Is Wetter Better? An Evaluation of Over-the-Counter Personal Lubricants for Safety and Anti-HIV-1 Activity

Abstract

Because lubricants may decrease trauma during coitus, it is hypothesized that they could aid in the prevention of HIV acquisition. Therefore, safety and anti-HIV-1 activity of over-the-counter (OTC) aqueous- (n = 10), lipid- (n = 2), and silicone-based (n = 2) products were tested. The rheological properties of the lipid-based lubricants precluded testing with the exception of explant safety testing. Six aqueous-based gels were hyperosmolar, two were nearly iso-osmolar, and two were hypo-osmolar. Evaluation of the panel of products showed Gynol II (a spermicidal gel containing 2% nonoxynol-9), KY Jelly, and Replens were toxic to Lactobacillus. Two nearly iso-osmolar aqueous- and both silicone-based gels were not toxic toward epithelial cell lines or ectocervical or colorectal explant tissues. Hyperosmolar lubricants demonstrated reduction of tissue viability and epithelial fracture/sloughing while the nearly iso-osmolar and silicon-based lubricants showed no significant changes in tissue viability or epithelial modifications. While most of the lubricants had no measurable anti-HIV-1 activity, three lubricants which retained cell viability did demonstrate modest anti-HIV-1 activity in vitro. To determine if this would result in protection of mucosal tissue or conversely determine if the epithelial damage associated with the hyperosmolar lubricants increased HIV-1 infection ex vivo, ectocervical tissue was exposed to selected lubricants and then challenged with HIV-1. None of the lubricants that had a moderate to high therapeutic index protected the mucosal tissue. These results show hyperosmolar lubricant gels were associated with cellular toxicity and epithelial damage while showing no anti-viral activity. The two iso-osmolar lubricants, Good Clean Love and PRÉ, and both silicone-based lubricants, Female Condom 2 lubricant and Wet Platinum, were the safest in our testing algorithm.

Broadly Neutralizing Anti-HIV Antibodies Prevent HIV Infection of Mucosal Tissue Ex Vivo

“…However, clinical evaluation of N-9 was stopped due to increased HIV incidence in women using an N-9 vaginal gel (3). Additionally, N-9 was shown to cause tight junction disruptions in epithelial cells in vitro (4) and to be harmful to beneficial vaginal flora (5). Other candidates, such as BufferGel (6), the carrageenan derivative Carraguard (7), and polyanionic gels (PRO 2000 [6] and cellulose sulfate [4]), were all unsuccessful as HIV microbicides.…”

Precise engineering of dapivirine-loaded nanoparticles for the development of anti-HIV vaginal microbicides

“…Moreover, onset of uptake 543 was rapid since no noticeable differences were observed between 544 incubation times from 30 min to 4 h (data not shown). for vaginal HIV prevention [56,57]. In this study, different epithe-555 lial and one macrophage cell lines were used for studying the abil-556 ity of NPs to modulate the toxicity of dapivirine.…”

The Effect of Commonly Used Excipients on the Epithelial Integrity of Human Cervicovaginal Tissue

“…8,28,29 Although identified as generally-regarded-as-safe excipients by the Food and Drug Administration (FDA), several of these excipients were reported to affect the epithelial barrier in human cell culture or animal models. [18][19][20][21] Excipients chosen for evaluation represent a variety of functional categories and diverse chemical structures. The excipient concentration used in this study (Table 2) was determined based on the following considerations: Disodium EDTA is widely reported to decrease the integrity of intestinal cell monolayer (Caco-2) 30 and excised intestinal epithelium, 31 so three concentrations (0.05%, 0.1%, and 1%) were chosen to cover the relevant levels of use.…”

“…Some hyperosmolar over-the-counter lubricant gels have been found to reduce the tissue viability and to result in epithelial fracture/sloughing in an ectocervical explant model. 18 Several other tissue explant and mouse studies reported that treatment with excipients that are frequently used in vaginal products could alter the cervicovaginal tissue integrity and even increase the rate of vaginal herpes simplex virus 2 (HSV-2) transmission. [19][20][21] McClelland et al evaluated the effect of vaginal washing on the incidence of HIV-1 infection in 1,270 African women between 1993 and 2003.…”