Journal of Pharmaceutics / 2014 / Article / Tab 6

Review Article

Microbicides for the Treatment of Sexually Transmitted HIV Infections

Table 6

Drug incorporated microbicidal vaginal formulations.

PolymersDrug (dosage form)Results

Sodium carboxymethyl celluloseDapivirine (vaginal tablet)Developed as a vaginal microbicide and improved wettability of the drug [17].

Polycarbophil, carbopol 974PTenofovir disoproxil fumarate (vaginal tablet)Assess acceptability, safety, and effectiveness in preventing HIV infection [18].

Polymethacrylate saltTenofovir (vaginal solution)Controlled microbicide delivery template by intravaginal route for HIV prevention [19].

Propylene glycol caprylateUC-781(vaginal emulsion)Enhancing the vaginal absorption of these microbicidal candidates [20].

Chromophore EL-capryol 90, tween 80Fluconazole (FLZ) (vaginal emulsion)Showed significantly higher ( ) in vitro bioadhesion and antifungal activity without any vaginal irritation in rabbit [21].

Carbopol, tween 80Nitro imidazole, ornidazole (vaginal emulsion)A high release was found in the alkaline pH and locally effective in vagina [22].

Phospholipon 90G, captex 300, pluronic F68, and Cremophor ELWHI-07, vanadocene dithiocarbamate (vaginal emulsion)Demonstrated that WHI-07 either alone or in combination with a vanadocene has clinical potential for the development of a dual-function anti-HIV microbicide for sexually active women [23].

Tragacanth gum, aacacia gumMiconazole nitrate (vaginal suspension)Exhibit uniformly distribution of drug and show locally effect to control the infection [24].

Polycarbophil, carbopol 974PTenofovir (TFV), IQP-0528 (vaginal gel)These gels have the potential for dual compartment use to inhibit the virus entry [25].

PluronicMetronidazole (vaginal gel)Successfully used for treatment of bacterial vaginosis [26].

Cellulose acetate phthalate (CAP)Model drug (vaginal cream)Use as a topical microbicide for preventing HIV-1 infection in humans [27].

Hydroxyethyl celluloseTenofovir (vaginal gel)Exhibit excellent effectiveness in preventing human immunodeficiency virus transmission [28].

Hydroxyethyl celluloseTenofovir (vaginal ring)Exhibit potential for the prevention of transmission of (HIV-1) in pig-tailed macaques [29].

PolyurethanePyrimidinedione IQP-0528 (PYD1) IQP-0532 (PYD2) (vaginal ring)Prophylactic drug delivery systems to prevent the sexual transmission of HIV-1 [30].

Polyether urethanesDapivirine(vaginal ring)Sustained delivery of microbicidal agents [31].

Silicone elastomerTMC120 (vaginal ring)Controlled release strategy for delivering microbicidal substances for the prevention of heterosexual transmission of HIV [32].

Polyvinyl alcohol(PVA)Pyrimidinedione, IQP-0528 (vaginal films)Nontoxic in nature and exhibit excellent prevention against HIV infection [33].

OctylglycerolDapivirine, tenofovir,UC781 (vaginal films)Prevent HIV infection and products are nontoxic to the endogenous vaginal Lactobacillus [34].

Span 60 or span 40, cholesterolNystatin (NYS) (vaginal films)Reducing its toxicity and making it a more active against vaginal infections [35].

Polyvinyl alcohol (PVA)Retrocyclin analog RC-101 (vaginal films)Shown to maintain bioactivity for a period of 6 months [36].

Hydroxypropyl cellulose, xanthan gumClindamycin (CL) phosphate (vaginal films)Exhibit potential vaginal delivery system of CL against bacterial vaginosis [37].

Hydroxypropyl cellulose/polyethylene glycol 400Itraconazole (vaginal films)Exhibit more effective treatment against vaginal candidiasis and do not affects normal vaginal flora [38].

Cellulose acetate 1,2-benzenedi carboxylate Octoxynol-9 or nonoxynol-9 (vaginal films)Exhibit biocompatibility of solid-dosage forms of anti-HIV virus type 1 microbicides with the human cervicovaginal mucosa modeled ex vivo [39].