title: Multivesicular liposomes for sustained release of naltrexone hydrochloride: design, characterization and in vitro/in vivo evaluation.
abstract: Multivesicular liposomes containing naltrexone hydrochloride (DepoNTX) was prepared by using the traditional DepoFoam technology and the key formulation factors on encapsulation efficiency and particle size were investigated. A morphological characterization and in vitro/in vivo release assay was also carried out. NTX was successfully encapsulated in DepoNTX with good yield and showing the spherical, smooth and multivesicular characteristics of particle by a light microscope. The in vitro studies in human plasma and sodium chloride showed that 80-85% of NTX encapsulated in MVLs released slowly from particles over 5 days. In vivo study, after a single dose of 2.0 mg/kg of DepoNTX formulation administered subcutaneously in rats, plasma NTX levels were maintained at a relatively constant level above 10 ng/mL for approximately 120 h, while after administered NTX solution, NTX level was quickly decreased below 10 ng/mL within 20 h. The results of the study demonstrated that DepoNTX was very promising candidate for sustained release delivery of naltrexone hydrochloride.
authors: Pharmaceutical Department, 309 Hospital of LAP Beijing, China.
authors: Lijun
authors: L
authors: Sun
authors: Tao
authors: T
authors: Wang
authors: Lijun
authors: L
authors: Gao
authors: Dongqin
authors: D
authors: Quan
authors: Duanhao
authors: D
authors: Feng
mesh_terms: D000818:Animals; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D006801:Humans; D007279:Injections, Subcutaneous; D008081:Liposomes; D008297:Male; D008853:Microscopy / Q000379:methods; D009271:Naltrexone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D009292:Narcotic Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D013678:Technology, Pharmaceutical; D013997:Time Factors
chemical_list: D003692:Delayed-Action Preparations; D008081:Liposomes; D009292:Narcotic Antagonists; D009271:Naltrexone