Rectal microbicides: Clinically relevant approach to the design of rectal specific placebo formulations

AIDS Research and Therapy

Volumn 8, Issue , 2011, Pages

  Wang, Lin ^a   Schnaare, Roger L ^a   Dezzutti, Charlene ^a,b   Anton, Peter A ^c   Rohan, Lisa C ^a,b,d  

^a UNIVERSITY OF PITTSBURGH   (United States)

^b UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d UNIVERSITY OF PITTSBURGH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CAPRIC TRIGLYCERIDE; CAPRYLIC TRIGLYCERIDE; CARBOMER; GELLING AGENT; GLYCEROL STEARATE; LIPID; MACROGOL STEARATE; MICROBICIDE; MYRISTIC ACID DERIVATIVE; MYRISTIC ACID ISOPROPYL ESTER; MYRISTIC ACID MYRISTYL ESTER; PLACEBO; POLOXAMER; POLYETHYLENE GLYCOL 75 STEARATE; POLYMER; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AQUEOUS SOLUTION; ARTICLE; CONTROLLED STUDY; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; EX VIVO STUDY; EXPLANT; FLOW KINETICS; GEL; HUMAN; HUMAN TISSUE; HYDROPHILICITY; IN VITRO STUDY; IN VIVO STUDY; LIQUID; NONHUMAN; OSMOLALITY; PH; PRIORITY JOURNAL; RABBIT; ROOM TEMPERATURE; SHEAR STRENGTH; THERMAL ANALYSIS; THIXOTROPY;

EID: 79952328020     PISSN: None     EISSN: 17426405     Source Type: Journal    
DOI: 10.1186/1742-6405-8-12     Document Type: Article

References (35)

1. Joint United Nations Programme on HIV/AIDS (UNAIS) 2007 AIDS Epidemic Update. , http://www.unaids.org/en/KnowledgeCentre/HIVData/EpiUpdate/EpiUpdArchive/2007/default.asp
2. Kinsley LA, Kaslow R, Rinaldo CR, Detre K, Odaka N, Vanraden M, Detels R, Polk BF, Chmeil J, Kelsey SF, Ostrow D, Visscher B. Risk factors for seroconversion to human immunodeficiency virus among male homosexuals: Results from the multicenter AIDS cohort study. Lancet 1987, 329(8529):345-400.
3. Multiple chances. Findings from the United Kingdom Gay Men's Sex Survey 2006. Sigma Research 2008 (ISBN 1 872956 94 7). , http://www.sigmaresearch.org.uk/files/report2008c.pdf
4. Out and about. Findings from the United Kingdom Gay Men's Sex Survey 2002. Sigma Research 2003 (ISBN 1 872956 71 8). , http://www.sigmaresearch.org.uk/files/report2003f.pdf
5. McGowan I. Rectal microbicides: a new focus for HIV prevention. Sex Transm Infect 2009, 84(6):413-7.
6. Anton PA. A Phase I safety and acceptability study of the UC-781microbicide gel applied rectally in HIV seronegative adults: an interim safety report at 50% completion. Microbicides 2008 Abstract BO5-290. , http://www.aidsmap.com/en/news/357B9187-9B33-45D8-AA17-570A37781B29.asp
7. Anton PA, Adler A, Khanukhova E, Elliott J, Cumberland W, Zhou Y, Ventuneac A, Carballo-Dieguez A, Mauck C, McGowan I. A phase I rectal safety and acceptability study of UC781 microbicide gel. 16th Conference on Retroviruses and Opportunistic Infections, Montreal, Canada 2009, [abstract Y-147]., http://retroconference.org/2009/Abstracts/33634.htm
8. Tabet SR, Surawicz C, Horton S, Paradise M, Coletti AS, Gross M, Fleming TR, Buchbinder S, Haffitt RC, Levine H, Kelly CW, Celum CL. Safety and toxicity of nonoxynol-9 gel as a rectal microbicide. Sex Transm Dis 1990, 26(10):564-71.
9. Phillips DM, Taylor CL, Zacharoupoulos VR, Maguire RA. Nonoxynol-9 causes rapid exfoliation of sheets of rectal epithelium. Contraception 2000, 62(3):149-54. 10.1016/S0010-7824(00)00156-6, 11124363.
10. Phillips DM, Sudol KM, Taylor CL, Guichard L, Elsen R, Maguire RA. Lubricants containing N-9 may enhance rectal transmission of HIV and other STDs. Contraception 2004, 70(2):107-10. 10.1016/j.contraception.2004.04.008, 15288213.
11. Patton DL, Cosgrove SYT, Rabe LK, Hiller SL. Rectal applications of Nonoxynol-9 cause tissue disruption in a monkey model. Sex Transm Dis 2002, 29(10):581-7. 10.1097/00007435-200210000-00004, 12370525.
12. Carbollo-Dieguez A, Stein Z, Saez H, Dolezal C, Nieves-Rosa L, Diaz F. Frequent use of lubricants for anal sex among men who have sex with men: the HIV prevention potential of a microbicidal gel. Am J Public Health 2000, 90(7):1117-21. 10.2105/AJPH.90.7.1117, 1446289, 10897191.
13. Sudol KM, Phillips DM. Relative safety of sexual lubricants for rectal intercourse. Sex Trans Dis 2004, 31(6):346-9.
14. Fuchs EJ, Lee LA, Torbenson MS, Parsons TL, Bakshi RP, Guidon AM, Wahl RL, Hendrix CW. Hyperosmolar sexual lubricant causes epithelial damage in the distal colon: potential implication for HIV transmission. J Infect Dis 2007, 195(1):703-10. 10.1086/511279, 17262713.
15. Hendrix CW, Fuchs EJ, Macura KJ, Lee LA, Parsons TL, Bakshi RP, Khan WA, Guidos A, Leal JP, Wahl R. Quantitative imaging and sigmoidoscopy to assess distribution of rectal microbicide surrogates. Clin Pharmacol and Ther 2008, 83(1):97-105.
16. Romano J, Malcolm RK, Garg S, Rohan LC, Kaptur PE. Microbicide delivery: formulation technologies and strategies. Curr Opin HIV Aids 2008, 3(5):558-66. 10.1097/COH.0b013e328305b96e, 19373022.
17. Patton DL, Gosgrove Sweeney YT, Paul KJ. A summary of preclinical topical microbicide rectal safety and efficacy evaluations in a pigtailed macaque model. Sex Transm Dis 2009, 36(6):350-6. 10.1097/OLQ.0b013e318195c31a, 2749653, 19556929.
18. Garg S, Kandarapu R, Vermani K, Tambwekar KR, Garg A, Waller DP, Zaneveld LJD. Development pharmaceutics of microbicide formulations. Part I: Preformulation considerations and challenges. Aids Pat Care and STDs 2003, 17(1):17-32.
19. Garg S, Tambwekar KR, Vermani K, Kandarapu R, Garg A, Waller DP, Zaneveld LJD. Development pharmaceutics of microbicide formulations. Part II: Formulation, evaluation, and challenges. Aids Pat Care and STDs 2004, 17(8):377-99.
20. Anton P. Compartment specific topical microbicide formulations. PAR-03-137. NIH/NIAID. U19 AI060614.8/1/06-7/31-09.
21. Guidance for Industry Q1A(R2) Stability Testing of New Drug Substances and Products. , http://www.fda.gov/downloads/regulatoryinformation/guidances/ucm128204.pdf
22. Porter CJH, Pouton CW, Cuine JF, Charman WN. Enhancing intestinal drug solubilization using lipid-based delivery systems. Adv Drug Del Rev 2008, 60:673-91.
23. Hoener B, Benet LZ. Factors influencing drug absorption and drug availability. Modern Pharmaceutics 2002, 93-117. New York: Marcel Dekker, Banker GS, Rhodes CT.
24. GRAS Substances (SCOGS) Database. 2006, http://www.fda.gov/Food/FoodIngredientsPackaging/GenerallyRecognizedasSafeGRAS/GRASSubstancesSCOGSDatabase/default.htm
25. Burdock GA, Carabin IG. Generally recognized as safe (GRAS): history and description. Toxicol Lett 2004, 150:3-18. 10.1016/j.toxlet.2003.07.004, 15068820.
26. Garg S, Tambwekar KR, Vermani K, Garg A, Kaul CL, Zaneveld LJD. Compendium of pharmaceutical excipients forvaginal formulations. Pharm Tech 2001, 25:14-24.
27. Thirawong N, Nunthanid J, Puttipipatkhachorn S, Sriamornsak P. Mucoadhesive properties of various pectins on gastrointestinal mucosa: An in vitro evaluation using texture analyzer. Eur J Pharm and Biopharm 2007, 67(1):132-40.
28. Jones DS, Lawlor MS, Woolfson AD. Examination of the flow, rheological and textural properties of polymer gels composed of poly(methylvinylether-co-maleic anhydride) and poly(vinylpyrrolidone): Rheological and mathematical interpretation of textural parameters. J Phar Sci 2002, 91(9):2090-101.
29. ISO 4074:2002. Natural latex rubber condoms -- Requirements and test methods. , http://www.ISO.org
30. ASTM D 3492. Standard specification for rubber contraceptives (male condoms). 2008, http://engineers.ihs.com/document/abstract/
31. The GCC guidelines for stability testing of drug substances and pharmaceutical products, Edition Two, 1428 h -2007 g. , http://www.ich.org
32. Microbial Limit Tests <61>. 2004, USP 27.
33. Antimicrobial Effectiveness Testing <51>. 2004, USP 27.
34. Abner SR, Guenthner PC, Guarner J, Hancock KA, Cunnins JE, Fink A, Gilmore GT, Staley C, Ward A, Ali O, Binderow S, Cohen S, Grohskopf LA, Paxton L, Hart CE, Dezzutti CS. A human colorectal explant culture to evaluate topical microbicides for the prevention of HIV infection. J Infect Dis 2005, 192:1545-56. 10.1086/462424, 16206069.
35. Rohan LC, Moncla BJ, Kunjara Na Ayudhya RP, Cost M, Huang Y, Gai F, Billitto N, Lynam JD, Pryke K, Graebing P, Hopkins N, Rooney JF, Friend D, Dezzutti CS. In vitro and ex vivo testing of tenofovir shows it is effective as an HIV-1 microbicide. PLoS One 2010, 5(2):e9310. 10.1371/journal.pone.0009310, 2824823, 20174579.