Abstract
The search for natural anticancer agents and nanocarrier uses are a part of the current strategies to overcome the side effects caused by chemotherapeutics. Liposomal nanocapsules loaded with purified tarin, a potential immunomodulatory and antitumoral lectin found in taro corms, were produced. Liposomes were composed by 1,2-dioleoyl-sn-glycerol-3-phosphoethanolamine, cholesterylhemisuccinate, and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[folate(polyethylene glycol)-2000 prepared by thin-film hydration. Small unilamellar vesicles were achieved by sonication and extrusion. Scanning electron microscopy evidenced round-shaped nanocapsules presenting a smooth surface, 150 nm diameter and polydispersity index <0.2, estimated by dynamic light scattering. Tarin entrapment rates were over 80% and leakage of ~3% under 40 days of storage at 4 °C. Entrapped tarin exhibited an 83% release after 6 h at pH 4.6–7.4 and 36 °C. Both free and encapsulated tarin exhibited no in vitro toxicity against healthy mice bone marrow and L929 cells but stimulated the production of fibroblast-like and large round-shaped cells. Encapsulated tarin resulted in inhibition of human glioblastoma (U-87 MG) and breast adenocarcinoma (MDA-MB-231) proliferation, with an IC50 of 39.36 and 71.38 µg/mL, respectively. The effectiveness of encapsulated tarin was similar to conventional chemotherapy drugs, such as cisplatin and temozolide. Tarin liposomal nanocapsules exhibited superior pharmacological activity compared to free tarin as a potential chemotherapy adjuvant.
Highlights
Cancer is among the leading causes of death worldwide, defined by the exacerbated proliferation of normal cells into tumor cells due to a multistage process that usually involves mutation [1]
Scanning electron microscopy (SEM) and dynamic light scattering (DLS) analyses revealed the presence of smooth-surfaced round-shaped vesicles, with an average size of ~150 nm and polydispersity index (PdI) of 0.168 on the first day, confirming successful liposomal nanocapsule production
Further pre-clinical trials may be performed, the results reported have encouraged us to invest in the development of liposomal tarin nanocapsules to be tested as an adjuvant candidate presenting immunomodulatory and antitumoral activities in a tumor-bearing murine model considering a classical chemotherapy regimen
Summary
Cancer is among the leading causes of death worldwide, defined by the exacerbated proliferation of normal cells into tumor cells due to a multistage process that usually involves mutation [1]. Due to the high number of new cancer diagnoses every year, over 4700 every day in the USA alone, many studies, including breast cancer and glioblastoma proliferation control research, are being developed in order to search for the best strategy to improve patient quality of life and life expectancy [2]. Most women with breast cancer require surgical intervention to remove the tumor and, may, before or after, undergo radiotherapy or chemotherapy to control or avoid metastasis. Anthracyclines, such as doxorubicin (Adriamycin) and epirubicin (Ellence), taxanes, like paclitaxel (taxol) and docetaxel (taxotere), 5-fluorouracil (5-FU), cyclophosphamide (cytoxan), and carboplatin (paraplatin) are the most common drugs applied in as a two or three-combination for breast cancer treatment [4]. A combination therapy has been suggested to improve survival rates [7]
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