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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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Slow-release Drug Delivery through Elvax 40W to the Rat Retina: Implications for the Treatment of Chronic Conditions

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Controlled release polymeric ocular delivery of acyclovir.

Praful Balavant Deshpande¹, Panchaxari Dandagi, Nayanabhirama Udupa

¹Department of Pharmaceutics, K.L.E.S. College of Pharmacy, JNMC campus, Nehru Nagar, Belgaum, Karnataka, India.

Pharmaceutical Development and Technology

|September 24, 2009

Summary

This study developed novel controlled-release ocular inserts for acyclovir delivery using biodegradable polymers. The formulation enhanced drug solubility and provided sustained release for improved ocular treatment.

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Area of Science:

Ophthalmic drug delivery
Polymer science
Pharmaceutics

Background:

Acyclovir is a key antiviral medication for ocular infections.
Poor solubility and short residence time limit conventional acyclovir ocular formulations.
Controlled-release systems offer potential for improved therapeutic outcomes.

Purpose of the Study:

To formulate and evaluate controlled-release polymeric ocular inserts for acyclovir.
To enhance the solubility and dissolution rate of acyclovir for ocular application.
To investigate the drug release kinetics and stability of the developed ocular inserts.

Main Methods:

Fabrication of reservoir-type ocular inserts using hydroxypropyl methylcellulose (HPMC) and cellulose acetate phthalate (CAP).
Enhancement of acyclovir solubility via beta-cyclodextrin complexation.
Physicochemical evaluations, in vitro drug release studies, and in vitro/in vivo correlation.
Sterilization by gamma radiation and stability testing.

Main Results:

Developed nine formulations (AB-1 to AB-9) with varying HPMC and CAP ratios.
Achieved steady, controlled acyclovir release up to 20 hours with non-Fickian diffusion.
Confirmed acyclovir-beta-cyclodextrin complex formation using differential scanning calorimetry.
Demonstrated high correlation between in vitro and in vivo release rates.
Exhibited good stability under study storage conditions.

Conclusions:

Successfully developed controlled-release acyclovir ocular inserts using biodegradable polymers.
Beta-cyclodextrin complexation effectively enhanced acyclovir solubility and dissolution.
The non-Fickian diffusion release mechanism supports sustained ocular drug delivery.
The formulation shows promise for improved management of ocular viral infections.