Original Article
Design of Eudragit RL 100 nanoparticles by nanoprecipitation method for ocular drug delivery

https://doi.org/10.1016/j.nano.2009.09.002Get rights and content

Abstract

The objective of the current study was to prepare positively charged amphotericin-B–loaded nanoparticles providing a controlled release formulation. The particles were prepared by solvent displacement or nanoprecipitation method. The non-biodegradable positively charged polymer Eudragit RL 100 was used to prepare the different formulations with varying ratios of drug and polymer. The formulations were evaluated in terms of particle size, zeta potential, and differential scanning calorimetry measurements. Drug entrapment and release properties were examined also. The antimicrobial activity against Fusarium solani was determined. In vivo eye irritation study was carried out by a modified Draize test. All the formulations remained within a size range of 130 to 300 nm in fresh preparation as well as after 2 months. The zeta potential was positive (+22 to +42 mV) for all the formulations and was suitable for ophthalmic application. A prolonged drug release was shown by all the formulations. The formulation possesses a good antifungal activity against Fusarium solani when tested by disk diffusion method, and no eye irritation on in vivo testing was found.

From the Clinical Editor

The objective of the current study was to prepare positively charged amphotericin-B -loaded nanoparticles providing a controlled release formulation. The described formulation displayed good antifungal activity against Fusarium solani when tested by disk diffusion method, and no eye irritation on in vivo testing was found.

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Materials

Amphotericin-B (AmB) was kindly supplied as a gift sample by Asence Pharma Pvt. Ltd. (Vadodara, India). Eudragit RL 100 was obtained as gift sample from FDC Ltd. (Mumbai, India). Acetone, dimethyl sulfoxide (DMSO), and methanol were purchased from S. D. Fine Chemical Limited (Mumbai, India) and were used as received. Polyvinyl alcohol (PVA) was of molecular weight 30,000 to 70,000 and was supplied by S. D. Fine Chemical Limited. Salts for the preparation of simulated tear fluid were of

Nanoparticle size and zeta potential

The prepared AmB NPs were intended for ocular administration. Thus, particle size and particle size distribution are crucial parameters for safe administration of such a formulation. Particle size for ophthalmic application should not exceed 10 μm.17

The effect of drug:polymer ratio and organic phase:aqueous phase ratio has an immense effect on particle size and distribution. All batches showed a small mean size, well suited for possible ocular application. The mean particle size for drug-loaded

Discussion

In the current study, the potential of Eudragit RL NPs for the specific delivery of antifungal drug to the ocular mucosa was investigated. The advantages of these systems in ocular drug delivery include their ability to contact intimately with the corneal and conjunctival surfaces, thereby increasing delivery to external ocular tissues without compromising inner ocular structures and systemic drug exposure, and to provide these target tissues with long-term drug levels. Consequently, these

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No conflict of interest was reported by the authors of this article.

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