ABSTRACT
Introduction@#Doxorubicin (DOX) and paclitaxel (PTX) are both widely used anticancer drugs with a broad spectrum of antitumor activity, commonly against breast, ovarian, and lung cancers. Currently, these drugs are commercially available in liposomal formulations for their use in chemotherapy. This study generally proposed coconut oil bodies (COB) obtained from Cocos nucifera L. as an alternative carrier for DOX and PTX rather than the currently used liposome. @*Objectives@#This study aimed to compare standard liposome and coconut oil bodies as drug carriers in terms of their microencapsulation efficiencies, lipid profiles, in vitro drug release and stability, as well as their cholesterol levels.@*Methods@#Coconut oil bodies (COB) were isolated and purified from Cocos nucifera L. by modified sucrose gradient method followed by microencapsulation of standard drugs (doxorubicin and paclitaxel) through selfassembly and freeze-thaw method. The two standard drugs were encapsulated using COB and standard liposome. Encapsulation efficiency of both materials were determined. Lipid profiles of both encapsulating materials were analyzed by Fourier-transform infrared spectroscopy, gas chromatography-flame ionization detector, and cholesterol level determination. In vitro drug release and pH stability of both encapsulated drugs were analyzed. @*Results@#Doxorubicin (DOX) and paclitaxel (PTX) were successfully incorporated in COB. Lauric acid was mainly abundant in COB and was able to lower cholesterol levels (5 mg/dL). COB incorporated with DOX and PTX showed stability at acidic and neutral pH. Drug release profile showed a rapid outburst within 3 hours compared to liposome encapsulated DOX and PTX. @*Conclusion@#Our study showed the encouraging potentials of using COB as wall materials that will make them attractive candidates for the formulation of pharmaceuticals for optimized drug delivery of cancer chemotherapeutics DOX and PTX
Subject(s)
Liposomes , Doxorubicin , PaclitaxelABSTRACT
@#Spider venoms and toxins are valuable sources of lead compounds for drug development due to their essential role in cellular and physiological processes targeting various receptors. Here, we present the protein profile of the venom of Phlogiellus bundokalbo, an endemic Philippine tarantula, to screen and characterize its cytotoxicity against MCF-7 cells, secretory phospholipase a2 (sPLA2), and neurotoxicity to evaluate its potential anticancer properties. Spider venom was extracted via electrical stimulation. Venom components were fractionated by reversed-phase high-performance liquid chromatography and characterized through liquid chromatography-mass spectrometry (LC-MS) and SDS-PAGE analysis before assay. The resulting five venom fractions were amphiphilic peptides showing cytotoxicity against MCF-7 cells in a concentrationdependent manner (IC50 ranging from 52.25μg/ml to 110.20μg/ml) after 24-hour incubation. Cells appeared detached, rounded, and shrunk with cytoplasmic condensation upon overnight incubation with venom fractions. The sPLA2 was observed in all the venom fractions tested for cytotoxicity. Venom fractions revealed a predominant mass of ~3-5 kDa with LC-MS analysis. Results showed distinct similar mass as μ- theraphotoxin-Phlo1a, an Australian tarantula, Phlogiellus sp. toxin with inhibitor cystine knot motif. The venom fractions exhibit excitatory neurotoxins that might activate presynaptic voltage-gated ion channels, such as an agonist or gating modifier toxins that slow down the channel inactivation similar to spider toxins. In conclusion, the spider venom of P. bundokalbo exhibits cytotoxic, phospholipase A2, and neuroactive properties suggesting that its venom components, upon further purification and structure-function analysis, can be potential tools in the development of targeted breast chemotherapeutics.