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Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

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Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...
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An Alternative and Validated Injection Method for Accessing the Subretinal Space via a Transcleral Posterior Approach
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Intravitreal injection of polysorbate 80: a functional and morphological study.

Francisco Max Damico1, Fábio Gasparin1, Gabriela Lourençon Ioshimoto2

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Polysorbate 80 (PS80) at concentrations used for intravitreal drug formulations showed no adverse effects on rabbit retinas. This study indicates PS80 is safe for preparing new intravitreal medications.

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Area of Science:

  • Ophthalmology
  • Pharmacology
  • Toxicology

Background:

  • Polysorbate 80 (PS80) is a common excipient in pharmaceutical formulations.
  • Its safety for intravitreal injection, particularly in drug preparations, requires thorough evaluation.
  • Understanding PS80's effects on retinal tissue is crucial for developing new ophthalmic treatments.

Purpose of the Study:

  • To assess the functional and morphological impact of PS80 on rabbit retinas.
  • To determine the safety of PS80 concentrations used in intravitreal drug preparation.

Main Methods:

  • Intravitreal injections of PS80 were administered to New Zealand rabbits.
  • Control eyes received saline injections.
  • Functional assessment included electroretinography (ERG), biomicroscopy, and retinal mapping.
  • Morphological analysis was performed using light microscopy post-euthanasia.

Main Results:

  • No clinical signs of intraocular inflammation were observed in PS80-injected eyes.
  • ERG measurements showed no significant alterations in scotopic or photopic conditions.
  • Light microscopy revealed no morphological changes in the retinas.

Conclusions:

  • Intravitreal PS80, at concentrations relevant to drug preparation, does not induce functional or morphological retinal damage in rabbits.
  • PS80 demonstrates a lack of toxicity to rabbit retinas.
  • These findings support the safe use of PS80 in novel lipophilic intravitreal drug formulations.