Cho, Jung-Kyo Hong, Ki-Yun Park, Jung Won Yang, Han-Kwang Song, Soo-Chang 2024-01-20T17:04:03Z 2024-01-20T17:04:03Z 2021-09-02 2011-05 1061-186X https://pubs.kist.re.kr/handle/201004/130422 2-Methoxyestradiol (2-ME) has been reported to have antiangiogenic and antitumor activity. Its biomedical application is limited due to its poor water solubility resulting in its low bioavailability. Poly(organophosphazenes) containing L-isoleucine ethyl ester, ethyl-2-(O-glycyl)lactate, and alpha alpha-amino-omega omega-methoxy-poly(ethylene glycol) 550 were synthesized having M(W) of 35-38 kDa and polydispersity index of 2.38-2.73. Using a viscometer, the thermosensitivity useful for locally injectable drug delivery was verified. The aqueous polymer solution showed a sol state at a low temperature and transformed to a gel state at body temperature. The polymer solution (10 wt%) enhanced the solubility of 2-ME by about 10<SU4</SU times compared to that of phosphate buffered saline. 2-ME was released from the hydrogel mainly by diffusion, hydrophobic interaction, and surface erosion of the matrix. This release profile could be confirmed through an in vitro release test as a function of polymers and the concentration of 2-ME in hydrogels. By monitoring tumor volume and CD31 immunohistochemical staining in mouse orthotopic breast tumor (MDA-MB-231) model, it was found that the hydrogel containing a relatively low concentration (15 mg/kg) of 2-ME showed the improved antitumor and antiangiogenic activity relative to the original formulation. This research suggests that the developed formulation of poly(organophosphazenes) may have injectable carrier potentials for 2-ME and other lipophilic drugs. English INFORMA HEALTHCARE ENDOGENOUS ESTROGEN METABOLITE DRUG-DELIVERY IN-VITRO CONTROLLED-RELEASE GENE DELIVERY TUMOR-GROWTH CELLS ANGIOGENESIS PROTEIN POLYPHOSPHAZENES Injectable delivery system of 2-methoxyestradiol for breast cancer therapy using biodegradable thermosensitive poly(organophosphazene) hydrogel Article 10.3109/1061186X.2010.499461 1 JOURNAL OF DRUG TARGETING, v.19, no.4, pp.270 - 280 JOURNAL OF DRUG TARGETING 19 4 270 280 scie scopus 000288670900004 2-s2.0-79953005259 Pharmacology & Pharmacy Pharmacology & Pharmacy Article ENDOGENOUS ESTROGEN METABOLITE DRUG-DELIVERY IN-VITRO CONTROLLED-RELEASE GENE DELIVERY TUMOR-GROWTH CELLS ANGIOGENESIS PROTEIN POLYPHOSPHAZENES Injectable hydrogel poly(organophosphazene) 2-methoxyestradiol thermosensitive biodegradable breast cancer