The present disclosure belongs to the field of pharmaceutical preparations and relates to the design of a series of lipophilic derivatives by using wild-type penetrating peptide penetratin. These penetratin derivatives have a strong ability to penetrate the ocular tissues and do not cause ocular tissue toxicity. As ocular absorption enhancers, non-invasive routes could be used to achieve intraocular drug delivery and increase the ocular bioavailability of drugs. These penetratin derivatives and the ophthalmic drug delivery system constructed by them are used for eye drop administration, which could replace the intraocular injection with poor patients compliance, which greatly enhances the convenience and safety of the treatment of intraocular and fundus diseases.