ENCAPSULATION OF HYDROPHILLIC ANTIRETROVIRAL DRUGS IN NANOCARRIERS
An encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle and a process for fabricating biodegradable polymeric nanoparticles to encapsulate hydrophilic antiretroviral drugs are described. In an implementation, an encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle includes a hydrophilic antiretroviral drug; and a biodegradable polymer polymeric nanoparticle that encapsulates the hydrophilic antiretroviral drug to form a nano-sized encapsulated hydrophilic antiretroviral drug.
1 . An encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle, comprising:
a hydrophilic antiretroviral drug; and
a biodegradable polymer polymeric nanoparticle that encapsulates the hydrophilic antiretroviral drug to form a nano-sized encapsulated hydrophilic antiretroviral drug.
2 . The encapsulated hydrophilic antiretroviral drug of claim 1 , where the hydrophilic antiretroviral drug includes at least one of tenofovir disoproxil fumarate, abacavir sulfate, or atazanavir sulfate.
3 . The encapsulated hydrophilic antiretroviral drug of claim 1 , where the biodegradable polymer polymeric nanoparticle includes polylactic-co-glycolic acid (PLGA).
4 . The encapsulated hydrophilic antiretroviral drug of claim 1 , where the biodegradable polymer polymeric nanoparticle includes a US Food and Drug Administration (US FDA) approved biodegradable polymer.
5 . The encapsulated hydrophilic antiretroviral drug of claim 1 , where the nano-sized encapsulated hydrophilic antiretroviral drug is a freeze-dried solid powder.
6 . The encapsulated hydrophilic antiretroviral drug of claim 1 , further comprising a thermosensitive gel base that forms a tenofovir disoproxil fumarate gel.
7 . A process for fabricating biodegradable polymeric nanoparticles to encapsulate hydrophilic antiretroviral drugs, comprising:
dissolving at least one of a biodegradable polymer, a poloxamer, or a hydrophilic antiretroviral drug to form a solution;
forming a homogenous phase of the solution;
emulsifying the solution to form an oil-in-water emulsion; and
evaporating the oil-in-water emulsion to form an encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle.
8 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein the biodegradable polymer includes polylactic-co-glycolic acid (PLGA).
9 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein the hydrophilic antiretroviral drug includes tenofovir disoproxil fumarate.
10 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein the hydrophilic antiretroviral drug includes at least one of abacavir sulfate or atazanavir sulfate.
11 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein dissolving at least one of the biodegradable polymer, the poloxamer, or the hydrophilic antiretroviral drug includes using at least one of ethyl acetate or ethanol.
12 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein forming the homogenous phase of the solution includes shaking the solution.
13 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein emulsifying the solution includes sonicating the solution with water in an ice bath.
14 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein evaporating the oil-in-water emulsion includes evaporating at least one of ethyl acetate or ethanol.
15 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , wherein the encapsulated hydrophilic antiretroviral drug including the biodegradable polymeric nanoparticle includes tenofovir disoproxil fumarate nanoparticles.
16 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , further comprising:
combining an anionic ion-pairing agent with the solution to form a lipophilic complex in-situ that is encapsulated into the biodegradable polymeric nanoparticles.
17 . The process for fabricating biodegradable polymeric nanoparticles of claim 16 , wherein the anionic ion-pairing agent includes at least one of sodium lauryl sulfate, sodium deoxycholate, monoammonium glycyrrhizinate, or docusate sodium.
18 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , further comprising:
freeze-drying the encapsulated hydrophilic antiretroviral drug including the biodegradable polymeric nanoparticle with a cryoprotectant to form a solid powder.
19 . The process for fabricating biodegradable polymeric nanoparticles of claim 7 , further comprising:
incorporating the encapsulated hydrophilic antiretroviral drug including the biodegradable polymeric nanoparticle into a thermosensitive gel base.
20 . A process for fabricating biodegradable polymeric nanoparticles to encapsulate tenofovir disoproxil fumarate, comprising:
dissolving a polylactic-co-glycolic acid (PLGA), a poloxamer, and tenofovir disoproxil fumarate in ethyl acetate and ethanol to form a solution;
forming a homogenous phase of the solution by using an orbital shaker at approximately 40° C.;
adding dissolved docusate sodium to the solution;
emulsifying the solution with water using an ice bath and a sonicator to form an oil-in-water emulsion; and
evaporating the ethyl acetate and the ethanol from the oil-in-water emulsion to form a biodegradable polylactic-co-glycolic acid (PLGA) encapsulated tenofovir disoproxil fumarate nanoparticle.