Presentation Information
[P03-348]Development of a nanogel-emulsion system capable of efficient topical delivery to the ocular posterior segment via eye drops
○CHONGZHI CHEN1, Norifumi Kawasaki1, Yasuhiro Ikegami1, Yusuke Sakai1, Hiroyuki Ijima1 (1. Department of Chemical Engineering, Faculty of Engineering, Graduate School of Engineering, Kyushu University (Japan))
Keywords:
Drug delivery system,Nanoemulsion,Nanoparticle,Topical delivery
Drug delivery to the posterior segment of the eye remains a major challenge due to multiple physiological barriers, including the corneal epithelium, sclera, and retinal pigment epithelium (RPE). Although intravitreal injection is widely used for treating retinal diseases, it is associated with patient discomfort and potential complications. Therefore, the development of a non-invasive eyedrop formulation capable of delivering drugs to the posterior segment of the eye is highly desirable.
In this study, we developed a functionalized Gel-in-Water (G/W) nanoemulsion designed for ocular drug delivery. In a PBS environment, the formulation consisted of castor oil and was stabilized by nonionic surfactants together with a gelation agent. To enhance the drug delivery to the retina, additional functional components were introduced into the nanoemulsion system to improve the permeability and prolong retention time after eyedrop administration.
The physicochemical properties of the nanoemulsions, including mean particle diameter, polydispersity index (PDI), and zeta potential, were characterized using dynamic light scattering. The mean particle size was approximately 250 nm with a narrow size distribution, which is considered suitable for posterior ocular drug delivery. Zeta potential measurements and drug release profiles further supported successful surface modification. Cytotoxicity and ocular irritation tests demonstrated favorable biocompatibility, indicating that the formulation is a safe carrier for ocular drug delivery. The results also suggested successful surface modification of the nanoemulsions with penetration enhancers. In vivo eye-drop experiments in mice showed enhanced fluorescence distribution and prolonged retention in posterior ocular tissues compared with the control formulation. In addition, an ex vivo porcine eye soaking model suggested the potential of this formulation to achieve drug delivery in human-scale ocular tissues.
These results suggest that the modified-G/W nanoemulsion system may serve as a promising non-invasive carrier for posterior ocular drug delivery via eye-drop administration. Further studies will focus on elucidating the penetration mechanism and evaluating therapeutic efficacy in retinal disease models.
In this study, we developed a functionalized Gel-in-Water (G/W) nanoemulsion designed for ocular drug delivery. In a PBS environment, the formulation consisted of castor oil and was stabilized by nonionic surfactants together with a gelation agent. To enhance the drug delivery to the retina, additional functional components were introduced into the nanoemulsion system to improve the permeability and prolong retention time after eyedrop administration.
The physicochemical properties of the nanoemulsions, including mean particle diameter, polydispersity index (PDI), and zeta potential, were characterized using dynamic light scattering. The mean particle size was approximately 250 nm with a narrow size distribution, which is considered suitable for posterior ocular drug delivery. Zeta potential measurements and drug release profiles further supported successful surface modification. Cytotoxicity and ocular irritation tests demonstrated favorable biocompatibility, indicating that the formulation is a safe carrier for ocular drug delivery. The results also suggested successful surface modification of the nanoemulsions with penetration enhancers. In vivo eye-drop experiments in mice showed enhanced fluorescence distribution and prolonged retention in posterior ocular tissues compared with the control formulation. In addition, an ex vivo porcine eye soaking model suggested the potential of this formulation to achieve drug delivery in human-scale ocular tissues.
These results suggest that the modified-G/W nanoemulsion system may serve as a promising non-invasive carrier for posterior ocular drug delivery via eye-drop administration. Further studies will focus on elucidating the penetration mechanism and evaluating therapeutic efficacy in retinal disease models.
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