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Inventi Impact - Pharmaceutical Process Development

Articles

  • Inventi:ppd/21828/17
    EVALUATION OF PROCESS AND FORMULATION VARIABLES INFLUENCING LEVODOPA LOADED POLY-E-CAPRO LACTONE NANOPARTICLES USING DESIGN OF EXPERIMENT FOR BRAIN TARGETING IN PARKINSON’S DISEASE
    Preethy Ani Jose*, Peter Christoper G V, Vijaya Raghavan C

    The process variables and formulation variables poly caprolactone (PCL), poloxamer and poly vinyl alcohol (PVA) were investigated in the formulation of levodopa loaded nanoparticles. Preformulation studies were done by UV Spectrophotometer, FTIR spectroscopy (Fourier Transform Infra Red) and DSC (Differential Scanning Calorimetry). The purity of levodopa and interaction of levodopa with polymer and other excipients were studied using FTIR and no interactions observed. DSC studies revealed the presence of levodopa in the nanoparticles in amorphous form. Design of experiment was employed to evaluate the effect of formulation variables on the characteristics of nanoparticles. Nanoprecipitation and homogenization techniques were compared in the preparation of PCL nanoparticles. Prepared formulations were evaluated for particle size, entrapment efficiency surface morphology, surface charge, in-vitro drug release and the data obtained from in-vitro release studies were fitted to various release kinetic models such as zero order, first order, Higuchi, hixson-crowell, korsemeyer–peppas, baker and lonsdalel and weibull. Homogenization technique yielded nanoparticles with size ranging from 97.25 to 132.14 nm and higher entrapment efficiency upto 63.4%w/w while nanoprecipitation technique yielded nanoparticles with size range of 101.33 to 129.74 nm and entrapment efficiency upto 29.3 %w/w. The drug release also increased with homogenization technique. PVA was found to be a better stabilizer than poloxamer 407. Levodopa release decreased with increasing PCL amount. Formulation FP 8 contained 1:2 drug polymer ratio was coated with polysorbate 80. Stability studies indicated that there was no degradation of the drug in the formulation after 60 days of preparation when stored in refrigerated condition.

    How to Cite this Article
    Preethy Ani Jose, Peter Christoper G V, Vijaya Raghavan C. Evaluation of Process and Formulation Variables Influencing Levodopa loaded Poly-E-Capro Lactone Nanoparticles using Design of Experiment for Brain Targeting in Parkinson’s Disease. Inventi Impact: Pharmaceutical Process Development, 2017(2):59-69, 2017.
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