Changhai Hospital, Second Military Medical University, Shanghai, China.
Drug Dev Ind Pharm. 2010 Oct;36(10):1131-8. doi: 10.3109/03639041003680826.
This study aims to investigate the suitability of thermosensitive triblock polymer poly-(DL-lactic acid-co-glycolic acid) (PLGA)-polyethylene glycol (PEG)-PLGA as a matrix material for ocular delivery of dexamethasone acetate (DXA).
The copolymer was synthesized and evaluated for its thermosensitive and gelation properties. DXA in situ gel-forming solution based on PLGA-PEG-PLGA copolymer of 20% (w/w) was prepared and evaluated for ocular pharmacokinetics in rabbit according to the microdialysis method, which was compared to the normal eye drop.
The copolymer with 20% (w/w) had a low critical solution temperature of 32 degrees C, which is close to the surface temperature of the eye. The C(max) of DXA in the anterior chamber for the PLGA-PEG-PLGA solution was 125.2 microg/mL, which is sevenfold higher than that of the eye drop, along with greater area under the concentration-time curves (AUC).
These results suggest that the PLGA-PEG-PLGA copolymer is potential thermosensitive in situ gel-forming material for ocular drug delivery, and it may improve the bioavailability, efficacy of some eye drugs.
本研究旨在探讨温敏性三嵌段共聚物聚(DL-丙交酯-共-乙交酯)(PLGA)-聚乙二醇(PEG)-PLGA 作为醋酸地塞米松(DXA)眼部递药基质材料的适用性。
合成共聚物并评价其温敏性和凝胶性能。根据微透析法,以 20%(w/w)PLGA-PEG-PLGA 共聚物为基础,制备 DXA 原位凝胶形成溶液,并评价其在兔眼的药代动力学,与普通滴眼剂进行比较。
20%(w/w)共聚物的低临界溶液温度为 32°C,接近眼部表面温度。房水中 DXA 的 PLGA-PEG-PLGA 溶液的 C(max)为 125.2μg/mL,是滴眼剂的 7 倍,浓度-时间曲线下面积(AUC)也更大。
这些结果表明,PLGA-PEG-PLGA 共聚物是一种有潜力的温敏性眼用原位凝胶形成材料,可能提高某些眼部药物的生物利用度和疗效。