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Traditional eye drops are administered via topical instillation. However, frequent dosing is needed due to their relatively rapid precorneal removal and low ocular bioavailability. To address these issues, stearoyl L-carnitine-modified nanoemulsions (SC-NEs) were fabricated. The physicochemical properties of SC-NEs in terms of size, morphology, zeta potential, encapsulation efficiency, and in vitro drug release behavior were characterized. The cellular uptake and mechanisms of SC-NEs were comprehensively studied in human corneal epithelial cells and the stearoyl L-carnitine ratio in SC-NEs was optimized. The optimized SC-NEs could target the novel organic cation/carnitine transporter 2 (OCTN2) and amino acid transporter B (0 +) (ATB 0,+ ) on the corneal epithelium, which led to superior corneal permeation, ocular surface retention ability, ocular bioavailability. Furthermore, SC-NEs showed excellent in vivo anti-inflammatory efficacy in a rabbit model of endotoxin-induced uveitis. The ocular safety test indicated that the SC-NEs were biocompatible. In general, the current study demonstrated that OCTN2 and ATB 0,+ -targeted nanoemulsions were promising ophthalmologic drug delivery systems that can improve ocular drug bioavailability and boost the therapeutic effects of drugs for eye diseases., (© 2024. The Author(s).)

Traditional eye drops are administered via topical instillation. However, frequent dosing is needed due to their relatively rapid precorneal removal and low ocular bioavailability. To address these issues, stearoyl L-carnitine-modified nanoemulsions (SC-NEs) were fabricated. The physicochemical properties of SC-NEs in terms of size, morphology, zeta potential, encapsulation efficiency, and in vitro drug release behavior were characterized. The cellular uptake and mechanisms of SC-NEs were comprehensively studied in human corneal epithelial cells and the stearoyl L-carnitine ratio in SC-NEs was optimized. The optimized SC-NEs could target the novel organic cation/carnitine transporter 2 (OCTN2) and amino acid transporter B (0 +) (ATB0,+) on the corneal epithelium, which led to superior corneal permeation, ocular surface retention ability, ocular bioavailability. Furthermore, SC-NEs showed excellent in vivo anti-inflammatory efficacy in a rabbit model of endotoxin-induced uveitis. The ocular safety test indicated that the SC-NEs were biocompatible. In general, the current study demonstrated that OCTN2 and ATB0,+-targeted nanoemulsions were promising ophthalmologic drug delivery systems that can improve ocular drug bioavailability and boost the therapeutic effects of drugs for eye diseases. [ABSTRACT FROM AUTHOR]

[Display omitted] • A summary of cyclodextrin (CD)-based ocular drug delivery systems based on formation of inclusion complexes with small molecules and polymers. • The methods for ocular safety evaluation of CD-based ocular delivery systems are summarized. • The patents and clinical trials for CD-based ocular drug delivery systems are summarized. • The challenges and perspectives of clinical translation of CD-based ocular drug delivery systems are also discussed. Cyclodextrin (CD), a class of cyclic oligosaccharides with an external hydrophilic surface and a central hydrophobic cavity is recognized as a promising pharmaceutical excipient due to its unique ability to form inclusion complexes with small molecules and polymers. CD has excellent biocompatibility, safety, and stability, promoting the rapid development of various CD-based ocular drug delivery systems over the last two decades. The review elaborates on the recent research progress of CD-based ocular drug delivery systems, including drug/CD complexes, CD-based nanocarriers and microcarriers (e.g., nanoemulsions, nanoparticles, micelles, liposomes, nanosponges, microparticles, and microspheres), CD-based hydrogels (e.g., in situ hydrogels, supramolecular hydrogels, and soft contact lenses), and CD-based inserts. In addition, the review systemically summarizes the methods for ocular safety evaluation of CD-based ocular delivery systems, as well as the patents and clinical trials for CD-based ocular drug delivery systems. [ABSTRACT FROM AUTHOR]

In this paper, we developed a vesicular phospholipid gels (VPGs) for topical ocular delivery of flurbiprofen (FLB) to treat anterior uveitis. FLB loaded VPGs (FLB VPGs), composed of FLB and egg yolk lecithin, were prepared by high-pressure homogenization technique. The effects of egg yolk lecithin content and homogenization pressure on properties of FLB VPGs, including size, encapsulation efficiency, yield and in vitro release profile were investigated. The resultant FLB VPGs were characterized by the transmission electron microscopy, differential scanning calorimetry, X-ray diffraction, fourier transform infrared spectroscopy, rheological behavior, and storage stability. Corneal permeation experiments revealed that VPGs could improve the transcorneal delivery of FLB under ex vivo conditions. VPGs were nonirritant toward to the rabbit eye, as indicated by slit lamp observation and histological observation. The results of tear pharmacokinetics and in vivo fluorescence imaging showed that VPGs could significantly prolong the precorneal retention time. In vivo biodistribution study indicated that VPGs could significantly improve drug bioavailability in ocular tissues. Moreover, FLB VPGs exhibited excellent anti-inflammatory effect in endotoxin induced uveitis in rabbits. Overall, VPGs are a promising ophthalmic drug delivery system for the treatment of anterior uveitis. The vesicular phospholipid gels showed prolonged precorneal retention time, and increased ocular bioavailability, as well as enhanced anti-inflammatory effect in rabbit model of anterior uveitis. [Display omitted] • FLB VPGs were prepared by high-pressure homogenization technique. • FLB VPGs significantly prolonged precorneal retention time. • FLB VPGs significantly increased drug bioavailability in the ocular tissues. • FLB VPGs exhibited excellent anti-inflammatory effect in rabbit model of anterior uveitis. [ABSTRACT FROM AUTHOR]

An increasing number of people worldwide are affected by eye diseases, eventually leading to visual impairment or complete blindness. Conventional treatment involves the use of eye drops. However, these formulations often confer low ocular bioavailability and frequent dosing is required. Therefore, there is an urgent need to develop more effective drug delivery systems to tackle the current limitations. Hydrogels are multifunctional ophthalmic drug delivery systems capable of extending drug residence time and sustaining release of drugs. In this review, common ocular diseases and corresponding therapeutic drugs are briefly introduced. In addition, various types of hydrogels reported for ophthalmic drug delivery, including in-situ gelling hydrogels, contact lenses, low molecular weight supramolecular hydrogels, cyclodextrin/poly (ethylene glycol)-based supramolecular hydrogels and hydrogel-forming microneedles, are summarized. Besides, marketed hydrogel-based opthalmic formulations and clinical trials are also highlighted. Finally, critical considerations regarding clinical translation of biologics-loaded hydrogels are discussed. [Display omitted] • Conventional eye drops often confer low ocular bioavailability. • Hydrogels are capable of extending drug residence time and sustaining release of drugs. • Many small molecular drug-containing ophthalmic hydrogels are in the market. • Discussion the opportunities and challenges toward regarding clinical translation of biologics-loaded hydrogels. [ABSTRACT FROM AUTHOR]