title: Localized delivery of paclitaxel using elastic liposomes: formulation development and evaluation.
abstract: In the present study an elastic liposomes-based paclitaxel formulation was developed with the objective to remove Cremophor EL. Cremophor EL is currently used for solubilizing paclitaxel in the marketed formulation and is known to produce toxic effects. Elastic liposomal paclitaxel formulation was extensively characterized in vitro, ex-vivo, and in vivo. The results obtained were compared against the marketed paclitaxel formulation. The maximum amount of paclitaxel loaded in the elastic liposomal formulation was found to be 6.0 mg/ml, which is similar to the commercial strength of marketed paclitaxel formulation. In vitro skin permeation and deposition studies showed 10.8-fold enhanced steady state transdermal flux and 15.0-fold enhanced drug deposition in comparison to drug solution. These results further confirmed with the vesicle-skin interaction study using FTIR technique. Results of the hemolytic toxicity assay indicate that elastic liposomal formulation induced only 11.2 ± 0.2% hemolysis in comparison to the commercial formulation which showed 38 ± 3.0%. Further, results of the Draize test showed no skin irritation of paclitaxel elastic liposomal formulation. Findings of the study demonstrate that elastic liposomes as a carrier is an attractive approach for localized delivery of paclitaxel.
authors.affiliation: Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, India.
authors.forename: Puneet
authors.initials: P
authors.lastname: Utreja
authors.forename: Subheet
authors.initials: S
authors.lastname: Jain
authors.forename: A K
authors.initials: AK
authors.lastname: Tiwary
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity; D003692:Delayed-Action Preparations; D004548:Elasticity; D005990:Glycerol / Q000031:analogs & derivatives / Q000737:chemistry / Q000633:toxicity; D006461:Hemolysis / Q000187:drug effects; D008081:Liposomes; D008297:Male; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D012869:Skin Absorption; D017550:Spectroscopy, Fourier Transform Infrared; D018675:Toxicity Tests / Q000379:methods
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D008081:Liposomes; C000515:cremophor EL; D017239:Paclitaxel; D005990:Glycerol