FABRICATION OF TWEEN 80 LIGAND COATED CHOLESTEROL-SOYA LECITHIN BILAYERED NANOLIPOSOMES FOR IMPROVED RELEASE OF MEROPENEM AGAINST ARTIFICIAL BLOOD BRAIN BARRIERAbstract
The blood-brain barrier is the most challenging physiological obstacle for drug moieties for reaching the central nervous system. Meropenem is a drug used against meningitis, however crossing BBB is also a challenging realm of problem for the same. Therefore attempt has been undertaken to strategically design Meropenem loaded cholesterol-soya lecithin nanoliposomes (MCSLN). MCSLN was prepared by nano-emulsification technique with tween 80 as its surface ligand. Molecular docking studies revealed that tween 80 interacts with apolipoprotein E through π-π interactions and hydrogen bonding, which might be its mechanism for transmembrane permeation across BBB. After characterization, in-vitro release study was carried out to evaluate cross-walking efficiency of liposomal drug delivery system through the simulated blood-brain barrier. Entrapment efficiency estimation showed that about 80% of the drug has been successfully entrapped within the liposome. Dynamic light scattering study exhibited bimodal distribution of particle with size ranges 70-75 nm and 300-350 nm. Zeta potential reveals good stability of the formulation. FTIR studies reveal that Meropenem has been successfully entrapped within the formulation. On a normalized scale, in-vitro release displays about five times improvement of the drug from liposome compared to free drug. These results suggested that ligand coated MCSLN may permeate BBB successfully and deliver the drug within the intrathecal fluid. The study, if successful, could potentiate a device through which molecules could reach brain cerebrospinal fluid to exert its action irrespective of molecular chemistry, size, shape and diameter.
A. Ghosh, S. Nandi, A. Roy, S. Singh, S. Singhmura and S. Basak *
Dr. B. C. Roy College of Pharmacy & Allied Health Sciences, Durgapur, West Bengal, India.
25 March 2019
22 July 2019
27 July 2019
01 December 2019