Optimization of long circulating mixed polymeric micelles containing vinpocetine using simple lattice mixture design, in vitro and in vivo characterization
| Autor: | Omaima N. El-Gazayerly, Nabaweya Abdelaziz Abd El Gawad, Ahmed H. Elshafeey, Ibrahim Elsayed, Rania Moataz El-Dahmy |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Scanning electron microscope Polymers Chemistry Pharmaceutical Dispersity Pharmaceutical Science Micelle Vinpocetine In vivo Zeta potential medicine Animals Particle Size Vinca Alkaloids Antihypertensive Agents Micelles Drug Carriers Chromatography Chemistry Poloxamer Drug Liberation Freeze Drying Injections Intravenous Microscopy Electron Scanning Nanoparticles Particle size Rabbits medicine.drug Half-Life |
| Zdroj: | International journal of pharmaceutics. 477(1-2) |
| ISSN: | 1873-3476 |
| Popis: | The aim of this study was to increase the in vivo mean residence time of vinpocetine after IV injection utilizing long circulating mixed micellar systems. Mixed micelles were prepared using Pluronics L121, P123 and F127. The systems were characterized by testing their entrapment efficiency, particle size, polydispersity index, zeta potential, transmission electron microscopy and in vitro drug release. Simple lattice mixture design was planned for the optimization using Design-Expert ® software. The optimized formula was lyophilized, sterilized and imaged by scanning electron microscope. Moreover, the in vivo behavior of the optimized formula was evaluated after IV injection in rabbits. The optimized formula, containing 68% w/w Pluronic L121 and 32% w/w Pluronic F127, had the highest desirability value (0.621). Entrapment efficiency, particle size, polydispersity index and zeta potential of the optimized formula were 50.74 ± 3.26%, 161.50 ± 7.39 nm, 0.21 ± 0.03 and −22.42 ± 1.72 mV, respectively. Lyophilization and sterilization did not affect the characteristics of the optimized formula. Upon in vivo investigation in rabbits, the optimized formula showed a significantly higher elimination half-life and mean residence time than the market product. Finally, mixed micelles could be considered as a promising long circulating nanocarrier for lipophilic drugs. |
| Databáze: | OpenAIRE |
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