Ogbonna John D N, Kenechukwu Franklin C, Nwobi Chinekwu S, Chibueze Onochie S, Attama Anthony A
a Drug Delivery Research Unit, Department of Pharmaceutics , University of Nigeria , Nsukka , Nigeria.
Pharm Dev Technol. 2015 Dec;20(8):941-948. doi: 10.3109/10837450.2014.949270. Epub 2014 Aug 18.
Formulation, characterization, in vitro and in vivo evaluation of halofantrine-loaded solid lipid microparticles (SLMs).
The objective of the study was to formulate and evaluate halofantrine-loaded SLMs.
Formulations of halofantrine-loaded SLMs were prepared by hot homogenization and thereafter lyophilized and characterized using particle size, pH stability, loading capacity (LC) and encapsulation efficiency (EE). In vitro release of halofantrine (Hf) from the optimized SLMs was performed in SIF and SGF. In vivo study using Peter's Four day suppressive protocol in mice and the mice thereafter subjected to histological studies in kidney and liver.
Results obtained indicated that EE of 76.32% and 61.43% were obtained for the SLMs containing 7% and 3% of Hf respectively. The SLMs loaded with 3% of Hf had the highest yield of 73.33%. Time-dependent pH stability analysis showed little variations in pH ranging from 3.49 ± 0.04 to 4.03 ± 0.05.
The SLMs showed pH-dependent release profile; in SIF (43.5% of the drug for each of H and H) compared with SGF (13 and 18% for H and H respectively) after 8 h. The optimized SLMs formulation and Halfan® produced a percentage reduction in parasitemia of 72.96% and 85.71% respectively. The histological studies revealed that the SLMs formulations have no harmful effects on the kidney and liver.
SLMs formulations might be an alternative for patients with parasitemia as there were no harmful effects on vital organs of the mice.
载卤泛群固体脂质微粒（SLMs）的处方、表征、体外和体内评价。
本研究的目的是制备并评价载卤泛群的固体脂质微粒。
采用热均质法制备载卤泛群的固体脂质微粒，然后冻干，并通过粒径、pH稳定性、载药量（LC）和包封率（EE）进行表征。在模拟肠液（SIF）和模拟胃液（SGF）中对优化后的固体脂质微粒进行卤泛群（Hf）的体外释放研究。采用彼得氏四天抑制方案在小鼠体内进行研究，之后对小鼠的肾脏和肝脏进行组织学研究。
结果表明，含7%和3%卤泛群的固体脂质微粒的包封率分别为76.32%和61.43%。载3%卤泛群的固体脂质微粒产率最高，为73.33%。随时间变化的pH稳定性分析表明，pH值在3.49±0.04至4.03±0.05范围内变化很小。
固体脂质微粒呈现pH依赖性释放曲线；8小时后，在模拟肠液中（H和H各自的药物释放量为43.5%）与模拟胃液中（H和H分别为13%和18%）相比。优化后的固体脂质微粒制剂和Halfan®分别使寄生虫血症降低了72.96%和85.71%。组织学研究表明，固体脂质微粒制剂对肾脏和肝脏没有有害影响。
固体脂质微粒制剂对小鼠重要器官无有害影响，可能是寄生虫血症患者的一种替代选择。
