Attama A.A., Okafor C.E., Builders P.F., Okorie O.
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Enugu State, Nigeria; Department of Pharmaceutical Technology and Raw Material Development, National Institute for Pharmaceutical Research and Developme
Attama, A.A., Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Enugu State, Nigeria; Okafor, C.E., Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Enugu State, Nigeria; Builders, P.F., Department of Pharmaceutical Technology and Raw Material Development, National Institute for Pharmaceutical Research and Development, Idu-Abuja, Nigeria; Okorie, O., Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Port Harcourt, Choba, Port Harcourt, Rivers State, Nigeria
The aim of this study was to formulate and evaluate in vitro, ceftriaxone sodium lipospheres dispersions for oral administration. Ceftriaxone sodium lipospheres were prepared by melt-emulsification using 30%w/w Phospholipon ® 90H in Softisan® 154 as the lipid matrix containing increasing quantities of PEG 4000 (10, 20, 30, and 40%w/w). Characterization based on particle size, particle morphology, encapsulation efficiency, loading capacity and pH were carried out on the lipospheres. Microbiological studies of the ceftriaxone sodium-loaded lipospheres were performed using Escherichia coli as the model organism. In vitro permeation of ceftriaxone sodium from the lipospheres through artificial membrane (0.22μm pore size) was carried out using Franz cell and simulated intestinal fluid (SIF) without pancreatin as acceptor medium. Photomicrographs revealed spherical particles within a micrometer range with minimal growth after 1 month (Maximum size=64.76±3.81μm). Microbiological studies indicated that lipospheres formulated with 20%w/w of PEG 4000 containing 2%w/w or 3%w/w of ceftriaxone sodium gave significantly (p<0.05) higher inhibition zone diameter than those with 30%w/w or 40%w/w of PEG 4000. The result also indicated that lipospheres with 10%w/w PEG 4000 resulted in significantly higher encapsulation efficiency (p<0.05) while those with 30%w/w gave the least, while the loading capacity values ranged from 3.22mg of ceftriaxone sodium/100mg of lipid to 6.36mg of ceftriaxone sodium/100mg of lipid. Permeation coefficient values varied and ranged from 8.55×10-7 cm/s to 2.08×10-6 cm/s depending on the concentration of PEG 4000. The result of this study gave insight that the issue of ceftriaxone stability in oral formulation could be adequately addressed by tactical engineering of lipid drug delivery systems such as lipospheres. © 2009 Informa UK Ltd.
avicef; ceftriaxone; macrogol 4000; palm oil; phosphatidylcholine; softisan; unclassified drug; article; artificial membrane; controlled study; drug delivery system; drug formulation; drug penetration; emulsion; encapsulation; Escherichia coli; intestine fluid; microphotography; minimum inhibitory concentration; nonhuman; particle size; pH; priority journal; Anti-Bacterial Agents; Ceftriaxone; Cell Membrane Permeability; Drug Carriers; Drug Compounding; Drug Delivery Systems; Drug Evaluation, Preclinical; Drug Stability; Escherichia coli; Membranes, Artificial; Microbial Sensitivity Tests; Microspheres; Particle Size; Phospholipids; Polyethylene Glycols; Time Factors
