A significant challenge in biomedicine is the inefficient delivery of drugs to the posterior segment of the eye. This study presents an innovative and minimally invasive approach for treating diabetic retinopathy, a complication of diabetes affecting the eye. We introduce novel near-infrared (NIR) light-responsive multifunctional microcapsules, which demonstrate a high loading efficiency of a NIR photothermally-active fluorophore (75%) and an even higher capability to bind the therapeutic drug Avastin on their surface. These polymeric multifunctional microcapsules, created using the Layer-by-Layer deposition technique, serve as microcarriers for targeted Avastin delivery to the retina, releasing the drug in vitro upon NIR laser exposure. The Avastin-targeted microsystem was thoroughly characterized in terms of morphology, phototherapeutic capacity, NIR-light stimulated drug release, and its potential as a fluorescent contrast agent for in vitro imaging. Re-Scanning Microscopy and Scanning Electron Microscopy revealed the formation of 4.5 ± 0.3 μm spherical microcapsules that maintained stability over seven months. The binding of Avastin to the microsystem’s surface was confirmed using various spectroscopic methods. The phototherapeutic potential of the microsystem in solution was initially assessed, followed by investigations into the shell rupture and subsequent drug release in vitro within human retina cells. The WST-1 assay demonstrated the biocompatibility of the microcapsules. Localization of the microcapsules inside human D407 retina cells was confirmed using Conventional Fluorescence Microscopy and 3D Re-scan Confocal Microscopy (RCM). Finally, the in vitro results validate the therapeutic potential of this multifunctional microsystem, demonstrating its effectiveness as a drug delivery and release system that could supplant conventional treatment strategies for diabetic retinopathy.