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  • Title: Spermicidal and antiviral properties of cholic acid: contraceptive efficacy of a new vaginal sponge (Protectaid) containing sodium cholate.
    Author: Psychoyos A, Creatsas G, Hassan E, Georgoulias V, Gravanis A.
    Journal: Hum Reprod; 1993 Jun; 8(6):866-9. PubMed ID: 7688380.
    Abstract:
    Cholic acid (sodium cholate) exhibits a strong spermicidal and antiviral [anti-human immunodeficiency virus (HIV)-1] activity. The same effects are observed for F-5 Gel, the active mixture of a new contraceptive sponge (Protectaid), which contains sodium cholate in association with low concentrations (0.5%) of nonoxynol-9 and benzalkonium chloride. Both cholic acid and the F-5 Gel exert a dose-dependent, in-vitro inhibitory effect (i) on the activity of HIV-1 associated reverse transcriptase in an acellular system and (ii) on the potential of HIV-1 efficiently to infect human lymphocytes. During 12 months use, the contraceptive efficacy of the 'Protectaid' sponge was 100% in 20 young women who had chosen this method for reasons of both contraception and anti-sexually transmitted disease. No side-effects were recorded throughout this period. Cervical cultures at 6-month intervals showed the presence of Mycoplasma hominis and Candida albicans in one or two cases. The combined spermicidal and anti-HIV properties of cholic acid reported in this paper and used in the 'Protectaid' sponge offer a new and modern protective method of contraception. Cholic acid (sodium cholate) exhibits a strong spermicidal and antiviral [anti-human immunodeficiency virus (HIV)-1] activity. The same effects are observed for F-5 Gel, the active mixture of a new contraceptive sponge (Protectaid), which contains sodium cholate together with low concentrations (0.5%) of nonoxynol-9 and benzalkonium chloride. Both cholic acid and the F-5 Gel exerted a dose-dependent, in-vitro inhibitory effect 1) on the activity of HIV-1 associated reverse transcriptase in an acellular system (their 50% inhibitory dose was 7.2 mM and 0.8 x 10 -3 v/v, respectively, and 2) on the potential of HIV-1 to infect human lymphocytes efficiently. In the 3 semen samples examined, sperm motility was instantaneously inhibited by the addition of a 6 mM solution of sodium cholate or of a 1:10 dilution of F-5 Gel. Both cholic acid and F-5 Gel affected in a dose-dependent manner the viability of normal peripheral blood lymphocytes (NPBL) and CEM cells. The Protectaid contraceptive sponge impregnated with F-5 Gel was given to 20 young women aged 19-25 years for a period of 1 year who had chosen this method for both contraception and against sexually transmitted diseases. All women were instructed to insert the sponge within the 12 hours preceding each sexual intercourse and to remove it 4-6 hours afterwards. During 12 months of use with at least 3 intercourse per week, the contraceptive efficacy of the Protectaid vaginal sponge was 100%. Cervical cultures at 6-month intervals showed the presence of Mycoplasma hominis and Candida albicans in 1 and 2 cases, respectively. The combined spermicidal and anti-HIV properties of cholic acid reported and used in the Protectaid sponge offer a new and modern protective method of contraception. At the end of the study, cervical cultures revealed the presence of Escherichia coli and Candida albicans in 1 case each. No slide effects were recorded, and only 1 woman complained of discomfort.
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