Compositions and methods for trapping and inactivating pathogenic microbes and spermatozoa

Antimicrobial and contraceptive compositions and methods that prevent or reduce the probability of transmission of sexually transmitted diseases during sexual activity as well as prevent or reduce the risk of pregnancy are supplied. The compositions contain (1) a matrix-forming representative, (2) per bio-adhesive representative, (3) a buffering agent, (4) optionally a humectant, (5) optionally a preservative, and (6) water; wherein the article is suitable for application within the vagina; wherein the compositions forms a semisolid matrix on contact with semen (hence trapping foul-smelling microbes and spermatozoa); wherein the makeup causes tingling of cervical mucus (hence diminishing the probability of sperm entry); whereas the composition forms a bio-adhesive layer over vaginal membranes (hence preventing or diminishing the risk of contact of STD-causing microbes with the vaginal membranes ); whereas the composition keeps an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; and whereas the composition doesn’t significantly impair the natural microbiological balance within the vagina. The anti inflammatory and contraceptive compositions can also contain additional antimicrobial and/or contraceptive agents (e.g., nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -altered mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, cyclopiroxolamine, and so on ).

 

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BACKGROUND

 

 
In recent decades, sexually transmitted diseases (STDs) are becoming an increasing medical problem and concern throughout the world. The HIV/AIDS epidemic over the past ten years or so has significantly and dramatically underscored the threat of STDsto the human inhabitants. The best, and possibly only realistic, way to this increasing problem of STDs (particularly HIV/AIDS) appears to be diminishing the risk of transmission of STDs by pathogenic organisms and thus reducing the amount of individualswho become newly infected. Even if treatments or cures become available, prevention of infections in the first case will likely stay as the very first line of defense. For medical, emotional, and financial reasons, it’s preferable to preventthe initial infection rather than treating, and even healing, people with STDs.
 

 
At the moment, education in regard to STDs, their modes of transmission, and also so called”safe-sex” methods has, at least to a degree at the more developed countries, demonstrated promise in reducing the risks of STD transmission via sexualactivity. Screening of the blood supply has helped to decrease the probability of transmission of these STD-causing organisms through blood transfusions and associated medical practices. Nevertheless, the spread of these STDs has not been halted to a satisfactory degreeeven in developed countries with active and progressive education applications. Despite their known effectiveness in preventing STDs, present safe-sex techniques aren’t always used, or aren’t always used properly, for many reasons (e.g. carelessness,lack of comprehension, improper methods, cultural obstacles, unplanned or spontaneous intercourse, and so on ). Additionally, even if used, safe-sex methods (except perhaps abstinence) aren’t always powerful. For instance, hens are generallyonly about 80 to about 90 percent effective in preventing conception when used independently; in the case of these failures, STD-causing organisms, if present, may pass from a sexual partner to the other.
 

 
Various birth control devices–including barrier techniques and vaginal contraceptives–are currently offered. Some of them may, in addition, have at least some amount of anti-STD action. For instance, condoms can help prevent thetransmission of STDs provided that they’re correctly used and/or they perform correctly. Nonoxynol-9, currently among the most frequently used health care agents, is reported, at least in some cases, to reduce the probability of transmission of a few STDs.Nonoxynol-9, which can be a nonionic detergent using powerful surfactant properties, acts, like most other chemical-based contraceptives, by killing or immobilizing spermatozoa (e.g., spermicidal activity). Nonoxynol-9 is a potent cytotoxic agentwhich will nonspecifically disrupt cell membranes. All these properties, however, contribute to a very significant advantages. Nonoxynol-9 can injure vaginal/cervical epithelial and other cells at concentrations as low as approximately 0.0005 percent (invitro). Clinical studies have confirmed epithelial disruption of the vagina and cervix at the concentrations normally within vaginal contraceptive formulations (usually greater than about 3 per cent nonoxynol-9). Nonoxynol-9 also disrupts thenormal vaginal flora which offers a protective mechanism, possibly by keeping a low pH, to guard against the intrusion of pathogenic microbes. Nonoxynol-9 can also partially dissolve or remove the protective glycoprotein coating in the vagina. Thecytotoxic, flora-disruptive, and glycoprotein-removal effects of nonoxynol-9 can result in vaginal harm or harm, including lesions. Some girls are particularly sensitive to nonoxynol-9 and manifest these effects with only occasional use. The disruptionof these protective mechanisms by nonoxynol-9 can really raise the dangers of STD infections because the breakdown of the protective mechanisms, and the incidence of lesions, enables STD-causing organisms an easier pathway to the cells.Additionally, the disturbance of the protective mechanisms by nonoxynol can boost the risk of vaginitis and/or bacterial vaginosis.
 

 
Of course, various commercial vaginal creams and lotions are currently available over the counter or by prescription or so are at a variety of stages of development. Nonoxynol-9, octoxynol-9, and benzalkonium chloride are generally available assuppositories, inserts, creams, films, foams, and gels. Examples of these commercial products include, for example, K-Y Plus.TM. (2.2 percentage nonoxynol-9; Advanced Care Products, Raritan, N.J.); Encare.TM. (3 percent nonoxynol-9; Thompson Medical Co.,West Palm Beach, Fla.); Gynol II (Advanced Care Products, Raritan, N.J.); Ortho Options Conceptrol (Advanced Care Products, Raritan, N.J.); Semicid (Whitehall Robbins Healthcare, Madison, N.J.); and Advantage-S (Columbia Laboratories, Aventura, Fla.).As discussed previously, the levels of nonoxynol-9 or other cytotoxic agents in these products are generally disruptive to the vagina and cervix and upset the normal vaginal milieu. Moreover, such formulations have only limited capability, if any,to avoid STD infections. Indeed, many girls utilizing such products report pain and burning enough to terminate the use of the merchandise. Gels designed to control vaginal pH can also be available. For example, Aci-Jel. TM. (Ortho-McNeil PharmaceuticalCorp., Raritan, N.J.) is a water-dispersible buffered gel with a pH of 3.9 to 4.1 which is used to restore and maintain normal vaginal acidity. Such gels are designed to control vaginal pH and aren’t designed to prevent STDs and/or conception; thesegels do not trap and/or inactivate STD-causing pathogens or spermatozoa.
 

 

U.S. Pat.

No. 5,439,685 (Aug.. 8, 1995) provides a pharmaceutical composition for the prevention of sexually transmitted diseases. These compositions are reported to produce a movie or barrier coating over the vagina mucosa which prevents contactof the STD-causing microbes with the vagina surfaces. Nonetheless, these formulations don’t form a semisolid matrix with the ejaculate to effectively trap STD-causing microbes or spermatozoa; nor do they cause hardening of cervical mucus to prevententry of spermatozoa. These gels can also comprise cytotoxic agents such as nonoxynol-9, benzalkonium chloride, and sodium cholate that, which in spite of the movie or barrier, may nonetheless be disruptive to the vagina and cervix. Ultimately, these gels aredesigned to be utilized together with a vaginal device such as a tampon, unlike the current invention.
 

 

More recently, BufferGel.TM.

(ReProtect LLC, Baltimore, Md.), developed at John Hopkins University, is undergoing clinical trials. BufferGel.TM. Is reported to be a negatively charged, non-absorbable high molecular weight polymer gel, designedto keep vaginal pH under 5 at the presence of semen. As detailed in U.S. Pat. No. 5,617,877 (Apr.. 8, 1997), BufferGel.TM. Relies on a plastic comprised of carboxylated monomers (preferably crosslinked polyacrylic acids such as, by way of example,Carbopol.RTM. Polymers (high molecular weight homo- and co-polymers of acrylic acid crosslinked using a polyalkenyl polyether; available in B F Goodrich)) to control the vaginal pH. BufferGel.TM. Does not trap STD-causing microbes and/or ejaculatedspermatozoa or harden cervical mucus, thus letting the STD-causing microbes and/or ejaculated spermatozoa to readily migrate throughout the lower genital tract. Moreover, the makeup is designed to be used with a device to be inserted to thevagina and placed covering the cervix. To be effective, the apparatus must stay in position covering the cervix. Removal of the device or a change of its own position relative to the cervix can ruin, or at least significantly reduce, itseffectiveness. As detailed in the patent, the”apparatus positions advantageous amounts of proper buffers at a dome shaped configuration that provides stable placement of the apparatus around the cervix. The huge surface area of the apparatus and itsresilient circular contour make it to project to the anterior vaginal fornix, softly spreading the vaginal mucosa from the surface of the apparatus, thereby preventing thickening of the ejaculate in a relatively inaccessible cul-de-sac. The device is highlyabsorptive, and rapidly sequesters and acidifies both semen and menstrual fluid” Of course, the use of these devices in conjunction with BufferGel.TM. Requires significant skill and motivation by the user to obtain, and keep, proper positioning of thedevice. Moreover, there is likely to be a reduction of sensitivity and pleasure of the sex act using this type of device. These apparatus are, hence, less likely to be used on a constant basis because of the difficulty of use, particularly in cases of”spontaneous” sexual activity.
 

 
Much like crosslinked polyacrylic acids (i.e., polycarbophil) also have been used for drug (e.g., nonoxynol-9 or progesterone) delivery within the vagina. Robinson et al., J. Controlled Release, 28, 87 (1994).
 

 
It could be desirable, therefore, to provide enhanced compositions and methods that reduce the risk of STD transmission and/or diseases during sexual activity. It would also be desirable if such advanced compositions and methods too possesscontraceptive action. Additionally, it could be desirable if such compositions and methods wouldn’t interfere with the protective and natural vaginal mechanics. Additionally, it could be desirable if such compositions and methods can be utilized to stop and/or treatvaginitis and/or bacterial vaginosis. It would also be desirable if such compositions and methods will be somewhat simple to use and also have significantly fewer side effects than currently available approaches (i.e., nonoxynol-9 at relatively high levels) sothat it would more likely be utilized on a consistent basis. It would also be desirable if such compositions and procedures did not require a physical apparatus to stay inside the clitoris during use. The present invention, as detailed in the presentspecification, supplies such procedures.
 

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