K. Kostarelos et al., Liposome-mediated delivery of radionuclides to tumor models for cancer radiotherapy: A quantitative analysis, J LIPOS RES, 9(3), 1999, pp. 407-424
Towards the design of therapeutically effective liposome-radionuclide conju
gates, the predominant focus should rest with the ability of such modalitie
s to efficiently target tumor sites;md thus selectively deliver cytotoxic l
evels of radiation doses. For this reason analytic dosimetric calculations
were carried out to quantitatively examine the critical physical parameters
for the potential clinical application of radionuclide-liposome conjugates
in internal radiotherapy. The radiodosimetric model employed followed the
mathematical formalism of the MIRD (Medical Internal Radiation Dose Committ
ee) scheme. Analytic pharmacokinetic functions for a variety of liposome co
nstructs coupled with the radiation properties of three of the most promisi
ng particle emitting radionuclides: Cu-67, Re-188, At-211 and the most wide
ly used in the clinic I-131, were used as input information to the model de
veloped. Results are presented in the form of radiation absorbed doses and
tumor-to-normal-tissue radiation ratios. It is concluded that liposome-medi
ated radionuclide tumor targeting for radiotherapy is certainly promising,
and critically dependent on the optimal matching between radionuclide half-
life and the time range when the tumor-to-(critical)organ liposome accumula
tion ratios become maximal. Liposome-mediated chemotherapy (drug targeting)
is also comparatively discussed demonstrating the predominant importance o
f "timing factors" in the case of radiotherapeutic (radionuclide targeting)
applications.