title: Formulation and characterization of albumin microspheres containing norcantharidate for liver tumor targeting.
abstract: The objectives of this study were first to encapsulate norcantharidate into albumin microspheres by the emulsion crosslinking method and second to characterize the microspheres in terms of the morphological examination, particle size, and encapsulation efficiency. The in vitro release of norcantharidate from the microspheres was studied by using the dialysis bag method. Pharmacokinetics and biodistribution studies were used to evaluate the advantages of microspheres than the conventional formulations. The microspheres prepared by crosslink emulsion were with uniform size, smooth surface, spherical shape, and disperse evenly. The particle size was uniform (13.3 ± 0.4 µm) and the encapsulation efficiency was 54.3 ± 4.18%. In vitro release indicated that the norcantharidate microspheres had a well-sustained release efficacy and fitted Korsmeyer's Peppas release model. In vivo studies showed that pharmacokinetics of norcantharidate microspheres could be described by the model of two-compartment after i.v. administration and had higher AUC inside liver and spleen than the injection group. No histological change occurred to the rat liver after the administration of norcantharidate microspheres.
authors.affiliation: a Department of Oncology , Changhai Hospital of Shanghai , Shanghai , PR China and.
authors.forename: Fang
authors.initials: F
authors.lastname: Yan
authors.affiliation: b Department of Chinese Triditional Medicine , Changhai Hospital of Shanghai , Shanghai , PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Li
authors.affiliation: a Department of Oncology , Changhai Hospital of Shanghai , Shanghai , PR China and.
authors.forename: Fengping
authors.initials: F
authors.lastname: Shen
authors.affiliation: a Department of Oncology , Changhai Hospital of Shanghai , Shanghai , PR China and.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Fu
mesh_terms: D000418:Albumins / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D019540:Area Under Curve; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005260:Female; D006207:Half-Life; D008099:Liver / Q000378:metabolism; D008113:Liver Neoplasms; D008297:Male; D008657:Metabolic Clearance Rate; D008863:Microspheres; D010316:Particle Size; D051381:Rats; D013154:Spleen / Q000378:metabolism; D013499:Surface Properties; D014018:Tissue Distribution
chemical_list: D000418:Albumins; D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004337:Drug Carriers; C069741:norcantharidin
keywords: Albumin microspheres; mulsion crosslinking; pharmacokinetics; sustained release