In this research article, we focused on lipid-based supramolecular assembly 'nanocochleates' composed of negatively charged phospholipids and divalent cation as drug carrier for systemic delivery system and discussed their formulations, optimisation, characterization, in vitro and in vivo performance.

Cochleates, a type of lipid based drug delivery system, are solid particulates made up of large continuous lipid bilayer sheets rolled up in a spiral structure with little or no internal aqueous phase. These nano-sized or sub-micron sized structures are generated on fusion of negatively charged liposomes with metal cations. They are efficient in encapsulating drug molecules that are hydrophobic and hydrophilic; positively charged as well as negatively charged. The interior of a cochleate structure remains substantially intact irrespective of outer harsh environmental conditions or enzymes. Cochleate technology is applicable for administration through parenteral, topical as well as oral routes and can be formulated in liquid or powder form. Cochleates have been reported to improve the oral bioavailability; improve the safety of the drugs by decreasing side effects and increasing drug efficacy; all of which lead to enhanced patient compliance. This review article highlights the important aspects of cochleates such as their structure, properties, methods of preparation, stability, advantages, applications and current status. The information provided herein should help formulators in judiciously selecting cochleate technology for delivery of drugs.

The natural flavonoid fisetin (FS) has shown anticancer properties but its in-vivo administration remains challenging due to its poor aqueous solubility. The aim of the study was to develop FS loaded pluronic127 (PF)-folic acid (FA) conjugated micelles (FS-PF-FA) by the way of increasing solubility, bioavailability and active targetability of FS shall increase its therapeutic efficacy. FA-conjugated PF was prepared by carbodiimide crosslinker chemistry. FS-PF-FA micelles were prepared by thin-film hydration method and evaluated in comparison with free FS and FS loaded PF micelles (FS-PF). The smooth surfaces with spherical in shape of FS-PF-PF micelles displayed smaller in size (103.2 ± 6.1 nm), good encapsulation efficiency (82.50 ± 1.78%), zeta potential (-26.7 ± 0.44 mV) and sustained FS release. Bioavailability of FS from FS-PF-PF micelles was increased by 6-fold with long circulation time, slower plasma elimination and no sign of tissue toxicity as compared to free FS. Further, the FS-PF-FA micelles demonstrated active targeting effect on folate overexpressed human breast cancer MCF-7 cells. The concentration of the drug needed for growth inhibition of 50% of cells in a designed time period (GI50) was 14.3 ± 1.2 µg/ml for FS while it was greatly decreased to 9.8 ± 0.78 µg/ml, i.e. a 31.46% decrease for the FS-PF. Furthermore, the GI50 value for FS-PF-FA was 4.9 ± 0.4 µg/ml, i.e. a 65.737% decrease compared to FS and 50% decrease compare to FS-PF. The results indicate that the FS-PF-FA micelles have the potential to be applied for targeting anticancer drug delivery.