Abstract

Age‐related macular degeneration (AMD) is the third largest eye disease. However, the eye has a variety of drug delivery barriers, which prevent the drug from reaching the lesions in the posterior segment of the eye, coupled with the pathogenesis of dry‐AMD; these lead to the lack of effective treatment drugs for dry‐AMD. Therefore, the developments of a suitable therapeutic drug and a novel ophthalmic preparation are of great significance for the treatment of dry‐AMD. The purposes of this study were to construct a novel traditional Chinese medicine (Chuanqi Fang) anti‐AMD microemulsion in situ gel for treating dry‐AMD and investigate its characteristic, efficiency, irritation, and tissue distribution. In this study, the characteristic of the Chuanqi microemulsion in situ gel was measured by dynamic light scattering. The electroretinogram (ERG) indicators and the number of retinal pigment epithelial cells were measured to evaluate the therapeutic effect of the novel ophthalmic nanopreparations. Irritation was evaluated according to Technical Guideline Principles (ZGPT4‐1). The analysis of tissue distribution was carried out with LC‐MS. The research showed that the particle size of microemulsion was 38.56 ± 0.21 nm. The Chuanqi microemulsion in situ gel had certain roles in repairing retina damage of the dry‐AMD animal model and showed no irritation. The tissue distribution study found that the microemulsion in situ gel could effectively deliver the drug to the posterior eye of the AMD model rat through the route of cornea‐vitreous body‐retina. In conclusion, this study provided a meaningful research strategy and research basis for the development of new dry‐AMD therapeutic drugs.

Highlights

  • Age-related macular degeneration (AMD) is the third largest eye disease all over the world according to the report Vision 2020 [1] released by the World Health Organization (WHO)

  • Characterization. e characterizations of the Chuanqi microemulsion in situ gel were investigated using the method given under Section “3.4 Characterizations of Chuanqi Microemulsion In Situ Gel.” e result showed that the particle size of microemulsion was 38.56 ± 0.21 nm (PDI 0.18), and the zeta potential was −17.99 ± 0.22 mv

  • Morphological Observation of Microemulsion. e morphology of Chuanqi microemulsion was observed using the method given under Section “3.5 Morphological Observation of Microemulsion,” and the pictures are shown in Figure 2; the particle size of the microemulsion was shown within 100 nm, and it was unevenly globular or quasiglobular

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Summary

Introduction

Age-related macular degeneration (AMD) is the third largest eye disease all over the world according to the report Vision 2020 [1] released by the World Health Organization (WHO). E eye has a special anatomical structure, forming a variety of drug delivery barriers, including the tear barrier, conjunctiva, corneal barrier, and blood-eye barrier. Due to the special physiological structure and pathogenesis of the eye, there is no clear treatment method and ideal drug treatment for dry-AMD treatment. Erefore, the selection of a suitable therapeutic drug and the preparation of a novel ophthalmic preparation for the efficient delivery of the posterior eye are of great significance for the treatment of dry-AMD. Ligusticum chuanxiong and Astragalus membranaceus are the two most commonly used TCMs [6, 7]. Modern ophthalmological pharmacological studies have found that Ligusticum chuanxiong could treat retinal vein occlusion [8], and Astragalus membranaceus could reduce retinal ischemia-reperfusion injury, and it had a significant

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