Abstract
Previous studies regarding malloapelta B (malB), a natural compound isolated from the Vietnamese medicinal plant, showed a strong NF-κB inhibitory effect, making it a promising source for the development of novel anticancer drugs. However, similar to many other natural compounds from plants, malB has several disadvantages for clinical applications, including high toxicity and low solubility. To improve its bioavailability, malB was conjugated into nanoliposomes, which are ideal drug carriers. The formulations with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, mPEG-cholesterol, malB, with or without cholesterol exhibited nanoliposomes with an average diameter of approximately 76.98 nm, PDI of 0.28, zeta potential of −5.53 mV, and the highest encapsulation efficiency of 78.73% ± 9.5%. These malB-nanoliposomes inhibited the survival of all lung cancer cell lines examined with IC50 values ranging from 11.86 to 13.12 µM. Moreover, malB-nanoliposomes showed stronger inhibition of A549 colony-forming activity compared to that of the free compound. The effects of malB and its nanoliposomal formulation may be mediated through activation of apoptosis by the significant induction of caspase 3 activity. The nanoliposomal formulations also showed potential to inhibit tumor growth (37.03%) and prolong survival (32.20 days) of tumor-bearing mice compared with the unloaded drug (p < 0.05). The improved antitumor activity of malB-nanoliposomes suggests their promising clinical applications.
Highlights
Lung cancer is the leading cause of cancer-related death worldwide (18.4%), and is especially prevalent in male smokers [1]
The physicochemical characteristics of the nanoliposomes formed were assessed by determining the mean diameter, polydispersity index (PDI), zeta potential, and encapsulation efficiency (EE)
The EE was dependent on the malloapelta B (malB) concentration; a lower malB concentration of 0.25 mg was associated with higher EE (78.73%), whereas a higher concentration of 0.5 mg showed a lower EE (51.33%)
Summary
Lung cancer is the leading cause of cancer-related death worldwide (18.4%), and is especially prevalent in male smokers [1]. The most common type of lung cancer is non-small cell lung cancer (NSCLC), accounting for 85% of cases of lung cancer [2]. 40% of lung cancers are adenocarcinomas, and most cases of lung cancer in smokers are of this type. Several therapeutic methods are available for treatment of lung adenocarcinomas, including surgery, radiofrequency ablation, radioactive therapy, chemotherapy, and immunotherapy, alone or in various combinations. These therapeutic options are expensive and insufficiently effective.
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