琥珀酸红霉素乙酯蜂蜡-卵磷脂SLMs治疗感染小鼠急性菌血症

U. Osonwa, Onyinye J. Uwaezuoke, Ngozi Ilunoh
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引用次数: 0

摘要

以myrj52为乳化剂,采用包封法提高琥珀酸红霉素乙酯在蜂蜡脂质基质中的药效。制备了不同批次的固体脂质微颗粒,并选择了稳定的固体脂质微颗粒。计算了封装效率和负载能力。用上载量最高的批进行进一步的测定。光镜法测定颗粒大小。采用体外培养法检测不同临床分离菌对红霉素的敏感性,选择大肠杆菌进行药效试验。在体外培养中测试了配方药物的活性,并与未配方药物进行了比较。白色白化小鼠感染大肠杆菌,并放置一天,出现明显的菌血症。随机分为4组(n = 4),分别给予制剂和非制剂药物,剂量为7.14 mg/kg, 8小时,连用56小时。第三组服用不含药物的SLM,而另一组不接受治疗。包封率为94.83%,载药量为3.88%。粒径为17±4 μm。3 d治疗结束时,未配伍红霉素组小鼠多便、虚弱,有死亡记录,配伍红霉素组菌血症发生率为33.8%,临床症状基本消退。另外两组记录了菌血症诱导后第二天的死亡情况。结果表明,以蜂蜡和卵磷脂为脂质基质,配制琥珀酸红霉素乙酯可显著提高其药效。
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Beeswax-Lecithin SLMs of Erythromycin Ethyl Succinate for Treatment of Acute Bacteremia in Infected Mice
The aim of this work was to increase the efficacy of erythromycin ethyl succinate by encapsulation in beeswax lipid matrix using Myrj 52 as emulsifier. Different batches of SLM’s (solid-lipid microparticles) were formulated and stable ones were selected. The encapsulation efficiency and loading capacities were calculated. The batch with the highest loading capacity was used for further assays. The particle size was determined by light microscopy. The sensitivity of different clinical bacterial isolates to erythromycin was tested using in vitro cultures and E. coli was selected for efficacy tests. The activity of the formulated drug was tested in the in vitro culture and compared to that of the unformulated drug. White albino mice were infected with E. coli and left for one day to develop significant bacteremia. They were then divided into 4 groups (n = 4) and treated with the formulation and unformulated drug at a dose of 7.14 mg/kg 8 hourly for 56 hours. A third group was given SLM’s that do not contain drug, while another group was left untreated. The selected batch has an encapsulation efficiency of 94.83% with a loading capacity of 3.88%. The particle size was 17 ± 4 μm. At the end of the three day period of treatment, the group treated with unformulated erythromycin had much stooling and weakness in the mice, and some deaths were recorded, while that treated with the formulation had 33.8% bacteremia and the clinical signs had largely subsided. The other two groups recorded deaths the following day after bacteremia induction. The results show marked improvement in efficacy of erythromycin ethyl succinate by formulation in SLMs with beeswax and lecithin as lipid matrix.
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