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Ophthalmic Drug Delivery Systems

Ophthalmic Drug Delivery Systems

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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Ultrasound Cyclo Plasty in Eyes with Glaucoma

Ultrasound Cyclo Plasty in Eyes with Glaucoma

Published on: January 26, 2018

[Cyclosporine 2% eye drops preparation].

F Chast¹, F Lemare, J-M Legeais

¹Service de Pharmacie, Pharmacologie et Toxicologie, Hôtel-Dieu, Paris. francois.chast@htd.ap-hop-paris.fr

Journal Francais D'Ophtalmologie

|September 3, 2004

Summary

This study details the preparation and stability of 2% cyclosporine eye drops, finding them stable for 12 months with minimal systemic absorption, making them suitable for ophthalmic use.

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Area of Science:

Ophthalmology
Immunology
Pharmaceutical Sciences

Context:

Immunological diseases of the eye (cornea, conjunctiva, uvea) often require effective treatments.
High-risk corneal transplantation frequently necessitates immunosuppressive therapy to prevent rejection.
Standard ophthalmic formulations may not always provide optimal cyclosporine delivery.

Purpose:

To present a stable and effective preparation of 2% cyclosporine eye drops.
To evaluate the manufacturing process ensuring sterility and quality control.
To assess the systemic bioavailability and toxicity of the prepared eye drops.

Summary:

A 2% cyclosporine eye drop formulation was prepared by diluting a commercial oral solution in sterile castor oil under strict aseptic conditions.
Chemical analysis confirmed stability for up to 12 months, with minimal statistical difference in concentration over time.
Pharmacokinetic analysis revealed very low systemic bioavailability, with blood concentrations below detection limits, indicating an absence of systemic toxicity.

Impact:

The developed 2% cyclosporine eye drops offer a stable, long-lasting (12 months) ophthalmic formulation.
The preparation demonstrates a favorable safety profile with negligible systemic absorption and no noted local adverse effects.
This formulation can be a valuable addition to hospital pharmacies for treating various ocular inflammatory and post-transplant conditions.