Abstract
This study attempted to prepare polyethylene-glycol modified (PEGylated) and folate-PEGylated liposomes containing paclitaxel (Ptx) in order to reduce the toxicity and improve the bioavailability and biocompatibility by targeting drugs to the lymphatics using cancer cell specific ligand folate to prevent metastasis via the lymphatic system. Liposomes were prepared by lipid film hydration method using PEG and folate-PEG as surface modifiers. The mean particle size and encapsulation efficiency of liposomes were114±6.81 nm and81±2.3% for PEGylated liposome and122±4.87 nm and88±2.0% for folate-PEGylated liposome, respectively. According to stability test, it could be confirmed that PEGylated and folate-PEGylated liposomes were stable for at least 5 days. After intravenous administration of the PEGylated and folate-PEGylated liposomes to rats, theCLt(total clearance) andt1/2(half-life) were significantly different (P<0.05) compared with those of PADEXOL Inj. In targeting efficiency, calculated as the concentration ratio of Ptx in lymph nodes and plasma, there was significant increase in targeting efficiency at lymph nodes (P<0.05). From these results, we could conclude that the prepared Ptx-containing PEGylated and folate-PEGylated liposomes are good candidates for the targeted delivery of the drug to lymphatic system.
Highlights
Paclitaxel is an anticancer drug that has a diterpenoid pseudoalkaloid structure having the molecular formula C47H51NO14, corresponding to molecular weight of 853 Da [1]
An adjuvant consisting of Cremophor EL and dehydrated alcohol has to be used in the current clinical administration of Ptx, which causes serious side effects [6]
Our results showed that the encapsulation efficiency was found to increase between 0 and 3 molar ratio of DSPE-mPEG
Summary
Paclitaxel is an anticancer drug that has a diterpenoid pseudoalkaloid structure having the molecular formula C47H51NO14, corresponding to molecular weight of 853 Da [1]. Ptx is the substrate of P-glycoprotein (P-gp) [4] The presence of this phenotype results in a decreased accumulation of drug within the cancer cell, which occurs by an increase in P-gp that functions as a drug efflux pump [4, 5]. Another limitation of Ptx is its difficulty in clinical administration. An adjuvant consisting of Cremophor EL (polyoxyethylated castor oil) and dehydrated alcohol has to be used in the current clinical administration of Ptx, which causes serious side effects [6]. It was reported that Cremophor EL has influence on the functions of endothelial and vascular muscle and causes vasodilation, laboured breathing, lethargy, and hypotension [8]
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