Yang, Tao Cui, Fu-De Choi, Min-Koo Cho, Jei-Won Chung, Suk-Jae Shim, Chang-Koo Kim, Dae-Duk 2024-01-21T01:00:48Z 2024-01-21T01:00:48Z 2021-08-31 2007-06-29 0378-5173 https://pubs.kist.re.kr/handle/201004/134312 An improved PEGylated liposomal formulation of paclitaxel has been developed with the purpose of improving the solubility of paclitaxel as well as the physicochemical stability of liposome in comparison to the current Taxol (R) formulation. The use of 3% (v/v) Tween 80 in the hydration media was able to increase the solubility of drug. The addition of sucrose as a lyoprotectant in the freeze-drying process increased the stability of the liposome particles. There was no significant difference in the entrapment efficiency of paclitaxel between the conventional non-PEGylated liposomes and our PEGylated liposomes. Cytotoxicity in human breast cancercell lines (MDA-MB-231 and SK-BR-3) of our paclitaxel formulation was less potent compared to Taxol (R) after 24 h incubation, but was equipotent after 72 h due to the slower release of drug from the liposome. Our PEGylated liposomes increased the biological half-life of paclitaxel from 5.05 (+/- 1.52) h to 17.8 (+/- 2.35) h compared to the conventional liposomes in rats. Biodistribution studies in breast cancer xenografted nude mouse model showed that our liposomes significantly decreased the uptake in reticuloendothelial system (RES)-containing organs (liver, spleen and lung) while increasing the uptake in tumor tissues after injection compared to Taxol (R) or the conventional liposomal formulation. Moreover, the PEGylated liposome showed greater tumor growth inhibition effect in in vivo studies. Therefore, our PEGylated liposomal formulation of paclitaxel could serve as a better alternative for the passive targeting of human breast tumors. English ELSEVIER SCIENCE BV PHARMACOKINETICS TAXOL THERAPY ASSAY NANOPARTICLES CYTOTOXICITY FORMULATION DOCETAXEL TREHALOSE DELIVERY Enhanced solubility and stability of PEGylated liposomal paclitaxel: In vitro and in vivo evaluation Article 10.1016/j.ijpharm.2007.02.011 1 INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.338, no.1-2, pp.317 - 326 INTERNATIONAL JOURNAL OF PHARMACEUTICS 338 1-2 317 326 scie scopus 000247494600043 2-s2.0-34248638766 Pharmacology & Pharmacy Pharmacology & Pharmacy Article PHARMACOKINETICS TAXOL THERAPY ASSAY NANOPARTICLES CYTOTOXICITY FORMULATION DOCETAXEL TREHALOSE DELIVERY paclitaxel PEGylated liposome cytotoxicity pharmacokinetics biodistribution