The article describes the development and evaluation of targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy. The researchers used docetaxel (Dtxl)-encapsulated nanoparticles formulated with biocompatible and biodegradable poly(o,l-lactic-co-glycolic acid)-block-poly(ethylene glycol) (PLGA-b-PEG) copolymer and surface-functionalized with A10 2'-fluoropyrimidine RNA aptamers that recognize the prostate-specific membrane antigen (PSMA), a well-characterized antigen expressed on prostate cancer cells. These bioconjugates were designed to bind to PSMA and enhance the uptake by prostate cancer cells, leading to increased in vitro cellular toxicity compared to nontargeted nanoparticles. In vivo studies in a LNCaP xenograft mouse model of prostate cancer showed that a single intratumoral injection of these bioconjugates resulted in complete tumor reduction in five out of seven animals, with a mean body weight loss of 7.7 ± 4% at the nadir, compared to 18 ± 5% for nontargeted nanoparticles. The study demonstrates the potential of nanoparticle-aptamer bioconjugates for targeted cancer therapy, offering enhanced efficacy and reduced toxicity.The article describes the development and evaluation of targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy. The researchers used docetaxel (Dtxl)-encapsulated nanoparticles formulated with biocompatible and biodegradable poly(o,l-lactic-co-glycolic acid)-block-poly(ethylene glycol) (PLGA-b-PEG) copolymer and surface-functionalized with A10 2'-fluoropyrimidine RNA aptamers that recognize the prostate-specific membrane antigen (PSMA), a well-characterized antigen expressed on prostate cancer cells. These bioconjugates were designed to bind to PSMA and enhance the uptake by prostate cancer cells, leading to increased in vitro cellular toxicity compared to nontargeted nanoparticles. In vivo studies in a LNCaP xenograft mouse model of prostate cancer showed that a single intratumoral injection of these bioconjugates resulted in complete tumor reduction in five out of seven animals, with a mean body weight loss of 7.7 ± 4% at the nadir, compared to 18 ± 5% for nontargeted nanoparticles. The study demonstrates the potential of nanoparticle-aptamer bioconjugates for targeted cancer therapy, offering enhanced efficacy and reduced toxicity.