Vaginal rings for delivery of HIV microbicides

International Journal of Women's Health

Volumn 4, Issue 1, 2012, Pages

  Karl Malcolm, R ^a   Fetherston, Susan M ^a   McCoy, Clare F ^a   Boyd, Peter ^a   Major, Ian ^a  

^a QUEEN'S UNIVERSITY BELFAST   (United Kingdom)

Author keywords

Antiretroviral; Controlled release; Dapivirine; SILCS diaphragm; Silicone elastomer; Sustained release; Thermoplastic

Indexed keywords

ACICLOVIR; CARBOPOL 974P; DAPIVIRINE; DIMETICONE; ELCOMETRINE; ESTRADIOL; ESTRADIOL ACETATE; ETHINYLESTRADIOL; ETHINYLESTRADIOL PLUS ETONOGESTREL; ETONOGESTREL; GANCICLOVIR; MARAVIROC; MICROBICIDE; N [4 CHLORO 3 (3 METHYL 2 BUTENYLOXY)PHENYL] 2 METHYL 3 FURANCARBOTHIOAMIDE; NONOXINOL 9; PLACEBO; POLYURETHAN; SILASTIC; TENOFOVIR;

BIOCOMPATIBILITY; COMBINATION CHEMOTHERAPY; CONTROLLED DRUG RELEASE; CROSS LINKING; DOSE TIME EFFECT RELATION; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG MANUFACTURE; DRUG SAFETY; DRUG TISSUE LEVEL; DRUG TOLERABILITY; EQUIPMENT DESIGN; ESTROGEN DEFICIENCY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MENOPAUSAL SYNDROME; MONOTHERAPY; NONHUMAN; OFF LABEL DRUG USE; REVIEW; SCALE UP; SUSTAINED DRUG RELEASE; TREATMENT DURATION; VAGINA RING; VIROTHERAPY;

EID: 84869762811     PISSN: None     EISSN: 11791411     Source Type: Journal    
DOI: 10.2147/IJWH.S36282     Document Type: Review

References (58)

1. Folkman J, Long DM, Rosenbaum R. Silicone rubber: a new diffusion property useful for general anesthesia. Science. 1966;154(3745): 148-149.
2. Folkman J, Long DM. The use of silicone rubber as a carrier for prolonged drug therapy. J Surg Res. 1964;4(3):139-142.
3. Dziuk PJ, Cook B. Passage of steroids through silicone rubber. Endocrinology. 1966;78(1):208-211.
4. Duncan G W, inventor; The Upjohn Company, assignee. Medicated devices and methods. United States patent US 3545439. December 8, 1970.
5. Hoffman AS. The origins and evolution of "controlled" drug delivery systems. J Control Release. 2008;132(3):153-163.
6. Gupta KM, Pearce SM, Poursaid AE, et al. Polyurethane intravaginal ring for controlled delivery of dapivirine, a nonnucleoside reverse tran-scriptase inhibitor of HIV-1. J Pharm Sci. 2008;97(10):4228-4239.
7. Johnson T, Gupta K, Fabian J, Albright T, Kiser P. Segmented polyurethane intravaginal rings for the sustained combined delivery of antiretroviral agents dapivirine and tenofovir. Eur J Pharm Sci. 2010;39(4):203-212.
8. Clark MR, Kiser PF, Loxley A, McConville C, Malcolm RK, Friend DR. Pharmacokinetics of UC781-loaded intravaginal ring segments in rabbits: a comparison of polymer matrices. Drug Deliv Transl Res. 2011;1(3):238-246.
9. Kaur M, Gupta KM, Poursaid AE, et al. Engineering a degradable polyurethane intravaginal ring for sustained delivery of dapivirine. Drug Delivery Trans Res. 2011;1(3):223-237.
10. Colas A, Curtis J. Silicone biomaterials: history and chemistry. In: Biomaterials Science: An Introduction to Materials in Medicine. 2nd ed. Elsevier Academic Press; 2004:80-85.
11. Curtis J, Colas A. Medical applications of silicones. In: Ratner BD, Hoffman AS, Schoen FJ, Lemons JE, editors. Biomaterials Science: An Introduction to Materials in Medicine. 2nd ed. Elsevier Academic Press; 2004:698-707.
12. Al-Azzawi F, Buckler HM; for the United Kingdom Vaginal Ring Investigator Group. Comparison of a novel vaginal ring delivering estradiol acetate versus oral estradiol for relief of vasomotor menopausal symptoms. Climacteric. 2003;6(2):118-127.
13. Barentsen R, vandeWeijer PHM, Schram JHN. Continuous low dose estradiol released from a vaginal ring versus estriol vaginal cream for urogenital atrophy. Eur J Obstet Gynecol Reprod Biol. 1997;71(1):73-80.
14. Buckler H, Al-Azzawi F; for the UK VR Multicentre Trial Group. The effect of a novel vaginal ring delivering oestradiol acetate on climacteric symptoms in postmenopausal women. Brit J Obstet Gynecol. 2003;110(8):753-759.
15. Speroff L. Efficacy and tolerability of a novel estradiol vaginal ring for relief of menopausal symptoms. Obstet Gynecol. 2003;102(4): 823-834.
16. Croxatto HB, Brache V, Massai R, et al. Feasibility study of Nestorone-ethinylestradiol vaginal contraceptive ring for emergency contraception. Contraception. 2006;73(1):46-52.
17. Kumar N, Koide SS, Tsong Y, Sundaram K. Nestorone: a progestin with a unique pharmacological profle. Steroids. 2000;65(10-11):629-636.
18. Fraser IS, Weisberg E, Brache V, et al. Serum Nestorone and ethinyl estradiol levels, and ovulation inhibition in women using three different dosage combinations of a Nestorone progestogen-ethinyl estradiol contraceptive vaginal ring on a bleeding-signaled regimen. Contraception. 2005;72(1):40-45.
19. Sivin I, Mishell DR Jr, Alvarez F, et al. Contraceptive vaginal rings releasing Nestorone and ethinylestradiol: a 1-year dose-finding trial. Contraception. 2005;71(2):122-129.
20. Malcolm K, Woolfson D, Russell J, Andrews C. In vitro release of nonoxynol-9 from silicone matrix intravaginal rings. J Control Release. 2003;91(3):355-364.
21. Van Damme L, Ramgee G, Alvary M, et al. Effectiveness of COL-1492, a nonoxynol-9 vaginal gel, on HIV-1 transmission in female sex workers: a randomised controlled trial. Lancet. 2002;360(9338): 971-977.
22. Roddy RE, Zekeng L, Ryan K, et al. A controlled trial of nonoxynol 9 flm to reduce male-to-female transmission of sexually transmitted diseases. N Engl J Med. 1998;339:504-510.
23. Malcolm RK, Woolfson AD, Toner CF, et al. Long-term, controlled release of the HIV microbicide TMC120 from silicone elastomer vaginal rings. J Antimicrob Chemother. 2005;56(5):954-956.
24. Romano J, Variano B, Coplan P, Van Roey J, Douville K, Rosenberg Z. Safety and availability of dapivirine (TMC120) delivered from an intravaginal ring. AIDS Res Hum Retroviruses. 2009;25(5):483-488.
25. Nel A, Smythe S, Young K, et al. Safety and pharmacokinetics of dapivirine delivery from matrix and reservoir intravaginal rings to HIV-negative women. J Acquir Immune Defc Syndr. 2009;51(4):416-423.
26. Di Fabio S, Van Roey J, Giannini G, et al. Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse tran-scriptase inhibitor TMC120 in a gel formulation. AIDS. 2003;17(11): 1597-1604.
27. Herrewege Y V, Michiels J, Van Roey J, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodefciency virus microbicides. Antimicrob Agents Chemother. 2004;48(1):337-339.
28. Woolfson AD, Elliott GR, Gilligan CA, Passmore CM. Design of an intravaginal ring for the controlled delivery of 17 beta-estradiol as its 3-acetate ester. J Control Release. 1999;61(3):319-328.
29. Woolfson AD, Malcolm RK, Gallagher RJ. Design of a silicone reservoir intravaginal ring for the delivery of oxybutynin. J Control Release. 2003;91(3):465-476.
30. Woolfson AD, Malcolm RK, Gorman S P, Jones DS, Brown AF, McCullagh SD. Self-lubricating silicone elastomer biomaterials. J Mater Chem. 2003;13(10):2465-2470.
31. Malcolm RK, McCullagh SD, Woolfson AD, Gorman SP, Jones DS, Cuddy J. Controlled release of a model antibacterial drug from a novel self-lubricating silicone biomaterial. J Control Release. 2004;97(2): 313-320.
32. Promadej-Lanier N, Smith J, Srinivasan P, et al. Development and evaluation of a vaginal ring device for sustained delivery of HIV microbicides to non-human primates. J Med Primatol. 2009;38(4):263-271.
33. Fetherston S, Geer L, Veazey RS, et al. Partial protection against multiple RT-SHIV162P3 vaginal challenge of rhesus macaques by a silicone elastomer vaginal ring releasing the NNRTI MC1220. J Antimicrob Chemother. In press.
34. Malcolm RK, Veazey RS, Geer L, et al. Sustained release of the CCR5 inhibitors CMPD167 and maraviroc from vaginal rings in rhesus macaques. Antimicrob Agents Chemother. 2012;56(5):2252-2258.
35. Sulak PJ, Smith V, Coffee A, et al. Frequency and management of breakthrough bleeding with continuous use of the transvaginal contraceptive ring: a randomized controlled trial. Obstets Gynecol. 2008;112(3):563-571.
36. Loxley A, Mitchnick M, Okoh O, et al. Ethylene vinyl acetate intrav-aginal rings for the simultaneous delivery of the antiretroviral UC781 and contraceptive levonorgestrel. Drug Delivery Trans Res. 2011;1(3): 247-255.
37. Clark MR, Johnson TJ, McCabe RT, et al. A hot-melt extruded intrav-aginal ring for the sustained delivery of the antiretroviral microbicide UC781. J Pharm Sci. 2012;101(2):576-587.
38. Baum MM, Butkyavichene I, Gilman J, et al. An intravaginal ring for the simultaneous delivery of multiple drugs. J Pharm Sci. 2012;101(8): 2833-2843.
39. Keller MJ, Malone AM, Carpenter CA, et al. Safety and pharmacokinet-ics of aciclovir in women following release from a silicone elastomer vaginal ring. J Antimicrob Chemother. 2012;67(8):2005-2012.
40. Moss JA, Malone AM, Smith TJ, et al. Simultaneous delivery of tenofovir and acyclovir via an intravaginal ring. Antimicrob Agents Chemother. 2012;56(2):875-882.
41. Morrow RJ, Woolfson AD, Donnelly L, et al. Sustained release of proteins from a modifed vaginal ring device. Eur J Pharm Biopharm. 2011;77(1):3-10.
42. Woolfson AD, Umrethia ML, Kett VL, et al. Freeze-dried, mucoadhe-sive system for vaginal delivery of the HIV microbicide, dapivirine: optimisation by an artifcial neural network. Int J Pharm. 2010;388: 136-143.
43. Vartiainen J, Wahlström T, Nilsson CG. Effects and acceptability of a new 17 beta-oestradiol-releasing vaginal ring in the treatment of postmenopausal complaints. Maturitas. 1993;17(2):129-137.
44. Han YA, Singh M, Saxena BB. Development of vaginal rings for sustained release of nonhormonal contraceptives and anti-HIV agents. Contraception. 2007;76(2):132-138.
45. Saxena B, Han Y, Fu D, et al. Sustained release of microbicides by newly engineered vaginal rings. AIDS. 2009;23(8):917-922.
46. Yang CC, Maravilla KR, Kilbourne-Brook M, Austin G. Magnetic resonance imaging of SILCS diaphragm: anatomical considerations and corroboration with clinical ft. Contraception. 2007;76(3):238-244.
47. Coffey PS, Kilbourne-Brook M, Brache V, Cochón L. Comparative acceptability of the SILCS and Ortho ALL-FLEX® diaphragms among couples in the Dominican Republic. Contraception. 2008;78(5): 418-423.
48. Coffey PS, Kilbourne-Brook M. Wear and care of the SILCS diaphragm: experience from three countries. Sex Health. 2010;7(2):159-164.
49. Coffey PS, Kilbourne-Brook M, Beksinska M, Thongkrajai E. Short-term acceptability of a single-size diaphragm among couples in South Africa and Thailand. J Fam Plann Reprod Health Care. 2008;34(4):233-236.
50. Schwartz JL, Ballagh SA, Creinin MD, et al. SILCS diaphragm: post-coital testing of a new single-size contraceptive device. Contraception. 2008;78(3):237-244.
51. Moench TR, Chipato T, Padian NS. Preventing disease by protecting the cervix: the unexplored promise of internal vaginal barrier devices. AIDS. 2001;15(13):1595-1602.
52. Friend D. Intravaginal rings: controlled release systems for contraception and prevention of transmission of sexually transmitted infections. Drug Deliv Transl Res. 2011;1(3):185-193.
53. Friend D, Doncel G. Combining prevention of HIV-1, other sexually transmitted infections and unintended pregnancies: development of dual-protection technologies. Antiviral Res. 2010;88 Suppl 1: S47-S54.
54. Thurman AR, Clark MR, Doncel GF. Multipurpose prevention technologies: biomedical tools to prevent HIV-1, HSV-2, and unintended pregnancies. Infect Dis Obstet Gynecol. Epub 2011 Aug 9.
55. Major I, Lowry D, Malcolm K, et al. Development of a microbicide-releasing diaphragm as an HIV prevention strategy. Conf Proc IEEE Eng Biol Soc. 2010:1089-1092.
56. Major I, Boyd P, Kilbourne-Brook M, et al. A modified SILCS contraceptive diaphragm for long-term controlled release of the HIV microbicide dapivirine. Contraception. In press.
57. Malcolm RK, Edwards KL, Kiser P, Romano J, Smith TJ. Advances in microbicide vaginal rings. Antiviral Res. 2010;88 Suppl 1: S30-S39.
58. Aravantinou M, Singer R, Derby N, et al. The nonnucleoside reverse transcription inhibitor MIV-160 delivered from an intravaginal ring, but not from a carrageenan gel, protects against simian/human immu-nodefciency virus-RT infection. AIDS Res Human Retrovir. 2012. In press.