title: Vincristine-sulphate-loaded liposome-templated calcium phosphate nanoshell as potential tumor-targeting delivery system.
abstract: Vincristine-sulfate-loaded liposomes were prepared with an aim to improve stability, reduce drug leakage during systemic circulation, and increase intracellular uptake. Liposomes were prepared by the thin-film hydration method, followed by coating with calcium phosphate, using the sequential addition approach. Prepared formulations were characterized for size, zeta potential, drug-entrapment efficiency, morphology by transmission electron microscopy (TEM), in vitro drug-release profile, and in vitro cell cytotoxicity study. Effect of formulation variables, such as drug:lipid ratio as well as nature and volume of hydration media, were found to affect drug entrapment, and the concentration of calcium chloride in coating was found to affect size and coating efficiency. Size, zeta potential, and TEM images confirmed that the liposomes were effectively coated with calcium phosphate. The calcium phosphate nanoshell exhibited pH-dependent drug release, showing significantly lower release at pH 7.4, compared to the release at pH 4.5, which is the pH of the tumor interstitium. The in vitro cytotoxicity study done on the lung cancer cell line indicated that coated liposomes are more cytotoxic than plain liposomes and drug solution, indicating their potential for intracellular drug delivery. The cell-uptake study done on the lung cancer cell line indicated that calcium-phosphate-coated liposomes show higher cell uptake than uncoated liposomes.
authors.affiliation: Center for Post Graduate Studies and Research in Pharmaceutical Sciences, The Maharaja Sayajirao University of Baroda, Vadodara, India. hetal_thakkar11@yahoo.com
authors.forename: Hetal Paresh
authors.initials: HP
authors.lastname: Thakkar
authors.forename: Amit Kumar
authors.initials: AK
authors.lastname: Baser
authors.forename: Mayur Prakashbhai
authors.initials: MP
authors.lastname: Parmar
authors.forename: Ketul Harshadbhai
authors.initials: KH
authors.lastname: Patel
authors.forename: Rayasa
authors.initials: R
authors.lastname: Ramachandra Murthy
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology*; D002130:Calcium Phosphates / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D057145:Nanoshells / Q000737:chemistry*; D010316:Particle Size; D013329:Structure-Activity Relationship; D013431:Sulfates / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D013499:Surface Properties; D014018:Tissue Distribution; D014750:Vincristine / Q000008:administration & dosage* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D002130:Calcium Phosphates; D008081:Liposomes; D013431:Sulfates; D014750:Vincristine; C020243:calcium phosphate