P18.07
Background: Male to female transmission is eight times more likely to occur than female to male transmission due to the anatomy of the vagina, socio-economic factors, and the disempowerment of women, unable to refuse unsafe sexual practices in some communities. Currently, the only prevention strategy available by using condoms or abstaining from sexual intercourse, but 67% did not use condoms consistently and 31% had never used them. The increased incidence of HIV in women has identified the urgent need for efficacious and safe intravaginal delivery of antiviral that can be used and controlled by women.
Methods: Vaginal gels were prepared by ionic gelation process. Water soluble antiviral abacavir/ didanosine was loaded in a hydrophilic polymer chitosan (CS) and a diblock copolymer of (PEO-PPO), cross linked with tripolyphosphate (TPP), to form nanoparticals were evaluated and added into slurry of polymeric solution of carbopol/HPMC to form a gel, and evaluated.
Results: Nanoparticals size ranges 307-355nm, DSC was 164.47°c, had Zeta potential 40 mV, FTIR peak found at 1664cm−1, loading efficacy 74%. Gel was uniform, transparent had pH 7.4. Gelling capacity and extrudability was good, viscosity 30000Cp, drug content 78%, spreadability 72.87gm.cm/sec. Irritation, reddening not showed in vaginal irritation study. In vitro drug release for nanoparticals was 70%, and for gel was up to 55%. Accelerated stability study for 12 weeks at 37°c/45°c/60°c nanoparticals and gel were stable and potent.
Conclusions: This research has led to the design, development and evaluation of novel antiviral formulations to be employed for the prophylaxis of HIV/AIDS and prevention of STD used by women. Polymers used are safe, biocompatible, mucoadhesive and having good antiviral entrapment capacity produces local effect on the vaginal mucosa, and controlled release for the antiviral with minimal side effects. Half life of the water soluble antiviral will be increased ultimately decrease the dose and dosing frequency, and cost of therapy.
