Podaralla, S., Liu, M., Francavilla, B., & Shankar, G. N. (2013, 10-14 November). Formulation development of acyclovir/tenofovir loaded two-polymer (SR-2P) bioadhesive vaginal gel. Paper presented at the AAPS’13, San Antonio, TX.
Gel formulations were prepared with different combinations of temperature sensitive polymer (Pluronic® F-127) and mucoadhesive polymer (Noveon® AA1). The gel formulations were evaluated for pH, osmolality, buffering capacity and viscosity under simulated vaginal and semen dilutions, and bioadhesivity using ex vivo mini pig vaginal tissues. The vaginal irritation of the gels was evaluated in mouse vaginal irritation model. The compatibility of the combinations of acyclovir and tenofovir in two polymers was investigated by stressing the samples at 40°C/75%RH for up to 6 weeks. The chemical stability of the drugs was measured using a HPLC method. The thermal properties of the drug, polymers and gel formulations were characterized by differential scanning calorimetry (DSC). The in vitro release of drugs from the optimized gel formulation in simulated vaginal fluid was characterized using in-line Franz diffusion cell with regenerated cellulose membrane.