Available online www.jocpr.com Journal of Chemical and Pharmaceutical Research, 2015, 7(3):2239-2243 Research Article ISSN : 0975-7384 CODEN(USA) : JCPRC5 2239 Developing and evaluating in vitro effect of pegylated liposomal doxorubicin on human cancer cells Hue Pham Thi Minh 1 , Linh Le Phương 1 , Lam Nguyen Van 1 , Hai Nguyen Thanh 2 , Son Ho Anh 3 , Toan Nguyen Linh 3 and Tung Bui Thanh 4* 1 Department of Pharmaceutics, Hanoi University of Pharmacy, 15 Lê Thánh Tông, Hoan Kiem, Ha Noi, Vietnam 2 Department of Pharmaceutics and Pharmaceutical Technology, School of Medicine and Pharmacy, Vietnam National University, Hanoi, 144 Xuan Thuy, Cau Giay, Ha Noi, Vietnam 3 Department of Pathophysiology, Vietnam Military Medical University, 160 Phung Hung, Ha Đong, Ha Noi, Vietnam 4 Department of Pharmacology and Clinical Pharmacy, School of Medicine and Pharmacy, Vietnam National University, Hanoi, 144 Xuan Thuy, Cau Giay, Ha Noi, Vietnam _____________________________________________________________________________________________ ABSTRACT A PEGylated liposomal formulation of doxoburicin has been developed and evaluated with the purpose of reducing toxicity and improving the tumor-targeting efficacy of doxorubicin.PEGylated liposomal doxorubicin was prepared by the lipid film hydration technique using hydrogenated soybean phosphatidylcholine (HSPC) combined with cholesterol and DSPE-PEG 2000 . Biological activity and toxicity were tested on A549 and HT 29 cancer cell lines by the MTT method. As the result, the obtained PEGylated liposomal doxorubicin using the lipid film hydration method had an entrapment efficiency of the drug more than 95%. The formulated liposomes were found to be relatively uniform in size (167.8± 3.6 nm) with a negative zeta potential (−27.5 ± 3.5 mV). The stability experiments results indicated that PEGylated liposomal doxorubicinwas stable for at least 3 months at 2-8 o C. The cytotoxic effect of PEGylated liposomal doxorubicin on A549 and HT29 cell lines was effected when the exposure time is over 48h.The A549 cell line was found more sensitive than the HT 29 line to PEGylated liposomal doxorubicin. The lowest IC 50 was observed after 72 hours for both cell lines. These results indicated that PEGylated liposomal doxorubicin was valued to develop as a practical formulation for the tumor-targeting efficacy. Future work will be needed to evaluate the antitumor efficacy of doxoburicin liposome formulation in vivo. Keywords: PEGylated; liposome doxorubicin; MTT; A549; HT29. _____________________________________________________________________________________________ INTRODUCTION Doxorubicin (DOX), an anthracycline antitumor antibiotic, is the most active agents used in the treatment of some cancer diseases including hematological malignancies, breast carcinoma. Doxorubicin binds to DNA-associated enzymes, intercalate with DNA base pairs, and target multiple molecule to produce a range of cytotoxic effects [1]. However, doxorubicin is limited in the clinical use because of its toxicity properties, especially cardiomyopathy, leading to congestive heart failure and myelosuppression [2]. Nowadays,, using targeted therapy would be one of the best choices today to reduce its toxicity while increasing therapeutic efficacy. Liposomes, phospholipid bilayer vesicles, are one of successful approach using drug carriers to alter the pharmacokinetics and biodistribution of drug. Until now, liposomes are the most advanced of the particulate drug carriers and considered as a mainstream drug- delivery system. Liposomes can trap principle active, avoid decomposition of the entrapped combinations, and release the entrapped at designated targets [3]. Liposomes, with biphasic character, can act as carriers for both lipophilic and hydrophilic drugs. Highly hydrophilic drugs, such as doxoburicin, are located exclusively in the aqueous compartment of liposomes. However, one of the major limitations of liposome isrecognized by opsonins,