Preformulation and stability in biological fluids of the retrocyclin RC-101, a potential anti-HIV topical microbicide

AIDS Research and Therapy

Volumn 8, Issue , 2011, Pages

  Sassi, Alexandra B ^a,b   Bunge, Katherine E ^c   Hood, Brian L ^a,d   Conrads, Thomas P ^a,d   Cole, Alexander M ^e   Gupta, Phalguni ^f   Rohan, Lisa C ^a,b,c  

^a UNIVERSITY OF PITTSBURGH   (United States)

^b UNIVERSITY OF PITTSBURGH   (United States)

^c UNIVERSITY OF PITTSBURGH   (United States)

^d UNIVERSITY OF PITTSBURGH CANCER INSTITUTE   (United States)

^e UNIVERSITY OF CENTRAL FLORIDA COLLEGE OF MEDICINE   (United States)

^f UNIVERSITY OF PITTSBURGH GRADUATE SCHOOL OF PUBLIC HEALTH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; HYDROGEN PEROXIDE; MICROBICIDE; RC 101; RETROCYCLIN 1; UNCLASSIFIED DRUG;

ADULT; ARTICLE; BODY FLUID; CLINICAL ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; DRUG STABILITY; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; OXIDATION; PH; PRIORITY JOURNAL; TEMPERATURE; VAGINA DISCHARGE; VAGINITIS;

EID: 79960857058     PISSN: None     EISSN: 17426405     Source Type: Journal    
DOI: 10.1186/1742-6405-8-27     Document Type: Article

References (35)

1. AIDS epidemic update. 2009, UNAIDS: WHO Library Cataloguing-in-Publication Data.
2. The Microbicide Development Strategy. MDS Working Groups - Alliance for Microbicide Development 2006, Silver Spring, MD: Alliance for Microbicide Development.
3. Shattock RJ, Moore JP. Inhibiting sexual transmission of HIV-1 infection. Nat Rev Microbiol 2003, 1:25-34. 10.1038/nrmicro729, 15040177.
4. Cole AM, Hong T, Boo LM, Nguyen T, Zhao C, Bristol G, Zack JA, Waring AJ, Yang OO, Lehrer RI. Retrocyclin: a primate peptide that protects cells from infection by T- and M-tropic strains of HIV-1. Proc Natl Acad Sci USA 2002, 99:1813-1818. 10.1073/pnas.052706399, 122276, 11854483.
5. Cole AL, Herasimtschuk A, Gupta P, Waring AJ, Lehrer RI, Cole AM. The retrocyclin analogue RC-101 prevents human immunodeficiency virus type 1 infection of a model human cervicovaginal tissue construct. Immunology 2007,
6. Lederman MM, Offord RE, Hartley O. Microbicides and other topical strategies to prevent vaginal transmission of HIV. Nat Rev Immunol 2006, 6:371-382. 10.1038/nri1848, 16639430.
7. Sassi AB, Isaacs CE, Moncla BJ, Gupta P, Hillier SL, Rohan LC. Effects of physiological fluids on physical-chemical characteristics and activity of topical vaginal microbicide products. J Pharm Sci 2008, 97:3123-3139. 10.1002/jps.21192, 17922539.
8. Lee VH. Enzymatic barriers to peptide and protein absorption. Critical Reviews in Therapeutic Drug Carrier Systems 1988, 5:69-97.
9. Al-Mushrif S, Jones BM. A study of the prevalence of hydrogen peroxide generating Lactobacilli in bacterial vaginosis: the determination of H2O2 concentrations generated, in vitro, by isolated strains and the levels found in vaginal secretions of women with and without infection. J Obstet Gynaecol 1998, 18:63-67. 10.1080/01443619868325, 15512007.
10. Rabe LK, Hillier SL. Optimization of media for detection of hydrogen peroxide production by Lactobacillus species. J Clin Microbiol 2003, 41:3260-3264. 10.1128/JCM.41.7.3260-3264.2003, 165346, 12843073.
11. Sassi AB, Cost MR, Cole AL, Cole AM, Patton DL, Gupta P, Rohan LC. Formulation Development of Retrocyclin 1 Analog RC-101 as an Anti-HIV Vaginal Microbicide Product. Antimicrob Agents Chemother 55:2282-2289.
12. Boskey ER, Moench TR, Hees PS, Cone RA. A self-sampling method to obtain large volumes of undiluted cervicovaginal secretions. Sex Transm Dis 2003, 30:107-109. 10.1097/00007435-200302000-00002, 12567165.
13. Little MC, Andrews J, Moore R, Bustos S, Jones L, Embres C, Durmowicz G, Harris J, Berger D, Yanson K, Rostkowski C, Yursis D, Price J, Fort T, Walters A, Collis M, Llorin O, Wood J, Failing F, O'Keefe C, Scrivens B, Pope B, Hansen T, Marino K, Williams K, Boenisch M. Strand displacement amplification and homogeneous real-time detection incorporated in a second-generation DNA probe system, BDProbeTecET. Clin Chem 1999, 45:777-784.
14. Nugent RP, Krohn MA, Hillier SL. Reliability of diagnosing bacterial vaginosis is improved by a standardized method of gram stain interpretation. J Clin Microbiol 1991, 29:297-301. 269757, 1706728.
15. Sassi AB, Cost MR, Cole AL, Cole AM, Patton DL, Gupta P, Rohan LC. Formulation development of retrocyclin-1 analog RC-101 as an anti-HIV vaginal microbicide product. Antimicrob Agents Chemother 2011, 55(5):2282-9. 10.1128/AAC.01190-10, 21321138.
16. Conrads KA, Yu LR, Lucas DA, Zhou M, Chan KC, Simpson KA, Schaefer CF, Issaq HJ, Veenstra TD, Beck GR, Conrads TP. Quantitative proteomic analysis of inorganic phosphate-induced murine MC3T3-E1 osteoblast cells. Electrophoresis 2004, 25:1342-1352. 10.1002/elps.200405892, 15174057.
17. Boyd MR, Gustafson KR, McMahon JB, Shoemaker RH, O'Keefe BR, Mori T, Gulakowski RJ, Wu L, Rivera MI, Laurencot CM, Currens MJ, Cardellina JH, Buckheit RW, Nara PL, Pannell LK, Sowder RC, Henderson LE. Discovery of cyanovirin-N, a novel human immunodeficiency virus-inactivating protein that binds viral surface envelope glycoprotein gp120: potential applications to microbicide development. Antimicrob Agents Chemother 1997, 41:1521-1530. 163952, 9210678.
18. Emau P, Tian B, O'Keefe B R, Mori T, McMahon JB, Palmer KE, Jiang Y, Bekele G, Tsai CC. Griffithsin, a potent HIV entry inhibitor, is an excellent candidate for anti-HIV microbicide. J Med Primatol 2007, 36:244-253. 10.1111/j.1600-0684.2007.00242.x, 17669213.
19. Kish-Catalone TM, Lu W, Gallo RC, DeVico AL. Preclinical evaluation of synthetic -2 RANTES as a candidate vaginal microbicide to target CCR5. Antimicrob Agents Chemother 2006, 50:1497-1509. 10.1128/AAC.50.4.1497-1509.2006, 1426989, 16569870.
20. Volkin DB, Sanyal G, Burke CJ, Middaugh CR. Preformulation studies as an essential guide to formulation development and manufacture of protein pharmaceuticals. Pharm Biotechnol 2002, 14:1-46. 10.1007/978-1-4615-0549-5_1, 12189723.
21. Ahern TJ, Manning MC. Stability of Protein Pharmaceuticals - Part A: Chemical and Physical Pathways of Degradation. 1992, New York: Plenum Press.
22. Owen SM, Rudolph DL, Wang W, Cole AM, Waring AJ, Lal RB, Lehrer RI. RC-101, a retrocyclin-1 analogue with enhanced activity against primary HIV type 1 isolates. AIDS Res Hum Retroviruses 2004, 20:1157-1165. 10.1089/aid.2004.20.1157, 15588337.
23. Peek LJ, Brey RN, Middaugh CR. A rapid, three-step process for the preformulation of a recombinant ricin toxin A-chain vaccine. J Pharm Sci 2007, 96:44-60. 10.1002/jps.20675, 16998874.
24. Kikwai L, Babu RJ, Kanikkannan N, Singh M. Preformulation stability of Spantide II, a promising topical anti-inflammatory agent for the treatment of psoriasis and contact dermatitis. J Pharm Pharmacol 2004, 56:19-25.
25. McNally EJ. Protein Formulation and Delivery. 2000, New York: Marcel Dekker Inc..
26. Dezzutti CS, Guenthner PC, Cummins JE, Cabrera T, Marshall JH, Dillberger A, Lal RB. Cervical and prostate primary epithelial cells are not productively infected but sequester human immunodeficiency virus type 1. J Infect Dis 2001, 183:1204-1213. 10.1086/319676, 11262202.
27. Hu J, Gardner MB, Miller CJ. Simian immunodeficiency virus rapidly penetrates the cervicovaginal mucosa after intravaginal inoculation and infects intraepithelial dendritic cells. J Virol 2000, 74:6087-6095. 10.1128/JVI.74.13.6087-6095.2000, 112107, 10846092.
28. Treves C, Vincenzini MT, Vanni P, Bardazzi F, Cattaneo A, Ogier E. Changes in enzyme levels in human cervical mucus during the menstrual cycle. Int J Fertil 1986, 31:59-66.
29. Bulletti C, de Ziegler D, Giacomucci E, Polli V, Rossi S, Alfieri S, Flamigni C. Vaginal drug delivery: The first uterine pass effect. Ann N Y Acad Sci 1997, 828:285-290. 10.1111/j.1749-6632.1997.tb48549.x, 9329849.
30. Rencher WB. Vaginal Microbicide Formulations Workshop. 2001, Arlington, VA: Lippincott-Raven.
31. Niklasson O, Skude G, Mardh PA. Lactate dehydrogenase and its isoenzymes in vaginal fluid in vaginitis/vaginosis cases and in healthy controls. Int J STD AIDS 2003, 14:270-273. 10.1258/095646203321264890, 12716498.
32. Olmsted SS, Meyn LA, Rohan LC, Hillier SL. Glycosidase and proteinase activity of anaerobic gram-negative bacteria isolated from women with bacterial vaginosis. Sex Transm Dis 2003, 30:257-261. 10.1097/00007435-200303000-00016, 12616147.
33. Roberton AM, Wiggins R, Horner PJ, Greenwood R, Crowley T, Fernandes A, Berry M, Corfield AP. A novel bacterial mucinase, glycosulfatase, is associated with bacterial vaginosis. J Clin Microbiol 2005, 43:5504-5508. 10.1128/JCM.43.11.5504-5508.2005, 1287821, 16272477.
34. Weiss TM, Yang L, Ding L, Waring AJ, Lehrer RI, Huang HW. Two states of cyclic antimicrobial peptide RTD-1 in lipid bilayers. Biochemistry 2002, 41:10070-10076. 10.1021/bi025853d, 12146971.
35. Allsworth JE, Peipert JF. Prevalence of bacterial vaginosis: 2001-2004 National Health and Nutrition Examination Survey data. Obstet Gynecol 2007, 109:114-120. 10.1097/01.AOG.0000247627.84791.91, 17197596.