Development of biodegradable enteric microcapsules of WR-2721 for oral delivery
10.3969/j.issn.1009-0754.2016.01.020
- VernacularTitle:WR-2721 口服肠溶生物降解微囊的制备研究
- Author:
Gula A
1
;
Yanlai XU
;
Shaolin ZHANG
Author Information
1. 济南军区青岛第一疗养院中医科
- Keywords:
WR-2721;
Amifostine;
Microcapsule;
Radioprotection;
Oral delivery;
Eudragit
- From:
Journal of Navy Medicine
2016;37(1):57-60
- CountryChina
- Language:Chinese
-
Abstract:
Objective Amifostine (WR-2721) is the first FDA-approved cyto-protective agent, which is prescribed to reduce certain side-effects during chemotherapy of ovarian , non-small cell lung cancer , and in the radiation treatment for head-and-neck cancer patients.However, due to the fact that intravenous infusion of the drug was the main route of medication and assimilation was low if taken orally , its wide application was therefore affected clinically .For this reason , we intended to develop biodegradable enteric micro-capsules of WR-2721 for oral delivery , so as to improve the bioavailability of the drug .Methods The preparation of the microcapsule was made by using the high-molecular and biodegradable Eudragit L 100-55 as its capsule material and by the spray drying technique . The diameter, shape, particle size distribution and yield rate of the capsules were measured by transversal distribution measurement of laser light scattering pattern in medium particle diameter .High performance liquid chromatography ( HPLC) was used to detect in vitro release of the drug and the drug amount remaining in the microcapsule at a specific sampling time .One hour after medication , radio-protective efficacy of the new drug formulation was determined by 30-day mice survival rate with whole-body exposure to 6Gy.Results The diameter of 90%microcapsules of the 3 batches was (2.8 ±0.24) μm.The shape of the microcapsule was spherical with a smooth surface, and the yield rate was 80%.In vitro release rate in 24 h was respectively [(95.35 ±2.13)%] at 37℃ and [(89.68 ± 3畅17 )%] at 4℃, with the release rate at 37℃being higher than that at 4℃.The 30-day survival rate for the WR-2721 microcapsule group was 80%, the rate for the WR-2721 oral group was 50%, the rate for the radiation group was 0%, and the rates for the blank control group and the abdominal injection group were as high as 100%.Conclusion As compared with the oral WR-2721 group, the WR-2721 microcapsule had significant radio-protective effect .
