Abstract. The present study mainly compared the effect of docetaxel-albumin nanoparticles (DANPs) and docetaxelloaded PEG-albumin nanoparticles (PEG-DANPs) against non-small cell lung cancer (NSCLC). We made systematic assessments on these three drugs against NSCLC both in vitro and in vivo. With the purpose of eliminating side-effects of the commercial formulation (Tween-80) and prolonging the blood circulation time, we used emulsion-evaporation crosslink method to prepare DANPs and PEG-DANPs. The DANPs had an average particle size of 163.4±3.76 nm, a zeta potential of -19.4±0.18 mV, a polydispersity index of 0.143±0.03, a drug loading of 8.71±0.98%, and an encapsulation efficiency of 93.58±0.86%; the average particle size of PEG-DANPs is 169.19±2.36 nm, zeta potential is -18.2±0.21 mV, with a polydispersity index of 1.56±0.05, a drug loading of 8.72±1.05% and an encapsulation efficiency of 95.4±5.5%. PEG-DANPs showed a dose-and time-dependent efficacy in cytotoxicity studies in vitro; the hemolysis test indicated that PEG-DANPs had less hemocytolysis than Aisu ® and DANPs; in addition, a more prolonged circulation time and sustained in vitro release behavior were observed in the PEG-DANPs compared with Aisu ® and DANPs; the cellular uptake test in vitro demonstrated that PEG-DANPs could be absorbed easier into the nucleus; furthermore, the tumor growth of NSCLC-bearing nude mice in vivo was reduced the most by PEG-DANPs. In conclusion, the PEG-DANPs have the lowest side-effects, the highest antitumor activity with the longest blood circulation time of the three drugs, and it will provide an alternative to patients with NSCLC.
IntroductionLung cancer is a very common malignant tumor with incidence and mortality rates the first worldwide, almost one million patients are diagnosed with lung cancer each year all over the world. NSCLC accounts for 75-85% among the total number of lung cancer, and elderly patients aged >65 years accounted for >50% (1). It is always at the late stage when patients were discovered (stage III or IV) and the 5-year survival rate is only 12-15% (2,3), thus, these patients cannot receive surgical treatment (4,5).For elderly advanced NSCLC patients, chemotherapy is still the first choice of treatment (6,7), it is a relatively effective treatment for elderly NSCLC patients who cannot tolerant surgical operation. It can effectively reduce the progress of lung cancer and the recurrence, enhance the effect of clinical treatment, prolong patient survival rate and improve their quality of life (8).There are some chemotherapy regimens and drugs for elderly NSCLC patients, such as cisplatin, VP-16, gemcitabine, paclitaxel and docetaxel (9). However, there is lack of a mature and effective way for NSCLC because most of the elderly patients refuse or are unable to complete the treatment. So how to choose a drug with good effect and little side reaction is a hot spot in tumor research (10,11). Docetaxel is a cell cycle specific antitumor drug which is applied to cells at the M phase. It is a relative...