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首页> 外文期刊>Journal of ocular pharmacology and therapeutics: The official journal of the Association for Ocular Pharmacology and Therapeutics >Controlled delivery of ganciclovir to the retina with drug-loaded Poly(d,L-lactide-co-glycolide) (PLGA) microspheres dispersed in PLGA-PEG-PLGA Gel: a novel intravitreal delivery system for the treatment of cytomegalovirus retinitis.
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Controlled delivery of ganciclovir to the retina with drug-loaded Poly(d,L-lactide-co-glycolide) (PLGA) microspheres dispersed in PLGA-PEG-PLGA Gel: a novel intravitreal delivery system for the treatment of cytomegalovirus retinitis.

机译：用分散在PLGA-PEG-PLGA凝胶中的载药聚（d，L-丙交酯-乙交酯）（PLGA）微球控制更昔洛韦向视网膜的递送：一种新型玻璃体内递送系统，用于治疗巨细胞病毒性视网膜炎。

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PURPOSE: The aim of this study was to develop a formulation for intravitreal delivery by dispersing ganciclovir (GCV)-loaded Poly(d,L-lactide-co-glycolide (PLGA) microspheres in thermogelling PLGA-PEG-PLGA gel and to study the mechanism of drug-release characteristics both in vitro and in vivo. METHODS: PLGA microspheres of GCV were prepared by the solvent evaporation method from Resomer RG 502H (D,L-lactide:glycolide::50:50; Mw, 8000 Da) and a 1:3 polymer blend of Resomer RG 502H and PLGA 6535 (D,L-lactide:glycolide::65:35; Mw, 45,000-75,000 Da). The prepared microspheres were dispersed uniformly and as a mixture (1:1) in 23% w/w of PLGA-PEG-PLGA aqueous gel solutions. GCV release in the aqueous medium was studied in vitro. A conscious rabbit microdialysis model with permanently implanted probes was selected as the method for investigating the vitreous GCV levels following an intravitreal administration of the formulation. RESULTS: The formulation prepared, by a physical mixture of microspheres, was prepared from Resomer RG 502H, and the polymer blend exhibited fairly constant in vitro GCV release profiles. The amounts of GCV entrapped in the microspheres were sufficient to administer therapeutically relevant doses in 60 microL of the formulation. The vitreal elimination half-life of GCV in the conscious rabbit microdialysis model was 6.45 +/- 0.83 h, with an apparent volume of distribution (V(z)) of 1.18 +/- 0.61 mL. A direct vitreous injection of GCV resulted in the maintenance of concentrations in the vitreous for only 54 h, whereas the gel formulation produced steady-state GCV levels in the vitreous for at least 14 days. CONCLUSIONS: PLGA microspheres containing GCV were prepared by two kinds of PLGA polymers and their blend (1:3). A formulation suitable for in vivo administration was prepared by dispersing GCV-loaded microspheres in a thermogelling PLGA-PEG-PLGA solution. An ideal in vitro release of encapsulated GCV was obtained by physically mixing microspheres prepared from different polymer blends prior to its dispersion in the thermogelling polymer. The formulation maintained mean vitreal concentrations of GCV at approximately 0.8 microg/mL for 14 days, whereas direct injections could maintain drug levels above 0.8 microg/mL for 54 h only.
机译：目的：本研究的目的是通过将载有更昔洛韦（GCV）的聚（d，L-丙交酯-乙交酯-乙交酯）（PLGA）微球分散在热凝胶PLGA-PEG-PLGA凝胶中来开发玻璃体内给药的配方，并对其进行研究。方法：采用溶剂蒸发法，从Resomer RG 502H（D，L-丙交酯：乙交酯:: 50：50; Mw，8000 Da）和溶剂中制备GCV的PLGA微球。 Resomer RG 502H和PLGA 6535的1：3聚合物共混物（D，L-丙交酯：乙交酯：: 65：35; Mw，45,000-75,000 Da），将制备的微球均匀分散为混合物（1：1）在23％w / w的PLGA-PEG-PLGA凝胶溶液中进行体外研究，研究了GCV在水介质中的释放，选择了永久植入探针的有意识的兔微透析模型作为玻璃体内玻璃体GCV水平的研究方法结果：该制剂是由mi的物理混合物制备的。从Resomer RG 502H制备了crosphere，该聚合物共混物显示出相当稳定的体外GCV释放曲线。捕获在微球中的GCV的量足以以60微升的制剂施用治疗上相关的剂量。在有意识的兔微透析模型中，GCV的玻璃体消除半衰期为6.45 +/- 0.83 h，表观分布体积（V（z））为1.18 +/- 0.61 mL。直接在玻璃体内注射GCV可使玻璃体内的浓度维持54小时，而凝胶制剂在玻璃体内产生的稳态GCV水平至少持续14天。结论：由两种PLGA聚合物及其混合物（1：3）制备了含GCV的PLGA微球。通过将载有GCV的微球分散在热凝胶PLGA-PEG-PLGA溶液中来制备适于体内给药的制剂。在将其分散在热胶凝聚合物中之前，通过物理混合由不同聚合物共混物制得的微球，可以得到理想的胶囊化GCV体外释放。该制剂在14天内保持平均玻璃体内GCV浓度在约0.8 microg / mL，而直接注射只能在54 h内保持高于0.8 microg / mL的药物水平。

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