Nanotechnology is considered to be significant innovative revolution that have found wide spectrum of applications in the fields ranging from medicine, diagnostics, electronics, and communications. Currently used pharmaceutical nanocarriers, such as dendrimers, micelles, nanoparticles, polymeric nanoparticles, microspheres, and many of the nanocarriers particularly in the area of drug delivery, offer a wide variety of useful properties, such as longevity in the blood allowing for their accumulation in pathological areas particularly those with compromised vasculature; specific targeting to certain disease sites; enhanced intracellular penetration of nanomaterial with contrast properties allowing for the direct visualization of carrier in vivo, and stimuli sensitivity allowing for triggered drug release from the carriers under certain physiological conditions. Some of the pharmaceutical carriers have already made their way into clinic, while others are still under preclinical development. Moreover, the engineering of multifunctional nanocarriers with several useful properties can significantly enhance the efficacy of many therapeutic and diagnostic protocols. These novel materials operate at the nanoscale range and provide new and powerful cutting edge tools for imaging, diagnosis, and therapy. This review considers current standing and possible future directions in the emerging area of multifunctional nanocarriers with primary attention on the combination of such properties as longevity, targetability, intracellular penetration, and contrast loading.