We developed transferrin (tf) conjugated docetaxel (dtx) loaded tpgs micelles for brain cancer targeted therapy. dtx used as a model anti-cancer agent and tf used as a model brain targeting ligand. firstly, tpgs-cooh was conjugated covalently to the amino ends of tf (i.e., tpgs-tf). the activation of tpgs into tpgs-cooh and tf conjugation with tpgs-cooh was confirmed by ftir and 1h nmr spectroscopy. ftir spectra and nmr spectra have revealed the characteristic peaks associated with the formation tpgs-cooh and tpgs-tf. secondly, conjugate (tpgs-tf) was assembled on the surface of the micelles and a therapeutic agent (i.e., dtx) was encapsulated in the lipophilic core of the micelles by solvent casting method. the micelles were then characterized for their size and size distribution, surface morphology, drug encapsulation efficiency, drug loading and drug release profile. further, micelles were tested in-vivo for brain distribution and its kinetics after i.v. administration to prove the transport efficiency of dtx across the bbb and its targeted delivery into brain. the mean particle size and polydispersity of the dtx loaded micelles (non-targeted and targeted) were measured by pcs. the particle sizes of the non-targeted and targeted micelles were <20 nm. about 85% of drug encapsulation efficiency was achieved with micelles. the drug release from tf-conjugated micelles was sustained for 24 h with 50% of drug release. the polydispersity of all the batches showed quite narrow size distribution, which is nearer to 0.2 to 0.5. the particle size distribution curves for all the samples were unimodal. tem analysis showed that the dtx loaded non-targeted and targeted micelles were spherical in shape. afm images of micelles showed the smooth surface without any noticeable pinholes or cracks. the in-vivo brain distribution of dtx formulated in the non-targeted (dtx-tpgs-150) and targeted tpgs micelles (dtx-tpgs-tf3) and doceltm was investigated in rats after i.v. administration. in comparison with the doceltm and non-targeted micelles, the tfr-targeted micelles showed significantly higher drug concentration in brain tissue due to targeting effect of tf modified micelles. also, developed theranostic tpgs liposomes for tfr targeted co-delivery of dtx and qds, and to prove their theranostic effects for brain cancer applications. for theranostic liposomes, dtx and qds were encapsulated in the lipophilic portion of the liposomes by solvent injection method. the liposomes were then characterized for their size and size distribution, surface morphology, drug encapsulation efficiency and drug release profile. further, liposomes were tested in-vivo for brain theranostics after i.v. administration to prove the transport efficiency of dtx and qds across the bbb and its targeted delivery into brain. biocompatibility and safety of theranostic liposomes were studied by ros generation study and histopathology of brain.the in vivo brain distribution of dtx formulated in the non-targeted (dtx-qd-tpgs) and targeted (dtx-qd-tpgs-tf) theranostic liposomes, doceltm free qds was investigated in rats after i.v. administration. the result showed that the mean concentration of dtx in the brain tissue at 0.5, 2 and 4 h after the i.v administration was significantly higher for the targeted theranostic liposomes (dtx-qd-tpgs-tf) than non-targeted theranostic liposomes (dtx-qd-tpgs) and doceltm (p<0.05). it was observed that the mean concentration of dtx in brain tissue at 0.5, 2 and 4 h after the i.v. administration was in the order of dtx-qd-tpgs-tf>dtx-qd-tpgs>doceltm. further we developed rgd-tpgs decorated theranostic tpgs liposomes for targeted co-delivery of dtx and qds, and to prove their in-vitro and in-vivo theranostic effects. firstly, rgd peptide was conjugated with tpgs-cooh). secondly, dtx and qds were encapsulated in the lipophilic portion of the liposomes by solvent injection method during the theranostic liposomes preparations. additionally, conjugate (rgd-tpgs) was decorated on the surface of the liposomes in the targeted liposomes. the in vivo brain distribution study showed that the targeted theranostic liposomes (dtx-qds-rgd-tpgs-lps) resulted in much higher concentration in brain tissue compared with non-targeted theranostic liposomes (dtx-qds-tpgs-lps) and doceltm. the drug concentrations in brain for each of three preparations, namely doceltm, dtx-qds-tpgs-lps and dtx-qds-rgd-tpgs-lps were 38.21 ± 4.2 ng/g, 150.99 ± 12.26 ng/g and 453.21 ± 14.52 ng/g respectively which imply that drug formulated in the non-targeted and targeted theranostic liposomes could be 2.95- and 10.86-fold more efficient than doceltm after 0.5 h of treatment, respectively. the drug concentrations in brain for each of the three preparations were 146.57 ± 15.23 ng/g, 589.64 ± 19.56 ng/g and 1095.9 ± 40.12 ng/g respectively which imply that drug formulated in the non-targeted and targeted theranostic liposomes could be 3.02- and 6.47-fold more efficient than doceltm after 2 h of treatment, respectively. the drug concentrations in brain for each of the three preparations were 78.24 ± 10.02 ng/g, 269.11 ± 13.65 ng/g and 624.88 ± 24.41 ng/g, respectively which imply that drug formulated in the non-targeted and targeted liposomes could be 2.43- and 6.98-fold more efficient than doceltm after 4 h of treatment, respectively. it is straightforward to understand that targeted theranostic liposomes showed 2.01-, 0.85- and 1.32-fold more drug concentration in brain tissue after 0.5, 2 and 4 h of treatment in comparison with non-targeted formulation which is mainly because of internalization of liposomes into brain by integrin receptor mediated endocytic mechanism.