Graphene oxide (GO)-laden agarose composite hydrogels (GOACHs) were utilized to deliver lipophilic molecules from organic to aqueous media without alteration of the lipophilic nature of the molecules and the hydrophilic nature of the GOACHs. After the agarose host networks of the GOACHs were impregnated with the non-polar organic solution of lipophilic molecules via stepwise solvent exchange, their GO guests wielded the edge polar groups to effectively adsorb the lipophilic molecules via hydrogen bonding. After being transferred to aqueous media, the GOACHs were able to not only release the loaded lipophilic molecules but also to adsorb the released lipophilic molecules on the GO non-polar carbon lattice planes via hydrophobic interactions, thus resulting in deliberately balanced release of lipophilic molecules in aqueous media. Based on this environment-specific, regioselective adsorption of their GO guests, the GOACHs were harnessed as carriers for sustained delivery of ibuprofen across rat skin, underpinning their applicability in transdermal medication.