[Preparation of cucurbitacinBE polylactic acid nano-particles for targeting cervical lymph nodes].
OBJECTIVE
Anti-cancer nano-particles for targeting cervical lymph nodes were designed and prepared on the basis of the physiologic and anatomic properties of the peri-oral cancer lymphatic capillaries.


METHODS
The biodegradable polylactic acid (PLA) was selected as the carrier material, and cucurbitacinBE (CuBE) with very high anticancer activity against oral squamous cell carcinoma was used as the model drug. According to the criteria of the diameter of the nano-particles, drug loading (DL) and embedding ratio (ER), the preparing technology was optimized by uniformly designing experiment on the basis of single-factor experiment. CucurbitacinBE poly-lactic acid nano-particles (CuBE-PLA-NP) was prepared with the method of emulsion solvent evaporation, and then CuBE-PLA-NP lyophilization injection was prepared by using 10% manninositose as the supporting agent.


RESULTS
The diameter distribution for optimized CuBE-PLA-NP lyophilization injection ranged from 47 nm to 120 nm, and the average diameter was 85 nm. DL and ER were 23.03% +/- 0.47% and 93.00% +/- 0.10% respectively. The release study of the thermostatics also demonstrated that Higuchi equation was adequate to fit the release curve of CuBE-PLA-NP.


CONCLUSIONS
CuBE-PLA-NP can be used as the release agent, as CuBE-PLA-NP can enter peri-oral cancer lymphatic capillaries for targeting cervical lymph nodes by the peri-cancer submucosal injection. Therefore, it can also used for animal and clinical experiments.
Yang
K
K
Department of Stomatology, First Affiliated Hospital, Chongqing Medical University, College of Stomatology, West China University of Medical Sicences.
Wen
Y
Y
Li
L
L
Wang
C
C
Hou
S
S
Li
C
C
D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D006801:Humans; D019344:Lactic Acid / Q000008:administration & dosage*; D008198:Lymph Nodes / Q000187:drug effects* / Q000473:pathology; D008207:Lymphatic Metastasis; D008863:Microspheres; D009062:Mouth Neoplasms / Q000188:drug therapy; D036103:Nanotechnology; D011091:Polyesters; D011108:Polymers / Q000008:administration & dosage*; D014315:Triterpenes / Q000008:administration & dosage*
D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D011091:Polyesters; D011108:Polymers; D014315:Triterpenes; D019344:Lactic Acid; C033616:poly(lactide)