Strategies to prolong the residence time of drug delivery systems on ocular surface

Grassiri, Brunella; Zambito, Ylenia; Bernkop‐Schnürch, Andreas

doi:10.1016/j.cis.2020.102342

Cited by 97 publications

(57 citation statements)

References 157 publications

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“…The FDA defines "any component of a pharmaceutical product other than the API" as an excipient [73], which are implemented in nanomedicine production as antiaggregation agents during processing, off-the-shelf stability agents, solubilizing agents, hydrophilization agents, or viscosity enhancers, among others. Excipients also provide additional pharmacological properties/functions, including mucoadhesion [74], enzyme inhibition [75][76][77], oral absorption enhancement [78], efflux pump inhibition [79], or tastemasking [80].…”

Section: Active Pharmaceutical Ingredients and Excipientsmentioning

confidence: 99%

Current hurdles to the translation of nanomedicines from bench to the clinic

Đorđević

Medel

Conejos‐Sánchez

et al. 2021

Drug Deliv. and Transl. Res.

138

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The field of nanomedicine has significantly influenced research areas such as drug delivery, diagnostics, theranostics, and regenerative medicine; however, the further development of this field will face significant challenges at the regulatory level if related guidance remains unclear and unconsolidated. This review describes those features and pathways crucial to the clinical translation of nanomedicine and highlights considerations for early-stage product development. These include identifying those critical quality attributes of the drug product essential for activity and safety, appropriate analytical methods (physical, chemical, biological) for characterization, important process parameters, and adequate pre-clinical models. Additional concerns include the evaluation of batch-to-batch consistency and considerations regarding scaling up that will ensure a successful reproducible manufacturing process. Furthermore, we advise close collaboration with regulatory agencies from the early stages of development to assure an aligned position to accelerate the development of future nanomedicines. Graphical abstract

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Section: Active Pharmaceutical Ingredients and Excipientsmentioning

confidence: 99%

Current hurdles to the translation of nanomedicines from bench to the clinic

Đorđević

Medel

Conejos‐Sánchez

et al. 2021

Drug Deliv. and Transl. Res.

138

View full text Add to dashboard Cite

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“…HA is found in various tissues in the eye, including the aqueous humor, trabecular meshwork, and vitreous body; through the cell surface glycoprotein CD44, HA can bind easily with the cell membrane [ 57 ]. HA also moisturizes the eye, increases biocompatibility, and prolongs drug residence time to enhance drug delivery [ 37 , 57 , 58 , 59 , 60 ]. These properties allow for HA’s use in artificial tears, eye drops, in situ forming hydrogels, modified nanoparticles, intravitreal injections, and tissue engineering ( Table 2 ).…”

Section: Applications Of Ha In Ophthalmologymentioning

confidence: 99%

Applications of Hyaluronic Acid in Ophthalmology and Contact Lenses

et al. 2021

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Hyaluronic acid (HA) is a glycosaminoglycan that was first isolated and identified from the vitreous body of a bull’s eye. HA is ubiquitous in the soft connective tissues of animals and therefore has high tissue compatibility for use in medication. Because of HA’s biological safety and water retention properties, it has many ophthalmology-related applications, such as in intravitreal injection, dry eye treatment, and contact lenses. Due to its broad range of applications, the identification and quantification of HA is a critical topic. This review article discusses current methods for analyzing HA. Contact lenses have become a widely used medical device, with HA commonly used as an additive to their production material, surface coating, and multipurpose solution. HA molecules on contact lenses retain moisture and increase the wearer’s comfort. HA absorbed by contact lenses can also gradually release to the anterior segment of the eyes to treat dry eye. This review discusses applications of HA in ophthalmology.

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“…Amphiphilic HA can be formulated without trehalose with a higher mucoadhesive effect. Mucoadhesion is related to the ocular residence time of the eye drops [37]. The robustness of the method is evaluated by using mucin from porcine stomach, Type II and III in HEPES (Figure S2).…”

Section: Mucoadhesive Properties Determined By Rheologymentioning

confidence: 99%

Insight into the Lubrication and Adhesion Properties of Hyaluronan for Ocular Drug Delivery

et al. 2021

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Hyaluronan (HA) is widely used for eye drops as lubricant to counteract dry eye disease. High and low molecular weight HA are currently used in ophthalmology. However, a large portion of the current literature on friction and lubrication addresses articular (joint) cartilage. Therefore, eye drops compositions based on HA and its derivatized forms are extensively characterized providing data on the tribological and mucoadhesive properties. The physiochemical properties are investigated in buffers used commonly in eye drops formulations. The tribological investigation reveals that amphiphilic HA-C12 decreases the friction coefficient. At the same time, the combination of trehalose/HA or HAC12 enhances up to eighty-fold the mucoadhesiveness. Thus, it is predicted a prolonged residence time on the surface of the eye. The incorporation of trehalose enhances the protection of human keratinocytes (HaCaT) cells, as demonstrated in an in-vitro cell-desiccation model. The presence of trehalose increases the friction coefficient. Medium molecular weight HA shows significantly lower friction coefficient than high molecular weight HA. This research represents a first, wide array of features of diverse HA forms for eye drops contributing to increase the knowledge of these preparations. The results here presented also provide valuable information for the design of highly performing HA-formulations addressing specific needs before preclinic.

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Strategies to prolong the residence time of drug delivery systems on ocular surface

Cited by 97 publications

References 157 publications

Current hurdles to the translation of nanomedicines from bench to the clinic

Current hurdles to the translation of nanomedicines from bench to the clinic

Applications of Hyaluronic Acid in Ophthalmology and Contact Lenses

Insight into the Lubrication and Adhesion Properties of Hyaluronan for Ocular Drug Delivery

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