Solid lipid microparticles of erythromycin ethyl succinate were prepared using solvent evaporation method to improve its bioavailability and efficacy. The solvent was allowed to evaporate after which the various entra...Solid lipid microparticles of erythromycin ethyl succinate were prepared using solvent evaporation method to improve its bioavailability and efficacy. The solvent was allowed to evaporate after which the various entrapments were determined; the best entrapment was used in the in vivo studies to determine the bioavailability and efficacy. This study was done with albino mice. The best entrapment obtained was 83% with a loading capacity of 2.9% （Batch D） and was used in comparison with the unformulated drug to check for the in vivo efficacy. The results show higher efficacy with the formulated drug than with the pure drug both in vitro and in vivo. The in vitro test results were better despite that some enzymes which need to act on the solid lipid microparticles were not present in the in vitro assay and could lead to a reduction in the release of the drugs. In conclusion, there was improvement in efficacy, and hence bioavailability.展开更多
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 f...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 anti 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.展开更多
文摘Solid lipid microparticles of erythromycin ethyl succinate were prepared using solvent evaporation method to improve its bioavailability and efficacy. The solvent was allowed to evaporate after which the various entrapments were determined; the best entrapment was used in the in vivo studies to determine the bioavailability and efficacy. This study was done with albino mice. The best entrapment obtained was 83% with a loading capacity of 2.9% （Batch D） and was used in comparison with the unformulated drug to check for the in vivo efficacy. The results show higher efficacy with the formulated drug than with the pure drug both in vitro and in vivo. The in vitro test results were better despite that some enzymes which need to act on the solid lipid microparticles were not present in the in vitro assay and could lead to a reduction in the release of the drugs. In conclusion, there was improvement in efficacy, and hence bioavailability.
文摘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 anti 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.
