GM-144, a novel lipophilic vaginal contraceptive gel-microemulsion

Abstract

In a systematic effort to develop a dual-function intravaginal spermicide as well as a drug delivery vehicle against sexually transmitted pathogens, a submicron particle size (30-80 nm), lipophilic and spermicidal gel-microemulsion (viz GM-144) containing the pharmaceutical excipients propylene glycol, Captex 300, Cremophor EL, Phospholipon 90G, Rhodigel, Pluronic F-68, and sodium benzoate was formulated. GM-144 completely immobilized sperm in human or rabbit semen in less than 30 seconds. Therefore, the in vivo contraceptive potency of intravaginally applied GM-144 was compared in the standard rabbit model to those of the detergent spermicide, nonoxynol-9 (N-9)-containing formulation. Eighty-four ovulated New Zealand White rabbits in subgroups of 28 were artificially inseminated with and without intravaginal administration of GM-144 or 2% N-9 (Gynol II) formulation and allowed to complete term pregnancy. GM-144 showed remarkable contraceptive activity in the rigorous rabbit model. When compared with control, intravaginal administration of GM-144 and Gynol II resulted in 75% and 70.8% inhibition of fertility (P <.0001 versus control, Fisher's exact test), respectively. Thus, GM-144 as a vaginal contraceptive was as effective as the commercially available N-9 gel. In the rabbit vaginal irritation test, none of the 6 rabbits given daily intravaginal application of spermicidal GM-144 for 10 days developed epithelial ulceration, edema, leukocyte influx, or vascular congestion characteristic of inflammation (total score = 5). Therefore, GM-144 has the potential to become a clinically useful safe vaginal contraceptive and a vehicle for formulating lipophilic drugs used in reducing the risk of heterosexual transmission of sexually transmitted diseases.

Optimization of curcumin loaded vaginal in-situ hydrogel by box-behnken statistical design for contraception

“…It reduces compared to the control group but there is no any significant difference in between them. This may be due to poloxamer, which may have sperm immobilization effect and these results also confirms the results of previous studies [51]. S4eS7 group containing pure curcumin and In-Situ Hydrogel different dose proportion also shows negative effects on sperm motility due to the presence of curcumin.…”

Nanoemulsion Components Screening and Selection: a Technical Note

“…Recently, there has been a surge in the exploration of nanoemulsions for transdermal delivery (6)(7)(8). They are also being investigated ardently for potential applications in ocular (9,10), pulmonary (11), nasal (12,13), vaginal (14,15), and parenteral drug delivery (16)(17)(18).…”

Effect of organogel components on in vitro nasal delivery of propranolol hydrochloride

“…Researchers have improved bioadhesive properties and have reported applications of microemulsion-based hydrogels. 10,11 Hydrogels as drugdelivery carriers necessitates the use of penetration enhancers and has limited stability against temperature, moisture, and microbial contamination. The use of thermoreversible pluronic gels of vitamin B 12 and melatonin for the treatment of pernicious anemia and chronobiological sleep disorders, respectively, has been reported by Pisal et al 12,13 The discoveries of several biocompatible substances capable of gelling organic solvents have been mentioned in reviews.…”