Uptake by breast carcinoma of a lipidic nanoemulsion after intralesional injection into the patients: a new strategy for neoadjuvant chemotherapy.
OBJECTIVE
Previously we showed that after intravenous injection a lipidic nanoemulsion concentrates in breast carcinoma tissue and other solid tumors and may carry drugs directed against neoplastic tissues. Use of the nanoemulsion decreases toxicity of the chemotherapeutic agents without decreasing the anticancer action. Currently, the hypothesis was tested whether the nanoemulsion concentrates in breast carcinoma tissue after locoregional injection.


METHODS
Three different techniques of injection of the nanoemulsion were tested in patients scheduled for surgical treatment: G1 (n=4) into the mammary tissue 5 cm away from the tumor; G2 (n=4) into the peritumoral mammary tissue; G3 (n=6) into the tumoral tissue. The nanoemulsion labeled with radioactive cholesteryl oleate was injected 12 h before surgery; plasma decay of the label was determined from blood samples collected over 24 h and the tissue fragments excised during the surgery were analyzed for radioactivity uptake.


RESULTS
Among the three nanoemulsion injection techniques, G3 showed the greatest uptake (data expressed in c.p.m/g of tissue) by the tumor (44,769+/-54,749) and by the lymph node (2356+/-2966), as well as the greatest concentration in tumor compared to normal tissue (844+/-1673). In G1 and G2, uptakes were, respectively, tumor: 60+/-71 and 843+/-1526; lymph node: 263+/-375 and 102+/-74; normal tissue: 139+/-102 and 217+/-413.


CONCLUSIONS
Therefore, with intralesional injection of the nanoemulsion, a great concentration effect can be achieved. This injection technique may be thus a promising approach for drug-targeting in neoadjuvant chemotherapy in breast cancer treatment.
Mendes
S
S
Lipid Metabolism Laboratory of the Heart Institute (InCor), University of São Paulo, São Paulo, Brazil.
Graziani
S R
SR
Vitório
T S
TS
Padoveze
A F
AF
Hegg
R
R
Bydlowski
S P
SP
Maranhão
R C
RC
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001943:Breast Neoplasms / Q000097:blood / Q000188:drug therapy / Q000378:metabolism* / Q000601:surgery; D017024:Chemotherapy, Adjuvant; D002784:Cholesterol / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D002788:Cholesterol Esters / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D015552:Injections, Intralesional; D008875:Middle Aged; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D020360:Neoadjuvant Therapy; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D014280:Triglycerides / Q000097:blood
D002788:Cholesterol Esters; D004655:Emulsions; D010713:Phosphatidylcholines; D014280:Triglycerides; C014409:cholesteryl oleate; D002784:Cholesterol