Preparation and Evaluation of Eudragit® L100 Nanoparticles Loaded Impregnated with KT Tromethamine Loaded PVA -HEC Insertions for Ophthalmic Drug Delivery.

Ghobad Mohammadi,Pardis Mohammadi,Shahla Mirzaeei,Shiva Taghe

doi:10.15171/apb.2019.068

Ghobad Mohammadi, Pardis Mohammadi + Show 2 more

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https://doi.org/10.15171/apb.2019.068

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Abstract

Purpose: The purpose of the present study was to improve the ocular delivery for ketorolac tromethamine (KT) used to treat inflammation of the eye. Methods: Eudragit nanoparticles loaded with KT were prepared and incorporated in polyvinyl alcohol (PVA) and hydroxyethyl cellulose (HEC) films. Nanoparticles were characterized by Fourier transform-infrared (FT-IR), scanning electron microscopy (SEM). Physicochemical properties and encapsulation effciency were investigated for nanoparticles. Also, the inserts were evaluated for their physiochemical parameters like percentage moisture absorption, percentage moisture loss, thickness and folding endurance. Results: Mean particle size and zeta potential were in range of 153.8-217 nm and (-10.8) - (-40.7) mV, respectively. The results show that the use of a surfactant has not led to any major change on drug loading. The loading increases with the amount of polymer. The insert had a thickness varying from 0.072 ± 0.0098 to 0.0865 ± 0.0035 mm. The thicknesses of the inserts and the folding endurance increased with the total polymer concentration. The physicochemical properties showed that the Eudragit® L-100 nanoparticles loaded PVA-HEC films could be an effective carrier for KT. Conclusion: For the first time, inserts of Eudragit nanoparticles were successfully prepared for ophthalmic drug delivery system to prevent frequent drug administration and enhance patient compliance.

Highlights

Ocular inflammation can be caused by a wide variety of factors including autoimmune disease, infection, allergies, injury or trauma, and surgery
The results show that the use of Tween 20 as a surfactant has not led to any major changes on entrapment efficiency and drug loading
Improvement in the entrapment efficiency percentage and drug loading in formulation K4 may be caused by the use of acetone as a solvent and the decrease in the relative amount of Eudragit® L100, respectively

Summary

Introduction

Ocular inflammation can be caused by a wide variety of factors including autoimmune disease, infection, allergies, injury or trauma, and surgery. The treatment of ocular inflammation involves the use of corticosteroids and non-steroidal anti-inflammatory drugs (NSAIDs). Corticoids have more or less lipophilic characters, NSAIDs are weak acids that are ionized at the lachrymal fluid pH level, a fact that limits their corneal permeability.[1,2] Ketorolac tromethamine (KT) is a nonsteroidal anti-inflammatory drug from the family of heterocyclic acetic acid derivatives. Drug delivery systems decrease the side effects of drugs such as postoperative inflammation of the eyes, postoperative pain and the conjunctivitis with no alteration of corneal opacity.[3,4] Despite eye drops cause a little blurring, they are popular due to low cost, great simplicity of formulation, development and production and better acceptance by patients. According to the physiology and anatomy of the eye, the prescription drug was absorbed in a very small percentage due to the protection mechanisms, such as tearing and blinking reflex.[5,6,7] Polymer nanoparticles are reported to be devoid of any irritant effect on cornea, iris, and conjunctiva and appear to be a suitable inert carrier for ophthalmic drug delivery

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