C. Polyalkylcyanoacrylate nanoparticles as polymeric carriers for antisense oligonucleotides. Pharm Res 1992; 9: 441-449.
59. Chavany C, Saisonbehmoaras T, Ledoan T, Puisieux F, Couvreur P, Helene C. Adsorption of oligonucleotides onto polyisohexylcyanoacrylate nanoparticles protects them against nucleases and increases their cellular uptake. Pharm Res 1994; 1: 1370-1378.
60. Bochot A, Fattal E, Gulik A, Couarraze G, Couvreur P. Liposomes dispersed within thermosensitive gel: a new dosage form for ocular delivery of oligonucleotides. Pharm Res 1998; 15: 1364-1369.
61. Wei Z, Tung CH, Zhu T, Dickerhof WA, Breslauer KJ, Georgopoulos DE, Leibowitz MJ, et al. Hybridization properties of oligodeoxynucleotide pairs bridged by polyarginine peptides. Nucleic Acids Res 1996; 24: 655-661.
62. Bochot A, Mashhour B, Puisieux F, Couvreur P, Fattal E. Comparison of the ocular distribution of a model oligonucleotide after topical instillation in rabbits of conventional and new dosage forms. J Drug Target 1998; 6: 309-313.
63. Delie F, Berton M, Allemann E, Gurny R. Comparison of two methods of encapsulation of an oligonucleotide into poly(D,L-lactic acid) particles. Int J Pharm 2001; 214: 25-30.
64. Rahman MA, Summerton J, Foster E, Cunningham K, Stirchak E, Weller D, et al. Antibacterial activity and inhibition of protein synthesis in Escherichia coli by antisense DNA analogs. Antisense Res Dev 1991; 1: 319-27.
65. Wang L, Kristensen J, Ruffner DE. Delivery of antisense oligonucleotides using HPMA polymer: synthesis of A thiol polymer and its conjugation to water-soluble molecules. Bioconjug Chem 1998; 9: 749-757.
66. Edelman ER, Simons M, Sirois MG, Rosenberg RD. c-myc in vasculoproliferative disease. Circ Res 1995; 76: 176-182.
67. Redenti E, Pietra C, Gerloczy A, Szente L. Cyclodextrins in oligonucleotide delivery. Adv Drug Deliv Rev 2001; 53: 235-244.
68. Fritz H, Maier M, Bayer E. Cationic polystyrene nanoparticles: Preparation and characterization of a model drug carrier system for antisense oligonucleotides. J Colloid Interface Sci 1997; 19: 272-288.
69. Pitha J. Polymer-cell surface interactions and drug targeting. Target drugs New York:Willey 1983; p.113-126.
70. Bochot A, Fattal E, Gulik A, Couarraze G, Couvreur P. Liposomes dispersed within a thermosensitive gel: a new dosage form for ocular delivery of oligonucleotides. Pharm Res 1998; 15: 1364-1369
71. Lamber G, Fattal E, Couvreur P. Nanoparticulate systems for the delivery of antisense oligonucleotides. Adv Drug Delivery Rev 2001; 47: 99-112.
72. Chavany C, Le Doan T, Couvreur P, Puisieux F, Helene C. Polyalkylcyanoacrylate nanoparticles as polymeric carriers for antisense oligonucleotides. Pharm Res 1992; 9: 441-449.
73. Emile C, Bazle D, Herman F, Helene C, Veillard M. Encapsulation of oligonucleotide in stealth Me.PEG-PLA50 nanoparticles by complexation with structured oligopeptide. Drug Delivery 1996; 3: 187-195.
74. Elaissari A, Cros P, Pichot C, Laurent V, Mandrand B. Adsoption of oligonucleotides onto negatively and positively charged latex particles. Colloids and Surface 1994; A 8: 325-31.
75. Chavany C, Saison-Behmoaras T, Le Doan T, Puisieux F, Couvreur P, Helene C, Adsorption of oligonucleotides onto polyisohexylcyanoacrylate nanoparticles protects them against nucleases and increases their cellular uptake. Pharm Res 1994; 11: 1370-1378.
76. Nakada Y, Fattal E, Foulquier M, Couvreur P. Pharmacokinetics and biodistribution of oligonucleotide adsorbed onto poly(isobutylcyanoacrylate) nanoparticles after intravenous administration in mice. Pharm Res 1996; 13: 38-43.
77. Schwab G, Duroux I, Chavany C, Helene C, Saison- Behmoaras E. An approach for new anticancer drugs:oncogene-targeted antisense DNA. Ann Oncol 1994; 5 (Supple 4): 55-58.
78. Schwab G, Chavany C, Duroux I, Goubin G, Lebeau C, Helen C, et al. Antisense oligonucleotides adsorbed to polyalkylcyanocarylate nanoparticles specifically inhibit mutated Ha-ras-mediated cell proliferation and tumorgenecity in nude mice. Proc Natl Acad Sci USA 1994; 91: 10460-10464.
79. Delong RK, Yoo H, Alahari SK, Fisher M, Short SM, Kang SH, et al. Novel cationic amphiphiles delivery agents for antisense oligonucleotides. Nucleic Acids Res 1999; 27: 3334-3341.
80. Hughe JA, Aronsohn AI, Avrutskaya AV, Juliano R.L. Evaluation of adjuvants that enhance the effectiveness of antisense oligonucleotides. Pharm Res 1996; 13: 404-410.
81. Jeong JH, Kim SW, Park TG. Novel intracellular delivery system of antisense oligonucleotide by self-assembled hybrid micelles composed of DNA/PEG conjugate and cationic fusogenic peptide. Bioconjug Chem 2003; 14: 473-479
82. Shi W, Siemann DW. Inhibition of renal cell carcinoma a angiogenesis and growth by antisens oligonucleotide targeting vascular endothelial growth factor. Br J Cancer 2002; 87: 119-126.
83. Yazaki T, Ahmad S, Chahlavi A, Zylberkatz E, Dean NM, Rabkin SD, et al. Treatment of blioblastoma U-87 by systemic administration of an antisense protein-kinase c-alpha phosphorothioate oligodeoxynucleotide. Mol Pharmacol 1996; 50: 236-242.
84. Takakura H, Nishikawa M, Yamashita F, Hashida M. Influence of physicochemical properties on pharmacokinetics of non-viral vectors for gene delivery. J Drug Target 2002; 10: 99-104.
85. Geary RS, Yu RZ, Levin AA. Pharmacokinetics of phosphorothioate antisense oligodeoxynucleotides. Curr Opin Investig Drugs 2001; 2: 562-573.
86. Garcia-Chaumont C, Seksek O, Grzybowska J, Borowski E, Bolard J. Delivery systems for antisense oligonucleotides. Pharmacol Ther 2000; 87: 255-277.
87. Agrawal S, Temsamani J, Galbraith W, Tang J. Pharmacokinetics of antisense oligonucleotides. Pharmacokinetics of atnisense oligonculeotides. Clin Pharmacokinet 1995; 287: 7-16.
88. Crook ST, Graham MJ, Zuckerman JE, Brooks D Conklin BS, Cummis LL, et al. Pharmacokinetic properties of several novel oligonucleotides in mice. J Pharmacol Exp Ther 1996; 277: 923-937.
89. Plenet F, Kelin-Monohoven N, Vignaud J, Duprez A. Cell and tissue distribution of synthetic oligonucleotides in healthy and tumor-bearing nude mice. Am J Pathol 1995; 147: 124-135.
90. Rifai A, Brysch W, Fadden K, Clark J, Schlingensiepen K. Clearance kinetics, biodistribution and organ saturability of phosphorothioate oligonucleotides in mice. Am J Pathol 1996; 149: 717-725.
91. Graham MJ, Crook ST, Monteith DK, Cooper SR, Lemonidis KM, Stechker KK, et al. In vivo distribution and metabolism of a phosphorothioate oligonucleotide within rat liver after intravenous administration. J Pharmacol Exp Ther 1998; 286: 447-458.
92. Tojo KJ, Ohtori A. Pharmacokinetic model of intravitreal drug injection. Math Biosci 1994; 123: 59-75.
93. Henry K, Cantril H, Fletcher C, Chinnock BJ, Balfour HH Jr. Use of intravitreal ganciclovir (dihydroxy propoxymethyl guanine) for cytomegalovirus retinitis in a patient with AIDS. Am J Ophthalmol 1987; 103: 17-23.
94. Bochot A, Fatta E, Couvreur P. Design of new eye delivery system for oligonucleotide based on a liposomal dispersion within a thermosensitive gel. In Proceeding of the Second World APG1/APV Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology Paris 1998; pp. 1089-1090.
95. Bochot A, Couvreur P, Fattal E. Intravitereal administration of antisense oligonucleotides:Potential of liposomal delivery. Progress Retinal Eye Res 2000; 19: 131-147.
96. Ogata N, Otsuji T, Matsushima M, Kimoto T, Yamanaka R, Takabashi K, et al. Phosphorothioate oligonucleotides induction into experimental colloidal neovasculization by HVJ-liposome system. Curr Eye Res 1999; 18: 261-269.
97. Vlassov VV, Karamyshev VN, Yakubov LA. Penetration of oligonucleotides into mouse organism through mucosa and skin. FEBS Lett 1993; 327: 271-274.
98. Oldenburg KR, Vo KT, Smith GA, Selick HE. Iontophoretic delivery of oligonucleotide across full thickness hairless mouse skin. J Pharm Sci 1995; 84: 915-921.
99. Zewert TE, Pliquett UF, Langer R, Weaver JC. Transdermal transport of DNA antisense oligonucleotides by electroporation. Biochem Biophys Res Commun 1995; 212: 286-292.
100. Lieb LM, Liimatta AP, Bryan RN, Brown BD, Kruger GG. Description of the intrafollicular delivery of large molecular weight to follicles of human scalp skin in vitro. J Pharm Sci 1997; 86: 1022-1029.
101. Noonberg SB, Garovoy MR, Hunt CA. Characteristics of oligonucleotide uptake in human keratinocyte cultures. J Invest Dermatol 1993; 101: 727-731.
102. Wigens M, Hooijdonk van CA, De Jongh GJ, Schalkwijk J, Van Erp PE. Flow cytometric and microscopic characterization of the uptake and distribution of phosphorothioate oligonucleotide in human keratinocytes. Arch Dermatol Res 1998; 290: 119-125.
103. Regnier V, Preat V. Locarization of a FITC-labeled phosphorothioate oligodeoxynucleotide in the skin after topical delivery by iontophoresis and electroporation. Pharm Res 1998; 15: 1596-1602.
104. Nestle FO, Mitra RS, Bennet SF, Chan H, Nickoloff BJ. Cationic lipid is not required for uptake and selective inhibitory activity of ICAM-1 phosphorothioate antisense oligonucleotides in keratinocytes. J Invest Dermatol 1994; 103: 569-575.
105. Brand RM, Hanna TL, Norris J, Iversen PL. Transdermal delivery of atnisense oligonucleotides can induce changes in gene expression in vivo. Antisense Nucleic Acid Dev 2001; 1: 1-6.
106. Brand RM, Haase K, Hannah TL, Iverswen PL. An experimental model for interpreting percutaneous penetration of oligonucleotides that incorporates the role of kerationocytes. J Invest Dermatol 1998; 11: 1166-1171.
107. Anderson JM, van Italie CM. Tight junctions and the molecular basis for regulation of paracellular permeability. Am J Physiol 1995; 269: G467-475.
108. Wang H, Cai Q, Zeng X, Yu D, Agrawal S, Zhang R. Antitumor activity and pharmacokinetics of a mixed-backbone antisense oligonucleotide targeted to the RI subunit or protein kinase A after oral administration. Proc Natl Acad Sci USA 1999; 96: 13989-13994.
109. Arora V, Knapp DC, Reddy MT, Weller DD, Iversen PL. Bioavailability and efficacy of antisense morpholino oligomers targeted to c-myc and cytochrome P-450 3A2 following oral administration in rats. J Pharm Sci 2002; 91: 1009-1018.
110. Agrawal S, Jiang Z, Zhao Q, Shaw D, Cai Q, Roskey A, et al. Mixed-backbone oligonucleotides as second generation antisense oligonucleotides: in vitro and in vivo studies. Proc Natl Acad Sci USA 1997; 94: 2620-2625.
111. Zhou W, Agrawal S. Mixed-backbone oligonucleotides as second generation antisense agents with reduced phosphorothioate-related side effects. Bioorg Med Chem Lett 1998; 8: 3269-3274.
112. Agrawal S, Zhang X, Zhao H, Lu Z, Yan J, Cai H, et al. Absorption, tissue distribution and in vivo stability in rats of a hybrid antisense oligonucleotide following oral administration. Biochem Pharmacol 1995; 50: 571-576.
113. Raoof AA, Ramtoola Z, McKenna B, Yu RZ, Hardee G, Geary RS. Effect of sodium caprate on the intestinal absorption of two modified antisense oligonucleotides in pigs. Eur J Pharm Sci 2002; 17: 131-138.
114. Gonzalez Ferreiro M, Tillman LG, Hardee G, Bodmeier R. Alginate/poly-L-lysine microparticles for the intestinal delivery of antisense oligonucleotides. Pharm Res 2002; 19: 755-764.
115. Kathmann M, Bauer U, Schlicker E. CBI receptor density and CBI receptor-mediated functional effects in rat hippocampus are decreased by an intracerebroventricularly administered antisense oligodeoxynucleotide. Naunyn-Schmiedebergs Arch Pharmacol 1999; 360: 421-427.
116. Trembly M, Rouillard C, Levesque D. Dopamine D-3 receptor antisense administration reduces basal c-fos and NGFI-B mRNA levels in the rat forebrain. Synapse 1999; 32: 51-57.
117. Yazaki T, Ahmad S, Chahlavi A, Zylberkatz E, Dean NM, Rabkin SD, et al. Treatment of glioblastoma U-87 by systemic administration of an antisense protein-kinase C-alpha phosphorothioate oligodeoxynucleotide. Mol Pharmacol 1996; 50: 236-242.
118. Khan A, Sommer W, Fux K, Akhtar S. Site-specific administration of antisense oligonucleotides using biodegradable polymer microspheres provides sustained delivery and improved subcellular biodistribution in the neostriatum of the rat brain. J Drug Target 2002; 8: 319-334.
119. Boado RJ, Pardridge WM. Complete inactivation of target mRNA by biotinylated antisense oligodeoxynucleotide-avidin conjugates. Bioconjug Chem 1994; 5: 406-410.
120. Walker TL, DeCruz EE, Dass CR, Burton MA. A method for intratumoral continuous infusion of atnisense oligonucleotides. J Pharm Sci 1998; 87: 387-389.
121. Putney SD, Brown J, Cueco C, Lee R, Skorski T, Leonetti C, et al. Enhanced anti-tumor effects wit microencapsulated c-myc antisense oligonucleotide. Antisense Nucleic Acids Drug Dev 1999; 9: 451-458.
122. Zhu X, Lu L, Windebank AJ, Yaszemski MJ. Controlled release of NFkappaB decoy oligonucleotides from biodegradable polymer microparticles. Biomaterials 2002; 23: 2683-2692.
123. Dancey JE. Agents targeting ras signaling pathway. Curr Pharm Design 2002; 8(25): 2259-67.
124. Maesaki S. Drug delivery system of anti-fungal and parasitic agents. Curr Pharm Design 2002; 8(6): 433-40.
125. Yanagihara K. Design of anti-bacterial drug and anti-mycobacterial drug for drug delivery system. Curr Pharm Design 2002; 8(6): 475-82.