title: Physicochemical characteristics and in vivo deposition of liposome-encapsulated tea catechins by topical and intratumor administrations.
abstract: Tea polyphenols, including (+)-catechin, (-)-epicatechin, and (-)-epigallocatechin-3-gallate (EGCG), have been shown to possess potent antioxidant and anticancer activities. The aim of this study was to evaluate the possibility of using liposomes for the local delivery, including skin and tumor deposition, of these polyphenols. Liposomes containing egg phosphatidylcholine, cholesterol, or anionic species were prepared by a solvent evaporation method and then were subjected to a probe sonicator. The size, zeta potential and entrapment efficiency of these liposomal formulations were determined to provide correlations with results from a subsequent in vivo study. The release rate study showed that inclusion of an anionic species, such as deoxycholic acid (DA) or dicetyl phosphate (DP), increased the permeability of the lipid bilayers, leading to the rapid release of these formulations. No significant increase in skin deposition of catechins was observed after topical application of liposomes. On the other hand, a greater amount of catechins were delivered into the solid tumor by liposomes than by the aqueous solution. The drug release rate and vesicle size of liposomes may influence drug deposition in tumor tissues. The isomers, (+)-catechin and (-)-epicatechin, showed different physicochemical properties in liposomes and for local deposition in the skin and tumor. Finally, the presence of gallic acid ester in the structure of EGCG significantly increased the tissue uptake of catechins.
authors.affiliation: Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, 259 Wen-Hwa 1st Road, Kweishan, Taoyuan 333, Taiwan. fajy@mail.cgu.edu.tw
authors.forename: Jia-You
authors.initials: JY
authors.lastname: Fang
authors.forename: Chi-Feng
authors.initials: CF
authors.lastname: Hung
authors.forename: Tsong-Long
authors.initials: TL
authors.lastname: Hwang
authors.forename: Yen-Ling
authors.initials: YL
authors.lastname: Huang
mesh_terms: D000287:Administration, Topical; D000818:Animals; D002392:Catechin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D003840:Deoxycholic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004355:Drug Stability; D015552:Injections, Intralesional; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051379:Mice; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000188:drug therapy; D010755:Organophosphates / Q000008:administration & dosage / Q000493:pharmacokinetics; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012878:Skin Neoplasms / Q000188:drug therapy / Q000378:metabolism; D013662:Tea / Q000737:chemistry*
chemical_list: D008081:Liposomes; D010755:Organophosphates; D013662:Tea; D003840:Deoxycholic Acid; C002290:dicetylphosphate; D002392:Catechin; C045651:epigallocatechin gallate