Preparation and Characterization Studies of Dorzolamide-Loaded Ophthalmic Implants for Treating Glaucoma.

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Turkish Journal of Pharmaceutical Sciences Pub Date : 2023-07-07 DOI:10.4274/tjps.galenos.2022.95752
Samet Özdemir, Egemen Çakırlı, Bilge Sürücü, Cemre İrem Aygüler, Burcu Üner, Ali Rıza Cenk Çelebi
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引用次数: 2

Abstract

Objectives: This study constructed dorzolamide (DRZ)-loaded ophthalmic implants for extended drug delivery and increased drug retention.

Materials and methods: Carboxymethyl cellulose (CMC) and chitosan (CHI) were used to describe the ophthalmic implants. The implants were prepared by the solvent casting technique in presence of polyethylene glycol 6000 (PEG 6000) as plasticizer. Physicochemical characterization studies including mechanical characteristics [tensile strength (TS), elongation at break, and Young's modulus], bioadhesion studies, and in vitro and ex vivo drug release studies were conducted.

Results: TS of drug-loaded ophthalmic implants was 10.70 and 11.68 MPa, respectively. Elongation at break of CMC and CHI implants was 62.00% and 59.05%, respectively. The in vitro release profiles fit into Higuchi type kinetic model. Ex vivo release study results for both implants were correlated with in vitro release investigations.

Conclusion: CMC and CHI-based implants provide extended drug delivery. Implants prepared using CMC provided a significantly slower in vitro release rate, and drug retention on ocular surfaces increased. Thus, it has been concluded that DRZ-loaded CMC implants could provide effective treatment for glaucoma.

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多唑胺眼植入体治疗青光眼的制备及表征研究。
目的:构建多唑胺(dorzolamide, DRZ)眼部植入物,延长药物传递时间,增加药物潴留。材料和方法:用羧甲基纤维素(CMC)和壳聚糖(CHI)描述眼植入物。以聚乙二醇6000 (PEG 6000)为增塑剂,采用溶剂铸造法制备了该植入物。进行了物理化学表征研究,包括机械特性[拉伸强度(TS),断裂伸长率和杨氏模量],生物粘附研究以及体外和体外药物释放研究。结果:载药眼植入体的TS分别为10.70 MPa和11.68 MPa。CMC和CHI的断裂伸长率分别为62.00%和59.05%。体外释放谱符合Higuchi型动力学模型。两种植入物的体外释放研究结果与体外释放研究结果相关。结论:CMC种植体和chi种植体可延长给药时间。使用CMC制备的植入物体外释放速度明显减慢,并且药物在眼表面的保留率增加。因此,载drz的CMC植入物是治疗青光眼的有效方法。
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CiteScore
3.60
自引率
5.90%
发文量
79
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