Development and evaluation of biodegradable polymeric lomustine nanofibres for the efficient tumor targeting: In vitro characterization, ex vivo permeation and degradation study

The aim of the study was to develop lomustine loaded biodegradable nanofibers using poly (lactic -co-glycolic acid) (PLGA) for the treatment of primary and metastatic brain tumors. Nanofibers were prepared by electro-spinning process and optimization was done for various process parameters such as polymer concentration (%), needle to collector distance and voltage (kV) to get appropriate size of the nanofibers. Nanofibers were char-acterized for size and surface morphology, entrapment efficiency (%EE), inter-component interaction (DSC, XRD, TGA & DTA analysis) and drug release. The fabricated lomustine loaded nanofibres were of desired size range 187-300 nm and surface quality. Approx. 95 +/- 2.2% of the drug was entrapped in the fiber matrix and showed biphasic drug release following Peppas Korsemeyer diffusion mechanism. Permeability coefficient for the PLGA-NF of Lomustine formulation was found to be 0.02228 better than that of the Lomustine suspension (0.02114) which indicated the increase in lomustine permeation across gut membrane. Further, Confocal laser scanning microscopy showed that the lomustine loaded formulation permeated to a depth of 64.9 mu m which is 10 mu m deeper than that obtained for lomustine suspension alone. Therefore the outcomes are in support of PLGA nanofibers as a delivery system for lomustine in the cerebral cavity to attain better therapeutic effect.

Automated summary

The study aimed to develop biodegradable nanofibers loaded with lomustine for the treatment of primary and metastatic brain tumors. The results showed that the nanofibers had desired size and drug release characteristics, improving lomustine permeation in the cerebral cavity.