Abstract
Dacarbazine (DTIC) loaded or blank methoxy poly (ethylene glycol)-poly (lactide) (MPEG-PLA) nanoparticles (NPs) were prepared by modified w/o/w double emulsion-solvent evaporation method through ultrasonic processor without any additional additives. The hemolytic test and cytotoxicity test of blank MPEG-PLA NPs demonstrated that the obtained drug delivery system is safety. Its particle size distribution, morphology, drug loading, drug release proi¬le and anticancer activity in vitro were studied in detail. The small sized nanoparticles (NPs) with a particle size of 144.2±7.8 nm in diameter and drug encapsulation efficiency of 70.1±2.3% are easy to be dispersed in water and suitable for vascular administration. The drug release pattern was biphasic with a fast release rate followed by a slow one. The in vitro and in vivo study results demonstrated that compared with free DTIC, DTIC loaded MPEG-PLA NPs could induce more apoptosis of cancer cell and showed enhanced antitumor activity. The described DTIC loaded MPEG-PLA nanoparticle in this paper might be a novel potential formulation for metastatic melanoma therapy. Key words: Malignant melanoma, dacarbazine, methoxy poly (ethylene glycol)-poly (lactide), double emulsion and solvent evaporation method, nanoparticles, anticancer activity.
Highlights
Malignant melanoma is one of the most lethal and aggressive human malignancies
To overcome the limitations of the current therapies for malignant melanoma, we developed a novel dacarbazine formulation based on MPEG-PLA diblock copolymer with great biodegradability and compatibility
The hemolytic test and cytotoxicity test of blank MPEG-PLA NPs demonstrated that the drug delivery system is safety
Summary
Melanoma accounts for only 4% of all dermatological malignancies, it is responsible for 80% of mortalities from skin tumors (Jemal et al, 2007). Common treatments for malignant melanoma involve a combination of therapies including surgical removal, chemotherapy, radiotherapy and so on. Management of systemic melanoma is a challenge because of a paucity of active treatment modalities (Svetomir et al, 2007). Alkylating agents are among the most widely used chemotherapeutic agents for the treatment of malignant melanoma (Mhaidat et al, 2007). Dacarbazine or dimethyl-triazeno-imidazol carboxamide (DTIC) is the only US Food and Drug Administration (FDA) approved chemotherapeutic agent for melanoma.
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