Abstract
Objective: To prepare Pingyangmycin gelatin microspheres (PYM-GMS) for carotid artery embolization therapy and to study the release characteristics in vivo and in vitro. Methods: PYM-GMS was prepared by optical double-phase emulsified condensation polymerization. Through UV-spectrophotometer drug content and encapsulation rate were measured. The characteristics of drug release in vitro which could simulate the actual state in vivo were tested by HPLC. Three ways of vein drop, artery perfusion and artery embolization were contrasted. Under the supervision of X-ray, PYM-GMS were perfused into the external carotid artery of rabbits by superselective artery embolization. Blood samples were tested at different time and analyzed statistically. Results: The roundness of PYM-GMS was 1.02±0.005. The mean diameter was 85.6 µm, 78% of them ranging from 50–200 µm, which fitted the use of embolization. PYM content and encapsulation rate were 6.8% and 91.3% respectively. 70% of the drug was released in 3 h in the simulated environment in vivo and total drug was released after more than 6 h. After artery embolization with small dosage of PYM-GMS, the local drug concentration was 8 times higher than the blood drug concentration and the high level of local drug concentration was kept for more than 120 min. Conclusion: External carotid artery embolization with PYM-GMS, which significantly reduced the circulating drug level and employment dosage, could prolong the duration higher drug concentration and suit the purpose of targeted tumor therapy.
Similar content being viewed by others
References
Li SL. Oncology of Head and Neck (in Chinese) [M]. 1st ed. Tianjin: Tianjin Technology Press, 1993; 126.
Coldwell DM, Stokes KR, Yakes WF, et al. Embolotherapy: agents, clinical applications, and techniques [J]. Radiographics 1994; 14:623.
Vandelli MA, Rivasi F, Guerra P, et al. Gelatin microspheres crosslinked with D, L-glyceraldehyde as a potential drug delivery system: preparation, characterization, in vitro and in vivo studies [J]. Int J Pharm 2001; 215:175.
Pharmacopoeia Committee of Peoples Republic of China. Pharmacopoeia of the Peoples Republic of China (in Chinese) [M]. Beijing: Chemistry Industry Press, 2000; 435.
Bastian P, Bartkowski R, Kohler H, et al. Chemoembolization of experimental liver metastases. Part I: distribution of biodegradable microspheres of different sizes in an animal model for the locoregional therapy [J]. Eur J Pharm Biopharm 1998; 46:243.
Laurent A, Beaujeux R, Wassef M, et al. Trisacryl gelatin microspheres for therapeutic embolization, I: development and in vitro evaluations [J]. Am J Neuroradiol 1996; 17:533.
Wein BB, Gunther RW. Embolization with gelatin-impregnated microspheres [J]. Rofo Fortschr Geb Rontgenstr Neuen Bildgeb Verfahr 1998; 168:171.
Li WX, Gao GD, Liang QC. Preparation of the X-ray developable gelatin-barium sulfate microspheres (in Chinese) [J]. J Fourth Mil Med Univ 2001; 22:1812.
Ma W, Feng XH, Wu DC. Preparation of gelatin microspheres encapsulated 5-Fu and related biological characteristics (in Chinese) [J]. J Pract Stomatol 2000; 16:402.
Deng R, Chen JM, Gao SC. In vitro drug release characteristics of gelatin microspheres containing zedoary turmeric oil for hepatical arterial embolization (in Chinese) [J]. J Chin Pharm Sci 2000; 9:146.
Digenis GA, Gold TB, Shah VP. Cross-linking of gelatin capsules and its relevance to their in vitro-in vivo performance [J]. J Pharm Sci 1994; 83:915.
Chen CX. Practical radiology (in Chinese) [M]. Beijing: People’s Health Publishing House. 1998; 1058.
Author information
Authors and Affiliations
Corresponding author
Additional information
Foundation item: This work was supported by the National Natural Science Foundation of China (No.30170271).
Biography: WU Hong (1971–), female, lecturer, Fourth Military Medical University, majors in medicine chemistry and drug medication.
Rights and permissions
About this article
Cite this article
Wu, H., Zhang, Zx., Wu, Dc. et al. Preparation and drug release characteristics of pingyangmycin gelatin microspheres for embolization therapy. Chin. J. Cancer Res. 15, 24–28 (2003). https://doi.org/10.1007/s11670-003-0006-2
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/s11670-003-0006-2