In an effort to develop novel, multifunctional pharmaceutical nanomaterials with enhanced bioavailability and targeted antitumor activity against prostate cancer we have:
a) synthesized PSMA inhibitors of the urea type, b) synthesized amino-terminated (fullgeneration) PAMAM dendrimers via the convergent and divergent synthetic methods, c)synthesized PEG6K-G4-OH via the general polycondensation procedure between BisMPA and PEG, d) synthesized Artemisinin (ART)-loaded (AHDSs) bis-MPA nano-matrices, e) investigated structural and textural properties of the newly synthesized materials by different and complementary characterization techniques such as elemental analysis, particle size distribution, z-potential, FT-IR, FESEM, HRTEM, and solution NMR, g) compared and evaluated the suitability of these matrices as potential nanocarriers regarding their drug loading, entrapment efficiency and release profile, and f) compared and evaluated the cytotoxicity potential of free and encapsulated ART in PC3 prostate cancer cells as well as in MCF-7 breast cancer cells and 3T3 murine healthy fibroblasts for comparison purposes. The incorporation of ART inside the HDSs interior was accomplished via the “molecular encapsulation process”. FESEM and HRTEM images of the AHDS sample indicated the presence of globular NPs with sizes between 125-350 nm. The ζ-potential value of the obtained AHDSs was -3.71 ± 1.2 mV. The in situ ART entrapment efficiency was estimated to be 70.82%, whereas the loading capacity was 19.14%, respectively. The average ART release percentage during 48 h of study was 77.12%. Treatment of the PC3 prostate cancer cells and MCF-7 breast cancer cells for 24 h, 48 h and 72 h, revealed the non-toxic nature of the empty HDSs and the significantly enhanced cytotoxicity of AHDSs compared to free ART after 48 h and 72 h of treatment.