Pharmaceutical Department, 309 Hospital of LAP Beijing, China.
Pharm Dev Technol. 2013 Jul-Aug;18(4):828-33. doi: 10.3109/10837450.2012.700934. Epub 2012 Jul 3.
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.
采用传统的 DepoFoam 技术制备了含有盐酸纳曲酮（DepoNTX）的多室脂质体，考察了包封效率和粒径的关键制剂因素。还进行了形态学表征和体外/体内释放试验。通过光学显微镜观察，NTX 成功地包封在 DepoNTX 中，产率高，且显示出颗粒的球形、光滑和多室特征。在人血浆和氯化钠中的体外研究表明，80-85%的包封在 MVLs 中的 NTX 在 5 天内从颗粒中缓慢释放。在大鼠单次皮下给予 2.0 mg/kg DepoNTX 制剂后的体内研究中，约 120 小时内，NTX 水平在相对恒定的水平上维持在 10ng/mL 以上，而给予 NTX 溶液后，NTX 水平在 20 小时内迅速降至 10ng/mL 以下。研究结果表明，DepoNTX 是盐酸纳曲酮持续释放递送的很有前途的候选药物。
