Polymeric nanoparticles in a thermosensitive gel for coital-independent vaginal prophylaxis of HIV
An antiretroviral composition that gels upon heating and can be administered prophylactically prior to exposure to a retrovirus following sexual intercourse, and methods of using the same.
1. An antiretroviral composition that can be administered prophylactically up to and including seven days prior to exposure to the retrovirus, the composition comprising:
a mixture of thermosensitive polymers comprising poloxamers including Poloxamers 188 and Poloxamers 407, wherein the ratio of Poloxamers 407 (% weight/volume) to Poloxamer 188 (% weight/volume) in the mixture is about 20:1, and
a nanoparticle comprising a biodegradable polymer and at least one antiretroviral drug,
wherein the composition is a solution at room temperature and is a gel at a temperature between 30° C. and 33° C.
2. The composition of claim 1 , wherein the biodegradable polymer is selected from the group consisting of poly-lactide-co-glycolide, polycaprolactone, cellulose acetate phthalate, or a combination thereof.
3. The composition of claim 1 , wherein the antiretroviral drug is encapsulated within the nanoparticle, directly conjugated to the nanoparticle, indirectly conjugated to the nanoparticle, or a combination thereof.
4. The composition of claim 3 , wherein the antiretroviral drug has a negative log P value at pH 7.4.
5. The composition of claim 3 , wherein the antiretroviral drug has a positive log P value at pH 7.4.
6. The composition of claim 3 , wherein the antiretroviral drug is selected from a group consisting of raltegravir, efavirenz, cellulose acetate phthalate, tenofovir, emtricitabine, and a combination thereof.